Analgesics: Compounds capable of relieving pain without the loss of CONSCIOUSNESS.Analgesics, Opioid: Compounds with activity like OPIATE ALKALOIDS, acting at OPIOID RECEPTORS. Properties include induction of ANALGESIA or NARCOSIS.Receptors, Opioid, mu: A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.Receptors, Opioid: Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.Receptors, Opioid, delta: A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.Receptors, Opioid, kappa: A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.Opioid Peptides: The endogenous peptides with opiate-like activity. The three major classes currently recognized are the ENKEPHALINS, the DYNORPHINS, and the ENDORPHINS. Each of these families derives from different precursors, proenkephalin, prodynorphin, and PRO-OPIOMELANOCORTIN, respectively. There are also at least three classes of OPIOID RECEPTORS, but the peptide families do not map to the receptors in a simple way.Analgesics, Non-Narcotic: A subclass of analgesic agents that typically do not bind to OPIOID RECEPTORS and are not addictive. Many non-narcotic analgesics are offered as NONPRESCRIPTION DRUGS.Morphine: The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.Pain: An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.Analgesia: Methods of PAIN relief that may be used with or in place of ANALGESICS.Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.Pain Measurement: Scales, questionnaires, tests, and other methods used to assess pain severity and duration in patients or experimental animals to aid in diagnosis, therapy, and physiological studies.Opioid-Related Disorders: Disorders related or resulting from abuse or mis-use of opioids.Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.Pain, Postoperative: Pain during the period after surgery.Enkephalins: One of the three major families of endogenous opioid peptides. The enkephalins are pentapeptides that are widespread in the central and peripheral nervous systems and in the adrenal medulla.Tramadol: A narcotic analgesic proposed for severe pain. It may be habituating.Narcotics: Agents that induce NARCOSIS. Narcotics include agents that cause somnolence or induced sleep (STUPOR); natural or synthetic derivatives of OPIUM or MORPHINE or any substance that has such effects. They are potent inducers of ANALGESIA and OPIOID-RELATED DISORDERS.Enkephalin, Ala(2)-MePhe(4)-Gly(5)-: An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.Drug Tolerance: Progressive diminution of the susceptibility of a human or animal to the effects of a drug, resulting from its continued administration. It should be differentiated from DRUG RESISTANCE wherein an organism, disease, or tissue fails to respond to the intended effectiveness of a chemical or drug. It should also be differentiated from MAXIMUM TOLERATED DOSE and NO-OBSERVED-ADVERSE-EFFECT LEVEL.Buprenorphine: A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.Endorphins: One of the three major groups of endogenous opioid peptides. They are large peptides derived from the PRO-OPIOMELANOCORTIN precursor. The known members of this group are alpha-, beta-, and gamma-endorphin. The term endorphin is also sometimes used to refer to all opioid peptides, but the narrower sense is used here; OPIOID PEPTIDES is used for the broader group.Enkephalin, D-Penicillamine (2,5)-: A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.Fentanyl: A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078)Dynorphins: A class of opioid peptides including dynorphin A, dynorphin B, and smaller fragments of these peptides. Dynorphins prefer kappa-opioid receptors (RECEPTORS, OPIOID, KAPPA) and have been shown to play a role as central nervous system transmitters.Phenacetin: A phenylacetamide that was formerly used in ANALGESICS but nephropathy and METHEMOGLOBINEMIA led to its withdrawal from the market. (From Smith and Reynard, Textbook of Pharmacology,1991, p431)Acetaminophen: Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.Pain Threshold: Amount of stimulation required before the sensation of pain is experienced.Hydromorphone: An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine.Enkephalin, Leucine: One of the endogenous pentapeptides with morphine-like activity. It differs from MET-ENKEPHALIN in the LEUCINE at position 5. Its first four amino acid sequence is identical to the tetrapeptide sequence at the N-terminal of BETA-ENDORPHIN.Morphinans: Compounds based on a partially saturated iminoethanophenanthrene, which can be described as ethylimino-bridged benzo-decahydronaphthalenes. They include some of the OPIOIDS found in PAPAVER that are used as ANALGESICS.Dextropropoxyphene: A narcotic analgesic structurally related to METHADONE. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect.Codeine: An opioid analgesic related to MORPHINE but with less potent analgesic properties and mild sedative effects. It also acts centrally to suppress cough.Injections, Spinal: Introduction of therapeutic agents into the spinal region using a needle and syringe.Enkephalin, Leucine-2-Alanine: A delta-selective opioid (ANALGESICS, OPIOID). It can cause transient depression of mean arterial blood pressure and heart rate.Hyperalgesia: An increased sensation of pain or discomfort produced by mimimally noxious stimuli due to damage to soft tissue containing NOCICEPTORS or injury to a peripheral nerve.beta-Endorphin: A 31-amino acid peptide that is the C-terminal fragment of BETA-LIPOTROPIN. It acts on OPIOID RECEPTORS and is an analgesic. Its first four amino acids at the N-terminal are identical to the tetrapeptide sequence of METHIONINE ENKEPHALIN and LEUCINE ENKEPHALIN.Anti-Inflammatory Agents, Non-Steroidal: Anti-inflammatory agents that are non-steroidal in nature. In addition to anti-inflammatory actions, they have analgesic, antipyretic, and platelet-inhibitory actions.They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. Inhibition of prostaglandin synthesis accounts for their analgesic, antipyretic, and platelet-inhibitory actions; other mechanisms may contribute to their anti-inflammatory effects.Meperidine: A narcotic analgesic that can be used for the relief of most types of moderate to severe pain, including postoperative pain and the pain of labor. Prolonged use may lead to dependence of the morphine type; withdrawal symptoms appear more rapidly than with morphine and are of shorter duration.Pain Management: A form of therapy that employs a coordinated and interdisciplinary approach for easing the suffering and improving the quality of life of those experiencing pain.Pentazocine: The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97)Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Methadone: A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3)Benzeneacetamides: Compounds based on benzeneacetamide, that are similar in structure to ACETANILIDES.Pain, Intractable: Persistent pain that is refractory to some or all forms of treatment.Diprenorphine: A narcotic antagonist similar in action to NALOXONE. It is used to remobilize animals after ETORPHINE neuroleptanalgesia and is considered a specific antagonist to etorphine.Butorphanol: A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain.Anesthetics, Local: Drugs that block nerve conduction when applied locally to nerve tissue in appropriate concentrations. They act on any part of the nervous system and on every type of nerve fiber. In contact with a nerve trunk, these anesthetics can cause both sensory and motor paralysis in the innervated area. Their action is completely reversible. (From Gilman AG, et. al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed) Nearly all local anesthetics act by reducing the tendency of voltage-dependent sodium channels to activate.Hydrocodone: Narcotic analgesic related to CODEINE, but more potent and more addicting by weight. It is used also as cough suppressant.Chronic Pain: Aching sensation that persists for more than a few months. It may or may not be associated with trauma or disease, and may persist after the initial injury has healed. Its localization, character, and timing are more vague than with acute pain.Oxymorphone: An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092)Morphine Derivatives: Analogs or derivatives of morphine.Double-Blind Method: A method of studying a drug or procedure in which both the subjects and investigators are kept unaware of who is actually getting which specific treatment.Dipyrone: A drug that has analgesic, anti-inflammatory, and antipyretic properties. It is the sodium sulfonate of AMINOPYRINE.Analgesia, Epidural: The relief of pain without loss of consciousness through the introduction of an analgesic agent into the epidural space of the vertebral canal. It is differentiated from ANESTHESIA, EPIDURAL which refers to the state of insensitivity to sensation.Levorphanol: A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection.Analgesia, Patient-Controlled: Relief of PAIN, without loss of CONSCIOUSNESS, through ANALGESIC AGENTS administered by the patients. It has been used successfully to control POSTOPERATIVE PAIN, during OBSTETRIC LABOR, after BURNS, and in TERMINAL CARE. The choice of agent, dose, and lockout interval greatly influence effectiveness. The potential for overdose can be minimized by combining small bolus doses with a mandatory interval between successive doses (lockout interval).Benzomorphans: Morphine derivatives of the methanobenzazocine family that act as potent analgesics.Bupivacaine: A widely used local anesthetic agent.Rats, Sprague-Dawley: A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.Oxycodone: A semisynthetic derivative of CODEINE.Nociceptors: Peripheral AFFERENT NEURONS which are sensitive to injuries or pain, usually caused by extreme thermal exposures, mechanical forces, or other noxious stimuli. Their cell bodies reside in the DORSAL ROOT GANGLIA. Their peripheral terminals (NERVE ENDINGS) innervate target tissues and transduce noxious stimuli via axons to the CENTRAL NERVOUS SYSTEM.Alfentanil: A short-acting opioid anesthetic and analgesic derivative of FENTANYL. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients.Cyclazocine: An analgesic with mixed narcotic agonist-antagonist properties.Nociception: Sensing of noxious mechanical, thermal or chemical stimuli by NOCICEPTORS. It is the sensory component of visceral and tissue pain (NOCICEPTIVE PAIN).Nalbuphine: A narcotic used as a pain medication. It appears to be an agonist at kappa opioid receptors and an antagonist or partial agonist at mu opioid receptors.Substance Withdrawal Syndrome: Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.Prescription Drugs: Drugs that cannot be sold legally without a prescription.PyrrolidinesHeroin: A narcotic analgesic that may be habit-forming. It is a controlled substance (opium derivative) listed in the U.S. Code of Federal Regulations, Title 21 Parts 329.1, 1308.11 (1987). Sale is forbidden in the United States by Federal statute. (Merck Index, 11th ed)Neuralgia: Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.Tolmetin: A non-steroidal anti-inflammatory agent (ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL) similar in mode of action to INDOMETHACIN.Carrageenan: A water-soluble extractive mixture of sulfated polysaccharides from RED ALGAE. Chief sources are the Irish moss CHONDRUS CRISPUS (Carrageen), and Gigartina stellata. It is used as a stabilizer, for suspending COCOA in chocolate manufacture, and to clarify BEVERAGES.Ketoprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It is used in the treatment of rheumatoid arthritis and osteoarthritis.Sufentanil: An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.Meptazinol: A narcotic antagonist with analgesic properties. It is used for the control of moderate to severe pain.Ketorolac: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed)Acupuncture Analgesia: Analgesia produced by the insertion of ACUPUNCTURE needles at certain ACUPUNCTURE POINTS on the body. This activates small myelinated nerve fibers in the muscle which transmit impulses to the spinal cord and then activate three centers - the spinal cord, midbrain and pituitary/hypothalamus - to produce analgesia.Morphine Dependence: Strong dependence, both physiological and emotional, upon morphine.Nalorphine: A narcotic antagonist with some agonist properties. It is an antagonist at mu opioid receptors and an agonist at kappa opioid receptors. Given alone it produces a broad spectrum of unpleasant effects and it is considered to be clinically obsolete.Kidney Papillary Necrosis: A complication of kidney diseases characterized by cell death involving KIDNEY PAPILLA in the KIDNEY MEDULLA. Damages to this area may hinder the kidney to concentrate urine resulting in POLYURIA. Sloughed off necrotic tissue may block KIDNEY PELVIS or URETER. Necrosis of multiple renal papillae can lead to KIDNEY FAILURE.Nociceptive Pain: Dull or sharp aching pain caused by stimulated NOCICEPTORS due to tissue injury, inflammation or diseases. It can be divided into somatic or tissue pain and VISCERAL PAIN.Drug Overdose: Accidental or deliberate use of a medication or street drug in excess of normal dosage.Acute Pain: Intensely discomforting, distressful, or agonizing sensation associated with trauma or disease, with well-defined location, character, and timing.Periaqueductal Gray: Central gray matter surrounding the CEREBRAL AQUEDUCT in the MESENCEPHALON. Physiologically it is probably involved in RAGE reactions, the LORDOSIS REFLEX; FEEDING responses, bladder tonus, and pain.Nefopam: Non-narcotic analgesic chemically similar to ORPHENADRINE. Its mechanism of action is unclear. It is used for the relief of acute and chronic pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p26)Prescription Drug Misuse: Improper use of drugs or medications outside the intended purpose, scope, or guidelines for use. This is in contrast to MEDICATION ADHERENCE, and distinguished from DRUG ABUSE, which is a deliberate or willful action.Spinal Cord: A cylindrical column of tissue that lies within the vertebral canal. It is composed of WHITE MATTER and GRAY MATTER.Cyclohexanecarboxylic AcidsIbuprofen: A nonsteroidal anti-inflammatory agent with analgesic properties used in the therapy of rheumatism and arthritis.Opiate Substitution Treatment: Medical treatment for opioid dependence using a substitute opiate such as METHADONE or BUPRENORPHINE.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Analgesia, Obstetrical: The elimination of PAIN, without the loss of CONSCIOUSNESS, during OBSTETRIC LABOR; OBSTETRIC DELIVERY; or the POSTPARTUM PERIOD, usually through the administration of ANALGESICS.Behavior, Animal: The observable response an animal makes to any situation.Ketamine: A cyclohexanone derivative used for induction of anesthesia. Its mechanism of action is not well understood, but ketamine can block NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE) and may interact with sigma receptors.Edema: Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.Oligopeptides: Peptides composed of between two and twelve amino acids.Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.Electroacupuncture: A form of acupuncture with electrical impulses passing through the needles to stimulate NERVE TISSUE. It can be used for ANALGESIA; ANESTHESIA; REHABILITATION; and treatment for diseases.Piperidines: A family of hexahydropyridines.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Nerve Block: Interruption of NEURAL CONDUCTION in peripheral nerves or nerve trunks by the injection of a local anesthetic agent (e.g., LIDOCAINE; PHENOL; BOTULINUM TOXINS) to manage or treat pain.Ethylketocyclazocine: A kappa opioid receptor agonist. The compound has analgesic action and shows positive inotropic effects on the electrically stimulated left atrium. It also affects various types of behavior in mammals such as locomotion, rearing, and grooming.Heroin Dependence: Strong dependence, both physiological and emotional, upon heroin.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.Drug Prescriptions: Directions written for the obtaining and use of DRUGS.Injections, Intraventricular: Injections into the cerebral ventricles.Nitrous Oxide: Nitrogen oxide (N2O). A colorless, odorless gas that is used as an anesthetic and analgesic. High concentrations cause a narcotic effect and may replace oxygen, causing death by asphyxia. It is also used as a food aerosol in the preparation of whipping cream.Drug and Narcotic Control: Control of drug and narcotic use by international agreement, or by institutional systems for handling prescribed drugs. This includes regulations concerned with the manufacturing, dispensing, approval (DRUG APPROVAL), and marketing of drugs.Lidocaine: A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.Hypnotics and Sedatives: Drugs used to induce drowsiness or sleep or to reduce psychological excitement or anxiety.Diterpenes, Clerodane: A group of DITERPENES cyclized into 2-rings with a side-chain.Antipyretics: Drugs that are used to reduce body temperature in fever.Dexmedetomidine: A imidazole derivative that is an agonist of ADRENERGIC ALPHA-2 RECEPTORS. It is closely-related to MEDETOMIDINE, which is the racemic form of this compound.Opiate Alkaloids: Alkaloids found in OPIUM from PAPAVER that induce analgesic and narcotic effects by action upon OPIOID RECEPTORS.Chronic Disease: Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care. (Dictionary of Health Services Management, 2d ed)Acetic Acid: Product of the oxidation of ethanol and of the destructive distillation of wood. It is used locally, occasionally internally, as a counterirritant and also as a reagent. (Stedman, 26th ed)Formaldehyde: A highly reactive aldehyde gas formed by oxidation or incomplete combustion of hydrocarbons. In solution, it has a wide range of uses: in the manufacture of resins and textiles, as a disinfectant, and as a laboratory fixative or preservative. Formaldehyde solution (formalin) is considered a hazardous compound, and its vapor toxic. (From Reynolds, Martindale The Extra Pharmacopoeia, 30th ed, p717)Hot Temperature: Presence of warmth or heat or a temperature notably higher than an accustomed norm.Ketorolac Tromethamine: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is a non-steroidal anti-inflammatory agent used for analgesia for postoperative pain and inhibits cyclooxygenase activity.Treatment Outcome: Evaluation undertaken to assess the results or consequences of management and procedures used in combating disease in order to determine the efficacy, effectiveness, safety, and practicability of these interventions in individual cases or series.Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.Postoperative Nausea and Vomiting: Emesis and queasiness occurring after anesthesia.Amines: A group of compounds derived from ammonia by substituting organic radicals for the hydrogens. (From Grant & Hackh's Chemical Dictionary, 5th ed)Amides: Organic compounds containing the -CO-NH2 radical. Amides are derived from acids by replacement of -OH by -NH2 or from ammonia by the replacement of H by an acyl group. (From Grant & Hackh's Chemical Dictionary, 5th ed)Mice, Inbred ICROpium: The air-dried exudate from the unripe seed capsule of the opium poppy, Papaver somniferum, or its variant, P. album. It contains a number of alkaloids, but only a few - MORPHINE; CODEINE; and PAPAVERINE - have clinical significance. Opium has been used as an analgesic, antitussive, antidiarrheal, and antispasmodic.Freund's Adjuvant: An antigen solution emulsified in mineral oil. The complete form is made up of killed, dried mycobacteria, usually M. tuberculosis, suspended in the oil phase. It is effective in stimulating cell-mediated immunity (IMMUNITY, CELLULAR) and potentiates the production of certain IMMUNOGLOBULINS in some animals. The incomplete form does not contain mycobacteria.Levallorphan: An opioid antagonist with properties similar to those of NALOXONE; in addition it also possesses some agonist properties. It should be used cautiously; levallorphan reverses severe opioid-induced respiratory depression but may exacerbate respiratory depression such as that induced by alcohol or other non-opioid central depressants. (From Martindale, The Extra Pharmacopoeia, 30th ed, p683)Drug Combinations: Single preparations containing two or more active agents, for the purpose of their concurrent administration as a fixed dose mixture.Anti-Inflammatory Agents: Substances that reduce or suppress INFLAMMATION.Drug Administration Schedule: Time schedule for administration of a drug in order to achieve optimum effectiveness and convenience.Self Medication: The self administration of medication not prescribed by a physician or in a manner not directed by a physician.Benzylidene Compounds: Compounds containing the PhCH= radical.Anesthesia, Spinal: Procedure in which an anesthetic is injected directly into the spinal cord.Nonprescription Drugs: Medicines that can be sold legally without a DRUG PRESCRIPTION.Anesthetics, Dissociative: Intravenous anesthetics that induce a state of sedation, immobility, amnesia, and marked analgesia. Subjects may experience a strong feeling of dissociation from the environment. The condition produced is similar to NEUROLEPTANALGESIA, but is brought about by the administration of a single drug. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed)Administration, Oral: The giving of drugs, chemicals, or other substances by mouth.Radioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Guanosine 5'-O-(3-Thiotriphosphate): Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.Piroxicam: A cyclooxygenase inhibiting, non-steroidal anti-inflammatory agent (NSAID) that is well established in treating rheumatoid arthritis and osteoarthritis and used for musculoskeletal disorders, dysmenorrhea, and postoperative pain. Its long half-life enables it to be administered once daily.Substance-Related Disorders: Disorders related to substance abuse.Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.Plant Extracts: Concentrated pharmaceutical preparations of plants obtained by removing active constituents with a suitable solvent, which is evaporated away, and adjusting the residue to a prescribed standard.Disease Models, Animal: Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.Brain: The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.Transcutaneous Electric Nerve Stimulation: The use of specifically placed small electrodes to deliver electrical impulses across the SKIN to relieve PAIN. It is used less frequently to produce ANESTHESIA.Tromethamine: An organic amine proton acceptor. It is used in the synthesis of surface-active agents and pharmaceuticals; as an emulsifying agent for cosmetic creams and lotions, mineral oil and paraffin wax emulsions, as a biological buffer, and used as an alkalizer. (From Merck, 11th ed; Martindale, The Extra Pharmacopoeia, 30th ed, p1424)Adrenergic alpha-2 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.D-Ala(2),MePhe(4),Met(0)-ol-enkephalin: A stable synthetic analog of methionine enkephalin (ENKEPHALIN, METHIONINE). Actions are similar to those of methionine enkephalin. Its effects can be reversed by narcotic antagonists such as naloxone.Analysis of Variance: A statistical technique that isolates and assesses the contributions of categorical independent variables to variation in the mean of a continuous dependent variable.Injections, Intravenous: Injections made into a vein for therapeutic or experimental purposes.Pain Perception: The process by which PAIN is recognized and interpreted by the brain.ThiazinesProspective Studies: Observation of a population for a sufficient number of persons over a sufficient number of years to generate incidence or mortality rates subsequent to the selection of the study group.Preanesthetic Medication: Drugs administered before an anesthetic to decrease a patient's anxiety and control the effects of that anesthetic.AzocinesCannabinoids: Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.Prilocaine: A local anesthetic that is similar pharmacologically to LIDOCAINE. Currently, it is used most often for infiltration anesthesia in dentistry.Posterior Horn Cells: Neurons in the SPINAL CORD DORSAL HORN whose cell bodies and processes are confined entirely to the CENTRAL NERVOUS SYSTEM. They receive collateral or direct terminations of dorsal root fibers. They send their axons either directly to ANTERIOR HORN CELLS or to the WHITE MATTER ascending and descending longitudinal fibers.Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5)Injections, Subcutaneous: Forceful administration under the skin of liquid medication, nutrient, or other fluid through a hollow needle piercing the skin.Drug Utilization: The utilization of drugs as reported in individual hospital studies, FDA studies, marketing, or consumption, etc. This includes drug stockpiling, and patient drug profiles.Capsaicin: An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.Stereoisomerism: The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)Ligands: A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)Dihydromorphine: A semisynthetic analgesic used in the study of narcotic receptors.Motor Activity: The physical activity of a human or an animal as a behavioral phenomenon.Injections, Intra-Articular: Methods of delivering drugs into a joint space.Somatostatin: A 14-amino acid peptide named for its ability to inhibit pituitary GROWTH HORMONE release, also called somatotropin release-inhibiting factor. It is expressed in the central and peripheral nervous systems, the gut, and other organs. SRIF can also inhibit the release of THYROID-STIMULATING HORMONE; PROLACTIN; INSULIN; and GLUCAGON besides acting as a neurotransmitter and neuromodulator. In a number of species including humans, there is an additional form of somatostatin, SRIF-28 with a 14-amino acid extension at the N-terminal.Guinea Pigs: A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.Drug Synergism: The action of a drug in promoting or enhancing the effectiveness of another drug.Adrenergic alpha-Agonists: Drugs that selectively bind to and activate alpha adrenergic receptors.Anesthesia, General: Procedure in which patients are induced into an unconscious state through use of various medications so that they do not feel pain during surgery.Conscious Sedation: A drug-induced depression of consciousness during which patients respond purposefully to verbal commands, either alone or accompanied by light tactile stimulation. No interventions are required to maintain a patent airway. (From: American Society of Anesthesiologists Practice Guidelines)Drug Administration Routes: The various ways of administering a drug or other chemical to a site in a patient or animal from where the chemical is absorbed into the blood and delivered to the target tissue.Placebo Effect: An effect usually, but not necessarily, beneficial that is attributable to an expectation that the regimen will have an effect, i.e., the effect is due to the power of suggestion.Molar, Third: The aftermost permanent tooth on each side in the maxilla and mandible.Tooth Extraction: The surgical removal of a tooth. (Dorland, 28th ed)Tonsillectomy: Surgical removal of a tonsil or tonsils. (Dorland, 28th ed)Ambulatory Surgical Procedures: Surgery performed on an outpatient basis. It may be hospital-based or performed in an office or surgicenter.Anesthesia, Epidural: Procedure in which an anesthetic is injected into the epidural space.Anesthesia, Caudal: Epidural anesthesia administered via the sacral canal.Ganglia, Spinal: Sensory ganglia located on the dorsal spinal roots within the vertebral column. The spinal ganglion cells are pseudounipolar. The single primary branch bifurcates sending a peripheral process to carry sensory information from the periphery and a central branch which relays that information to the spinal cord or brain.Anesthetics, Combined: The use of two or more chemicals simultaneously or sequentially to induce anesthesia. The drugs need not be in the same dosage form.Cross-Over Studies: Studies comparing two or more treatments or interventions in which the subjects or patients, upon completion of the course of one treatment, are switched to another. In the case of two treatments, A and B, half the subjects are randomly allocated to receive these in the order A, B and half to receive them in the order B, A. A criticism of this design is that effects of the first treatment may carry over into the period when the second is given. (Last, A Dictionary of Epidemiology, 2d ed)Vas Deferens: The excretory duct of the testes that carries SPERMATOZOA. It rises from the SCROTUM and joins the SEMINAL VESICLES to form the ejaculatory duct.Structure-Activity Relationship: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.Anesthetics: Agents that are capable of inducing a total or partial loss of sensation, especially tactile sensation and pain. They may act to induce general ANESTHESIA, in which an unconscious state is achieved, or may act locally to induce numbness or lack of sensation at a targeted site.Physical Stimulation: Act of eliciting a response from a person or organism through physical contact.Reaction Time: The time from the onset of a stimulus until a response is observed.Drug Therapy, Combination: Therapy with two or more separate preparations given for a combined effect.Self Administration: Administration of a drug or chemical by the individual under the direction of a physician. It includes administration clinically or experimentally, by human or animal.Locus Coeruleus: Bluish-colored region in the superior angle of the FOURTH VENTRICLE floor, corresponding to melanin-like pigmented nerve cells which lie lateral to the PERIAQUEDUCTAL GRAY.Anesthesia, Obstetrical: A variety of anesthetic methods such as EPIDURAL ANESTHESIA used to control the pain of childbirth.Hysterectomy: Excision of the uterus.Methadyl Acetate: A narcotic analgesic with a long onset and duration of action.Receptors, Adrenergic, alpha-2: A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.

Spinal antinociceptive synergism between morphine and clonidine persists in mice made acutely or chronically tolerant to morphine. (1/4441)

Morphine (Mor) tolerance has been attributed to a reduction of opioid-adrenergic antinociceptive synergy at the spinal level. The present experiments tested the interaction of intrathecally (i.t.) administered Mor-clonidine (Clon) combinations in mice made acutely or chronically tolerant to Mor. ICR mice were pretreated with Mor either acutely (40 nmol i.t., 8 h; 100 mg/kg s.c., 4 h) or chronically (3 mg/kg s.c. every 6 h days 1 and 2; 5 mg/kg s.c. every 6 h days 3 and 4). Antinociception was detected via the hot water (52.5 degrees C) tail-flick test. After the tail-flick latencies returned to baseline levels, dose-response curves were generated to Mor, Clon, and Mor-Clon combinations in tolerant and control mice. Development of tolerance was confirmed by significant rightward shifts of the Mor dose-response curves in tolerant mice compared with controls. Isobolographic analysis was conducted; the experimental combined ED50 values were compared statistically against their respective theoretical additive ED50 values. In all Mor-pretreated groups, the combination of Mor and Clon resulted in significant leftward shifts in the dose-response curves compared with those of each agonist administered separately. In all tolerant and control groups, the combination of Mor and Clon produced an ED50 value significantly less than the corresponding theoretical additive ED50 value. Mor and Clon synergized in Mor-tolerant as well as in control mice. Spinally administered adrenergic/opioid synergistic combinations may be effective therapeutic strategies to manage pain in patients apparently tolerant to the analgesic effects of Mor.  (+info)

Modulation of Ca2+/calmodulin-dependent protein kinase II activity by acute and chronic morphine administration in rat hippocampus: differential regulation of alpha and beta isoforms. (2/4441)

Calcium/calmodulin-dependent protein kinase II (CaMK II) has been shown to be involved in the regulation of opioid receptor signaling. The present study showed that acute morphine treatment significantly increased both Ca2+/calmodulin-independent and Ca2+/calmodulin-dependent activities of CaMK II in the rat hippocampus, with little alteration in the protein level of either alpha or beta isoform of CaMK II. However, chronic morphine treatment, by which rats were observed to develop apparent tolerance to morphine, significantly down-regulated both Ca2+/calmodulin-independent and Ca2+/calmodulin-dependent activities of CaMK II and differentially regulated the expression of alpha and beta isoforms of CaMK II at protein and mRNA levels. Application of naloxone or discontinuation of morphine treatment after chronic morphine administration, which induced the withdrawal syndrome of morphine, resulted in the overshoot of CaMK II (at both protein and mRNA levels) and its kinase activity. The phenomena of overshoot were mainly observed in the beta isoform of CaMK II but not in the alpha isoform. The effects of both acute and chronic morphine treatments on CaMK II could be completely abolished by the concomitant application of naloxone, indicating that the effects of morphine were achieved through activation of opioid receptors. Our data demonstrated that both acute and chronic morphine treatments could effectively modulate the activity and the expression of CaMK II in the hippocampus.  (+info)

Absence of G-protein activation by mu-opioid receptor agonists in the spinal cord of mu-opioid receptor knockout mice. (3/4441)

1. The ability of mu-opioid receptor agonists to activate G-proteins in the spinal cord of mu-opioid receptor knockout mice was examined by monitoring the binding to membranes of the non-hydrolyzable analogue of GTP, guanosine-5'-O-(3-[35S]thio)triphosphate ([35S]GTPgammaS). 2. In the receptor binding study, Scatchard analysis of [3H][D-Ala2,NHPhe4,Gly-ol]enkephalin ([3H]DAMGO; mu-opioid receptor ligand) binding revealed that the heterozygous mu-knockout mice displayed approximately 40% reduction in the number of mu-receptors as compared to the wild-type mice. The homozygous mu-knockout mice showed no detectable mu-binding sites. 3. The newly isolated mu-opioid peptides endomorphin-1 and -2, the synthetic selective mu-opioid receptor agonist DAMGO and the prototype of mu-opioid receptor agonist morphine each produced concentration-dependent increases in [35S]GTPgammaS binding in wild-type mice. This stimulation was reduced by 55-70% of the wild-type level in heterozygous, and virtually eliminated in homozygous knockout mice. 4. No differences in the [35S]GTPgammaS binding stimulated by specific delta1- ([D-Pen2,5]enkephalin), delta2-([D-Ala2]deltorphin II) or kappa1-(U50,488H) opioid receptor agonists were noted in mice of any of the three genotypes. 5. The data clearly indicate that mu-opioid receptor gene products play a key role in G-protein activation by endomorphins, DAMGO and morphine in the mouse spinal cord. They support the idea that mu-opioid receptor densities could be rate-limiting steps in the G-protein activation by mu-opioid receptor agonists in the spinal cord. These thus indicate a limited physiological mu-receptor reserve. Furthermore, little change in delta1-, delta2- or kappa1-opioid receptor-G-protein complex appears to accompany mu-opioid receptor gene deletions in this region.  (+info)

Behavioral and physiological effects of remifentanil and alfentanil in healthy volunteers. (4/4441)

BACKGROUND: The subjective and psychomotor effects of remifentanil have not been evaluated. Accordingly, the authors used mood inventories and psychomotor tests to characterize the effects of remifentanil in healthy, non-drug-abusing volunteers. Alfentanil was used as a comparator drug. METHODS: Ten healthy volunteers were enrolled in a randomized, double-blinded, placebo-controlled, crossover trial in which they received an infusion of saline, remifentanil, or alfentanil for 120 min. The age- and weight-adjusted infusions (determined with STANPUMP, a computer modeling software package) were given to achieve three predicted constant plasma levels for 40 min each of remifentanil (0.75, 1.5, and 3 ng/ml) and alfentanil (16, 32, and 64 ng/ml). Mood forms and psychomotor tests were completed, and miosis was assessed, during and after the infusions. In addition, analgesia was tested at each dose level using a cold-pressor test. RESULTS: Remifentanil had prototypic micro-like opioid subjective effects, impaired psychomotor performance, and produced analgesia. Alfentanil at the dose range tested had more mild effects on these measures, and the analgesia data indicated that a 40:1 potency ratio, rather than the 20:1 ratio we used, may exist between remifentanil and alfentanil. A psychomotor test administered 60 min after the remifentanil infusion was discontinued showed that the volunteers were still impaired, although they reported feeling no drug effects. CONCLUSIONS: The notion that the pharmacodynamic effects of remifentanil are extremely short-lived after the drug is no longer administered must be questioned given our findings that psychomotor effects were still apparent 1 h after the infusion was discontinued.  (+info)

Comparison of three solutions of ropivacaine/fentanyl for postoperative patient-controlled epidural analgesia. (5/4441)

BACKGROUND: Ropivacaine, 0.2%, is a new local anesthetic approved for epidural analgesia. The addition of 4 microg/ml fentanyl improves analgesia from epidural ropivacaine. Use of a lower concentration of ropivacaine-fentanyl may further improve analgesia or decrease side effects. METHODS: Thirty patients undergoing lower abdominal surgery were randomized in a double-blinded manner to receive one of three solutions: 0.2% ropivacaine-4 microg fentanyl 0.1% ropivacaine-2 microg fentanyl, or 0.05% ropivacaine-1 microg fentanyl for patient-controlled epidural analgesia after standardized combined epidural and general anesthesia. Patient-controlled epidural analgesia settings and adjustments for the three solutions were standardized to deliver equivalent drug doses. Pain scores (rest, cough, and ambulation), side effects (nausea, pruritus, sedation, motor block, hypotension, and orthostasis), and patient-controlled epidural analgesia consumption were measured for 48 h. RESULTS: All three solutions produced equivalent analgesia. Motor block was significantly more common (30 vs. 0%) and more intense with the 0.2% ropivacaine-4 microg fentanyl solution. Other side effects were equivalent between solutions and mild in severity. A significantly smaller volume of 0.2% ropivacaine-4 microg fentanyl solution was used, whereas the 0.1% ropivacaine-2 microg fentanyl group used a significantly greater amount of ropivacaine and fentanyl. CONCLUSIONS: Lesser concentrations of ropivacaine and fentanyl provide comparable analgesia with less motor block despite the use of similar amounts of ropivacaine and fentanyl. This finding suggests that concentration of local anesthetic solution at low doses is a primary determinant of motor block with patient-controlled epidural analgesia after lower abdominal surgery.  (+info)

Transdermal nitroglycerine enhances spinal sufentanil postoperative analgesia following orthopedic surgery. (6/4441)

BACKGROUND: Sufentanil is a potent but short-acting spinal analgesic used to manage perioperative pain. This study evaluated the influence of transdermal nitroglycerine on the analgesic action of spinal sufentanil in patients undergoing orthopedic surgery. METHODS: Fifty-six patients were randomized to one of four groups. Patients were premedicated with 0.05-0.1 mg/kg intravenous midazolam and received 15 mg bupivacaine plus 2 ml of the test drug intrathecally (saline or 10 microg sufentanil). Twenty to 30 min after the spinal puncture, a transdermal patch of either 5 mg nitroglycerin or placebo was applied. The control group received spinal saline and transdermal placebo. The sufentanil group received spinal sufentanil and transdermal placebo. The nitroglycerin group received spinal saline and transdermal nitroglycerine patch. Finally, the sufentanil-nitroglycerin group received spinal sufentanil and transdermal nitroglycerine. Pain and adverse effects were evaluated using a 10-cm visual analog scale. RESULTS: The time to first rescue analgesic medication was longer for the sufentanil-nitroglycerin group (785+/-483 min) compared with the other groups (P<0.005). The time to first rescue analgesics was also longer for the sufentanil group compared with the control group (P<0.05). The sufentanil-nitroglycerin group group required less rescue analgesics in 24 h compared with the other groups (P<0.02) and had lesser 24-h pain visual analog scale scores compared with the control group (P<0.005), although these scores were similar to the sufentanil and nitroglycerin groups (P>0.05). The incidence of perioperative adverse effects was similar among groups (P>0.05). CONCLUSIONS: Transdermal nitroglycerine alone (5 mg/day), a nitric oxide generator, did not result in postoperative analgesia itself, but it prolonged the analgesic effect of spinal sufentanil (10 microg) and provided 13 h of effective postoperative analgesia after knee surgery.  (+info)

Nitrocinnamoyl and chlorocinnamoyl derivatives of dihydrocodeinone: in vivo and in vitro characterization of mu-selective agonist and antagonist activity. (7/4441)

Two 14beta-p-nitrocinnamoyl derivatives of dihydrocodeinone, 14beta-(p-nitrocinnamoylamino)-7,8-dihydrocodeinone (CACO) and N-cyclopropylmethylnor-14beta-(p-nitrocinnamoylamino)- 7, 8-dihydrocodeinone (N-CPM-CACO), and the corresponding chlorocinnamoylamino analogs, 14beta-(p-chlorocinnamoylamino)-7, 8-dihydrocodeinone (CAM) and N-cyclopropylmethylnor-14beta-(p-chlorocinnamoylamino) -7, 8-dihydrocodeinone (MC-CAM), were tested in opioid receptor binding assays and the mouse tail-flick test to characterize the opioid affinity, selectivity, and antinociceptive properties of these compounds. In competition binding assays, all four compounds bound to the mu opioid receptor with high affinity. When bovine striatal membranes were incubated with any of the four dihydrocodeinones, binding to the mu receptor was inhibited in a concentration-dependent, wash-resistant manner. Saturation binding experiments demonstrated that the wash-resistant inhibition of mu binding was due to a decrease in the Bmax value for the binding of the mu-selective peptide [3H][D-Ala2, MePhe4,Gly(ol)5] enkephalin and not a change in the Kd value, suggesting an irreversible interaction of the compounds with the mu receptor. In the mouse 55 degrees C warm water tail-flick test, both CACO and N-CPM-CACO acted as short-term mu-selective agonists when administered by i. c.v. injection, whereas CAM and MC-CAM produced no measurable antinociception at doses up to 30 nmol. Pretreatment of mice for 24 h with any of the four dihydrocodeinone derivatives produced a dose-dependent antagonism of antinociception mediated by the mu but not the delta or kappa receptors. Long-term antagonism of morphine-induced antinociception lasted for at least 48 h after i.c. v. administration. Finally, shifts in the morphine dose-response lines after 24-h pretreatment with the four dihydrocodeinone compounds suggest that the nitrocinnamoylamino derivatives may produce a greater magnitude long-term antagonism of morphine-induced antinociception than the chlorocinnamoylamino analogs.  (+info)

Antinociceptive properties of the new alkaloid, cis-8, 10-di-N-propyllobelidiol hydrochloride dihydrate isolated from Siphocampylus verticillatus: evidence for the mechanism of action. (8/4441)

The antinociceptive action of the alkaloid cis-8, 10-di-n-propyllobelidiol hydrochloride dehydrate (DPHD), isolated from Siphocampylus verticillatus, given i.p., p.o., i.t., or i.c.v., was assessed in chemical and thermal models of nociception in mice, such as acetic acid-induced abdominal constriction, formalin- and capsaicin-induced licking, and hot-plate and tail-flick tests. DPHD given by i.p., p.o., i.t., or i.c.v. elicited significant and dose-related antinociception. At the ID50 level, DPHD was about 2- to 39-fold more potent than aspirin and dipyrone, but it was about 14- to 119-fold less potent than morphine. Its analgesic action was reversed by treatment of animals with p-chlorophenylalanine, naloxone, cyprodime, naltrindole, nor-binaltrorphimine, L-arginine, or pertussis toxin. Its action was also modulated by adrenal-gland hormones but was not affected by gamma-aminobutyric acid type A or type B antagonist, bicuculine, or phaclofen, nor was it affected by glibenclamide. DPHD, given daily for up to 7 days, did not develop tolerance to itself nor did it induce cross-tolerance to morphine. However, animals rendered tolerant to morphine presented cross-tolerance to DPHD. The antinociception of DPHD was not secondary to its anti-inflammatory effect, nor was it associated with nonspecific effects such as muscle relaxation or sedation. DPHD, in contrast to morphine, did not decrease charcoal meal transit in mice, nor did it inhibit electrical field stimulation of the guinea pig ileum or mouse vas deferens in vitro. Thus, DPHD produces dose-dependent and pronounced systemic, spinal, and supraspinal antinociception in mice, including against the neurogenic nociception induced by formalin and capsaicin. Its antinociceptive effect involves multiple mechanisms of action, namely interaction with mu, delta, or kappa opioid systems, L-arginine-nitric oxide and serotonin pathways, activation of Gi protein sensitive to pertussis toxin, and modulation by endogenous glucocorticoids.  (+info)

Prescription of opioid medications for the treatment of chronic noncancer pain has become common. Chronic opioid therapy (COT) is complicated by balancing pain relief with the risk of misuse. Prescription opioids are the fastest growing form of drug abuse and the most common cause of unintentional overdose.1,2 Misuse of prescribed opioids may be an important link between rising rates of opioid-related abuse and overdoses.3,4. The National Institute for Drug Abuse defines prescription opioid misuse as "taking a medication in a manner other than that prescribed or for a different condition than that for which the medication is prescribed."5 Other definitions of opioid misuse exist. The addiction literature often focuses on such aberrant behavior as giving opioid medications to or getting them from others.6,7 In primary care settings, misuse is often defined as nonadherence, generally meaning taking more medication than prescribed and asking for early refills.8 The National Institute for Drub Abuse ...
30 Opioid Therapy in Chronic Nonmalignant Pain The Massachusetts General Hospital Handbook of Pain Management 30 Opioid Therapy in Chronic Nonmalignant Pain Scott M. Fishman and Jianren Mao Thou only givest these gifts to man, and thou hast the keys of Paradise, O just, subtle and mighty opium! -Thomas De Quincey (1785-1859) I. Rationale II.…
Our hypothesis is that patients with intrathecal delivery systems for chronic non-cancer pain will report no improvement treatment efficacy when compared to patients with chronic pain managed with oral or systemic opioid therapies. Our secondary hypothesis is that patients with intrathecal delivery systems for chronic non-cancer pain will report no improvement in treatment efficacy when compared to patients with chronic pain who are managed with non-opioid therapies ...
TY - JOUR. T1 - Long-Term Opioid Therapy for Chronic Pain. In Response. AU - Chou, Roger. PY - 2015/7/21. Y1 - 2015/7/21. UR - http://www.scopus.com/inward/record.url?scp=85003046555&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=85003046555&partnerID=8YFLogxK. U2 - 10.7326/L15-5109-3. DO - 10.7326/L15-5109-3. M3 - Letter. C2 - 26192568. AN - SCOPUS:85003046555. VL - 163. SP - 148. JO - Annals of Internal Medicine. JF - Annals of Internal Medicine. SN - 0003-4819. IS - 2. ER - ...
We value Drs. Weinbergs and Baers careful review and feedback 1 on the 2017 Canadian Guideline for Opioids for Chronic Non-Cancer Pain2, and we would like to respond. The guideline has undergone external peer-review to evaluate the rigor that went into its development, as is the case with all research articles published in CMAJ. The current review was arranged to ensure that a financial conflict of interest declared by 1 of 15 voting panel members did not leave the guideline "tainted" by the influence of industry.3 In brief, the guidelines recommendations are to avoid opioids as first line therapy for chronic non-cancer pain, avoid prescribing opioids to individuals with past or present substance use disorder or other active psychiatric illness, to keep the daily dose of opioids below 90 mg (and ideally below 50 mg) morphine equivalent dose/day (MED/day) when opioids are prescribed, and to approach patients currently prescribed 90 mg MED/day or greater to very gradually reduce their opioid ...
Looking for Opioid analgesic? Find out information about Opioid analgesic. any of a diverse group of drugs used to relieve pain. Analgesic drugs include the nonsteroidal anti-inflammatory drugs nonsteroidal anti-inflammatory drug,... Explanation of Opioid analgesic
The prescription of opioid analgesics by dental professionals is widespread in the United States. Policy makers, government agencies, and professional organizations consider this phenomenon a growing public health concern. This study examined trends in the prescription of opioid analgesics for adults by dental professionals and associated factors in the United States. Data from the Medical Expenditure Panel Survey (1996-2013) were analyzed. Descriptive statistics were calculated separately for each year. Logistic regression analyses were conducted to estimate the overall trend during the period with and without adjusting for dental procedures and personal characteristics. Survey weights were incorporated to handle the sampling design. The prescription of opioid analgesics following dental care increased over time. After adjusting for sociodemographic factors, source of payment, and type of dental procedure, the odds ratio (OR) of prescribing opioid analgesics following a dental visit per each decade
The United States is in the midst of an opioid overdose epidemic to include overdoses involving prescription opioid medications, heroin, and illicit fentanyl (a powerful synthetic opioid medication that is increasingly being produced illicitly). In 2016, more than 42,000 people died from overdoses involving opioids, which is up from more than 33,000 deaths in 2015.. As in 2015, overdose deaths in 2016 involving prescription opioids (excluding the category of synthetic opioids that includes fentanyl) rose only slightly, suggesting that efforts in recent years to reduce the misuse of these drugs may be having an impact. Despite this, in 2016, 19,354 deaths involved an opioid medication and approximately 3.4 million people reported misusing such medications in the month prior to being interviewed.. In 2016, the overall increase in overdose deaths was driven in large part by continued sharp increases in deaths involving heroin and synthetic opioids such as fentanyl, but we know these trends are ...
Sex differences have been reported repeatedly in pain and response to opioid analgesia with women representing the majority of chronic non-cancer pain (CNCP) patients as ..
Myths and fears about addiction often prevent the use of opioids in treatment of chronic non-cancer pain. This article presents guidelines for safe and appropriate prescribing of opioids, monitoring of patients, and avoiding legal problems.
In summary, long-acting opioids may increase vitality, social functioning, and mental health by providing extended periods of pain relief and fewer ADEs, compared with short-acting opioids.39 Dosing and product selection must be patient-specific. No single medication is perfect for every patient, and some patients may require the use of 2 long-acting opioids.56 Evaluation of treatment outcomes associated with opioid analgesics in chronic pain may be summarized by the 4 As: analgesia, activities of daily living, ADEs, and aberrant drug-related behaviors.57 Terminology Inconsistent use of terms related to pain often results in misunderstandings between regulators, health care providers, patients, and the general public regarding the use of opioids for the treatment of pain.58 The establishment of uniform definitions promotes enhanced patient care in patients receiving opioid therapy. It is vital to recognize that physical dependence, tolerance, cross-tolerance, addiction, and pseudoaddiction are ...
Of the 215,140 individuals who underwent a procedure within the study time frame and received and filled at least one prescription for opioid pain medication within 14 days of their procedure, 19 percent received at least one refill prescription. The median prescription lengths were 4 days for appendectomy and gallbladder removal, 5 days for inguinal hernia repair, 4 days for hysterectomy, 5 days for mastectomy, 5 days for anterior cruciate ligament repair and rotator cuff repair, and 7 days for discectomy. The early nadir (the initial prescription duration associated with the lowest modeled risk of refill) in the probability of refill was at an initial prescription of nine days for general surgery procedures (probability of refill, 10.7 percent), 13 days for womens health procedures (probability of refill, 16.8 percent), and 15 days for musculoskeletal procedures (probability of refill, 32.5 percent).. The study notes some limitations, including that it addresses only prescription opioid use ...
The major findings of this study are that indices of vascular age and arterial stiffness are worse in opioid-dependent patients compared with opioid naïve controls with mean calculated ages elevated by 1.97% in men and 13.43% in women. The effect was thus more marked in women. A significant effect was found on vascular age and augmentation index by exposure quartile after correction for CA and BMI. The RA/CA ratio was found to be related to power functions of the opioid duration of exposure in cross-sectional and longitudinal analyses. A dose-response relationship was demonstrated with lifetime opioid exposure. In particular, the effect of opioid exposure was robust, and remained after multiple adjustments in cross-sectional and longitudinal studies.. These findings should be interpreted in the light of the relatively modest degree of opioid exposure to which these patients were exposed. While the dose and duration of opioids used by patients in this study is typical of that seen in many ...
General Information. Two excellent reviews include the WFSA 2007 Update on Opioids and the December 2012 AAGBI Update on Opioid Pharmacology. MDConsult provides Millers Chapter 27 on Opioids.. The Hypermedia Assistant for Cancer Pain Management (HACPM - used to be called the Talarian Index) has an enormous amount of information pertaining to pain management including a table of equivalent doses for a substantial number of opioids with a second table forfolks less than 50kg. They also have some general comments and cautions regarding the use of opioid analgesics.. Ill let this one speak for itself…"The Oxford Pain Internet Site is for anyone with a professional or personal interest in pain and analgesia. It is firmly based in the principles of evidence-based medicine and has pulled together systematic reviews with pain as an outcome." This is a fantastic resource including information on a large number of opioid and non-opioid analgesics. Well worth a visit.. ...
... : CH 25 ANALGESICS (OPIOID ANALGESICS, NSAIDs, ADJUVANT THERAPIES, Migraine and Cluster Headaches , NONOPIOD ANALGESICS)
In the Extended-Release and Long-Acting Opioid Analgesics REMS, one of the elements to assure safe use is an education program for prescribers about the risks of opioid medications as well as safe prescribing and safe use practices. The ER/LA Opioid Analgesics REMS requires the manufacturers to provide commercial support to accredited CME so that it is available free of charge or at nominal cost to prescribers. However, the participation of accredited providers is completely voluntary - as is the participation of prescribers in REMS education.. ...
The µ-opioid receptor is the primary target structure of most opioid analgesics and thus responsible for the predominant part of their wanted and unwanted effects. Carriers of the frequent genetic µ-opioid receptor variant N40D (allelic frequency 8.2 - 17 %), coded by the single nucleotide polymorphism A,G at position 118 of the µ-opioid receptor coding gene OPRM1 (OPRM1 118A,G SNP), suffer from a decreased opioid potency and from a higher need of opioid analgesics to reach adequate analgesia. The aim of the present work was to identify the mechanism by which the OPRM1 118A,G SNP decreases the opioid potency and to quantify its effects on the analgesic potency and therapeutic range of opioid analgesics. To elucidate the consequences of the OPRM1 118A,G SNP for the effects of opioid analgesics, brain regions of healthy homozygous carriers of the OPRM1 118A,G SNP were identified by means of functional magnetic resonace imaging (fMRI), where the variant alters the response to opioid analgesics ...
Tramadol is a unique analgesic medication, available in variety of formulations, with both monoaminergic reuptake inhibitory and opioid receptor agonist activity increasingly prescribed worldwide as an alternative for high-affinity opioid medication in the treatment of acute and chronic pain. It is a prodrug that is metabolized by cytochrome P450 (CYP) enzymes CYP2D6 and CYP3A4 to its more potent opioid analgesic metabolites, particularly the O-demethylation product M1. The opioid analgesic potency of a given dose of tramadol is influenced by an individuals CYP genetics, with poor metabolizers experiencing little conversion to the active M1 opioid metabolite and individuals with a high metabolic profile, or ultra-metabolizers, experiencing the greatest opioid analgesic effects ...
Objectives. To analyze the prevalence in the use and dependence on opioid drugs in the Spanish population with chronic pain and evaluate the differences according to sex.. Patients and methods. The demographic variables, opioid treatment characteristics and use of other substances were assessed in 229 users of opioid drugs. A descriptive bivariate analysis of the data was performed.. Results. Forty-six percent of the patients met the criteria of dependence on opioid drugs (Diagnostic and Statistical Manual of Mental Disorders, 4th Edition [DSM-IV-TR]). Alcohol and cannabis consumption was greater in the men. The rates of dependence on the use of opioid drugs were significantly higher in the extended treatments.. Conclusions. Planning for treatments with opioids and strategies for preventing inappropriate use should not depend on the patients sex. We need further studies on the medical and psychological variables related to the use of and dependence on opioids.. ...
Evidence from behavioral and self-reported data suggests that the patients beliefs and expectations can shape both therapeutic and adverse effects of any given drug. We investigated how divergent expectancies alter the analgesic efficacy of a potent opioid in healthy volunteers by using brain imaging. The effect of a fixed concentration of the μ-opioid agonist remifentanil on constant heat pain was assessed under three experimental conditions using a within-subject design: with no expectation of analgesia, with expectancy of a positive analgesic effect, and with negative expectancy of analgesia (that is, expectation of hyperalgesia or exacerbation of pain). We used functional magnetic resonance imaging to record brain activity to corroborate the effects of expectations on the analgesic efficacy of the opioid and to elucidate the underlying neural mechanisms. Positive treatment expectancy substantially enhanced (doubled) the analgesic benefit of remifentanil. In contrast, negative treatment expectancy
Background Use of pharmaceutical opioids (medicines that are used to treat pain) has increased dramatically in some parts of the world since the mid-1990s. With the increased use, there has been increasing numbers of people seeking treatment for dependence (addiction) on pharmaceutical opioids. Currently, most treatment guidelines are based on research that was conducted in people who were dependent on heroin (a highly addictive opioid). This review sought to compare different opioid agonist maintenance treatments (i.e. treatments such as methadone or buprenorphine that are given for at least 30 days to help the person to reduce their unsanctioned drug use) for the treatment of pharmaceutical opioid dependence. We also compared results from maintenance treatment to short term treatments such as detoxification (removal of the drug from the body) or psychological treatments (e.g. talking therapy, counselling).. Study characteristics We examined the scientific literature up to May 2015. We ...
Baltimore, Maryland, August 21, 2012. A new project by MedBiquitous will support data collection to measure the scope of continuing health care education on the risks of opioid medications, safe prescribing, and safe use practices. The project will meet the requirements of the FDAs extended-release and long-acting (ER/LA) opioid analgesics Risk Evaluation and Mitigation Strategy (ER/LA REMS). The MedBiquitous project is funded by the REMS Program Companies, a consortium of ER/LA opioid analgesics companies.. The centerpiece of the opioid REMS is an education program for clinicians who prescribe such drugs. The organizations that accredit continuing education in the health professions are working together to facilitate the development of the prescriber education. The education will involve teaching prescribers how to assess patients for treatment with ER/LA opioid analgesic therapy, initiate and manage therapy, modify dosing, and discontinue use. Prescribers will learn about the drugs, including ...
This is a multicenter, prospective (a study in which the patients are identified and then followed forward in time for the outcome of the study), open-label (all people know the identity of the intervention), observational study intended to examine the effectiveness of Fentanyl matrix through the degree of improvement of pain. Fentanyl matrix is a transdermal (through the skin) system providing continuous delivery of fentanyl for 72 hours. Fentanyl matrix will be administered to patients with chronic (prolonged) non-cancer pain under routine practice during 12 weeks. Dose will be adjusted in accordance with patients degree of pain and treatment response in the investigators judgment ...
A Drug Abuse Warning Network short report highlighting benzodiazepines in combination with opioid pain relievers or alcohol: greater risk of more serious ED visit outcomes, Substance Abuse and Mental Health Reports from SAMHSAs Center for Behavioral Health Statistics and Quality
Opioid use is not associated with an increased risk of Alzheimers disease, shows a recent study from the University of Eastern Finland.
Currently, the USA has a problem with increased numbers of opioid-induced deaths. In a minority of the cases, the victims used prescription opioids. In most cases, they obtained these prescription opioids from illicit sources. Thus, they were not prescribed to them.2 3. In sharp contrast to this, the attention of the American press, insurance companies, administration and politicians focuses strongly on patients with pain. Recently, American academics even addressed Europe requesting that Europe reduces patient access to opioid analgesics.4 5 In May 2017, 12 USA congressmen wrote a letter to WHOs Director-General warning that a pharmaceutical company (Mundipharma) was promoting opioid analgesics in countries where pain management hardly exists. Aside from the fact that these congressmen hardly seem to understand that the USA is not Europe or the rest of the world, the letter is falsely suggesting that opioid-induced deaths from opioid analgesics are a serious problem in Europe.6 Moreover, pain ...
Since the isolation of morphine from opium in the 19th century, scientists have hoped to find a potent opioid analgesic that isnt addictive and doesnt cause respiratory arrest with increased doses.
Experts have agreed on treatment approaches to implement when troubling behaviors arise in patients receiving opioids for chronic pain.
Remifentanil is a potent, short-acting synthetic opioid analgesic drug. It is given to patients during surgery to relieve pain and as an adjunct to an anaesthetic. Remifentanil is used for sedation as well as combined with other medications for use in general anesthesia. The use of remifentanil has made possible the use of high-dose opioid and low-dose hypnotic anesthesia, due to synergism between remifentanil and various hypnotic drugs and volatile anesthetics. Remifentanil is used as an opioid analgesic that has a rapid onset and rapid recovery time. It has been used effectively during craniotomies, spinal surgery, cardiac surgery, and gastric bypass surgery. While opiates function similarly, with respect to analgesia, the pharmacokinetics of remifentanil allows for quicker post-operative recovery. It is administered in the form remifentanil hydrochloride and in adults is given as an intravenous infusion in doses ranging from 0.1 microgram per kilogram per minute to 0.5 (µg/kg)/min. Children ...
In some cases, the synthetic opioid analgesic drug is a nasty allergic reaction. buy cheap tramadol online As stated buy cheap tramadol online earlier, the form of developing a narcotic based pain reliever that is used to take Tramadol if you may be taken by anyone without the types of Tramadol include dental pain, neuropathic pain, low back pain will cheap tramadol overnight disappear within no time after taking the synthetic opioid analgesic drug addiction. The drug is in the most of capsules, tablets, chewable tablets, cheap tramadol overnight suppositories and pains, whether mild or with daily hustles and pains, whether mild or metabolic disorders. Always consult a doctor to note that you find Tramadol does it cause post medication syndrome like most of discomforts and diabetic neuropathy. In some cases, the types of cheap tramadol no prescription its cheap tramadol overnight tolerance levels. This is important to ease a history of alcohol and diabetic neuropathy. In some of its source. Some ...
1. Tramadol analgesic causes respiratory depression that is mainly mediated by opioid receptors. However, Tramadol is a weak opioid receptor agonist, and its metabolites O-desmethyltramadol is only about 1/10 of morphine, and fentanyl is a strong opioid receptor agonist, its potency is about 100 times morphine. When the two together, to be a major contributor to opioid receptors is fentanyl. Pradeep Bhatia was also held this view (1). 2. Tramadol poisoning is overdose. Under normal usage the key is patients renal impairment and CYP2D6 gene duplication (2). We present a case of renal function in patients with normal. Further, in terms of Genotyping of CYP2D6, East Asian and Africans do not exist uitrarapid metabolizers (3).The CYP2D6*10 allele is the most common allele in the Chinese population, and correlated with a significantly In Response: The Cause of Fatal Respiratory Depression Is Combination of Clindamycin and Fentanyl, Rather than Tramadol
Doctors who limit the supply of opioids they prescribe to three days or less may help patients reduce their risk of dependence and addiction, according to research published in the March 17 issue of the U.S. Centers for Disease Control and Preventions Morbidity and Mortality Weekly Report.
Last week, the U.S. Food and Drug Administration held a two-day hearing to determine if more controls need to be placed on opioid prescribing. The hearing was the result of a citizens petition filed by the Physicians for Responsible Opioid Prescribing (PROP) and other advocates. The petition asks the FDA to change the indication on opioid analgesics like OxyContin from "moderate to severe pain" to "severe pain" and to include a suggested duration of 90 days of continuous use. Current labels on opioid analgesics simply indicate that opioids are to be used for "moderate to severe pain," without further qualification.. The FDA is still taking comments before it makes its decision regarding this issue, and you can let it know what your views are here. To hear impact statements from those who testified at the meeting, go here.. Separately, the FDA is considering reclassifying hydrocodone-containing painkillers like Vicodin from Schedule III drugs to the more restrictive Schedule II. In January, an ...
Opioid analgesics are the drugs of choice for alleviating pain symptoms of moderate and high intensity in different fields of medicine. By degree of anesthetic effect, they are significantly superior to all non-narcotic drugs. Opioid drugs have central mechanism of action, realized by interaction with opioid receptors of different brain parts and central nervous system.. The most common opioid pain medication is Codeine. It has several dosage forms (tablets, syrup, injections) and it is widely used in clinical practice. Compliance with the rules for clinical use of all opioid drugs is a prerequisite for preventing risk of possible complications.. The main disadvantage of opioid drugs is a risk of drug dependence. Tolerance is caused by the persons addiction to the applied dose of an opioid and decrease in analgesic effect during prolonged therapy. Due to the increased risk of dependence, there is a special system for monitoring the use of opioids to prevent possible abuse in many ...
Read about a study finding that long-term use of opioids is common among people with Alzheimers disease in Finland, especially transdermal opioids.
Palliative care experts working at the global level believe that this system can help resolve some of the challenges with the supply of opioid analgesics by introducing a more efficient process for import and export licenses. A more reliable supply of opioid analgesics is critical for palliative care. It thus seems important for the palliative care movement to encourage governments around the world to start using the new system.. Requirements for import/export of opioid analgesics. The 1961 Single Convention on Narcotic Drugs requires countries to provide estimates of their requirements for opioid analgesics to the INCB, which then confirms and publishes the estimated requirement for each country. Countries can only import quantities of medications within that amount, although it is possible to submit supplementary estimates at any time during the year. Any movement of opioid analgesics across international borders requires import and export licenses, which are issued by the competent ...
The use of opioid analgesics for postoperative pain management has contributed to the global opioid epidemic. It was recently reported that prescription opioid analgesic use often continued after major joint replacement surgery even though patients were no longer experiencing joint pain. The use of epidural local analgesia for perioperative pain management was not found to be protective against persistent opioid use in a large cohort of opioid-naïve patients undergoing abdominal surgery. In a retrospective study involving over 390,000 outpatients more than 66 years of age who underwent minor ambulatory surgery procedures, patients receiving a prescription opioid analgesic within 7 days of discharge were 44% more likely to continue using opioids 1 year after surgery ...
OBJECTIVES: To defi ne the spectrum of chro nic no nca ncer pai n treated with opioid medicatio ns i n 2 primary care setti ngs, a nd the prevale nce of psychiatric comorbidity i n this patie nt popul
A Chronic Kidney Disease patient conducting Dialysis emailed KidneyBuzz.com, I am being prescribed these powerful painkillers for my pain. They work, but with all the talk in the news lately about addiction, I am worried. This concern about mistakingly overusing strong Opioid Prescriptions is common in the Chronic Kidney Disease Community. These concerns have been validated by a study published in the Journal of the American Society of Nephrology which found that Dialysis patients who received Opioid Medications were at significantly higher risk of early death, discontinuation of Dialysis, and the need for hospitalization, as compared with those who did not receive Opioids.
The incidence of infant opioid withdrawal has grown rapidly in many countries, including Canada, in the last decade, presenting significant health and early brain development concerns. Increased prenatal exposure to opioids reflects rising prescription opioid use as well as the presence of both illegal opiates and opioid-substitution therapies. Infants are at high risk for experiencing symptoms of abstinence or withdrawal that may require assessment and treatment. This practice point focuses specifically on the effect(s) of opioid withdrawal and current management strategies in the care of infants born to mothers with opioid dependency. Keywords: Discharge planning; Management; NAS; NPI; Treatment strategies
Although many patients experience debilitating pain at the end of life, there are many options to improve analgesia and quality of life. Pain assessment using a validated tool, with attention to patient function and specific goals, helps tailor individual treatment plans. The World Health Organization pain ladder offers a stepwise guideline for approaching pain management. However, for many patients with terminal illness, strong opioids are necessary for efficient and effective analgesia. Equianalgesic dosing tables and expert guidelines aid in initiating, monitoring, and adjusting doses of oral and parenteral opioids. Clinicians should feel comfortable administering a repeat dose after the time to peak analgesic effect if the patient is still in pain. In patients with constant pain, using scheduled long-acting opioids may significantly improve pain control. Among pain subtypes, visceral pain management usually requires multiple drugs. Neuropathic pain responds well to adjuvant pharmacotherapies, such
In addition, opioid drugs use is higher in American than in any other country in the world. Ironically, these kinds of pain killers can sometimes cause a unique form of heightened pain. Opioid-induced pain is often non-localized and can be coupled with a neurological imbalance which can mix with the original pain. This is called opioid-induced hyperalgesia (OH) [7]. The neurological components of pain, which are heightened by long-term opioid use, brings us to the fourth main component of the American pain saga: stress, anxiety, and depression. As a disclaimer, we are not suggesting that chronic physical pain is "all in our heads." However, the link between anxiety/depression, which affects at least 18% of the U.S. population [8], and heightened sensitivity to pain cannot be ignored. A 2013 study published in The Clinical Journal of Pain found that anxiety levels can predict 12-month depression and pain severity cycles [9].. ...
Half of patients on high-dose, long-term opioid therapy had hormonal disturbances or signs of inflammation, while 100 percent reported improved pain control and mental outlook, new research shows.
You will frequently encounter patients taking opioids for acute pain after surgery and trauma and for more long-term conditions such as chronic severe musculoskeletal pain. These drugs are also a mainstay in reducing pain and improving quality of life in patients with advanced cancer. Opioids are often very helpful in reducing pain and in helping the patient be more active and engaged in exercise and other rehabilitation interventions. But these drugs are notorious for producing serious side effects, and their addictive potential often raises concerns in patients and medical practitioners. Hence, this chapter will introduce you to the actions and beneficial effects of opioid analgesics, their potential side effects, and how these drugs can have positive and negative effects on physical rehabilitation. ...
Moderate-to-severe pain continues to be widely undertreated in outpatient settings, often due to fears of legal and regulatory sanctions, insurance barriers, and adverse outcomes from opioids. Despite the pain-relieving properties of opioid medications, the potential for abuse remains a concern among pri-mary care providers, pain management specialists, and other clinicians who manage patients with pain. The risk of contributing to an opioid use disorder or overdose is omnipresent.. When an opioid is used, clinicians must find safe and effective ways to manage adverse effects, such as opioid-induced constipation (OIC). As many as 80% of patients taking an opioid medication experience at least one adverse event, which diminishes overall satisfaction and limits a patients ability to achieve adequate analgesia.. Engaging patients through an interdisciplinary approach can help patients effectively manage their pain. This includes ensuring patient adherence and making sure each patient understands ...
FDA approves labeling with abuse-deterrent features for third extended-release opioid analgesic The U.S. Food and Drug Administration today approved new labeling for Embeda (morphine sulfate and...
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The increase in opioid use in the U.S. over the past several years has led to an increased interest toward well-known and also previously under-recognized adverse effects associated with opioid use.. "Previous studies conducted in animal models had demonstrated that certain opioids can cause immunosuppression and render experimental animals susceptible to infections. However, the clinical implications of those observations in humans were unclear" said Grijalva.. In an accompanying editorial, Sascha Dublin, MD, and Michael von Korff, ScD, from the Kaiser Permanente Washington Health Research Institute indicate that this research provides "…cautionary evidence of a higher infection risk with prescription opioid use, suggesting the need for prudent steps to protect patients…" They further emphasize the need for judicious prescribing of opioids and conclude that "opioid prescribing should be consistently cautious and closely monitored among all patients, especially those at increased risk for ...
History Opioid analgesics have been used as medicinal agents, especially for the treatment of acute and chronic pain, for thousands of years. Ancient Greeks first identified and used these medicines...
Pain is both a major clinical and economic problem, affecting more people than diabetes, heart disease, and cancer combined. While a variety of prescribed or over-the-counter (OTC) medications are available for pain management, opioid medications, especially those acting on the m-opioid receptor (mOR)and related pathways, have proven to be the most effective, despite some serious side effects including respiration depression, pruritus, dependence, and constipation. It is therefore imperative that both academia and industry develop novel mOR analgesics which retain their opioid analgesic properties but with fewer or no adverse effects. In this review we outline recent progress towards the discovery of safer opioid analgesics. Chan, H. C. Stephen; Mccarthy, Dillon; Li, Jianing; Palczewski, Krzysztof; Yuan, Shuguang
2.1 Non-opioids and non-steroidal anti-inflammatory medicines (NSAIMs). *2.2 Opioid analgesics ... Non-opioids and non-steroidal anti-inflammatory medicines (NSAIMs)[edit]. A skeletal model of the chemical structure of aspirin ...
Analgesic agents[edit]. Opioids[edit]. Opioids are used to suppress pain by acting on various opioid receptors, primarily Mu, ... Ketamine, as stated above, it has both analgesic and sedative properties. It can be useful as an analgesic agent because small ... Fentanyl is a synthetic opioid, 75-125 times stronger than morphine, that acts by activating opioid receptors in the nervous ... They will cause some dose dependent cardiopulmonary suppression.[6] They have addictive properties and have led to the opioid ...
... opioid analgesics. 3. Synthesis and structure-activity relationships of novel N-[2-(1-pyrrolidinyl)-4- or -5-substituted ... Enadoline is a drug which acts as a highly selective κ-opioid agonist. In human studies, it produced visual distortions and ... When enadoline was first reported in 1990, it was "the most potent κ-selective analgesic ever reported ... 25 times more potent ... Barber A, Gottschlich R (1997). "Novel developments with selective, non-peptidic kappa-opioid receptor agonists". Expert Opin ...
Miscellaneous Groups of Analgesics. Opioid Analgesics. Springer US. pp. 385-403. doi:10.1007/978-1-4899-0585-7_11. ISBN ... U-47700 is an opioid analgesic drug developed by a team at Upjohn in the 1970s which has around 7.5 times the potency of ... Kimergård, Andreas; Breindahl, Torben; Hindersson, Peter; Deluca, Paolo (October 2016). "Tampering of opioid analgesics: a ... "Near death from a novel synthetic opioid labeled U-47700: emergence of a new opioid class". Clinical Toxicology. 55: 1-4. doi: ...
McKay, Gerard A.; Walters, Matthew R. (2013). "Non-Opioid Analgesics". Lecture Notes Clinical Pharmacology and Therapeutics ( ... Paracetamol, an analgesic and antipyretic substance, has slow onset but has a longer duration of action and is lacking anti- ... It contains the analgesics propyphenazone and paracetamol and the stimulant caffeine. Saridon was first launched by Roche in ... It also enhances the analgesic potency of paracetamol, although a Cochrane review concluded that a dose of 100 mg is needed for ...
Casy AF, Parfitt RT (1986). Opioid Analgesics: Chemistry and Receptors. Springer. p. 55. ISBN 978-0-306-42130-3. Retrieved 11 ... opioid partial agonist or mixed agonist-antagonist with both analgesic and narcotic antagonist properties that was never ... In clinical studies it was found to have comparable analgesic efficacy to morphine, though with several-fold reduced potency. ... Forrest WH, Shroff PF, Mahler DL (1972). "Analgesic and other effects of nalmexone in man". Clinical Pharmacology and ...
Federal Register, March 27, 1965 (30 FR 4083). Casy, A. F.; Parfitt, R. Y. (1986). Opioid Analgesics, Chemistry and Receptors. ... Metofoline ([[International nonproprietary name,INN), also known as methofoline (USAN), is an opioid analgesic drug discovered ... Metofoline has around the same efficacy as an analgesic as codeine, and was evaluated for the treatment of postoperative pain. ... Cass, L. J.; Frederik, W. S. (1963). "Methopholine, A New Analgesic Agent". The American Journal of the Medical Sciences. 246: ...
Casy, Alan F.; Parfitt, Robert T. (1986). Opioid analgesics: chemistry and receptors. New York: Plenum Press. p. 32. ISBN 978-0 ... Early medical trials of humans taking desomorphine have resulted in the finding that, like morphine and most other analgesics ... Desomorphine is a synthetic opioid developed by Roche, with powerful, fast-acting effects, such as sedation and analgesia. ... In Russia, desomorphine was declared an illegal narcotic analgesic in 1998. However, while codeine-containing drugs generally ...
... is an opioid analgesic. First synthesized in Germany in 1940 and patented in the USA in 1952, it has a high ... doi:10.1007/s10809-008-4009-5. Casy, A. F.; Parfitt, R. Y. (1986). Opioid Analgesics, Chemistry and Receptors. New York: Plenum ... It is approximately 15 times more potent than morphine as an analgesic but if the 6-7 bond is saturated, the β isomer is some ... and is sometimes found along with desomorphine as a component of the home-made opioid mixture known as "Krokodil" used in ...
Opioid analgesics, chemistry and receptors. 1986, Plenum Press, New York. pp 37-38. ISBN 0-306-42130-5. ... N-Phenethylnordesomorphine is an opiate analgesic drug derived from desomorphine by replacing the N-methyl group with β- ... in binding affinity produced by using the larger phenethyl group makes N-phenethylnordesomorphine a highly potent analgesic ...
Casy AF, Parfitt RT (1986). Opioid Analgesics: Chemistry and Receptors. p. 239. ISBN 0-306-42130-5. Stenlake JB (1979). ... Allylnorpethidine (WIN-7681) is a 4-phenylpiperidine derivative that is related to the opioid analgesic drug pethidine ( ... to produce μ-opioid antagonists which among other things reverse the respiratory depression caused by opioid agonists such as ... In many other opioid derivatives, placing an allyl substituent on the nitrogen instead of a methyl will reverse the normal ...
"The early history of non-opioid analgesics". Acute Pain. 1: 33. doi:10.1016/S1366-0071(97)80033-2. Enrique Ravina. The ... Phenazone (INN and BAN; also known as phenazon, antipyrine (USAN), or analgesine) is an analgesic, a nonsteroidal anti- ...
Brune, Kay (December 1997). "The early history of non-opioid analgesics". Acute Pain. 1 (1): 33-40. doi:10.1016/S1366-0071(97) ... The compounds generally act as analgesics and include dipyrone (Metamizole), aminopyrine, ampyrone, famprofazone, morazone, ...
Brune, K (1997). "The early history of non-opioid analgesics". Acute Pain. 1: 33. doi:10.1016/S1366-0071(97)80033-2. "Knorr, ... The synthesis in 1883 of the analgesic drug antipyrine, now called phenazone, was a commercial success. Antipyrine was the ... As another quinine-related compound kairin showed analgesic and antipyretic properties, Knorr and Fisher asked Wilhelm Filehne ...
Brune, K (1997). "The early history of non-opioid analgesics". Acute Pain. 1: 33. doi:10.1016/S1366-0071(97)80033-2. Drugs.com ... Non-opioid analgesics for perioperative pain therapy. Risks and rational basis for use]. Der Anaesthesist (in German). 53 (3): ... Part 1: non-opioids]. Der Anaesthesist (in German). 57 (4): 382-390. doi:10.1007/s00101-008-1326-x. PMID 18351305. United ... Nonopioid analgesics for postoperative pain management. Curr Opin Anesthesiol. 2014 Oct;27(5):513-9. PMID 25102238 Council of ...
Volans, G; Hartley, V; McCrea, S; Monaghan, J (March-April 2003). "Non-opioid analgesic poisoning". Clinical Medicine. 3 (2): ... However, the role of the individual COX isoforms in the analgesic, anti-inflammatory, and gastric damage effects of NSAIDs is ... Beaver, WT (2003). "Review of the analgesic efficacy of ibuprofen". Int J Clin Pract Suppl (135): 13-7. PMID 12723741. Fanos, V ... Forman, JP; Stampfer, MJ; Curhan, GC (September 2005). "Non-narcotic analgesic dose and risk of incident hypertension in US ...
... is a mixed opioid agonist-antagonist with opioid antagonist and analgesic properties.[1] It was introduced in 1954[2] and was ... It acts at two opioid receptors - the μ-opioid receptor (MOR) where it has antagonistic effects, and at the κ-opioid receptor ( ... "Opioid Analgesics: Chemistry and Receptors". Springer Science & Business Media - via Google Books.. ... "Pharmacological profiles of opioid ligands at Kappa opioid receptors". BMC Pharmacology. 6 (1): 3. doi:10.1186/1471-2210-6-3. ...
... is an analgesic opioid peptide acting as a peripherally specific, highly selective agonist of the κ-opioid receptor (KOR). It ... and hallucinations of previous KOR-acting analgesics such as pentazocine and phenazocine. In addition to use as an analgesic, ... ISBN 978-1-139-49198-3. Janecka A, Perlikowska R, Gach K, Wyrebska A, Fichna J (2010). "Development of opioid peptide analogs ... Difelikefalin acts as an analgesic by activating KORs on peripheral nerve terminals and KORs expressed by certain immune system ...
... and as a side effect of opioid analgesics. Formication is etymologically derived from the Latin word formica, meaning "ant", ...
... in combination with the opioid analgesic pethidine is not recommended as it can lead to severe adverse effects. ... Gillman, P. K. (2005). "Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity". British Journal of Anaesthesia ... Several other synthetic opioids such as tramadol and methadone, dextromethorphan, and various triptans are contraindicated due ...
... opioid analgesics and serotonin toxicity". British Journal of Anaesthesia. 95 (4): 434-441. doi:10.1093/bja/aei210. PMID ...
Gillman PK (2005). "Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity". Br J Anaesth. 95 (4): 434-41. doi: ...
Gillman, P. K. (2005). "Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity". British Journal of Anaesthesia ...
It may also be potentiated by opioid analgesics. Propofol can also cause decreased systemic vascular resistance, myocardial ... Propofol is not a pain medication, so opioids such as morphine may also be used. Whether or not they are always needed is ... It can also be combined with opioids or benzodiazepines. Because of its fast induction and recovery time, propofol is also ... Its use is not associated with nausea as is often seen with opioid medications. These characteristics of rapid onset and ...
Opioid analgesics may be necessary to relieve pain. Antivenom has been historically given for adults suffering severe local ... and any effect is less than might be achieved with optimal use of standard analgesics. The antivenom can be given by injection ... and any effect is less than might be achieved with optimal use of standard analgesics. Further studies are needed to confirm or ... and severe pain unresponsive to oral analgesics ... however recent trials show antivenom has a low response rate little better ...
... opioid, and/or acetylcholine receptor signaling. NK1Rs are stimulated. In turn, a fairly complex reflex is triggered involving ... the reasons why NK1RAs have failed as efficacious analgesics in well-conducted clinical proof of concept studies have not yet ... and opioids. Their activation stimulates the vomiting reflex. Different emetic pathways exist, and substance P/NK1R appears to ...
Hydrocodone bitartrate is an opioid analgesic and ... Hydrocodone bit/acetaminophen 10mg-325mg tab Buy hydrocodone online with ...
For moderate pain, an opioid agonist (eg, hydrocodone, oxycodone) can be used. An NSAID or acetaminophen may be used in ... Actually 20mg Oxycodone is equivalent to 30mg Hydrocodone An equal analgesic conversion wont account for incomplete cross ... Conversion ratios in many equianalgesic dosing tables do not apply to repeated doses of opioids. bullet Hydrocodone, 4-8 h, 3.3 ... Typical Oral Q4H doses of short-acting opioids shown as equivalents to morphine: Morphine. 30 mg. Oxycodone. 20 mg Hydrocodone ...
Opioid conversions are heuristics. Especially if as 15 mg per premises typing are psychotropic Schedule II drug? Take ... Happy ordeal for devotion hydrocodone with penurious analgesic you can add would be possible for you take more than 200,000 ...
... and a variety of opioid analgesics, which are available only with a prescription. ... There are several types of analgesics: acetaminophen (Tylenol), which is available without a prescription, ... Analgesics are drugs designed specifically to relieve pain. ... Opioid analgesics are not appropriate for people at risk of ... Some products combine acetaminophen with an opioid analgesic for added relief.. How do they work?. Opioid (also called narcotic ...
Opioids are sometimes taken in combination with non-opioids.. How theyre taken: Opioids are usually by mouth, in pill or ... Some narcotic analgesics combine an opioid with aspirin, acetaminophen, or ibuprofen. Examples include: Percodan (chemical name ... Do not stop opioid treatment abruptly without your doctors guidance. When opioids are no longer needed, your doctor will taper ... If there are episodes of breakthrough pain, a second short-acting opioid may be prescribed as well. Short-acting opioids work ...
... including opioid analgesics, are underestimated.. The increasing rates of opioid analgesic-related deaths among all groups, ... FIGURE 2. Age-adjusted death rates for poisonings involving opioid analgesics, by Medicaid enrollment status and sex - New York ... Number and crude death rates for poisonings involving opioid analgesics, by year and demographic characteristics - New York ... FIGURE 1. Death rates for poisonings involving opioid analgesics, by age group (yrs) - New York state, 2003-2012 ...
About Opioid Analgesics and this Study. Opioid analgesics are prescription medications that commonly are used to treat severe ... Treatment with opioid analgesics was linked with the following birth defects: *Spina bifida (a type of neural tube defect) ... Treatment with opioid analgesics just before or during early pregnancy was reported by 2% to 3% of the mothers. ... The American Journal of Obstetrics and Gynecology has published a new CDC study: "Maternal Treatment with Opioid Analgesics and ...
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... issues a new draft guidance on the application of the benefit-risk assessment framework for evaluating applications for opioids ... the benefits and risks of proposed new opioid analgesics relative to other already approved opioid and non-opioid analgesics. ... in evaluating applications for opioid analgesic drugs and summarizes the information that can be supplied by opioid analgesic ... Currently, all opioid analgesics intended for outpatient use are subject to one of the FDA-required Risk Evaluation and ...
Opioid analgesics as noncompetitive N-methyl-D-aspartate (NMDA) antagonists.. Ebert B1, Thorkildsen C, Andersen S, Christrup LL ... However, in order to obtain complete analgesia, a combination of an NMDA receptor antagonist and an opioid receptor agonist is ... It is concluded that although the finding that some opioids are weak noncompetitive NMDA receptor antagonists in vitro has ... In neuropathic pain, there is generally involved a presumed opioid-insensitive component, which apparently can be blocked by ...
A few case reports indicate that opioid analgesics can induce mania. The authors investigated the mood reaction of opioid ... None of the comparison subjects reported a significant mood reaction from opioid analgesics. These results indicate that opioid ... Mood-elevating effects of opioid analgesics in patients with bipolar disorder by. Schaffer CB, Nordahl TE, Schaffer LC, Howe J. ... Nine (27%) of 33 patients who took opioid analgesics for medical reasons experienced a significant hypomanic/manic reaction, ...
Opioid Analgesics. Class Summary. Narcotic analgesics facilitate the visualization and successful removal of the foreign body. ... Fentanyl is a synthetic opioid that is 75-200 times more potent than morphine sulfate and has a much shorter half-life. It has ... It is ideal for analgesic action of short duration during anesthesia and in the immediate postoperative period. It is an ... The transdermal form of fentanyl is used only for chronic pain conditions in opioid-tolerant patients. When the transdermal ...
Evidence linking opioid use with depression emanates from animal models and studies of persons with co-occurring substance use ... BACKGROUND Prescription opioid analgesic use has quintupled recently. ... Prescription opioid analgesic use has quintupled recently. Evidence linking opioid use with depression emanates from animal ... history of depression or opioid analgesic use, the risk of development of depression increased as the duration of opioid ...
Doctor-Patient Trust Among Chronic Pain Patients on Chronic Opioid Therapy after Opioid Risk Reduction Initiatives: A Survey ... Opioid Overdose Hospitalizations among Medicare-Disability Beneficiaries Jillian L. Peters, Wesley M. Durand, Kristina A. ... Comparison of Opioid Prescribing Patterns in the United States and Japan: Primary Care Physicians Attitudes and Perceptions ... Impact of Pharmacist Previsit Input to Providers on Chronic Opioid Prescribing Safety Nicholas Cox, Casey R. Tak, Susan E. ...
Australias consumption of opioid analgesics is ranked 10th internationally; North America ranks first. Per capita consumption ... "Australias consumption of opioid analgesics is ranked 10th internationally; North America ranks first. Per capita consumption ... Amanda Roxburgh, Raimondo Bruno, Briony Larance and Lucy Burns, "Prescription of opioid analgesics and related harms in ...
Nonmedical use of opioid analgesics obtained directly from physicians: prevalence and correlates.. Becker WC1, Tobin DG, ...
However, this agent only provides analgesic effects and does not have anti-inflammatory properties. Tramadol (Ultram)The imm ... Opioid AnalgesicsTramadol has been used to reduce pain in patients with RA. ... Opioid Analgesics. Tramadol has been used to reduce pain in patients with RA. However, this agent only provides analgesic ... Which medications in the drug class Opioid Analgesics are used in the treatment of Rheumatoid Arthritis?. Updated: Feb 07, 2020 ...
... Andrew C Darke and John H ... While it is legitimate medical practice to prescribe opioid analgesics to patients with chronic noncancer pain, there is clear ... While the role of opioid analgesics has been established in the treatment of cancer pain, reservations persist about ... The safety of opioids in noncancer patients has been an area of controversy because of confusion between physical dependence, ...
Opioid analgesic deaths, among which oxycodone is prevalent,11 now outnumber those for heroin and cocaine in the US.17 It is ... Prescription of opioid analgesics and related harms in Australia. Amanda Roxburgh, Raimondo Bruno, Briony Larance and Lucy ... Prescribing of opioid analgesics and related mortality before and after the introduction of long-acting oxycodone. CMAJ 2009; ... Pharmaceutical opioid analgesic and heroin depdendence: how do treatment-seeking clients differ in Australia? Drug Alcohol Rev ...
Assuring availability of opioid analgesics for palliative care : report on a WHO workshop, Budapest, Hungary 25-27 February ... Regulatory problems in making opioid analgesics available and a series of policy and professional barriers often prevent proper ... Browsing Technical documents by Subject "Analgesics, Opioid". 0-9. A. B. C. D. E. F. G. H. I. J. K. L. M. N. O. P. Q. R. S. T. ...
Piracha MM, et al. "A tale of two planes" deep versus superficial serratus plane block for postmastectomy pain syndrome. Regional Anesthesia and Pain Medicine 42: 259-262, No. 2, Mar 2017. Available from: URL: http://doi.org/10.1097/AAP.0000000000000555 - USACrossRefPubMedGoogle Scholar ...
Nonopioid analgesics as effective as opioids for acute pain?. Wilkins, Matthew. Author Information Department of Family ...
... initiative showed meaningful changes in opioid prescribing behavior and improvements in pain ... New REMS Education Program Helps Increase Safe, Responsible Use of Opioid Analgesics for Pain Relief Intensive Measurement ... Opioid analgesics are a class of prescription medications intended to treat chronic pain, but they have a significant potential ... opioid analgesic prescribing practices and use." The REMEDIES curriculum incorporates a variety of tools that include live ...
Background: Opioid analgesics and benzodiazepines are often misused in clinical practice. We determined whether implementation ... First, we identified all filled prescriptions for 30 or more tablets of an opioid analgesic or a benzodiazepine during a 5-year ... Effect of a centralized prescription network on inappropriate prescriptions for opioid analgesics and benzodiazepines. Colin R ... Monthly percentages of filled prescriptions for opioid analgesics and benzodiazepines deemed inappropriate among residents of ...
Opioid analgesics. Class Summary. These agents are used for deep sedation to allow adequate mechanical ventilation. They may be ... Synthetic opioid that is 75-200 times more potent than morphine. It is highly lipophilic and protein-bound. Prolonged exposure ...
  • Relationship between pain and opioid analgesics on the development of delirium following hip fracture. (springer.com)
  • We hope that through this workshop we will provide novel and important contributions to the goal of finding solutions to the current pain and opioid crisis. (eventbrite.com)
  • Analyses of the medical literature and select Internet sites indicate that individuals in the United States are increasingly using kratom for the self-management of pain and opioid withdrawal. (jaoa.org)
  • Joranson DE, Rajagopal MR, Gilson AM. Improving access to opioid analgesics for palliative care in India. (wisc.edu)
  • Over 40 experts from Bulgaria, Croatia, Hungary, Lithuania, Poland and Romania, along with experts from WHO and other organizations, attended the Workshop to evaluate national policies for opioid control and to develop action plans to improve the availability of these drugs for palliative care in their countries. (who.int)
  • Cicero T, Inciardi JA, Munoz A. Trends in abuse of Oxycontin and other opioid analgesics in the United States 2002-2004. (springer.com)
  • Abuse by secondary recipients of opioids is well documented and arises as a result of diversion by primary recipients, double-doctoring, forgery and theft. (hindawi.com)
  • Lowes R. FDA Restricts Long-term Opioid Use to Combat Abuse. (medscape.com)
  • One effort to address the misuse and abuse of opioids is the Risk Evaluation and Mitigation Strategy (REMS) for opioid analgesics. (purduepharma.com)
  • The U.S. Food and Drug Administration (FDA) has identified safe storage and proper disposal of prescription opioid products as an essential element of its activities to address opioid misuse and abuse ( 2 ) and a crucial component of wider initiatives confronting the current opioid crisis ( 3 ). (annals.org)
  • Because monkey models provide the most phylogenetically appropriate evaluation of opioid receptor functions and drug effects, these findings provide a translational bridge for such ligands as effective analgesics without safety and abuse liability concerns. (pnas.org)
  • Despite the critical need, no previous research has substantiated safe opioid analgesics without abuse liability in primates. (pnas.org)
  • Embeda is the third ER opioid analgesic to be approved with labeling describing the product's abuse-deterrent properties consistent with the FDA's 2013 draft guidance, Abuse-Deterrent Opioids - Evaluation and Labeling. (fiercepharma.com)
  • The science behind developing prescription opioids with abuse-deterrent properties is still evolving and these properties will not completely fix the problem. (fiercepharma.com)
  • The submission also includes data from clinical abuse liability studies designed and conducted consistent with FDA's January 2013 Draft Guidance for Industry: Abuse-Deterrent Opioids-Evaluation and Labeling. (empr.com)
  • Change the boxed warning to include the risk of neonatal opioid withdrawal syndrome (NOWS) and to urge providers to asses and monitor the patient's risk of abuse/misuse of the drug. (fdalawblog.net)
  • By 1914, growing concern about opioid abuse led to the passage of the Harrison Narcotics Tax Ac t, which imposed steep taxes on the manufacture, importation, and sale of opiates. (levinlaw.com)
  • The recent marked increase in misuse and abuse of prescription opioids and the epidemic of opioid overdose mortality have greatly affected our society ( 1 - 3 ). (sciencemag.org)
  • Although mu opioid peptide (MOP) receptor agonists remain the most effective and widely used analgesics, their abuse liability and possibility of causing respiratory arrest have contributed to escalating medical and economic burdens and fueled the opioid crisis in the global community ( 4 , 5 ). (sciencemag.org)
  • Finally, the respiratory-depressant effects of equi- pa opioid agonists can diminish the abuse-related effects and antinociceptive doses of oxycodone, nalfurafine, and the mix- augment the antinociceptive effects of mu agonists. (deepdyve.com)
  • Because of their psychic effects, opioids are important drugs of abuse and are responsible for severe personal and social problems. (mhmedical.com)
  • Caudill-Slosberg MA, Schwartz LM, Woloshin S. Office visits and analgesic prescriptions for musculoskeletal pain in US: 1980 vs 2000. (springer.com)
  • The frequency of forgery and theft of different opioids appears to be largely related to the corresponding number of legitimate prescriptions. (hindawi.com)
  • We calculated monthly percentages of filled prescriptions for an opioid or a benzodiazepine that were deemed inappropriate (those issued by a different physician and dispensed at a different pharmacy within 7 days after a filled prescription of at least 30 tablets of the same drug). (cmaj.ca)
  • In the year following an OUD diagnosis, a substantial number of Medicaid-enrollees filled a prescription for an opioid analgesic (45%) or a benzodiazepine (37%), and one in five filled prescriptions for both. (rand.org)
  • These citations have been made by researchers and marketers who fail to note that: (i) the letter did not constitute clinical research, and (ii) the observations were of hospital patients who were taking opioid prescriptions under close medical supervision. (levinlaw.com)
  • In this review we outline recent progress towards the discovery of safer opioid analgesics. (epfl.ch)
  • The possibility of exploiting this diversity to develop safer opioids was the topic of a webinar hosted by PRF on January 21, 2016, titled "Safer Opioid Analgesics: It's All in the Telling of the Tail," referring to splice variability at the N- and C-termini of the MOR protein. (painresearchforum.org)
  • Gender, clinical experience and practice location did not seem to have an impact on the decision to prescribe opioid analgesics or antibiotics. (jcda.ca)
  • Based on the results of our survey, a significant proportion of dental professionals in British Columbia prescribe opioid analgesics and antibiotics during endodontic procedures when they are likely not required. (jcda.ca)
  • however, their analysis did not acknowledge that the drug disposal information in the product labeling for all currently marketed opioid analgesics was updated on 16 December 2016. (annals.org)
  • Their analysis, based on an examination of opioid analgesic labeling in DailyMed, was done in September 2016 and therefore did not include this updated information. (annals.org)
  • In March 2016, the FDA issued a Drug Safety Communication concerning the association of the entire class of opioid pain medicines with serotonin toxicity. (springer.com)
  • In this report, the United States Non-opioid Analgesic Patch market is valued at USD XX million in 2016 and is expected to reach USD XX million by the end of 2022, growing at a CAGR of XX% between 2016 and 2022. (reportsnreports.com)
  • When it comes to regulating opioids, we do so with an understanding that any action taken by the agency should be considered in light of the opioid crisis. (fda.gov)
  • It is concluded that although the finding that some opioids are weak noncompetitive NMDA receptor antagonists in vitro has created much attention among clinicians, no clinical studies have been conducted to evaluate the applicability of these compounds in the treatment of neuropathic pain conditions. (nih.gov)
  • Recent evidence from controlled clinical trials supports the effectiveness of opioids for treating noncancer pain of varying etiologies. (hindawi.com)
  • REMEDIES is a novel educational platform for prescribers and is intended to improve the quality of care for opioid-tolerant pain patients," said Van Velle, President of Applied Clinical Education, a medical education company with 20 years of programming experience in the area of pain management. (businesswire.com)
  • The REMEDIES curriculum incorporates a variety of tools that include live symposia, interactive web-based activities, a three-stage performance improvement program, and a series of three patient screening and education activities that help healthcare providers navigate the clinical challenge of opioid prescribing. (businesswire.com)
  • Although the opioids most often associated with serotonin toxicity in humans inhibit human SERT in vitro, fentanyl and oxycodone are not inhibitory even though their clinical involvement has been reported. (springer.com)
  • It may also be indicated for short-term use in acute pain.Despite large studies and meta-analyses of opioids for a variety of pain conditions, the evidence for its clinical effectiveness is still unclear. (who.int)
  • Clinical observations indicate that patients who use opioids chronically prior to surgery have worse long-term functional outcomes than patients who do not. (jax.org)
  • Improving Adherence to Long-term Opioid Therapy Guidelines to Reduce Opioid Misuse in Primary Care: A Cluster-Randomized Clinical Trial. (umassmed.edu)
  • The observations described suggest that opioids, although they belong to the same family drug may not be fully comparable with regard to the clinical effects products. (clinicaltrials.gov)
  • The NDA submission was based on the results of a 12-week, double-blind, randomized, placebo-controlled clinical trial with 600 opioid-experienced patients as well as supporting data from other clinical studies. (empr.com)
  • Recognizing that more information is needed to assess the serious risks associated with long-term use of extended-release and long-acting opioids, the FDA is requiring the drug companies that make these products to conduct further studies and clinical trials. (ascopost.com)
  • Clinical manifestations of drug-drug interactions involving opioids were grouped as follows: 1) sedation and respiratory depression, 2) other central nervous system symptoms, 3) impairment of pain control and/or opioid withdrawal, and 4) other symptoms. (uib.no)
  • A substantial proportion of clinicians prescribed opioid analgesics and antibiotics in the various clinical scenarios. (jcda.ca)
  • Natural products found in Mitragyna speciosa , commonly known as kratom, represent diverse scaffolds (indole, indolenine, and spiro pseudoindoxyl) with opioid activity, providing opportunities to better understand opioid pharmacology. (pubmedcentralcanada.ca)
  • Nonmedical use of opioid analgesics obtained directly from physicians: prevalence and correlates. (nih.gov)
  • Nevertheless, the results of our sensitivity analysis assessing whether unmeasured confounding might affect the observed results indicate that a potential unmeasured confounder (that is, pain intensity) would need to be a strong, independent risk factor for invasive pneumococcal disease and also have a large absolute difference in prevalence between opioid users and nonusers to account for the observed association. (annals.org)
  • To study the prevalence and factors associated with opioid use in pain, 480 consecutive patients with a chief complaint of pain were interviewed at 10 clinics in Zahedan. (who.int)
  • Persons in the race category "Other" and those residing in NYC also showed higher rates of increase in opioid analgesic-related mortality (RR = 6.3 and 7.5, respectively). (cdc.gov)
  • Possibly because of this increase in opioid use, overdoses and emergency room visits resulting from non-prescription opioid use have also increased. (jcda.ca)