Receptors, Opioid, mu
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
Receptors, Opioid, kappa
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.
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.
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.
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.
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)-
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.
Dose-Response Relationship, Drug
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.
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)
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).
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.
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.
Substance Withdrawal Syndrome
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.
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.
Prescription Drug Misuse
Opiate Substitution Treatment
Drug and Narcotic Control
Hypnotics and Sedatives
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)
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)
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.
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.
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 Administration Schedule
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)
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.
Disease Models, Animal
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
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
Analysis of Variance
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.
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)
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)
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.
Drug Administration Routes
Ambulatory Surgical Procedures
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.
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)
Drug Therapy, Combination
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.
Any dummy medication or treatment. Although placebos originally were medicinal preparations having no specific pharmacological activity against a targeted condition, the concept has been extended to include treatments or procedures, especially those administered to control groups in clinical trials in order to provide baseline measurements for the experimental protocol.
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)
Depression and Prescription Opioid Misuse Among Chronic Opioid Therapy Recipients With No History of Substance Abuse | Annals...
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 ...
What proportion of patients with chronic noncancer pain are prescribed an opioid medicine? Systematic review and meta...
TY - JOUR. T1 - What proportion of patients with chronic noncancer pain are prescribed an opioid medicine? Systematic review and meta-regression of observational studies. AU - Mathieson, S.. AU - Wertheimer, G.. AU - Maher, C. G.. AU - Christine Lin, C. W.. AU - McLachlan, A. J.. AU - Buchbinder, R.. AU - Pearson, S. A.. AU - Underwood, M.. PY - 2020/5. Y1 - 2020/5. N2 - Guidelines now discourage opioid analgesics for chronic noncancer pain because the benefits frequently do not outweigh the harms. We aimed to determine the proportion of patients with chronic noncancer pain who are prescribed an opioid, the types prescribed and factors associated with prescribing. Database searches were conducted from inception to 29 October 2018 without language restrictions. We included observational studies of adults with chronic noncancer pain measuring opioid prescribing. Opioids were categorized as weak (e.g. codeine) or strong (e.g. oxycodone). Study quality was assessed using a risk of bias tool designed ...
30 Opioid Therapy in Chronic Nonmalignant Pain | Free Medical Textbook
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.…
Intrathecal Therapy for Chronic Non-Cancer Pain: An Analysis of Its Efficacy - Full Text View - ClinicalTrials.gov
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 ...
Pain, alcohol use disorders and risky patterns of drinking among people with chronic non-cancer pain receiving long-term opioid...
Background. The utilisation of pharmaceutical opioids has increased internationally, and there is evidence of increasing risky alcohol consumption with ageing. This study examines the patterns and correlates of risky drinking among people with chronic non-cancer pain (CNCP) prescribed opioids, and the associations between alcohol consumption and pain.. Methods. The Pain and Opioids IN Treatment cohort comprises 1514 people in Australia prescribed pharmaceutical opioids for CNCP. Participants reported lifetime, past year and past month alcohol use, as well as mental and physical health, other substance use, pain characteristics, and current opioid dose.. Results. Less than one-tenth of the sample were lifetime abstainers (7%); 34% were former drinkers; 34% were non-risky drinkers (i.e., past 12 month use ≤4 standard drinks); 16% were occasional risky drinkers; and 8% were regular risky drinkers (i.e., ≥weekly use of >4 standard drinks). Males reported greater levels of alcohol use, ...
Identifying communicative factors affecting opioid management for chronic pain - Regenstrief Institute
The use of opioid medications for the treatment of chronic non-cancer pain has risen dramatically in the past two decades. There are a number of risks associated with the long term use of opioids, most notably the potential for misuse. Successful opioid management strategies for chronic non-cancer pain depend upon effective patient-provider communication. Improving the communication between providers and patients about opioids has tremendous potential to improve opioid management and reduce opioid misuse.. The purpose of this pilot study is to evaluate how patients with chronic non-cancer pain and their physicians communicate about opioid management. The data from this pilot study will be used to guide further research on the mechanisms behind communication about opioid management and the design of an intervention to improve physician communication with patients with chronic non-cancer pain about opioid treatment. ...
Long-Term Opioid Therapy for Chronic Pain. In Response<...
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 - ...
Guideline for opioid therapy and chronic noncancer pain | CMAJ
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 ...
Opioid analgesic | Article about Opioid analgesic by The Free Dictionary
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
Opioid Analgesic Prescribing Practices of Dental Professionals in the by C. N. Steinmetz, C. Zheng et al.
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
HHS Guide for Clinicians on the Appropriate Dosage Reduction or Discontinuation of Long-Term Opioid Analgesics | National...
The HHS Guide for Clinicians on the Appropriate Dosage Reduction or Discontinuation of Long-Term Opioid Analgesics was developed for clinicians who are considering or beginning to reduce opioid dosage or to discontinue long-term opioid therapy for patients with chronic pain. Each clinician should review the risks and benefits of current therapy with his or her patient, and decide if tapering is appropriate based on individual circumstances.
Prescription Opioid Misuse, Heroin, and Fentanyl | The White House
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 ...
The use of as-needed range orders for opioid analgesics in the management of acute pain: a consensus statement of the...
TY - JOUR. T1 - The use of as-needed range orders for opioid analgesics in the management of acute pain. T2 - a consensus statement of the American Society for Pain Management Nursing and the American Pain Society.. AU - Gordon, Debra B.. AU - Dahl, June. AU - Phillips, Peggy. AU - Frandsen, Jan. AU - Cowley, Charlene. AU - Foster, Roxie L.. AU - Fine, Perry G.. AU - Miaskowski, Christine. AU - Fishman, Scott M. AU - Finley, Rebecca S.. PY - 2005/6. Y1 - 2005/6. N2 - The use of as-needed or PRN range orders for opioid analgesics in the management of acute pain is a common clinical practice. This approach provides flexibility in dosing to meet individual patients unique analgesic requirements. Range orders enable necessary and safe dose adjustments based on an individuals response to treatment. This paper presents the consensus statement of the American Society for Pain Management Nursing and the American Pain Society on the use of as-needed range orders for opioid analgesics in the ...
Sex Differences in Overlapping Chronic Non-cancer Pain Conditions in a Tertiary Pain Clinic | OMICS International
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 ..
Management of Chronic Non-Cancer Pain: A guide to appropriate use of Opioids
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.
Managing Chronic Pain: An Analysis of the Use of Opioids
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 ...
NPS Webinar: Supporting patients living with chronic non-cancer pain - the role of the pharmacist
NPS Webinar: Join our panel of chronic pain experts as they discuss evidence-based approaches for managing chronic non-cancer pain and the role of pharmacists in reducing opioid-related harms.
Interventions for the reduction of prescribed opioid use in chronic non-cancer pain - Nottingham ePrints
Three studies are new to this update, resulting in five included studies in total (278 participants). Participants were primarily women (mean age 49.63 years, SD = 11.74) with different chronic pain conditions. We judged the studies too heterogeneous to pool data in a meta-analysis, so we have summarised the results from each study qualitatively. The studies included acupuncture, mindfulness, and cognitive behavioral therapy interventions aimed at reducing opioid consumption, misuse of opioids, or maintenance of chronic pain management treatments. We found mixed results from the studies. Three of the five studies reported opioid consumption at post-treatment and follow-up. Two studies that delivered Mindfulness-Oriented Recovery Enhancement or Therapeutic Interactive Voice Response found a significant difference between groups at post-treatment and follow-up in opioid consumption. The remaining study found reduction in opioid consumption in both treatment and control groups, and ...
Evaluation of opioid-related deaths associated with opioid utilisation and the impacts of tramadol classification as a Schedule...
After tramadol classification, the levels of monthly tramadol utilisation and the prevalence of tramadol users decreased by 12.9 defined daily dose/1000 registrants and 6.4 tramadol users/10000 registrants. In addition, the trends of monthly tramadol utilisation and the prevalence of tramadol users decreased by 1.6 defined daily dose/1000 registrants and 0.37 tramadol users/10000 registrants. The impacts of tramadol classification seems predominantly associated with the reduced accessibility of tramadol to both new and existing users. Of the 232 cases of opioid-related deaths, 62 (26.7%) cases did not receive any opioid in the one year before opioid-related death. Only 48 cases received a daily dose of opioid of more than 120 mg oral morphine equivalent (OMEQ) dose in the final year, and an opioid daily dose more than 120 mg OMEQ dose was not significantly associated with opioid-related deaths (adjusted odds ratios [aOR]: 1.4; 95% confidence interval [95%CI]: 0.52, 3.6). In addition, most of the ...
What is the optimal length of a prescription for an opioid pain medication after surgery? - Scienmag: Latest Science and Health...
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 ...
Impact of lifetime opioid exposure on arterial stiffness and vascular age: cross-sectional and longitudinal studies in men and...
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 ...
Opioid Analgesics | Virtual Anaesthesia Textbook
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.. ...
The use of as-needed range orders for opioid analgesics in the management of acute pain: A consensus statement of the...
TY - JOUR. T1 - The use of as-needed range orders for opioid analgesics in the management of acute pain. T2 - A consensus statement of the American Society for Pain Management Nursing and the American Pain Society. AU - Gordon, Debra B.. AU - Dahl, June. AU - Phillips, Peggy. AU - Frandsen, Jan. AU - Cowley, Charlene. AU - Foster, Roxie L.. AU - Fine, Perry G.. AU - Miaskowski, Christine. AU - Fishman, Scott M. AU - Finley, Rebecca S.. PY - 2004/6. Y1 - 2004/6. N2 - The use of as needed or PRN range orders for opioid analgesics in the management of acute pain is a common clinical practice. This approach provides flexibility in dosing to meet individual patients unique analgesic requirements. Range orders enable necessary and safe dose adjustments based on an individuals response to treatment. The purpose of this paper is to present the consensus statement of the American Society for Pain Management Nursing and the American Pain Society on the use of as-needed range orders for opioid ...
Opioid therapy: optimizing analgesic outcomes - Oxford Medicine
Treatment with analgesic drugs is the mainstay of cancer pain management. The major group of drugs used in cancer pain management is the opioid analgesics. During the last 30 years, there has been a dramatic increase in our knowledge of the sites and mechanism of action of the opioids. The development of analytical methods has also been of great importance in facilitating pharmacokinetic studies of the disposition and fate of opioids in patients. More recently, advances in genomic research have indicated the potential importance of pharmacogenetic factors in the response to opioid analgesics. These studies have begun to offer us a better understanding of some of the sources of variation between individuals in their response to opioids and to suggest ways of minimizing some of their adverse effects. This chapter presents a comprehensive discussion of the pre-clinical pharmacology and clinical aspects of opioid analgesia and the principles of opioid administration.
CH 25 ANALGESICS (OPIOID ANALGESICS (Most potent (Action site (Act on CNS…
CH 25 ANALGESICS (OPIOID ANALGESICS (Most potent (Action site (Act on CNS…: CH 25 ANALGESICS (OPIOID ANALGESICS, NSAIDs, ADJUVANT THERAPIES, Migraine and Cluster Headaches , NONOPIOD ANALGESICS)
What is the role of accredited continuing education in the FDA ER/LA Opioid Analgesics REMS? | Accreditation Council for...
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.. ...
OPUS 4 | Search
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 ...
Most recent papers in the shared collection Psychogenomics | Read by QxMD
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 ...
Neurostimulation for chronic noncancer pain<...
TY - JOUR. T1 - Neurostimulation for chronic noncancer pain. AU - Burchiel, Kim J.. PY - 2006/8/22. Y1 - 2006/8/22. UR - http://www.scopus.com/inward/record.url?scp=33747245764&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=33747245764&partnerID=8YFLogxK. U2 - 10.3171/jns.2006.105.2.174. DO - 10.3171/jns.2006.105.2.174. M3 - Editorial. C2 - 17219819. AN - SCOPUS:33747245764. VL - 105. JO - Journal of Neurosurgery. JF - Journal of Neurosurgery. SN - 0022-3085. IS - 2. ER - ...
Use and dependence on opioid drugs in the Spanish population with chronic pain: Prevalence and differences according to sex |...
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.. ...
The effect of treatment expectation on drug efficacy: imaging the analgesic benefit of the opioid remifentanil. - Oxford...
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
Abuse of Prescription Opioid Pain Medication A Vast Problem - Cakehealth
The scope of the problem is vast - opioid overdose is now the second leading cause of accidental death in the United States, and the prevalence is second only to marijuana, said Thomas McLellan, director of the new Center for Substance Abuse Solutions at the University of Pennsylvania School of Medicine.. In a new study, McLellan and his colleagues found 11.7 percent of the 202 million opioid prescriptions issued in the United States in 2009 went to children and young adults. Additional research is needed to determine whether this relatively high rate of prescriptions is warranted, the researchers say. Medical professionals may need to consider alternative medications for young people in some situations, McLellan said.. The results also showed that 56 percent of opioid prescriptions given in 2009 went to patients who had already filled a prescription in the previous month. Not all of them may be justified, McLellan said.. More research is needed to see if current practices are working, with a ...
Opioid maintenance medicines for the treatment of dependence on opioid pain medicines | Cochrane
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 ...
JOHNS HOPKINS MEDBIQUITOUS PROJECT SUPPORTS FDA REMS INITIATIVE ADDRESSING ER/LA OPIOID ABUSE | MedBiquitous Development Site
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 ...
The Effectiveness and Tolerability of Fentanyl Matrix in Chronic Non-cancer Pain; Assessment of Patient's Pain Treatment...
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 ...
QuickStats: Rates of Deaths from Drug Poisoning and Drug Poisoning Involving Opioid Analgesics - United States, 1999-2013 |...
In 2013, a total of 43,982 deaths in the United States were attributed to drug poisoning, including 16,235 deaths (37%) involving opioid analgesics. From 1999 to 2013, the drug poisoning death rate more than doubled from 6.1 to 13.8 per 100,000 population, and the rate for drug poisoning deaths involving opioid analgesics nearly quadrupled from…
The DAWN Report: Benzodiazepines in Combination with Opioid Pain Relievers or Alcohol: Greater Risk of More Serious ED Visit...
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
Long-term opioid use does not increase risk of Alzheimers disease | Journal of Anaesthesia Practice
Opioid use is not associated with an increased risk of Alzheimers disease, shows a recent study from the University of Eastern Finland.
European drug report 2017 and opioid-induced deaths | European Journal of Hospital Pharmacy
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 ...
Scientists Report on Safe, Non-addictive Opioid Analgesic in Animal Model
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.
Management Strategies for Long-Term Opioid Therapy
Experts have agreed on treatment approaches to implement when troubling behaviors arise in patients receiving opioids for chronic pain.
Remifentanil - Wikipedia
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 ...
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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 ...
In Response: The Cause of Fatal Respiratory Depression Is Combination of Clindamycin and Fentanyl, Rather than Tramadol. -...
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
Initial Rx Can Affect Likelihood of Long-Term Opioid Use - Pain Management
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.
FDA mulls stronger controls on opioid prescribingOxy Watchdog
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 ...
Long-term Opioid Use Common in Alzheimers Patients, But Not Excessive, Finnish Study Says
Read about a study finding that long-term use of opioids is common among people with Alzheimers disease in Finland, especially transdermal opioids.
New import/export system for controlled medicines launched by International Narcotics Control Board - ehospice
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 ...
Most recent papers in the journal F1000Research | Read by QxMD
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 ...
Thus, mu-opioid receptors induce relaxation, trust, satisfaction and have a strong analgesic effect. This system is also ... Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are ... The functionality of kappa- and delta-opioid receptors, might be less associated with relaxation and analgesic effects as kappa ... Lemke, Thomas L.; Williams, David H.; Foye, William O. (2002). "Opioid Analgesics; Fries, DS". Foye's principles of medicinal ...
ISBN 978-0-553-34631-2; ISBN 978-0-553-17616-2 (British edition); ISBN 978-0-553-05261-9 Fries, DS (2002). "Opioid Analgesics ...
Miscellaneous Groups of Analgesics. Opioid Analgesics. Springer US. pp. 385-403. doi:10.1007/978-1-4899-0585-7_11. ISBN ... U-47700, also known as pink heroin, pinky, and pink, is an opioid analgesic drug developed by a team at Upjohn in the 1970s ... Kimergård A, Breindahl T, Hindersson P, Deluca P (October 2016). "Tampering of opioid analgesics: a serious challenge for ... Synthetic opioids, Benzamides, Mu-opioid receptor agonists, Dimethylamino compounds, Chlorobenzenes, Designer drugs). ...
However, since opioid antagonists also block the beneficial effects of opioid analgesics, they are generally useful only for ... In this context the term opioid refers to opioid agonists, opioid antagonists, opioid peptides, and opioid receptors. Davies PS ... However, a new report showed a clear risk of prolonged opioid use when opioid analgesics are initiated for an acute pain ... Unique to each opioid is its distinct binding affinity to the various classes of opioid receptors (e.g. the μ, κ, and δ opioid ...
Opioid use disorder
Included in this number are opioid analgesics, along with heroin and illicit synthetic opioids. US yearly deaths by drug ... opiates and opioids MME of common opioids Long-term opioid use occurs in about 4% of people following their use for trauma or ... Opioid replacement therapy (ORT) involves replacing an opioid, such as heroin, with a longer-acting but less euphoric opioid. ... For more specific mitigation strategies regarding opioid overdoses, see Opioid overdose. Opioid use disorders typically require ...
Opioid analgesics (e.g., Fentanyl) may be combined with Propofol, although anesthesiology must weight the benefits against ...
3.3 Synthetic Opioids.". Analgesics. pp. 159-169. ISBN 978-3-527-30403-5. Casy AF, Parfitt RY. Opioid analgesics, chemistry and ... Furethidine is a 4-phenylpiperidine derivative that is related to the clinically used opioid analgesic drug pethidine ( ... Mu-opioid receptor agonists, All stub articles, Analgesic stubs). ... doi:10.1111/j.1476-5381.1960.tb01240.x. Cahal DA, Dare JG, Keith D (February 1961). "A sequential trial of analgesics in labour ...
Mu-opioid receptor agonists, Mu-opioid receptor antagonists, Semisynthetic opioids, All stub articles, Analgesic stubs). ... 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. ...
... (INN), also known as methofoline (USAN), is an opioid analgesic drug discovered in the 1950s by a team of Swiss ... 30 FR 4083 March 27, 1965 Casy AF, Parfitt RY (1986). Opioid Analgesics, Chemistry and Receptors. New York: Plenum Press. p. ... Synthetic opioids, Norsalsolinol ethers, Chloroarenes, Mu-opioid receptor agonists, Abandoned drugs). ... Metofoline has around the same efficacy as an analgesic as codeine, and was evaluated for the treatment of postoperative pain. ...
Analgesics, Designer drugs, Opioids, All stub articles, Analgesic stubs). ... Casy AF, Parfitt RY (1986). Opioid analgesics, chemistry and receptors. New York: Plenum Press. p. 289. ISBN 978-0-306-42130-3 ... It is a homologue of fentanyl, with similar analgesic and sedative effects but lower potency, around 14x stronger than ... Homofentanyl (N-Phenylpropylnorfentanyl, Fentanyl propyl analogue) is an opioid derivative which has been sold as a designer ...
Analgesics, 4,5-Epoxymorphinans, Mu-opioid receptor agonists, Opioids, Phenols, Semisynthetic opioids, Adulteration). ... Casy AF, Parfitt RT (1986). Opioid analgesics: chemistry and receptors. New York: Plenum Press. p. 32. ISBN 978-0-306-42130-3. ... Early medical trials of humans taking desomorphine have resulted in the finding that like morphine and most other analgesics of ... Desomorphine is a semi-synthetic opioid commercialized by Roche, with powerful, fast-acting effects, such as sedation and ...
Mu-opioid receptor agonists, Opioids, Phenols, Semisynthetic opioids, All stub articles, Analgesic stubs). ... Methyldesorphine is an opioid analgesic. First synthesized in Germany in 1940 and patented in the US in 1952, it has a high ... Casy AF, Parfitt RY (1986). Opioid Analgesics, Chemistry and Receptors. New York: Plenum Press. pp. 37-38. ISBN 0-306-42130-5. ... 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 ...
Passik, SD; Webster, L (2014). "Opioid analgesics: does potency matter?". J Opioid Manag. 10 (4): 263-75. doi:10.5055/jom. ... Opioid rotation or opioid switching is the process of changing one opioid to another to improve pain control or reduce unwanted ... One issue with opioid rotation is that an opioid therapy failure poorly predicts whether other opioids would be effective. In ... there is less evidence for what particular opioid analgesics are most suitable, and in practice the choice of opioid drugs used ...
Semisynthetic opioids, Mu-opioid receptor agonists, All stub articles, Analgesic stubs). ... Opioid analgesics, chemistry and receptors. New York: Plenum Press. pp. 37-38. ISBN 978-0-306-42130-3. v t e (Articles with ... 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 (2013). Opioid Analgesics: Chemistry and Receptors. Springer Science & Business Media. p. 312. ISBN ... Synthetic opioids, Antidiarrhoeals, Nitriles, 4-Phenylpiperidines, Mu-opioid receptor agonists, Janssen Pharmaceutica, Belgian ... Diphenoxylate is an opioid and acts by slowing intestinal contractions; the atropine is present to prevent drug abuse and ... Like other opioids, diphenoxylate acts by slowing intestinal contractions, allowing the body to consolidate intestinal contents ...
"Chemistry of Opioid Analgesics". PHA 5155- Neurology Pharmacotherapeutics Medicinal Chemistry Tutorials. Archived from the ... in other countries it is usually controlled as a strong opioid. Homocodeine is a synonym for pholcodine. Bicodeine is a dimer ... Mu-opioid receptor agonists, Phenols, Semisynthetic opioids). ...
Agkistrodon contortrix phaeogaster
... opiate/opioid narcotic analgesics (ex. morphine, fentanyl), muscle relaxerss (ex. diazepam, tizanidine, orphenadrine), and ... A few days' supply of weaker analgesics and muscle relaxers may be prescribed for the patient to control pain after he or she ...
Brune K (1997). "The early history of non-opioid analgesics". Acute Pain. 1: 33-40. doi:10.1016/S1366-0071(97)80033-2. Ravina E ... Analgesics, Pyrazolones, Nonsteroidal anti-inflammatory drugs, Antipyretics, All stub articles, Analgesic stubs). ... One of the earliest widely used analgesics and antipyretics, phenazone was gradually replaced in common use by other ... Phenazone (INN and BAN; also known as phenazon, antipyrine (USAN), or analgesine) is an analgesic (pain reducing), antipyretic ...
Brune, Kay (December 1997). "The early history of non-opioid analgesics". Acute Pain. 1 (1): 33-40. doi:10.1016/S1366-0071(97) ... Compounds containing this functional group are useful commercially in analgesics and dyes. Pyrazolone can exist in two isomers ... The compounds generally act as analgesics and include dipyrone (Metamizole), aminophenazone, ampyrone, famprofazone, morazone, ...
Brune, K (1997). "The early history of non-opioid analgesics". Acute Pain. 1: 33-40. 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 (December 1997). "The early history of non-opioid analgesics". Acute Pain. 1: 33-40. doi:10.1016/S1366-0071(97)80033-2 ... Part 1: non-opioids]" [Drugs for postoperative analgesia: routine and new aspects. Part 1: non-opioids]. Der Anaesthesist (in ... Brack A, Rittner HL, Schäfer M (March 2004). "Nichtopioidanalgetika zur perioperativen Schmerztherapie" [Non-opioid analgesics ... Amid the opioid crisis, a study pointed the legal status of metamizole have a relation to the consumption of oxycodone, showing ...
Maul C, Buschmann H, Sundermann B (2005). "Opioids: 3.3 Synthetic Opioids.". Analgesics. pp. 159-169. ISBN 978-3-527-30403-5. ... Benzethidine is a 4-phenylpiperidine derivative that is related to the clinically used opioid analgesic drug pethidine ( ... Mu-opioid receptor agonists, Ethyl esters, All stub articles, Analgesic stubs). ... It has similar effects to other opioid derivatives, such as analgesia, sedation, nausea and respiratory depression. In the ...
Volans G, Hartley V, McCrea S, Monaghan J (March-April 2003). "Non-opioid analgesic poisoning". Clinical Medicine. 3 (2): 119- ... However, the role of the individual COX isoforms in the analgesic, anti-inflammatory, and gastric damage effects of NSAIDs is ... Forman JP, Stampfer MJ, Curhan GC (September 2005). "Non-narcotic analgesic dose and risk of incident hypertension in US women ... Beaver WT (April 2003). "Review of the analgesic efficacy of ibuprofen". International Journal of Clinical Practice. Supplement ...
It is designed to be an opioid analgesic with a low chance of recreational use. Created by Kempharm, Inc., a biopharmaceutical ... Mustafa AA, Rajan R, Suarez JD, Alzghari SK (June 2018). "A Review of the Opioid Analgesic Benzhydrocodone-Acetaminophen". ... Acetaminophen is a non-opioid, non-salicylate analgesic. The specific mechanism of analgesia has not been determined. ... Mixed agonist/antagonist and partial agonist opioids may reduce the analgesic effect of benzhydrocodone/APAP or cause ...
... and as a side effect of opioid analgesics. Formication is etymologically derived from the Latin word formica, ...
... in combination with the opioid analgesic pethidine is not recommended, as it can lead to severe adverse effects. ... Gillman PK (October 2005). "Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity". British Journal of ... Several other synthetic opioids such as tramadol and methadone, as well as various triptans, are contraindicated due to ...
Gillman PK (October 2005). "Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity". British Journal of ... It is often, particularly as palliation, used in small doses to reduce nausea by opioid-treated cancer patients and to ... Richter PA, Burk MP (July-August 1992). "The potentiation of narcotic analgesics with phenothiazines". The Journal of Foot ... Chlorpromazine can also potentiate the CNS depressant effects of drugs like barbiturates, benzodiazepines, opioids, lithium and ...
... is an opioid pain killer -- narcotic analgesic.[medical citation needed] It is a derivative of isonipecotic acid ... Phenoperidine(Operidine or Lealgin), is an opioid analgesic which is structurally related to pethidine and is used clinically ... which lacked the opioid's analgesic properties but still stopped peristalsis in the intestines, a typical side effect of ... figure 20-80 times as potent as pethidine as an analgesic. The greatly increased potency essentially eliminates the toxic ...
... is a drug which acts as a highly selective κ-opioid agonist. It is a potent analgesic with around the same potency as ... July 2002). "Diazabicyclononanones, a potent class of kappa opioid analgesics". Farmaco. 57 (7): 531-4. CiteSeerX 10.1.1.619. ... Siener T, Cambareri A, Kuhl U, Englberger W, Haurand M, Kögel B, Holzgrabe U (October 2000). "Synthesis and opioid receptor ... Kögel B, Christoph T, Friderichs E, Hennies HH, Matthiesen T, Schneider J, Holzgrabe U (1998). "HZ2, a Selective Kappa-Opioid ...
Serotonin reuptake inhibitor
Gillman PK (2005). "Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity". Br J Anaesth. 95 (4): 434-41. doi: ...
... an opioid analgesic Piperidolate, an antimuscarinic This set index page lists chemical structure articles associated with the ...
Analgesics, Neurotransmitters, Mu-opioid receptor agonists, Kappa-opioid receptor agonists, Opioid peptides). ... and κ-opioid receptor agonist while having no effects on δ-opioid receptors. It possesses analgesic and respiratory depressive ... Opioid peptide Matsuo H, Miyata A, Mizuno K (1983). "Novel C-terminally amidated opioid peptide in human phaeochromocytoma ... April 1985). "The analgesic and respiratory depressant actions of metorphamide in mice and rabbits". Neuropeptides. 6 (2): 121- ...
Opioids such as fentanyl may be used, but if given too close to birth there is a risk of respiratory depression in the infant.[ ... Some women prefer to avoid analgesic medication during childbirth. Psychological preparation may be beneficial. Relaxation ... Various methods may help with pain, such as relaxation techniques, opioids, and spinal blocks. It is best practice to limit the ... Kumar, Manoj; Paes, Bosco (July 2003). "Epidural Opioid Analgesia and Neonatal Respiratory Depression". Journal of Perinatology ...
Single Convention on Narcotic Drugs
"Assuring Availability of Opioid Analgesics for Palliative Care"). The Senlis Council, a European drug policy thinktank, ... agonist-antagonist opioid) butorphanol (agonist-antagonist opioid) There are of course many opioid designer drugs, not used in ... pentazocine Synthetic open chain opioids having also stimulant effects: lefetamine Some opioids currently or formerly used in ... Semisynthetic agonist-antagonist opioids: buprenorphine Synthetic agonist-antagonist opioids - benzomorphans: ...
... similar to the opioids tramadol and tapentadol, and mutually complements the analgesic effect of its NMDA receptor antagonism. ... Levorphanol acts predominantly as an agonist of the μ-opioid receptor (MOR), but is also an agonist of the δ-opioid receptor ( ... Kappa-opioid receptor agonists, Morphinans, Mu-opioid receptor agonists, NMDA receptor antagonists, Nociceptin receptor ... Levorphanol's exceptionally high analgesic efficacy in the treatment of neuropathic pain is also conferred by its action on ...
... (trade names Prisilidine and Nisentil) is an opioid analgesic that is an analog of pethidine (meperidine). It was ... Mu-opioid receptor agonists, Opioids, 4-Phenylpiperidines, Propionate esters). ... Prodine has broadly similar effects to other opioids, producing analgesia, sedation and euphoria. Side effects can include ...
Synthetic opioids, Thiophenes, Dimethylamino compounds, Mu-opioid receptor agonists, All stub articles, Analgesic stubs). ... is an opioid analgesic drug, most often used in veterinary medicine in Japan and to a lesser extent in other countries in the ... a series of open-chain opioids structurally related to methadone which are also called the thienyl derivative opioids which ... also includes diethylthiambutene and ethylmethylthiambutene, as well as the non-opioid cough suppressant tipepidine. ...
It has been found to act as both a mu opioid agonist and an NMDA antagonist, both of which are mechanisms of action shared with ... but has mainly been researched for the analgesic effects that it produces, and is thought to be one of the components ... responsible for the analgesic effects seen when Psychotria colorata is used in traditional medical practice in humans. ... commonly used painkillers (morphine and ketamine respectively, and which occur concurrently in the clinical analgesics tramadol ...
Semisynthetic opioids, Mu-opioid receptor agonists, All stub articles, Analgesic stubs). ... 14-Cinnamoyloxycodeinone is the most potent example in a series of opiate analgesic drugs discovered in the 1960s, with > ×100 ... Buckett WR (December 1964). "The relationship between analgesic activity, acute toxicity and chemical structure in esters of 14 ...
Mark A Gillman
2012) Psychotropic Analgesic Nitrous oxide (PAN) also an opioid: Beneficial action in substance abuse. Frontiers of Psychiatry ... J Neurol Sci 45: 41-45 Sandyk R, Gillman MA (1986) The opioid system in the restless legs and nocturnal myoclonus Syndromes. ... Gillman MA (2019) Psychotropic Analgesic Nitrous Oxide (PAN) Sedation 4th Edition - Textbook (in CD form). USA,: Udemy.com ... Gillman MA (2004) Psychotropic Analgesic Nitrous Oxide (PAN) Sedation 1st Edition - Textbook (in CD form). Gillman MA (2006) ...
Tolerance to the analgesic and rewarding effects of opioids is complex and occurs due to receptor-level tolerance (e.g., MOR ... Opioids like oxycodone are thought to produce their analgesic effects via activation of the MOR in the midbrain periaqueductal ... Oxycodone, like other opioid analgesics, tends to induce feelings of euphoria, relaxation and reduced anxiety in those who are ... "ER/LA Opioid Analgesic Class Labeling Changes and Postmarket Requirements" (PDF). FDA. Archived (PDF) from the original on 18 ...
... an opioid analgesic Panicudine, an alkaloid Traxoprodil, an NMDA antagonist This set index page lists chemical structure ...
In 1997, The dogma of avoiding analgesics in patients with acute abdominal pain was challenged, and in one of the first studies ... Edsitty, Charly (7 February 2018). "FDA warns Kratom supplement is an opioid". 12news.com/. 12 News. Retrieved 16 October 2021 ... LoVecchio, Frank; Sturmann, Kai; Nelson, Lewis S.; Flashner, Scott; Finger, Ralph (24 June 1997). "The use of analgesics in ... "Administration of analgesics in patients with acute abdominal pain: a survey of the practice of doctors in a developing country ...
... (ebanicline, ABT-594) is a potent synthetic nicotinic (non-opioid) analgesic drug developed by Abbott. It was ... January 1998). "Broad-spectrum, non-opioid analgesic activity by selective modulation of neuronal nicotinic acetylcholine ... May 2000). "Analgesic profile of the nicotinic acetylcholine receptor agonists, (+)-epibatidine and ABT-594 in models of ... Zhang CX, Ge ZM, Cheng TM, Li RT (April 2006). "Synthesis and analgesic activity of secondary amine analogues of ...
1996). "Brain opioid receptors in relation to stereotypies, inactivity, and housing in sows". Physiology & Behavior. 59 (4-5): ... Siegel S; Hinson RE; Krank MD (April 1978). "The role of predrug signals in morphine analgesic tolerance: support for a ... Eating sugary foods causes the brain to release natural chemicals called opioids and dopamine in the limbic system. Tasty food ... Dependence is created through these natural rewards, the sugary treats, and the opioid and dopamine released into the synapses ...
... is an opioid analgesic that is an analog of fentanyl and structural isomer of cyclopropylfentanyl and has been ... Mu-opioid receptor agonists, Piperidines, Synthetic opioids). ... "Opioid-like antinociceptive and locomotor effects of emerging ...
... both substitution products for opioid addiction. Other products include remedies for cocaine and opioid analgesic overdose and ... "Indivior Solutions Pleads Guilty to Felony Charge as Part of DOJ's Largest Opioid Resolution". uspsoig.gov. United States ... 600 million to resolve criminal and civil liability associated with the marketing of the opioid-addiction-treatment drug ... Federal investigation into sales and marketing of opioid addiction treatment. In July 2020, Indivior Solutions, Indivior Inc., ...
... of the brain has led to continued development of an intravenous formulation of CX-717 for use alongside opioid analgesics, ... "Selective antagonism of opioid-induced ventilatory depression by an ampakine molecule in humans without loss of opioid ... and demonstrated that it can be used in humans alongside opioid drugs to reduce this side effect without affecting analgesia. ...
... other physiological capacities are also required such as opioid sensitivity and central modulation of responses by analgesics. ... Injections of naloxone (an opioid antagonist) inhibit the escape responses of earthworms. This indicates that opioid substances ...
Deep brain stimulation
... study of 17 people with intractable cancer pain found that 13 were virtually pain free and only four required opioid analgesics ... Most ultimately did resort to opioids, usually in the last few weeks of life. DBS has also been applied for phantom limb pain. ...
"Opioid glycopeptide analgesics derived from endogenous enkephalins and endorphins". Future Medicinal Chemistry. 4 (2): 205-226 ... Opioid peptides are peptides that bind to opioid receptors in the brain; opiates and opioids mimic the effect of these peptides ... The opioid food peptides have lengths of typically 4-8 amino acids. The body's own opioids are generally much longer. Opioid ... Exorphins include opioid food peptides like Gluten exorphin and opioid food peptides and are mostly contained in cereals and ...
... which are important precursors and intermediates in the synthesis of semi-synthetic opioid analgesic drugs, especially those ... Chloromorphide is one of a series of opioids known as morphides and codides, ... analgesic potency, toxicity, and interaction with narcotic receptors in vitro". J Pharm Sci. 65 (6): 902-4. doi:10.1002/jps. ...
Particularly, mixed kappa receptor agonist mu receptor antagonist opioid analgesics can cause dose-related psychotomimesis. ... Pentazocine and butorphanol fall under this opioid class. There is evidence that cannabinoids are psychotomimetic, especially ... Some rarely used drugs of the opioid class have psychotomimetic effects. ... Cathinones Deliriants Depressants Depressogens Designer drugs Dissociatives Hallucinogens Hypnotics Narcotics Opioids ...
... is a major metabolite of the opioid analgesic drug dextropropoxyphene, and is responsible for many of the side ... Synthetic opioids, Opioid metabolites, Propionate esters, Amines, Potassium channel blockers, Sodium channel blockers). ... It has weaker analgesic effects than dextropropoxyphene itself, but is a relatively potent pro-convulsant and blocker of sodium ... up to 10 times more likely to cause death following overdose compared to other similar mild opioid analgesics, and has led to ...
Analgesics, Opioids, Peptides). ... June 1990). "New features of the delta opioid receptor: ... Deltorphin I, also known as [D-Ala2]deltorphin I or deltorphin C, is a naturally occurring, exogenous opioid heptapeptide and ... Deltorphin possesses very high affinity and selectivity as an agonist for the δ-opioid receptor, and on account of its ... July 1989). "Deltorphins: a family of naturally occurring peptides with high affinity and selectivity for delta opioid binding ...
Mu-opioid receptor agonists, Semisynthetic opioids, Benzyl compounds). ... It is weaker than morphine as an analgesic but longer-lasting in effects, and was thought to have more local anesthetic effect ... Consequently, it was thought to be useful in treating pain in addicts who were being detoxified from other opioid drugs. It is ...
Acetaminophen is an analgesic that can also be used, but NSAIDS and ASA should be selecting first due to their anti ... Opioids are not recommended for treatment of acute migraines due to their significant side effect profile, including twice the ... Opioids are not recommended for treatment of migraines. The triptan drug class includes 1st generation sumatriptan (which has ... Importantly, there is also risk of addiction and opioid use disorder. For patients who require preventive therapy with symptoms ...
Cicero TJ, Inciardi JA, Muñoz A (2005). "Trends in abuse of Oxycontin and other opioid analgesics in the United States: 2002- ... Purdue continued to market and sell opioids as late as 2019 and continued to be involved in lawsuits around the opioid epidemic ... "Opioid talks break down; Purdue owners balk at paying $4.5 billion". Associated Press. Archived from the original on 2019-09-21 ... The company is one of the largest producers of off-patent generic opioids in the US. Sister companies to Purdue that are also ...
... is an opioid analgesic drug used in scientific research. JTC-801 is a selective antagonist for the nociceptin receptor ... Drugs acting at the noiciceptin receptor may influence the effects of traditional analgesics such as NSAIDs, μ-opioid agonists ... JTC-801 is an orally active drug that blocks the nociceptin receptor and produces analgesic effects in a variety of animal ... Zaveri N, Jiang F, Olsen C, Polgar W, Toll L (October 2005). "Small-molecule agonists and antagonists of the opioid receptor- ...
Convention on Psychotropic Substances
... glutethimide Semisynthetic agonist-antagonist opioids: buprenorphine Synthetic agonist-antagonist opioids - benzomorphans: ... strongly sedative benzodiazepines like flunitrazepam and some analgesics like buprenorphine. The only ATS in this category is ... open chain opioid having also stimulant effects Salts of all the substances covered by the four schedules, whenever the ... agonist-antagonist opioid) caffeine (stimulant) dextromethorphan (dissociative, used medically as a cough suppressant) and its ...