Analgesics, Opioid
Receptors, Opioid, mu
Receptors, Opioid
Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.
Receptors, Opioid, delta
Receptors, Opioid, kappa
Opioid Peptides
The endogenous peptides with opiate-like activity. The three major classes currently recognized are the ENKEPHALINS, the DYNORPHINS, and the ENDORPHINS. Each of these families derives from different precursors, proenkephalin, prodynorphin, and PRO-OPIOMELANOCORTIN, respectively. There are also at least three classes of OPIOID RECEPTORS, but the peptide families do not map to the receptors in a simple way.
Analgesics, Non-Narcotic
Morphine
Pain
Naloxone
Pain Measurement
Naltrexone
Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.
Enkephalins
Narcotics
Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
Drug Tolerance
Progressive diminution of the susceptibility of a human or animal to the effects of a drug, resulting from its continued administration. It should be differentiated from DRUG RESISTANCE wherein an organism, disease, or tissue fails to respond to the intended effectiveness of a chemical or drug. It should also be differentiated from MAXIMUM TOLERATED DOSE and NO-OBSERVED-ADVERSE-EFFECT LEVEL.
Buprenorphine
A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.
Endorphins
One of the three major groups of endogenous opioid peptides. They are large peptides derived from the PRO-OPIOMELANOCORTIN precursor. The known members of this group are alpha-, beta-, and gamma-endorphin. The term endorphin is also sometimes used to refer to all opioid peptides, but the narrower sense is used here; OPIOID PEPTIDES is used for the broader group.
Enkephalin, D-Penicillamine (2,5)-
Fentanyl
Dynorphins
Phenacetin
Acetaminophen
Hydromorphone
Enkephalin, Leucine
Morphinans
Dextropropoxyphene
Codeine
Injections, Spinal
Enkephalin, Leucine-2-Alanine
Hyperalgesia
beta-Endorphin
Anti-Inflammatory Agents, Non-Steroidal
Anti-inflammatory agents that are non-steroidal in nature. In addition to anti-inflammatory actions, they have analgesic, antipyretic, and platelet-inhibitory actions.They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. Inhibition of prostaglandin synthesis accounts for their analgesic, antipyretic, and platelet-inhibitory actions; other mechanisms may contribute to their anti-inflammatory effects.
Meperidine
Pain Management
Pentazocine
Dose-Response Relationship, Drug
Methadone
Benzeneacetamides
Diprenorphine
Butorphanol
Anesthetics, Local
Drugs that block nerve conduction when applied locally to nerve tissue in appropriate concentrations. They act on any part of the nervous system and on every type of nerve fiber. In contact with a nerve trunk, these anesthetics can cause both sensory and motor paralysis in the innervated area. Their action is completely reversible. (From Gilman AG, et. al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed) Nearly all local anesthetics act by reducing the tendency of voltage-dependent sodium channels to activate.
Hydrocodone
Chronic Pain
Oxymorphone
An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092)
Double-Blind Method
Dipyrone
Analgesia, Epidural
Levorphanol
Analgesia, Patient-Controlled
Relief of PAIN, without loss of CONSCIOUSNESS, through ANALGESIC AGENTS administered by the patients. It has been used successfully to control POSTOPERATIVE PAIN, during OBSTETRIC LABOR, after BURNS, and in TERMINAL CARE. The choice of agent, dose, and lockout interval greatly influence effectiveness. The potential for overdose can be minimized by combining small bolus doses with a mandatory interval between successive doses (lockout interval).
Rats, Sprague-Dawley
Nociceptors
Peripheral AFFERENT NEURONS which are sensitive to injuries or pain, usually caused by extreme thermal exposures, mechanical forces, or other noxious stimuli. Their cell bodies reside in the DORSAL ROOT GANGLIA. Their peripheral terminals (NERVE ENDINGS) innervate target tissues and transduce noxious stimuli via axons to the CENTRAL NERVOUS SYSTEM.
Alfentanil
A short-acting opioid anesthetic and analgesic derivative of FENTANYL. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients.
Nociception
Nalbuphine
Substance Withdrawal Syndrome
Heroin
Neuralgia
Tolmetin
Carrageenan
Ketoprofen
Sufentanil
Meptazinol
Ketorolac
Acupuncture Analgesia
Analgesia produced by the insertion of ACUPUNCTURE needles at certain ACUPUNCTURE POINTS on the body. This activates small myelinated nerve fibers in the muscle which transmit impulses to the spinal cord and then activate three centers - the spinal cord, midbrain and pituitary/hypothalamus - to produce analgesia.
Nalorphine
Kidney Papillary Necrosis
A complication of kidney diseases characterized by cell death involving KIDNEY PAPILLA in the KIDNEY MEDULLA. Damages to this area may hinder the kidney to concentrate urine resulting in POLYURIA. Sloughed off necrotic tissue may block KIDNEY PELVIS or URETER. Necrosis of multiple renal papillae can lead to KIDNEY FAILURE.
Nociceptive Pain
Drug Overdose
Acute Pain
Periaqueductal Gray
Nefopam
Prescription Drug Misuse
Spinal Cord
Ibuprofen
Opiate Substitution Treatment
Drug Interactions
Analgesia, Obstetrical
Ketamine
Edema
Diclofenac
Electroacupuncture
Nerve Block
Ethylketocyclazocine
Rats, Wistar
Nitrous Oxide
Drug and Narcotic Control
Lidocaine
Hypnotics and Sedatives
Dexmedetomidine
Opiate Alkaloids
Chronic Disease
Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care. (Dictionary of Health Services Management, 2d ed)
Acetic Acid
Formaldehyde
A highly reactive aldehyde gas formed by oxidation or incomplete combustion of hydrocarbons. In solution, it has a wide range of uses: in the manufacture of resins and textiles, as a disinfectant, and as a laboratory fixative or preservative. Formaldehyde solution (formalin) is considered a hazardous compound, and its vapor toxic. (From Reynolds, Martindale The Extra Pharmacopoeia, 30th ed, p717)
Ketorolac Tromethamine
Treatment Outcome
Loperamide
Amines
Amides
Opium
The air-dried exudate from the unripe seed capsule of the opium poppy, Papaver somniferum, or its variant, P. album. It contains a number of alkaloids, but only a few - MORPHINE; CODEINE; and PAPAVERINE - have clinical significance. Opium has been used as an analgesic, antitussive, antidiarrheal, and antispasmodic.
Freund's Adjuvant
An antigen solution emulsified in mineral oil. The complete form is made up of killed, dried mycobacteria, usually M. tuberculosis, suspended in the oil phase. It is effective in stimulating cell-mediated immunity (IMMUNITY, CELLULAR) and potentiates the production of certain IMMUNOGLOBULINS in some animals. The incomplete form does not contain mycobacteria.
Levallorphan
An opioid antagonist with properties similar to those of NALOXONE; in addition it also possesses some agonist properties. It should be used cautiously; levallorphan reverses severe opioid-induced respiratory depression but may exacerbate respiratory depression such as that induced by alcohol or other non-opioid central depressants. (From Martindale, The Extra Pharmacopoeia, 30th ed, p683)
Drug Combinations
Drug Administration Schedule
Self Medication
Anesthetics, Dissociative
Intravenous anesthetics that induce a state of sedation, immobility, amnesia, and marked analgesia. Subjects may experience a strong feeling of dissociation from the environment. The condition produced is similar to NEUROLEPTANALGESIA, but is brought about by the administration of a single drug. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed)
Radioligand Assay
Guanosine 5'-O-(3-Thiotriphosphate)
Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.
Piroxicam
Clonidine
Plant Extracts
Disease Models, Animal
Brain
The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.
Transcutaneous Electric Nerve Stimulation
Tromethamine
An organic amine proton acceptor. It is used in the synthesis of surface-active agents and pharmaceuticals; as an emulsifying agent for cosmetic creams and lotions, mineral oil and paraffin wax emulsions, as a biological buffer, and used as an alkalizer. (From Merck, 11th ed; Martindale, The Extra Pharmacopoeia, 30th ed, p1424)
Adrenergic alpha-2 Receptor Agonists
D-Ala(2),MePhe(4),Met(0)-ol-enkephalin
Analysis of Variance
Prospective Studies
Preanesthetic Medication
Cannabinoids
Prilocaine
Posterior Horn Cells
Neurons in the SPINAL CORD DORSAL HORN whose cell bodies and processes are confined entirely to the CENTRAL NERVOUS SYSTEM. They receive collateral or direct terminations of dorsal root fibers. They send their axons either directly to ANTERIOR HORN CELLS or to the WHITE MATTER ascending and descending longitudinal fibers.
Aspirin
The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5)
Injections, Subcutaneous
Drug Utilization
Stereoisomerism
Ligands
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
Somatostatin
A 14-amino acid peptide named for its ability to inhibit pituitary GROWTH HORMONE release, also called somatotropin release-inhibiting factor. It is expressed in the central and peripheral nervous systems, the gut, and other organs. SRIF can also inhibit the release of THYROID-STIMULATING HORMONE; PROLACTIN; INSULIN; and GLUCAGON besides acting as a neurotransmitter and neuromodulator. In a number of species including humans, there is an additional form of somatostatin, SRIF-28 with a 14-amino acid extension at the N-terminal.
Guinea Pigs
Anesthesia, General
Conscious Sedation
Drug Administration Routes
Placebo Effect
Ambulatory Surgical Procedures
Ganglia, Spinal
Sensory ganglia located on the dorsal spinal roots within the vertebral column. The spinal ganglion cells are pseudounipolar. The single primary branch bifurcates sending a peripheral process to carry sensory information from the periphery and a central branch which relays that information to the spinal cord or brain.
Anesthetics, Combined
Cross-Over Studies
Studies comparing two or more treatments or interventions in which the subjects or patients, upon completion of the course of one treatment, are switched to another. In the case of two treatments, A and B, half the subjects are randomly allocated to receive these in the order A, B and half to receive them in the order B, A. A criticism of this design is that effects of the first treatment may carry over into the period when the second is given. (Last, A Dictionary of Epidemiology, 2d ed)
Vas Deferens
Structure-Activity Relationship
Anesthetics
Drug Therapy, Combination
Self Administration
Locus Coeruleus
Anesthesia, Obstetrical
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.
Placebos
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)
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Use and dependence on opioid drugs in the Spanish population with chronic pain: Prevalence and differences according to sex |...
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in Animal Model
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In Response: The Cause of Fatal Respiratory Depression Is Combination of Clindamycin and Fentanyl, Rather than Tramadol. -...
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Most recent papers in the journal F1000Research | Read by QxMD
Opioid receptor
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 ...
BDSM
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 ...
U-47700
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). ...
Opioid
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 ...
Cardioversion
Opioid analgesics (e.g., Fentanyl) may be combined with Propofol, although anesthesiology must weight the benefits against ...
Furethidine
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 ...
Nalmexone
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. ...
Metofoline
... (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. ...
Homofentanyl
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 ...
Desomorphine
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 ...
Methyldesorphine
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 ...
Opioid rotation
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 ...
N-Phenethylnordesomorphine
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 ...
Diphenoxylate
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 ...
Heterocodeine
"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 ...
Phenazone
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 ...
Pyrazolone
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, ...
Ludwig Knorr
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 ...
Metamizole
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 ...
Benzethidine
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 ...
Ibuprofen
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 ...
Benzhydrocodone
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 ...
Formication
... and as a side effect of opioid analgesics.[citation needed] Formication is etymologically derived from the Latin word formica, ...
Selegiline
... 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 ...
Chlorpromazine
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 ...
Phenoperidine
... 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 ...
HZ-2
... 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: ...
C21H25NO2
... an opioid analgesic Piperidolate, an antimuscarinic This set index page lists chemical structure articles associated with the ...
Adrenorphin
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- ...
Childbirth
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: ...
Levorphanol
... 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 ...
Prodine
... (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 ...
Dimethylthiambutene
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. ...
Hodgkinsine
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 ...
14-Cinnamoyloxycodeinone
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) ...
Oxycodone
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 ...
C20H25NO3
... an opioid analgesic Panicudine, an alkaloid Traxoprodil, an NMDA antagonist This set index page lists chemical structure ...
Frank LoVecchio
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 ...
Tebanicline
... (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 ...
Animal psychopathology
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 ...
Crotonylfentanyl
... 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 ...
Indivior
... 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., ...
CX717
... 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. ...
Earthworm
... 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 peptide
"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 ...
Chloromorphide
... 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. ...
Psychotomimetism
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 ...
Norpropoxyphene
... 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 ...
Deltorphin I
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 ...
Myrophine
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 ...
Antimigraine drug
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 ...
Purdue Pharma
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 ...
JTC-801
... 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 ...