Opioid agonist-antagonist

Mixed Opioid Agonist-Antagonists or Partiai Agonists... 

Mechanism of Action An opioid agonist-antagonist that binds with opioid receptors in the CNS. Therapeutic Effect Alters the perception of and emotional response to pain blocks the effects of heroin and produces minimal opioid withdrawal symptoms. Pharmacokinetics Rapidly absorbed following IM administration. Protein binding Very high. Metabolized in liver. Primarily excreted in feces minimal excretion in urine. Half-life 2 hr... 

Effective long-acting opioid agonist-antagonist unconfirmed reported lower physical dependence no significant advantages... 

Hoskin, P.J., Hanks, G.W. Opioid agonist-antagonist drugs in acute and chronic pain states, Drugs 1991, 41, 326-344. 

Opioid receptor binding Pentazocine (Brogden et al., 1973) is a mixed opioid agonist-antagonist with agonistic effects at the kappa and partial antagonistic effects at the p-type of opioid receptor. 

Christoph, T. and Buschmann, H. Zwei komplexe Wirkprinzipien in einer Struktur - Gemischte opioide Agonisten/Antagonisten und partielle Agonisten (Two complex action principles in one structure -mixed opioid agonists/antagonists and partial agonists), Pharm. i. u. Zeit 2002, 31, 40-43. 

Preston, K.L. and Jasinski, D.R., Abuse liability studies of opioid agonist-antagonists in humans, Drug Alcohol Depend., 28, 49, 1991. 

As nonsteroidal anti-inflammatory drugs (NSAIDs) exacerbate ALPE, the administration of NSAIDs should be avoided even after onset. When patients require analgesic agents, synthetic opioid agonist/antagonist analgesics (pentazocine hydrochloride or buprenorphine hydrochloride) should be administered. 

The opioid agonist-antagonists include butor-phanol, pentazocine, and buprenorphine... 

Butorphanol is the opioid agonist-antagonist that is most frequently used in the horse. It is a K receptor agonist and can antagonize the effect of JL agonists at the x opioid receptor (Sellon et al 2001). Butorphanol is used in combination with another sedative for standing chemical restraint and as part of premedication protocols for anesthesia. Recommended dose rates for butorphanol are 0.02-0.05 mg/kg i.v. in combination with acepromazine (0.05 mg/kg), xylazine (0.5-1.0 mg/kg) or detomidine (10-20 (xg/kg). 

Indications Opioid dependence, moderate to severe pain Category Analgesic Mixed opioid agonist/antagonist Narcotic Half-life 37 hours... 

Mertz, H., Stockhaus, K., Wick, H., 1997. Diastereoisomeric N-tetrahy-dro-furfuryluoroxy morphones with opioid agonist-antagonist properties. J. Med. Chem. 20, 844-846. 

Buprenorphine is an opioid agonist-antagonist analgesic. Its analgesic effect is caused by binding to opiate receptors in the CNS. Antagonist effects decrease its abuse potential. It is indicated in tablet treatment of opioid dependence injection relief of moderate to severe pain. 

Opioid Agonist-Antagonist or Butorphanol (stadol) Nalbuphine (nubain) Partud Agonist (continued) Not available Not available 2 mg q3 h 10 mg q3 h Not available Not available 2 mg q3 h 10 mg q3 h Not available Not available Not recommended 0.1 mg/kg q3-4h... 

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