Opioid Antagonists

Behavioral characterization of opioid mixed agonist-antagonists.

The effects of agonists and partial agonists of both mu and kappa receptor systems are described in several behavioral tests in rhesus monkeys. Procedures measuring drug discrimination, drug self-administration, drug dependence, and drug-induced analgesia are differentially sensitive to the agonist and antagonist effects of various opioids. The sensitivity of each of the procedures may be modif...

Marketed New Drug Delivery Systems for Opioid Agonists/Antagonists ‎Administration: A Rapid Overview

Novel drug delivery systems for controlled-release of opioid agonists as a long time painkillers or opioid antagonists for opium, heroin, and alcohol addiction are under development or in clinical use today. In this article, the field of “new drug delivery systems” is momentarily reviewed from the viewpoint of the marketed opioid agonists/antagonists dosage forms today.

Opioid antagonists, partial agonists, and agonists/antagonists: the role of office-based detoxification.

BACKGROUND The opioid receptor antagonists naloxone and naltrexone are competitive antagonists at the mu, kappa, and sigma receptors with a higher affinity for the mu receptor and lacking any mu receptor efficacy. Buprenorphine is classified as a partial agonist. It has a high affinity, but low efficacy at the mu receptor where it yields a partial effect upon binding. It also, however, possesse...

Safety of the newer class of opioid antagonists in pregnancy.

QUESTION I have a patient recently confirmed to be 6 weeks pregnant. For the past 6 months she has been treated for an opioid addiction with buprenorphine-naloxone combination. Should I be concerned about her exposure to this drug combination up to this point of the pregnancy? Should I switch her medication to methadone now that she is pregnant? ANSWER The limited data on buprenorphine exposu...

Behavioral interactions of opioid agonists and antagonists with serotonergic systems.