Narcotic Antagonists

Narcotic (opioid) antagonists are not psychoactive agents but rather drugs that bind to the opioid receptors with greater affinity than do opioid agonists without activating mu, delta, or kappa receptor sites and without producing tolerance. Through this blocking action, they prevent the body from responding to both externally administered opioids and natural endorphins. The two most prominent are naloxone (Narcan, Nalone) and naltrexone (Revia, Depade, Vivitrol). Narcan’s primary use is to reverse the negative effects of an opioid overdose, counteracting the effects of respiratory depression, sedation, and hypotension (low blood pressure). Naltrexone, a long-acting competitive antagonist at opioid receptors that blocks both the subjective and objective effects of opioids, can be orally administered. Initially used as a treatment adjunct for those with a heroin dependency, ...