Methadone-like agonists

Diphenylheptanes (methadone-like agonists) Methadone Synthetic +... 

Methadone-Like Agonists Methadone Transmucosal for breakthrough pain only IM (acute) Variable ... 

In October 2002, the FDA approved two new medications for treating opiate addiction, both developed by Reckitt Benckiser Pharmaceuticals. The new drugs, Subutex (buprenorphine hydrochloride) and Suboxone tablets (buprenorphine hydrochloride and naloxone hydrochloride) contain buprenorphine, a partial opioid agonist. Like methadone, buprenorphine binds to the brain s opioid receptors, but produces significantly reduced pleasurable effects than heroin. 

Buprenorphine is a potent and long-acting phenanthrene derivative that is a partial receptor agonist. Its long duration of action is due to its slow dissociation from receptors. This property renders its effects resistant to naloxone reversal. Its clinical applications are much like those of nalbuphine. In addition, studies continue to suggest that buprenorphine is as effective as methadone in the detoxification and maintenance of heroin abusers. 

Nonopioid. The withdrawal sjmdrome is also treatable with nonopioid drugs. Lofexidine inhibits sympathetic autonomic outflow by its agonist action on central presynaptic cc -adrenoceptors and so reduces the effects of noradrenergic hyperactivity (see above). It is similar to clonidine (see p. 482) but less likely to cause hypotension. Evidence indicates that lofexidine is as effective as methadone in withdrawal supervised in residential or community settings having no street value it is not liable to be traded. 

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