Levo-Alpha Acetyl Methadol

There are currently three Food and Drug Administration (FDA)-approved opioid agonist treatments for opioid addiction, which include methadone hydrochloride, buprenorphine hydrochloride, and levo-alpha acetyl methadol (LAAM). All three of these drugs are long-acting opioids, which bind to opioid receptors and thus block opioids from binding to these receptors. LAAM, as well as the other opioid agonist treatments, are long-acting drugs that have minimal psychoactive effects. Use of LAAM thus permits opioid-addicted individuals to engage normally in daily routines while decreasing craving or drug-seeking behaviors.

LAAM may also be labeled as levomethadyl acetate hydrochloride or levacetylmethadol. LAAM was developed in the 1960s and was under investigation as a medication in the treatment of opioid dependence until the 1990s. In 1993, LAAM was approved by the FDA as a medication for opioid dependence. LAAM offers improvements over drugs like methadone because it has a significantly longer duration of action. However, despite the initial excitement over the introduction of LAAM for the treatment of opioid dependence, use of LAAM was found to be associated with adverse side effects, in particular, cardiac symptomatology. Such findings have since decreased the enthusiasm and thus have limited the demand for this drug.

Similar to methadone, LAAM is an oral medication. It is a synthetic opioid whose properties ameliorate symptoms for patients experiencing withdrawal from opioids. The mechanism of action for LAAM is to bind to pain receptors in the brain, and this binding [Page 514]action results in a decrease in patient cravings for heroin or other opioids and a decrease in withdrawal symptoms. More specifically, LAAM acts as a mu (u) opioid receptor agonist. It has effects that are qualitatively similar to both morphine and methadone, but has the unique characteristic of a longer duration of action. LAAM provides opioid effects for 48 to 72 hours or longer depending on the dose. In contrast, methadone provides opioid effects for approximately 24 hours. This increase in the duration of action presents a significant improvement for patients being treated for opioid dependence. Although some studies indicate that LAAM is less potent than methadone, at least one study has demonstrated that under acute dosing conditions, LAAM may be significantly more potent relative to methadone. Despite its long duration of action, it should be noted that withdrawal from LAAM can be difficult.