BACKGROUND Methadone is a unique µ-opioid receptor agonist. Although several researchers have insisted that the pharmacological effects of methadone are mediated through the blockade of NMDA receptor, the underlying mechanism by which methadone exerts its distinct pharmacological effects compared to those of other µ-opioid receptor agonists is still controversial. In the present study, we furth...

Methadone was found to significantly inhibit the in vitro and in vivo growth of human lung cancer cells. The in vitro growth inhibition (occurring at 1-100 nM methadone) was associated with changes in cell morphology and viability detectable within 1 hr and was irreversible after a 24-hr exposure to the drug. These effects of methadone could be reversed in the first 6 hr by naltrexone, actinomy...

The l-isomer of methadone possesses opioid activity, whereas the d-isomer is weak or inactive as an opioid. Both d- and l-methadone have been shown to bind to the N-methyl-D-aspartate (NMDA) receptor. To determine whether d-methadone has functional, in vivo NMDA receptor antagonist activity, the antinociceptive effects of d-methadone were evaluated in the rat tail-flick and formalin tests. Cumu...

Research demonstrates that drug treatment staff members' knowledge and attitudes about methadone are positively correlated with treatment success among opiate-dependent clients. However the bulk of this research is on outpatient treatment in methadone clinics. This study examined a residential treatment program that allowed clients on methadone, a rare treatment opportunity that is growing nati...

Introduction: Methadone has been an essential medication in the treatment of opioid addiction worldwide. Aim: To discuss dosing considerations related to different methadone programs. Method: A search was performed the Ovid (all resources) including: Medline, Cochrane, and EMBASE databases using the following terms: methadone dose, methadone optimization, and methadone adequacy. We compared and...

Methadone is administered as a racemate, although opioid activity resides in the R-enantiomer. Methadone disposition is stereoselective, with considerable unexplained variability in clearance and plasma R/S ratios. N-Demethylation of methadone in vitro is predominantly mediated by cytochrome P450 CYP3A4 and CYP2B6 and somewhat by CYP2C19. This investigation evaluated stereoselectivity, models, ...

BACKGROUND The pharmacokinetics of methadone is altered during pregnancy, but the most appropriate dosing and monitoring regimen has yet to be identified. OBJECTIVE To review dosing and monitoring of methadone therapy in pregnancy. METHODS A literature search was performed in several databases (PubMed, MEDLINE, Embase, International Pharmaceutical Abstracts, and the Cochrane Database of Sys...

BACKGROUND Opioid dependence is a chronic, relapsing disorder with important public health implications. METHODS In a 17-week randomized study of 220 patients, we compared levomethadyl acetate (75 to 115 mg), buprenorphine (16 to 32 mg), and high-dose (60 to 100 mg) and low-dose (20 mg) methadone as treatments for opioid dependence. Levomethadyl acetate and buprenorphine were administered thr...

BACKGROUND Methadone is a synthetic, narcotic analgesic used in the treatment of drug misuse. Tragedies involving children being poisoned by the accidental ingestion of methadone are no longer a rare occurrence. Following an audit of the effectiveness of the provision and recall of information to patients attending an NHS Methadone Clinic a protocol was introduced to ensure that staff documente...

BACKGROUND Vital statistics data suggest that the opioid pain reliever (OPR) methadone is involved in one third of OPR-related overdose deaths, but it accounts for only a few percent of OPR prescriptions. METHODS CDC analyzed rates of fatal methadone overdoses and sales nationally during 1999-2010 and rates of overdose death for methadone compared with rates for other major opioids in 13 stat...