BACKGROUND Opioids enhance and prolong analgesia when applied as adjuvants to local anaesthetics (LAs). A possible molecular mechanism for this property is a direct inhibition of voltage-gated Na(+) channels which was reported for some opioids. Methadone is an effective adjuvant to LA and was recently reported to inhibit cardiac Na(+) channels. Here, we explore and compare LA properties of meth...

Homomeric 5-hydroxytryptamine (5-HT)(3A) and heteromeric 5-HT(3AB) receptors mediate rapid excitatory responses to serotonin in the central and peripheral nervous systems. The alkaloid morphine, in addition to being a mu-opioid receptor agonist, is a potent competitive inhibitor of 5-HT(3) receptors. We examined whether methadone, an opioid often used to treat morphine dependence, also exhibite...

We report persistent galactorrhoea and raised prolactin in a woman taking methadone, which is commonly prescribed for the treatment of opiate dependence. A heroin smoking 28 year old mother of two (younger child aged 4), with hepatitis C (of nine years’ duration), weighing 50 kg, was first prescribed 30 mg methadone a day for opiate dependence. She reported newly emergent galactorrhoea after fo...

PURPOSE To define the dose ratio between morphine and methadone in relation to the previous morphine dose and the number of days needed to achieve the same level of analgesia in a group of patients with advanced cancer with pain who switched from morphine to oral methadone. PATIENTS AND METHODS A cross-sectional prospective study of 38 consecutive cancer patients who switched from morphine to...

The peripheral conversion of testosterone to estradiol by aromatase is the primary source of endogenous estrogen in postmenopausal women. Studies indicating that placental aromatase is able to metabolize methadone to its primary metabolite, 2-ethylidene-1, 5-dimethyl-3, 3-diphenylpyrrolidin (EDDP), led us to test the hypothesis that methadone is able to act as an inhibitor of aromatase. Using r...

BACKGROUND The first evidence that the hazard ratio (HR) for methadone-specific death rises more steeply with age-group than for all drug-related deaths (DRDs) came from Scotland's cohort of 33,000 methadone-prescription clients. We aim to examine, for England, whether illicit opioid users' risk of methadone-specific death increases with age; and to pool age-related HRs for methadone-specific d...

Radioimmunoassay was compared to thin-layer and gas--liquid chromatographic methods for detection of methadone in the urine of patients undergoing methadone maintenance therapy as treatment of heroin abuse. With urine samples known to contain methadone, 84% were positive by thin-layer chromatography as compared to 99% positives by the other two methods. This difference is attributed to the diff...

This study examines the pharmacokinetic/pharmacodynamic interactions between (1) lopinavir-ritonavir (L/R), a fixed combination of protease inhibitors used for the treatment of HIV disease, and (2) ritonavir alone at the same dosage as that in the L/R formulation, with methadone, an opiate frequently used in substance abuse pharmacotherapy for opioid (heroin)-dependent injection drug users, man...

Methadone has beneficial characteristics as an analgesic against cancer pain, including high bioavailability, multiple receptor affinities, and lack of active metabolites that might induce adverse side effects. However, methadone has an own pharmacological profile that should be considered in the treatment of cancer patients. There is evidence from preclinical studies that methadone could also ...

BACKGROUND Methadone is a synthetic opioid that is widely used for the treatment of chronic pain. The association between methadone treatment and QT interval prolongation or which can lead to torsades de pointes has been confirmed with larger studies on high dose methadone. The aim of this study was to determine the effect of methadone on the QTc interval in patients, whether the daily dose of ...