Definition
Description
Top Gene Interactions
Related Pathways
General Information
- Metabolism: Hepatic. Cytochrome P450 enzymes, primarily CYP3A4, CYP2B6, and CYP2C19 and to a lesser extent CYP2C9 and CYP2D6, are responsible for conversion of methadone to EDDP and other inactive metabolites, which are excreted mainly in the urine. Route of Elimination: The elimination of methadone is mediated by extensive biotransformation, followed by renal and fecal excretion. Unmetabolized methadone and its metabolites are excreted in urine to a variable degree. Half Life: 24-36 hours
- Uses/Sources: For the treatment of dry cough, drug withdrawal syndrome, opioid type drug dependence, and pain (A308).
- Health Effects: Bradycardia and hypotension. In severe overdosage, particularly by the intravenous route, apnea, circulatory collapse, cardiac arrest, and death may occur (RxList, A308). Medical problems can include congested lungs, liver disease, tetanus, infection of the heart valves, skin abscesses, anemia and pneumonia. Death can occur from overdose.
- Symptoms: In severe overdosage, particularly by the intravenous route, apnea, circulatory collapse, cardiac arrest, and death may occur.
- Treatment: Primary attention should be given to the reestablishment of adequate respiratory exchange through provision of a patent airway and institution of assisted or controlled ventilation. If a non-tolerant person, takes a large dose of methadone, effective opioid antagonists are available to counteract the potentially lethal respiratory depression. (L1712)
- Route of Exposure: Inhalation (MSDS, RxList, A308); dermal (MSDS, RxList, A308); ingestion (MSDS, RxList, A308); intravenous injection (MSDS, RxList, A308). Well absorbed following oral administration. The bioavailability of methadone ranges between 36 to 100%.
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
Potassium voltage-gated channel subfamily H member 2 Multidrug resistance protein 1 Kappa-type opioid receptor Delta-type opioid receptor 5-hydroxytryptamine receptor 3A Toll-like receptor 4 Alpha-1-acid glycoprotein 2 |
20178837 7932177 11408360 11585443 19131665 8114680 15911273 19843777 8946472 |
|
Glutamate receptor ionotropic, NMDA 3A Neuronal acetylcholine receptor subunit alpha-10 Mu-type opioid receptor |
Methadone is a mu-agonist; a synthetic opioid analgesic with multiple actions qualitatively similar to those of morphine, the most prominent of which involves the central nervous system and organs composed of smooth muscle. The principal therapeutic uses for methadone are for analgesia and for detoxification or maintenance in opioid addiction. The methadone abstinence syndrome, although qualitatively similar to that of morphine, differs in that the onset is slower, the course is more prolonged, and the symptoms are less severe. Some data also indicate that methadone acts as an antagonist at the N-methyl-D-aspartate (NMDA) receptor. The contribution of NMDA receptor antagonism to methadone's efficacy is unknown. Other NMDA receptor antagonists have been shown to produce neurotoxic effects in animals. |
17016423 14991152 17139284 11933204 11585443 17850768 |
Methadone Interacts with Diseases
Disease | Inference Score | References/Inference Genes |
Hepatitis, Autoimmune | 26.38 |
|
Brain Ischemia | 23.84 |
|
HIV Wasting Syndrome | 19.72 |
|
Burns | 19.3 |
|
Entamoebiasis | 19.18 |
|
Reperfusion Injury | 19.14 |
|
Leishmaniasis, Cutaneous | 18.17 |
|
Crohn's disease | 17.76 |
|
Allergy | 17.68 |
|
Heat Stroke | 17.53 |
|
Glomerulonephritis | 17.01 |
|
Arthritis, Experimental | 16.91 |
|
Brain Injuries | 16.6 |
|
Anthracosis | 16.28 |
|
Pneumonia | 16.19 |
|
Radiation Injuries, Experimental | 16.03 |
|
Mitochondrial Myopathies | 15.22 |
|
Pleurisy | 15.03 |
|
Prostatic Neoplasms | 14.9 |
|
Trigeminal Neuralgia | 14.51 |
|