Methadone

Methadone treatmentAmidonAmidonesDolophineFizziesMethadone hydrochlorideMethadone treatmentsmethadone withdrawalMethadosephyseptone
Methadone, sold under the brand name Dolophine among others, is an opioid used for opioid maintenance therapy in opioid dependence and for chronic pain management.wikipedia
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Opioid

opioidsopioid-induced constipationopioid analgesic
Methadone, sold under the brand name Dolophine among others, is an opioid used for opioid maintenance therapy in opioid dependence and for chronic pain management.
Research suggests that when methadone is used long-term it can build up unpredictably in the body and lead to potentially deadly slowed breathing.

WHO Model List of Essential Medicines

World Health Organization's List of Essential MedicinesList of Essential MedicinesModel List of Essential Medicines
Methadone is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.

Gustav Ehrhart

Methadone was developed in Germany around 1937 to 1939 by Gustav Ehrhart and Max Bockmühl.
He synthesized the first fully synthetic opioid analgesic, methadone, together with Max Bockmühl.

Opioid use disorder

heroin addictionopioid addictionheroin addict
Methadone, sold under the brand name Dolophine among others, is an opioid used for opioid maintenance therapy in opioid dependence and for chronic pain management.
Individuals with an opioid use disorder are often treated with opioid replacement therapy using methadone or buprenorphine.

Analgesic

analgesiaanalgesicspainkillers
Methadone is used as an analgesic in chronic pain, often in rotation with other opioids.
Some analgesics such as methadone and ketobemidone and perhaps piritramide have intrinsic NMDA action.

Opioid rotation

opioid rotation therapyopioid switchingrotation with other opioids
Methadone is used as an analgesic in chronic pain, often in rotation with other opioids.
The reasons for this are still not completely understood, but are thought to result from variations in opioid receptor affinity and occupancy levels at equianalgesic doses, as well as additional mechanisms of action possessed by some drugs such as the NMDA antagonist action of methadone or levorphanol, or the SNRI activity of tramadol or tapentadol.

QT interval

QTcQTc intervalCorrected QT interval
Abnormal heart rhythms may also occur due to a prolonged QT interval.
Many drugs, such as haloperidol, vemurafenib, ziprasidone, methadone sertindole, and pitolisant can prolong the QT interval.

Rhinorrhea

runny nosenasal dischargerhinorrhoea
It can be a side effect of crying, exposure to cold temperatures, cocaine abuse or withdrawal, such as from opioids like methadone.

NMDA receptor

NMDANMDARNMDA receptors
Due to its activity at the NMDA receptor, it may be more effective against neuropathic pain; for the same reason, tolerance to the analgesic effects may be less than that of other opioids.

Neuropathic pain

neuropathicpaincentral neuropathic pain
Due to its activity at the NMDA receptor, it may be more effective against neuropathic pain; for the same reason, tolerance to the analgesic effects may be less than that of other opioids.
Several opioids, particularly levorphanol, methadone and ketobemidone, possess NMDA antagonism in addition to their µ-opioid agonist properties.

Naltrexone

Revianaltrexone hydrochlorideSinclair method
Naloxone is preferred to the newer, longer acting antagonist naltrexone.
It has benefits over methadone and buprenorphine in that it is not a restricted medication.

Miosis

mioticconstricted pupilsmiotics
Adverse effects include sedation, hypoventilation, constipation and miosis, in addition to tolerance, dependence and withdrawal difficulties.

Max Bockmühl

Methadone was developed in Germany around 1937 to 1939 by Gustav Ehrhart and Max Bockmühl.
Together with Gustav Ehrhart working for I.G. Farbenindustrie AG at the Farbwerke Hoechst, the pair developed Methadone in Germany, 1937, a drug synthesised from 1,1-diphenylbutane-2-sulfonic acid and dimethylamino-2-chloropropane, as they were looking for a synthetic opioid that could be created with readily available precursors, to solve Germany's opium shortage problem.

NMDA receptor antagonist

NMDA antagonistNMDA antagonistsNMDA receptor antagonists
The dextrorotary form (dextromethadone), which acts as an NMDA receptor antagonist and is devoid of opioid activity, has been shown to produce analgesia in experimental models of chronic pain.
Several synthetic opioids function additionally as NMDAR-antagonists, such as pethidine, levorphanol, methadone, dextropropoxyphene, tramadol and ketobemidone.

CYP2B6

2B6CYP2B6 inhibitors
Methadone is metabolized by CYP3A4, CYP2B6, CYP2D6 and is a substrate for the P-glycoprotein efflux protein in the intestines and brain.

Dextromethadone

The dextrorotary form (dextromethadone), which acts as an NMDA receptor antagonist and is devoid of opioid activity, has been shown to produce analgesia in experimental models of chronic pain. Dextromethadone (the S enantiomer) does not affect opioid receptors but binds to the glutamatergic NMDA (N-methyl-D-aspartate) receptor, and acts as an antagonist against glutamate.
Dextromethadone (developmental code name REL-1017) is the (S)-enantiomer of methadone.

Methadone maintenance

methadone maintenance treatmentmethadone treatmentaddiction treatment
The formulation sold under the brand name Methadose (flavored liquid suspension for oral dosing, commonly used for maintenance purposes) should not be injected either.
Methadone maintenance treatment is the use of methadone, administered over a prolonged period of time, as treatment for someone who is addicted to opioids such as heroin, where detoxification has been unsuccessful and/or admittance to a substance abuse treatment facility requires complete abstinence.

CYP3A4

cytochrome P450 3A43A4cytochrome P450-3A4
Methadone is metabolized by CYP3A4, CYP2B6, CYP2D6 and is a substrate for the P-glycoprotein efflux protein in the intestines and brain.

Levomethadone

Levomethadone (the L enantiomer) is a μ-opioid receptor agonist with higher intrinsic activity than morphine, but lower affinity.
In addition to being used as a pharmaceutical drug itself, levomethadone is the main therapeutic component of methadone.

Biological half-life

elimination half-lifehalf-lifeterminal half-life
The bioavailability and elimination half-life of methadone are subject to substantial interindividual variability.

Eli Lilly and Company

Eli LillyLillyEli Lilly & Company
Methadone was introduced into the United States in 1947 by Eli Lilly and Company as an analgesic under the trade name Dolophine.
Lilly is currently the largest manufacturer of psychiatric medications and produces Prozac (fluoxetine), Dolophine (methadone), Cymbalta (duloxetine), and Zyprexa (olanzapine).

Hallucination

hallucinationshallucinatehallucinating
Hallucinations, pseudohallucinations, or intensification of pareidolia, particularly auditory, are known side effects of opioids to different degrees—it may be associated with the absolute degree of agonism or antagonism of especially the kappa opioid receptor, sigma receptors, delta opioid receptor and the NMDA receptors or the overall receptor activation profile as synthetic opioids like those of the pentazocine, levorphanol, fentanyl, pethidine, methadone and some other families are more associated with this side effect than natural opioids like morphine and codeine and semi-synthetics like hydromorphone, amongst which there also appears to be a stronger correlation with the relative analgesic strength.

Levacetylmethadol

LAAMlevomethadyl acetateOrlaam
Isomethadone, noracymethadol, LAAM, and normethadone were first developed in Germany, United Kingdom, Belgium, Austria, Canada, and the United States in the thirty or so years after the 1937 discovery of pethidine, the first synthetic opioid used in medicine.
Levacetylmethadol (INN), levomethadyl acetate (USAN), OrLAAM (trade name) or levo-α-acetylmethadol (LAAM) is a synthetic opioid similar in structure to methadone.

Noracymethadol

Isomethadone, noracymethadol, LAAM, and normethadone were first developed in Germany, United Kingdom, Belgium, Austria, Canada, and the United States in the thirty or so years after the 1937 discovery of pethidine, the first synthetic opioid used in medicine.
Noracymethadol (INN) is a synthetic opioid analgesic related to methadone that was never marketed.