pharmacopeia
GET
/api/v1/drug/methadone

Boxed warning

SERIOUS AND LIFE-THREATENING RISKS FROM USE OF METHADONE HYDROCHLORIDE INJECTION Addiction, Abuse, and Misuse Because the use of Methadone Hydrochloride Injection exposes patients and other users to the risks of opioid addiction, abuse, and misuse, which can lead to overdose and death, assess each patient’s risk prior to prescribing and reassess all patients regularly for the development of these behaviors and conditions (see WARNINGS ). Life-Threatening Respiratory Depression Serious, life-threatening, or fatal respiratory depression may occur with use of Methadone Hydrochloride Injection, especially during initiation or following a dosage increase. To reduce the risk of respiratory depression, proper dosing and titration of Methadone Hydrochloride Injection are essential (see WARNINGS ). Neonatal Opioid Withdrawal Syndrome (NOWS) Neonatal opioid withdrawal syndrome (NOWS) is an expected and treatable outcome of use of Methadone Hydrochloride Injection during pregnancy. NOWS may be life-threatening if not recognized and treated in the neonate. The balance between the risks of NOWS and the benefits of maternal Methadone Hydrochloride Injection use may differ based on the risks associated with the mother’s underlying condition, pain, or addiction. Advise the patient of the risk of NOWS so that appropriate planning for management of the neonate can occur (see WARNINGS ).

2D structure
6-(dimethylamino)-4,4-diphenylheptan-3-one
SMILES CCC(=O)C(CC(C)N(C)C)(C1=CC=CC=C1)C2=CC=CC=C2
InChIKey USSIQXCVUWKGNF-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

Methadone hydrochloride is a mu-agonist; a synthetic opioid analgesic with multiple actions qualitatively similar to those of morphine, the most prominent of which involve 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.

Full OpioidNMDA ReceptorOpioid

Indications

Sourced from openFDA
  • 1. Methadone Hydrochloride Injection is indicated for the management of severe and persistent pain that requires an opioid analgesic and that cannot be adequately treated with alternative options, including immediate-release opioids.

Contraindications

Sourced from openFDA
  • Methadone Hydrochloride Injection is contraindicated in patients with: • Significant respiratory depression • Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment • Known or suspected gastrointestinal obstruction, including paralytic ileus • Hypersensitivity to methadone hydrochloride (e.g. anaphylaxis) or any other ingredient in Methadone Hydrochloride Injection.contraindicated

Dosage & administration

Sourced from openFDA

Important General Information Consider the following important factors that differentiate methadone from other opioids: • The peak respiratory depressant effect of methadone occurs later and persists longer than its peak pharmacologic effect. • A high degree of opioid tolerance does not eliminate the possibility of methadone overdose, iatrogenic or otherwise. Deaths have been reported during conversion to methadone from chronic, high-dose treatment with other opioid agonists and during initiation of methadone treatment of addiction in subjects previously abusing high doses of other opioid agonists. • There is high interpatient variability in absorption, metabolism, and relative analgesic potency. Population-based conversion ratios between methadone and other opioids are not accurate when applied to individuals. • With repeated dosing, methadone is retained in the liver and then slowly released, prolonging the duration of potential toxicity. • Steady-state plasma concentrations are not attained until 3 to 5 days after initiation of dosing . • Methadone has a narrow therapeutic index, especially when combined with other drugs. It is safer to underestimate a patient’s 24-hour methadone dosage and provide rescue medication (e.g., immediate-release opioid) than to overestimate the 24-hour methadone dosage and manage an adverse reaction due to an overdose. While useful tables of opioid equivalents are readily available, there is substantial inter-patient variability in the relative potency of different opioid drugs and products.

Warnings & precautions

Sourced from openFDA

Addiction, Abuse and Misuse Methadone Hydrochloride Injection contains methadone, a Schedule II controlled substance. As an opioid, Methadone Hydrochloride Injection exposes users to the risks of addiction, abuse, and misuse. Although the risk of addiction in any individual is unknown, it can occur in patients appropriately prescribed Methadone Hydrochloride Injection. Addiction can occur at recommended doses and if the drug is misused or abused. The risk of opioid-related overdose or overdose-related death is increased with higher opioid doses, and this risk persists over the course of therapy. In postmarketing studies, addiction, abuse, misuse, and fatal and non-fatal opioid overdose were observed in patients with long-term opioid use (see ADVERSE REACTIONS ; Postmarketing Experience). Assess each patient’s risk for opioid addiction, abuse, or misuse prior to prescribing Methadone Hydrochloride Injection, and reassess all patients receiving Methadone Hydrochloride Injection for the development of these behaviors and conditions. Risks are increased in patients with a personal or family history of substance abuse (including drug or alcohol addiction or abuse) or mental illness (e.g., major depression). The potential for these risks should not, however, prevent the prescribing of Methadone Hydrochloride Injection for the proper management of pain in any given patient. Opioids are sought for nonmedical use and are subject to diversion from legitimate prescribed use. Consider these risks when prescribing or dispensing Methadone Hydrochloride Injection.

Adverse reactions

Sourced from openFDA

The following serious adverse reactions are described, or described in greater detail, in other sections: • Addiction, Abuse, and Misuse (see WARNINGS ) • Life Threatening Respiratory Depression (see WARNINGS ) • QT Prolongation (see WARNINGS ) • Neonatal Opioid Withdrawal Syndrome (see WARNINGS ) • Interactions with CNS Depressants (see WARNINGS ) • Serotonin Syndrome (see WARNINGS ) • Adrenal Insufficiency (see WARNINGS ) • Severe Hypotension (see WARNINGS ) • Gastrointestinal Adverse Reactions (see WARNINGS ) • Seizures (see WARNINGS ) • Withdrawal (see WARNINGS ) • Hypoglycemia (see WARNINGS ) The following adverse reactions associated with the use of methadone were identified in clinical studies or post-marketing reports. Because some of these reactions were reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. The major hazards of methadone are respiratory depression and, to a lesser degree, systemic hypotension. Respiratory arrest, shock, cardiac arrest, and death have occurred. The most frequently observed adverse reactions include lightheadedness, dizziness, sedation, nausea, vomiting, and sweating. These effects seem to be more prominent in ambulatory patients and in those who are not suffering severe pain. In such individuals, lower doses of methadone are advisable.

Use in specific populations

Sourced from openFDA

Pregnancy There are no pharmacokinetic studies of parenteral methadone in pregnancy. The disposition of oral methadone has been studied in approximately 30 pregnant patients in 2 nd and 3 rd trimesters. Elimination of methadone was significantly changed in pregnancy. Total body clearance of methadone was increased in pregnant patients compared to the same patients postpartum or to non-pregnant opioid-dependent women. The terminal half-life of methadone is decreased during second and third trimesters. The decrease in plasma half-life and increased clearance of methadone resulting in lower methadone trough levels during pregnancy can lead to withdrawal symptoms in some pregnant patients. The dosage may need to be increased or the dosing interval decreased in pregnant patients receiving methadone (see DOSAGE AND ADMINISTRATION ).

Pharmacokinetics

Sourced from openFDA
Metabolism
Absorption Methadone Hydrochloride Injection is intended for parenteral (intravenous, subcutaneous and intramuscular) administration. Methadone pharmacokinetics following subcutaneous and intramuscular administration have not been systematically studied and differences among the various parenteral routes have not been well characterized.

Overdosage

Sourced from openFDA

Clinical Presentation Acute overdosage with methadone can be manifested by respiratory depression, somnolence progressing to stupor or coma, skeletal-muscle flaccidity, cold and clammy skin, constricted pupils, and, in some cases, pulmonary edema, bradycardia, hypotension, hypoglycemia, partial or complete airway obstruction, atypical snoring, and death. Marked mydriasis rather than miosis may be seen with hypoxia in overdose situations (see CLINICAL PHARMACOLOGY ). In severe overdosage, particularly by the intravenous route, apnea, circulatory collapse, cardiac arrest, and death may occur. Methadone overdosage is associated with rhabdomyolysis. Seek medical attention, especially if abuse/misuse results in prolonged immobilization. Toxic leukoencephalopathy has been reported after opioid overdose, and can present hours, days, or weeks after apparent recovery from the initial intoxication. Hearing loss has been reported after methadone overdose, in some cases permanent. Treatment of Overdose In the case of overdose, priorities are the reestablishment of a patent and protected airway and institution of assisted or controlled ventilation, if needed.

Approval history

Sourced from openFDA
  • Aug 13, 1947NDANDA021624Mylan Institutional
  • Mar 14, 1973NDANDA017116Specgx Llc
  • Mar 14, 1973NDANDA017058Hikma
  • May 22, 1981ANDAANDA087393Hikma
  • Aug 30, 1982ANDAANDA087997Hikma
  • Mar 8, 1983ANDAANDA088109Hikma
  • Sep 6, 1988ANDAANDA089897Hikma
  • Apr 29, 1993ANDAANDA074184Specgx Llc

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
45,526 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Drug Dependence5,93413%
  2. 2Toxicity To Various Agents5,35612%
  3. 3Drug Abuse5,01411%
  4. 4Overdose4,0708.9%
  5. 5Pain3,8238.4%
  6. 6Death3,7338.2%
  7. 7Foetal Exposure During Pregnancy2,5415.6%
  8. 8Emotional Distress2,4885.5%
  9. 9Drug Withdrawal Syndrome2,4665.4%
  10. 10Drug Withdrawal Syndrome Neonatal2,2805.0%
  11. 11Drug Ineffective1,8224.0%
  12. 12Nausea1,6623.7%
  13. 13Drug Interaction1,6453.6%
  14. 14Anxiety1,4633.2%
  15. 15Completed Suicide1,3983.1%

Literature

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Recent PubMed references pinned to Methadone as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 570 ClinicalTrials.gov registrations naming Methadone as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Methadone. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

Frequently asked questions

How does Methadone work?
Methadone hydrochloride is a mu-agonist; a synthetic opioid analgesic with multiple actions qualitatively similar to those of morphine, the most prominent of which involve 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.
What is Methadone used for?
According to FDA labeling, Methadone carries indications including: 1. Methadone Hydrochloride Injection is indicated for the management of severe and persistent pain that requires an opioid analgesic and that cannot be adequately treated with alternative options, including immediate-release opioids.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Methadone?
Methadone is classified as Drugs used in opioid dependence, Opioid Agonist, Full Opioid Agonists, NMDA Receptor Antagonists, Opioid Agonists, Analgesia, Decreased Organized Electrical Activity.
What are the brand names for Methadone?
Methadone is marketed under brand names including Diskets, Dolophine, Methadose.
What are the contraindications for Methadone?
Methadone labeling lists contraindications including: Methadone Hydrochloride Injection is contraindicated in patients with: • Significant respiratory depression • Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment • Known or suspected gastrointestinal obstruction, including paralytic ileus • Hypersensitivity to methadone hydrochloride (e.g. anaphylaxis) or any other ingredient in Methadone Hydrochloride Injection.. Always consult the full prescribing information and a clinician.
Note. Data for methadone is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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