Methadone
Generic Name: methadone
Brand Names:
Methadone Hydrochloride
11 DESCRIPTION Methadone hydrochloride is chemically described as 6-(dimethylamino)-4,4-diphenyl-3-hepatanone hydrochloride. Methadone hydrochloride USP is a white powder. Its molecular formula is C 21 H 27 NO• HCl and it has a molecular weight of 345.91. Methadone hydrochloride has a melting point of 235°C, and a pKa of 8.25 in water at 20°C. Its octanol/water partition coefficient at pH 7.4 is 117. A solution (1:100) in water has a pH between 4.5 and 6.5.
Overview
11 DESCRIPTION Methadone hydrochloride is chemically described as 6-(dimethylamino)-4,4-diphenyl-3-hepatanone hydrochloride. Methadone hydrochloride USP is a white powder. Its molecular formula is C 21 H 27 NO• HCl and it has a molecular weight of 345.91. Methadone hydrochloride has a melting point of 235°C, and a pKa of 8.25 in water at 20°C. Its octanol/water partition coefficient at pH 7.4 is 117. A solution (1:100) in water has a pH between 4.5 and 6.5.
Uses
1 INDICATIONS AND USAGE Methadone hydrochloride tablets 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. Limitations of Use Because of the risks of addiction, abuse, misuse, overdose, and death, which can occur at any dosage or duration and persist over the course of therapy [see WARNINGS AND PRECAUTIONS ( 5.1 )], reserve opioid analgesics, including methadone hydrochloride tablets, for use in patients for whom alternative analgesic treatment options are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain. Methadone hydrochloride tablets are not indicated as an as-needed (prn) analgesic.
Dosage
2 DOSAGE AND ADMINISTRATION Consider recommending or prescribing an opioid overdose reversal agent (e.g., naloxone, nalmefene) based on the patient’s risk factors for overdose ( 2.3 , 5.1 , 5.2 , 5.3 ). Methadone hydrochloride tablets should be prescribed only by healthcare professionals who are knowledgeable about the use of extended-release/long-acting opioids and how to mitigate the associated risks. ( 2.1 ) Use the lowest effective dosage for the shortest duration of time consistent with individual patient treatment goals. Reserve titration to higher doses of methadone hydrochloride tablets for patients in whom lower doses are insufficiently effective and in whom the expected benefits of using a higher dose opioid clearly outweigh the substantial risks.
Side Effects
6 ADVERSE REACTIONS The following serious adverse reactions are described, or described in greater detail, in other sections: Addiction, Abuse, and Misuse [see WARNINGS AND PRECAUTIONS ( 5.1 ) ] Life Threatening Respiratory Depression [see WARNINGS AND PRECAUTIONS ( 5.2 ) ] QT Prolongation [see WARNINGS AND PRECAUTIONS ( 5.4 ) ] Neonatal Opioid Withdrawal Syndrome [see WARNINGS AND PRECAUTIONS ( 5.5 ) ] Interactions with Benzodiazepines and other CNS Depressants [see WARNINGS AND PRECAUTIONS ( 5.3 ) ] Opioid-Induced Hyperalgesia and Allodynia [see WARNINGS AND PRECAUTIONS ( 5.8 ) ] Serotonin Syndrome [see WARNINGS AND PRECAUTIONS ( 5.9 ) ] Adrenal Insufficiency [see WARNINGS AND PRECAUTIONS ( 5.11 ) ] Severe Hypotension [see WARNINGS AND PRECAUTIONS ( 5.12 ) ] Gastrointestinal Adverse Reac...
Interactions
7 DRUG INTERACTIONS Inhibitors of CYP3A4, CYP2B6, CYP2C19, CYP2C9, or CYP2D6 Clinical Impact: Methadone undergoes hepatic N-demethylation by several cytochrome P450 (CYP) isoforms, including CYP3A4, CYP2B6, CYP2C19, CYP2C9, and CYP2D6. The concomitant use of methadone hydrochloride tablets and CYP3A4, CYP2B6, CYP2C19, CYP2C9, or CYP2D6 inhibitors can increase the plasma concentration of methadone, resulting in increased or prolonged opioid effects, and may result in a fatal overdose, particularly when an inhibitor is added after a stable dose of methadone hydrochloride tablets is achieved. These effects may be more pronounced with concomitant use of drugs that inhibit more than one of the CYP enzymes listed above.
Warnings
WARNING: SERIOUS AND LIFE-THREATENING RISKS FROM USE OF METHADONE HYDROCHLORIDE TABLETS A ddiction, Abuse, and Misuse Because the use of methadone hydrochloride tablets 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 AND PRECAUTIONS ( 5.1 )]. 5 WARNINGS AND PRECAUTIONS Opioid Induced Hyperalgesia and Allodynia : Opioid-Induced Hyperalgesia (OIH) occurs when an opioid analgesic paradoxically causes an increase in pain, or an increase in sensitivity to pain. If OIH is suspected, carefully consider appropriately decreasing the dose of the current opioid analgesic or opioid rotation. ( 5.8) Serotonin Syndrome : Potentially life-threatening condition could result from concomitant serotonergic drug administration. Discontinue methadone hydrochloride tablets if serotonin syndrome is suspected. ( 5.9 ) Ri s k of Life-Threatening Respiratory Depression in Patients with Chronic P u l monary Disease or in Elderly, Cachectic, or Debilitated Patients : Regularly evaluate closely, particularly during initiation and titration. 4 CONTRAINDICATIONS Methadone hydrochloride tablets are contraindicated in patients with: Significant respiratory depression [see WARNINGS AND PRECAUTIONS ( 5.2 ) ]. Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment [see WARNINGS AND PRECAUTIONS ( 5.10 ) ].
Pregnancy
8.1 Pregnancy Risk Summary The majority of available data from clinical trials, observational studies, case series, and case reports on methadone use in pregnancy do not indicate an increased risk of major malformations specifically due to methadone. Pregnant women involved in methadone maintenance programs have been reported to have improved prenatal care leading to reduced incidence of obstetric and fetal complications and neonatal morbidity and mortality when compared to women using illicit drugs.
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING Methadone Hydrochloride Tablets, USP 10 mg tablets are white, round, biconvex tablets , scored on one side and debossed with "N" above the score and "128" below the score and plain on the other side.
Frequently Asked Questions
What is Methadone used for?▼
1 INDICATIONS AND USAGE Methadone hydrochloride tablets 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. Limitations of Use Because of the risks of addiction, abuse, misuse, overdose, and death, which can occur at any dosage or duration and persist over the course of therapy [see WARNINGS AND PRECAUTIONS ( 5.1 )], reserve opioid analgesics, including methadone hydrochloride tablets, for use in patients for whom alternative analgesic treatment options are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain. Methadone hydrochloride tablets are not indicated as an as-needed (prn) analgesic.
What are the side effects of Methadone?▼
6 ADVERSE REACTIONS The following serious adverse reactions are described, or described in greater detail, in other sections: Addiction, Abuse, and Misuse [see WARNINGS AND PRECAUTIONS ( 5.1 ) ] Life Threatening Respiratory Depression [see WARNINGS AND PRECAUTIONS ( 5.2 ) ] QT Prolongation [see WARNINGS AND PRECAUTIONS ( 5.4 ) ] Neonatal Opioid Withdrawal Syndrome [see WARNINGS AND PRECAUTIONS ( 5.5 ) ] Interactions with Benzodiazepines and other CNS Depressants [see WARNINGS AND PRECAUTIONS ( 5.3 ) ] Opioid-Induced Hyperalgesia and Allodynia [see WARNINGS AND PRECAUTIONS ( 5.8 ) ] Serotonin Syndrome [see WARNINGS AND PRECAUTIONS ( 5.9 ) ] Adrenal Insufficiency [see WARNINGS AND PRECAUTIONS ( 5.11 ) ] Severe Hypotension [see WARNINGS AND PRECAUTIONS ( 5.12 ) ] Gastrointestinal Adverse Reac...
Can I take Methadone during pregnancy?▼
8.1 Pregnancy Risk Summary The majority of available data from clinical trials, observational studies, case series, and case reports on methadone use in pregnancy do not indicate an increased risk of major malformations specifically due to methadone. Pregnant women involved in methadone maintenance programs have been reported to have improved prenatal care leading to reduced incidence of obstetric and fetal complications and neonatal morbidity and mortality when compared to women using illicit drugs.
What are the important warnings for Methadone?▼
WARNING: SERIOUS AND LIFE-THREATENING RISKS FROM USE OF METHADONE HYDROCHLORIDE TABLETS A ddiction, Abuse, and Misuse Because the use of methadone hydrochloride tablets 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 AND PRECAUTIONS ( 5.1 )]. 5 WARNINGS AND PRECAUTIONS Opioid Induced Hyperalgesia and Allodynia : Opioid-Induced Hyperalgesia (OIH) occurs when an opioid analgesic paradoxically causes an increase in pain, or an increase in sensitivity to pain. If OIH is suspected, carefully consider appropriately decreasing the dose of the current opioid analgesic or opioid rotation. ( 5.8) Serotonin Syndrome : Potentially life-threatening condition could result from concomitant serotonergic drug administration. Discontinue methadone hydrochloride tablets if serotonin syndrome is suspected. ( 5.9 ) Ri s k of Life-Threatening Respiratory Depression in Patients with Chronic P u l monary Disease or in Elderly, Cachectic, or Debilitated Patients : Regularly evaluate closely, particularly during initiation and titration. 4 CONTRAINDICATIONS Methadone hydrochloride tablets are contraindicated in patients with: Significant respiratory depression [see WARNINGS AND PRECAUTIONS ( 5.2 ) ]. Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment [see WARNINGS AND PRECAUTIONS ( 5.10 ) ].
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.