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NERVOUS SYSTEM › OTHER NERVOUS SYSTEM DRUGS › DRUGS USED IN ADDICTIVE DISORDERS › Drugs used in opioid dependence
levomethadone
N07BC05
Forms & Strengths
- Oral solution: 5 mg/mL, 10 mg/mL
- Tablet: 2.5 mg, 5 mg, 10 mg
- Injectable solution: 10 mg/mL
Adult Dosing
- Opioid dependence maintenance: Initial 10-20 mg daily, titrate by 10-20 mg increments to a typical maintenance dose of 60-120 mg daily
- Severe chronic pain: Initial 2.5-5 mg every 8-12 hours, titrate cautiously based on clinical response
Pediatric Dosing
- Not recommended for pediatric patients due to lack of established safety and efficacy data in this population
Indications
- Management of opioid use disorder (medication-assisted treatment)
- Management of severe chronic pain unresponsive to alternative non-opioid options
Mechanism of Action
- Full agonist at mu-opioid receptors in the central nervous system
- NMDA receptor antagonist, which may contribute to reduced tolerance and neuropathic pain efficacy
- Inhibits reuptake of monoamines (norepinephrine and serotonin)
Contraindications
- Hypersensitivity to levomethadone
- Significant respiratory depression in unmonitored settings
- Acute or severe bronchial asthma
- Known or suspected gastrointestinal obstruction, including paralytic ileus
- Concurrent use of monoamine oxidase inhibitors (MAOIs) or use within 14 days
Adverse Reactions
- Respiratory depression
- QT prolongation and risk of torsades de pointes
- Sedation, dizziness, and headache
- Constipation, nausea, and vomiting
- Hypotension and orthostatic hypotension
- Androgen deficiency and sexual dysfunction with chronic use
- Opioid withdrawal syndrome upon abrupt cessation
Drug Interactions
- CYP3A4 inhibitors (e.g., ketoconazole, macrolides) increase levomethadone levels and toxicity risk
- CYP3A4 inducers (e.g., rifampin, carbamazepine) decrease levomethadone levels and may precipitate withdrawal
- Drugs that prolong the QT interval (e.g., antipsychotics, class III antiarrhythmics) increase arrhythmia risk
- Central nervous system depressants (e.g., benzodiazepines, alcohol) cause profound sedation, respiratory depression, and death
- Serotonergic agents increase the risk of serotonin syndrome
Curated Content: Needs Vetting Before Put to Clinical Use