dextropropoxyphene, combinations with psycholeptics

N02AC74

Forms & Strengths

Combination oral capsules containing dextropropoxyphene hydrochloride with psycholeptics (e.g., diazepam, chlorprothixene)
Combination oral tablets of varying strengths (historically withdrawn in many jurisdictions due to toxicity)

Adult Dosing

Dosing highly variable based on specific regional combination products; generally discontinued globally due to safety concerns
Historically: 32.5 mg to 100 mg dextropropoxyphene component combined with psycholeptic agent every 4 to 6 hours as needed for moderate pain
Maximum daily doses strictly limited due to cumulative cardiac and central nervous system toxicity of components

Pediatric Dosing

Not recommended or indicated for pediatric patients due to lack of safety and efficacy data and high risk of toxicity

Indications

Management of mild to moderate pain accompanied by anxiety or tension (largely obsolete and withdrawn worldwide)

Mechanism of Action

Dextropropoxyphene acts as a weak mu-opioid receptor agonist in the central nervous system
Psycholeptic component provides synergistic sedative, anxiolytic, or antipsychotic effects

Contraindications

Known hypersensitivity to dextropropoxyphene, opioids, or the specific psycholeptic agent
Significant respiratory depression
Acute or severe bronchial asthma in an unmonitored setting
Known or suspected paralytic ileus
Acute intoxication with alcohol, hypnotics, analgesics, opioids, or psychotropic drugs
Severe hepatic or renal impairment

Adverse Reactions

Central nervous system depression, somnolence, dizziness, sedation, and confusion
Respiratory depression and apnea
Nausea, vomiting, constipation, and abdominal pain
QT prolongation, fatal cardiac arrhythmias, and conduction abnormalities
Hypotension and syncope
Risk of drug dependence, tolerance, abuse, and severe withdrawal syndrome

Drug Interactions

Profound CNS depression and fatal respiratory depression when combined with alcohol, other opioids, sedatives, hypnotics, or general anesthetics
Increased risk of QT prolongation and fatal arrhythmias when co-administered with other QT-prolonging agents (e.g., antipsychotics, class IA/III antiarrhythmics)
Enhanced anticholinergic and extrapyramidal effects due to psycholeptic combinations
Inhibition or induction of hepatic cytochrome P450 enzymes (particularly CYP3A4) altering clearance of either component

Curated Content: Needs Vetting Before Put to Clinical Use