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NERVOUS SYSTEM › ANALGESICS › OPIOIDS › Natural opium alkaloids
codeine, combinations with psycholeptics
N02AA79
Forms & Strengths
- Oral tablets/capsules: Codeine phosphate combined with psycholeptics (e.g., sedatives, barbiturates, or minor tranquilizers) in variable milligram strengths.
Adult Dosing
- Pain/Cough: 15 mg to 60 mg codeine component orally every 4 to 6 hours as needed.
- Maximum daily dose: Typically not to exceed 360 mg of codeine per 24 hours due to additive CNS depression.
Pediatric Dosing
- Contraindicated in children under 12 years of age.
- Contraindicated for post-tonsillectomy/adenoidectomy pain management in patients under 18 years.
- Not recommended in adolescents due to variable CYP2D6 metabolism risks.
Indications
- Short-term management of moderate acute pain inadequately controlled by non-opioids.
- Symptomatic treatment of non-productive cough refractory to other agents (in jurisdictions where approved).
Mechanism of Action
- Codeine is a mu-opioid receptor agonist providing analgesic and antitussive effects via central nervous system action.
- Psycholeptic component provides synergistic central nervous system depression, sedation, and anxiolysis.
Contraindications
- Hypersensitivity to codeine or psycholeptic agents.
- Significant respiratory depression or acute severe bronchial asthma.
- Known or suspected gastrointestinal obstruction, including paralytic ileus.
- Known CYP2D6 ultra-rapid metabolizers.
Adverse Reactions
- Central nervous system depression, somnolence, dizziness, and sedation.
- Respiratory depression and apnea.
- Constipation, nausea, vomiting, and dry mouth.
- Hypotension, orthostatic hypotension, and bradycardia.
- Risk of dependence, abuse, and tolerance with prolonged use.
Drug Interactions
- Profound CNS depression, respiratory depression, coma, and death when combined with other CNS depressants, alcohol, or benzodiazepines.
- Enhanced adverse effects with CYP2D6 or CYP3A4 inhibitors (e.g., amiodarone, quinidine, macrolides).
- Decreased analgesic efficacy when combined with CYP2D6 inducers or strong inhibitors.
Curated Content: Needs Vetting Before Put to Clinical Use