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NERVOUS SYSTEM › ANALGESICS › OPIOIDS › Natural opium alkaloids
codeine, combinations excl. psycholeptics
N02AA59
Forms & Strengths
- Tablets: Codeine phosphate combinations with acetaminophen, aspirin, or ibuprofen (various strengths)
- Oral Solution/Syrup: Codeine combinations with expectorants or antihistamines
Adult Dosing
- Mild to moderate pain: 15 mg to 60 mg orally every 4 to 6 hours as needed, combined with non-opioid analgesics
- Cough (antitussive): 10 mg to 20 mg orally every 4 to 6 hours as needed
Pediatric Dosing
- Contraindicated in children under 12 years of age for all indications
- Contraindicated for post-operative management in tonsillectomy and/or adenoidectomy in children under 18 years
Indications
- Management of mild to moderate pain where use of an opioid is appropriate
- Temporary relief of cough associated with colds and upper respiratory tract infections
Mechanism of Action
- Agonist at mu-opioid receptors in the central nervous system, providing analgesia and antitussive effects
- Prodrug metabolized by hepatic CYP2D6 into morphine, the primary active moiety responsible for analgesic activity
Contraindications
- Hypersensitivity to codeine or formulation components
- Significant respiratory depression
- Acute or severe bronchial asthma in an unmonitored setting
- Known or suspected gastrointestinal obstruction, including paralytic ileus
- Children under 12 years of age and post-tonsillectomy/adenoidectomy in pediatric patients
- Known CYP2D6 ultra-rapid metabolizers
Adverse Reactions
- Central nervous system depression, dizziness, drowsiness, sedation
- Respiratory depression
- Constipation, nausea, vomiting, abdominal pain
- Pruritus, rash, urticaria
- Hypotension, flushing
Drug Interactions
- CNS depressants (alcohol, benzodiazepines, other opioids): increased risk of profound sedation, respiratory depression, coma, and death
- CYP2D6 inhibitors (quinidine, bupropion, fluoxetine): may decrease the analgesic efficacy of codeine by reducing conversion to morphine
- CYP3A4 inducers (rifampin, carbamazepine): may increase metabolism of codeine
- Monoamine Oxidase Inhibitors (MAOIs): potential for severe and unpredictable potentiation, leading to CNS excitation or depression
Curated Content: Needs Vetting Before Put to Clinical Use