Opioid Analgesic; Antitussive
Binds to opioid receptors in the CNS, causing inhibition of ascending pain pathways, altering the perception of and response to pain; causes cough suppression by direct central action in the medulla; produces generalized CNS depression
藥動學
1. Onset of action: 10 to 30 minutes
2. Duration: 4 to 6 hours
3. Protein binding: ~7% to 25%
4. Metabolism: Hepatic via UGT2B7 and UGT2B4 to codeine-6-glucuronide, via CYP2D6 to morphine (active), and via CYP3A4 to norcodeine. Morphine is further metabolized via glucuronidation to morphine-3-glucuronide and morphine-6-glucuronide (active)
5. Half-life elimination: ~3 hours
6. Excretion: Urine (~90%, ~10% of the total dose as unchanged drug); feces
禁忌症
1. Hypersensitivity (eg, anaphylaxis) to codeine or any component of the formulation
2. Pediatric patients <12 y/o; postoperative management in pediatric patients <18 y/o who have undergone tonsillectomy and/or adenoidectomy
3. Significant respiratory depression; acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment
4. GI obstruction, including paralytic ileus
5. Concurrent use with MAOIs or use of MAOIs within the last 14 days
Opioid-naive patients : IM, SubQ
30 to 60 mg every 4 to 6 hours as needed (use the lowest effective dose for the shortest period of time necessary) Conversion from oral codeine or another opioid: IM, SubQ
Refer to product labeling for dose conversions
小兒調整劑量
腎功能調整劑量
1. GFR >50 mL/minute: No dosage adjustment necessary.
2. GFR 10 to 50 mL/minute: Administer 75% of dose.
3. GFR <10 mL/minute: Administer 50% of dose.
4. Continuous renal replacement therapy (CRRT): Administer 75% of dose; titrate.
肝功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied)