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Author: Admin | 2025-04-28
(limited, particularly for generics); consult specific product labeling.Tablet, Oral, as sulfate:Generic: 15 mg, 30 mg, 60 mg PharmacologyMechanism of ActionBinds 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 Pharmacokinetics/PharmacodynamicsAbsorptionOral: AdequateDistribution~3 to 6 L/kgMetabolismHepatic 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).ExcretionUrine (~90%, ~10% of the total dose as unchanged drug); fecesOnset of ActionOral: Immediate release: 0.5 to 1 hour; Injection [Canadian product]: 10 to 30 minutesPeak effect: Oral: Immediate release: 1 to 1.5 hours; Injection [Canadian product]: 30 to 60 minutesTime to PeakPlasma: Immediate release: 1 hour; Controlled release [Canadian product]: 3.3 hoursDuration of ActionOral: Immediate release: 4 to 6 hours; Injection [Canadian product]: 4 to 6 hoursHalf-Life Elimination~3 hoursProtein Binding~7% to 25% Use: Labeled IndicationsPain management: Management of mild- to moderately-severe painLimitations of use: Reserve codeine for use in patients for whom alternative treatment options (eg, nonopioid analgesics, opioid combination products) are ineffective, not tolerated, or would be otherwise inadequate. Use: Off LabelCough in select patientscyesIn a metaanalysis of trials evaluating the treatment of chronic cough, the use of codeine demonstrated efficacy in patients with this condition Yancy 2013. In a systematic review of the evidence, it was found that there is no good evidence for or against this use and determined that higher quality evidence is needed (Smith 2010). Additional data may be necessary to further define the role of codeine for the treatment of chronic cough.Based on the American College of Chest Physicians (ACCP) guidelines on the diagnosis and management of cough, the use of codeine (among other central cough suppressants such as dextromethorphan) in patients with chronic bronchitis is recommended for the short-term symptomatic relief of coughing. Routine use of codeine as an antitussive in patients with upper respiratory infections is not recommended. The ACCP guidelines on symptomatic treatment of cough among adult patients with lung cancer recommends the use of codeine to help suppress non-specific cough in patients with lung cancer in the palliative stage of their illness. Note: In palliative medicine, codeine is less preferred compared to other opioids due to its greater side effect profile.Persistent diarrhea (palliative care)cClinical experience suggests the utility of codeine in managing persistent and bothersome diarrhea in palliative care patients von Guten 2013. Additional data may be necessary to further define the role of codeine in this condition.Restless legs syndromecyesEvidence from noncontrolled trials suggests that the use of opioids, including codeine, may be of benefit in the treatment of RLS in adults, particularly in those who do not respond to dopaminergics or other therapies. Guideline recommendations are conflicting. American Academy of Sleep Medicine guidelines note that low-level evidences supports use of opioids, including codeine, in the management of RLS AASM [Aurora 2012]. The Willis-Ekbom Disease Foundation suggests the use of low-potency opioids (eg, codeine
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