Codeine

Chemical formula: C₁₈H₂₁NO₃  Molecular mass: 299.364 g/mol  PubChem compound: 5284371

Pharmacodynamic properties

Codeine is a centrally acting analgesic. The anti-tussive activity of codeine is probably due to its depressant effect on the medullary cough centre in the brain.

Codeine is a centrally acting weak analgesic. Codeine exerts its effect through μ opioid receptors, although codeine has low affinity for these receptors, and its analgesic effect is due to its conversion to morphine. Codeine, particularly in combination with other analgesics such as paracetamol, has been shown to be effective in acute nociceptive pain.

Pharmacokinetic properties

Absorption

Codeine phosphate is readily absorbed from the gut.

Biotransformation and Elimination

The drug is metabolized in the liver and is excreted through urine as conjugates. The plasma half–life is 3-4 hours. Codeine crosses the blood-brain and placental barriers and detectable amounts have been reported to occur in the breast milk.

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