explain the pharmacokinetics process of codeine druge? Absorption( how and how many (MDNS), Distribution, metabolism and...

explain the pharmacokinetics process of codeine druge? Absorption( how and how many (MDNS), Distribution, metabolism and excretion??

Expert Solution

Codeine is widely used as anti-tussive and analgesic drug and it is known that O-demethylation of codeine into morphine is mediated by the genetically polymorphic enzyme cytochrome P450 2D6 Whereas this O-demethylation reaction accounts only for less than 10% of codeine clearance, it is regarded to be the bioactivation reaction essential for the analgesic activity of codeine preparations. A strong correlation between debrisoquine metabolic ratio (MR), reflecting CYP2D6 activity, and the urinary recovery of codeine and its metabolites formed by O- and N-demethylation has been shown.

the oral absorption is unreliable because of high and variable first-pass metabolism

oral bioavailability is 1/6th to 1/4th of the parenterally administered drug

30% plasma bounded, only a small fraction enters the brain

crosses placenta affect fetus

metabolize in the liver by glucuronide conjugation

restrict across the blood-brain barrier

plasma half life is 2 to 3 hour

effect of parenentral dose last in 4 to 6 hour

elimination complete in 24 hourand morphine is noncumlative

Sydney Mullin answered 11 months ago

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