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Lecture 9

BIO200 Lecture 9

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University of Toronto Mississauga
Mc Intyre Burnham

Lecture 9 October-10-13 4:39 PM High P o/w molecules are taken back during renal process Biotransformation of high P o/w to low P o/w (non-polar to polar) Drugs are eliminated as they are biotransformed for drugs going through the hepatic route (for polar molecules its when its in urine) Many drugs, once they have been transformed, they lose their pharmacological abilities Depends on liver enzymes Liver will work faster if blood flow is faster It works best if not limited by blood flow Can only measure this experimentally through animal preparation Lectures Page 1 Both input and output are internal so the only way to calculate is through animal preparation -> Can change by inducing liver enzymes (Liver can increase or decrease enzymatic content) Lectures Page 2 Fast extraction = liver can biotransform drug very quickly There is short half-life If blood flow goes faster, elimination/clearance goes faster If blood flow goes slower, elimination goes slower Slow extraction = liver can biotransform drug very slowly Increasing blood flow will not increase clearance Sensitive to changes in enzymatic functions (increase # of enzymes) Induction of enzymes increase extraction of drugs 100% biotransform but very slowly (long half-life) Lectures Page 3 Intrinsic clearance = enzyme function (Hepatic ) Plasma protein binding doesn’t prevent elimination of drugs (may even increase elimination and shorten half-life) Lectures Page 4 F = Fraction of drug that enters -
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