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Lecture, 5/16/2011


Antiprotozoal/antimalarial; G6PD leads to increased sensitivity to drug-induced hemolysis through reuction of GSH; high prevalance of G6PD in Mediterraneans and Asians; patients should be tested for G6PD before prescribing drugs.


Antimycobacterial; metabolized by acetylation by liver N-acetyltransferase; rate of acetylation is genetically determined.


Skeletal muscle relaxant (block transmission on muscle side of NMJ); metabolised by cholinesterase and plasma pseudo-cholinesterase; adverse side effects include respiratory distress to the point of apnea; pts should be tested by homozygous atypical cholisterase gene

Imatinib (Gleevac)

Antineoplastic "designer drug'; inhibitor of tyrosine kinase domain of bcr-abl oncoprotein for tx of CML; Side effects include hepatotoxicity, edema, fluid retention; metabolized by P450


Commonly used cancer drug against solid tumors; mechanism: inhibit DNA synthesis and RNA processing; side effects: bone marrow suppression & GI toxicity due to its effect to inhibit rapidly dividing cells; 5-FU is metabolized by dihydropyrimidine dehydrogenase (DHD); a SNP of DPD present in 5% cancer patients, which increases half-life from 15 min to 160 min.

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