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Absorption, Distribution, Metabolism and Elimination: Part II

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Presentation on theme: "Absorption, Distribution, Metabolism and Elimination: Part II"— Presentation transcript:

1 Absorption, Distribution, Metabolism and Elimination: Part II
Joseph Graziano, Ph.D.

2 Aspirin Metabolism

3 Organs Involved in Drug Biotransformation
Liver Gastrointestinal mucosa Lung Skin Placenta

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7 1.Oxidation a. Aromatic hydroxylation

8 b. Aliphatic hydroxylation

9 d. Oxidative O-dealkylation

10 e. S-oxidation

11 4. Conjugation a. Glycine

12 b. Glucuronic acid

13 d. Acetylation

14 Examples of Characteristic Inducers of the Major P450 Gene Families
CYP 1A2: CYP 2C19: CYP 2C9: CYP 2D6: CYP 2E1: CYP 3A4, 5, 7: Tobacco Prednisone Rifampin Dexamethasone? Ethanol Barbiturates

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20 Examples of Inhibitors of the Major P450 Gene Families
CYP 1A2: CYP 2C19: CYP 2C9: CYP 2D6: CYP 2E1: CYP 3A4, 5, 7: Cimetidine Ketoconazole Isoniazid Water Cress Cimetidine, grapefruit juice

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27 Erythromycin (an antibiotic) and Verapamil ( a calcium channel blocker) are also important inhibitors of P-450

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