Absorption, Distribution, Metabolism and Elimination: Part II - PowerPoint PPT Presentation

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Absorption, Distribution, Metabolism and Elimination: Part II

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Dexamethasone? Ethanol. Barbiturates. Examples of Inhibitors of the Major P450 Gene Families ... Erythromycin (an antibiotic) and Verapamil ( a calcium channel ... – PowerPoint PPT presentation

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Title: Absorption, Distribution, Metabolism and Elimination: Part II


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

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Aspirin Metabolism
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Organs Involved in Drug Biotransformation
  • Liver
  • Gastrointestinal mucosa
  • Lung
  • Skin
  • Placenta

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1.Oxidation a. Aromatic hydroxylation
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b. Aliphatic hydroxylation
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d. Oxidative O-dealkylation
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e. S-oxidation
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4. Conjugationa. Glycine
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b. Glucuronic acid
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d. Acetylation
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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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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
  • Cimetidine
  • Water Cress
  • Cimetidine, grapefruit juice

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