Term
| Drug are eliminated from the body by what two different processes? what is the measurement of drug elimination? |
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Definition
| excretion + biotransformation, clearance |
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Term
| what is the CLEARANCE of a drug? |
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Definition
| the volume of a biological fluid (generally plasma) from which that drug is removed ("cleared") per unit time |
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Term
| what does the following phrase mean: "For drugs eliminated with first order kinetics clearance is a constant"? |
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Definition
| the same fraction of the plasma concentration of the drug is cleared per unit time |
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Term
| what is true regarding the product of all BIOTRANSFORMATION reactions? |
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Definition
| the products of biotransformation are MORE WATER SOLUBLE than the original drug |
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Term
| what is the purpose of BIOTRANSFORMATION? |
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Definition
| to make insoluble compounds soluble for excretion via the kidney |
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Term
| what are the three possible outcomes of drug BIOTRANSFORMATION? |
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Definition
-INACTIVATION
-MAINTENANCE OF ACTIVITY
-ACTIVATION |
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Term
| BIOTRANSFORMATIONS are made up of what reactions? examples of each? |
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Definition
PHASE I (oxidation, reduction, hydrolyses) and PHASE II reactions (conjugation)
*can undergo only one reaction or I followed by II |
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Term
| what are MICROSOMAL ENZYMES? |
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Definition
| mainly monooxygenases devoted to biotransformation of xenobiotics and can only catalyze reaction of compounds that are lipid soluble |
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Term
| where are MICROSOMAL DRUG METABOLIZING ENZYMES found? they are abundant/sparse and specific/nonspecific- |
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Definition
| SER of LIVER cells, abundant and non specific |
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Term
| MICROSOMAL ENZYMES catalyze mainly what rxns? |
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Definition
| oxidations and glucuronidations |
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Term
| what are the DRUG EFFECTS on MICROSOMAL ENZYMES? |
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Definition
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Term
| name examples of the most common DRUGS that are used to INDUCE drug METABOLIZING ENZYMES? INHIBIT? |
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Definition
INDUCE- barbiturates, rifampin
INHIBIT-Cimetidine, Amiodarone |
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Term
| where are NON-MICROSOMAL DRUG METABOLIZING ENZYMES found? |
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Definition
| cytosol & mitochondria (liver), and extra cellular fluid (plasma) |
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Term
| what types of reactions do NON-MICROSOMAL DRUG METABOLIZING ENZYMES catalyze? |
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Definition
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Term
| do XENOBIOTICS inhibit or induce NON-MICROSOMAL DRUG METABOLIZING ENZYMES? |
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Definition
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Term
| what are some factors that affect BIOTRANSFORMATION of drugs? |
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Definition
-individual differences
-age
-nutrition and diet
-genetic factors
-drug-drug interactions
-diseases |
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Term
| what are the ROUTES of DRUG EXCRETION? |
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Definition
| kidney, intestine, lungs, others (saliva, sweat, sebum, etc.) |
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