Metabolism of drugs
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| show | Drug metabolism is the transformation by the body of the administered drug into a different
molecular entity.
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| show | Drugs are eliminated by the body either by
excretion of intact drug molecules (usually by kidney)
or by metabolism (usually by liver).
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| Why are most drugs designed to be lipophilic? | show 🗑
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| Are lipophilic drugs excreted efficiently well by the kidneys? Why? | show 🗑
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| What is the main route of elimination for lipophilic drugs? | show 🗑
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| What was evolutionary reason allowed animals to metabolize drugs for removal? Why does it matter clinically? | show 🗑
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| show | Phase I and Phase II reactions
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| show | Introduces or exposes a functionality group on
parent molecule and increases water solubility.
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| What are Phase II reactions in drug metabolism? | show 🗑
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| Is a Phase II reaction necessary for excretion via urine (or bile)? Is a phase I reaction necessary for Phase II reaction? | show 🗑
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| show | Oxidation, reduction, and hydrolysis
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| show | Dealkylation (N and O), hydroxylation (aliphatic or aromatic), deamination, dehydrogenation (alcohol and aldehyde), and oxidation (N, S, monoamine)
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| show | (Nitro and azo) group reduction
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| show | Terminal oxidases in multi-component electron transport chain
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| show | In cell biology, microsomes are vesicle-like artifacts formed from the endoplasmic reticulum (ER) when eukaryotic cells are broken-up in the laboratory; by definition, microsomes are not ordinarily present in living cells.
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| Describe how P450S works | show 🗑
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| show | According to amino acid sequence similaritie, e.g. CYP3A5: 3 = family # (40% identity within family); A = subfamily letter (55% identity within subfamily); 5=isoform #, each isoform given unique number)
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| show | CYP3A; CYP2D6, CYP2C9, and CYP2C19 important due to genetic variations that result in inter-individual variations in rate of drug metabolism
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| What are the two major types of hydrolysis reactions in Phase I reactions? | show 🗑
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| Where do Phase I reactions take place in body? In cell? | show 🗑
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| What other enzymes besides cytochrome P450S can mediate phase I reactions? | show 🗑
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| What results in individuals that are poor drug metabolizers? What about extensive and ultrarapid metabolizers? | show 🗑
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| show | Inactive parent drug that is activated by metabolism
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| show | Codeine is an inactive prodrug that is metabolized by CYP2D6 to morphine; 2D6 PMs do not get pain relief from codeine-->give morphine or oxycodone (doesn't need metabolism for action)
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| What are he (6) major forms of phase II reactions? | show 🗑
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| What is glucuronidation? | show 🗑
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| show | UGTs: uridine diphosphate glucuronosyltransferases
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| show | In the LIVER, intestines, kidney
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| What is sulfanation? | show 🗑
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| show | STs: Sulfotransferases (found in cytosol)
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| What is acetylation? | show 🗑
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| show | NATs: N-acetyltransferases; cytosol; two isoforms (NAT1 and NAT2); most American are slow-acetylators
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| show | Acetylated metabolites are often less water soluble than parent drugs, and may result in crystalluria unless high urine flow rate is maintained
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| show | GST: glutathione S-transferase; typically found in cytosol, but some are microsomial
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| show | Anti-cancer drugs
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| show | Mainly in liver (also in lungs, kidneys, GI tract); mainly in cytosol (except for glucoronidation, which takes place in ER)
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| show | Genetic variations (change activity or expression of drug metabolizing enzymes); drug-drug interactions (can induce or inhibit metabolyzing enzymes); interactions with food, smoking, disease state, and environment
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| show | Inhibits CYP3A4 in gut-->increases bioavailability of drugs metabolized by this enzyme
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| show | Induces certain isoforms of CYPs resulting in enhanced drug metabolims-->stopping smoking may cause spike in drug levels as enzyme goes back to basal level
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| show | Diseases that reduce liver blood flow or cause damage to hepatocytes will decrease drug metabolism
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