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26 Cards in this Set
- Front
- Back
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Definition of drug metabolism |
Chemical modification of drugs by enzymes to make them more polar (less lipid soluble) and render them excretable by the kidneys |
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Kidneys possess these enzymes |
CyP450, renders drugs more polar |
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Renal clearance of drugs defn |
Apparent volume of blood cleared of drug per unit time |
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Drug clearance proportional to |
GFR |
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Reduced GFR states |
Newborn Elderly (+75 years) Kidney disease Heart disease |
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If reduced GFR, do this to avoid adverse effects |
Lower dose Increase drug interval (Or both) |
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Why is creatinine clearance a good estimate of GFR? |
Freely filtered, not reabsorbed, minimally secreted |
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Calculate clearance |
(ml/min) Urine concenctration (mg/ml) x urine flow rate (ml/min) / plasma concentration (mg/ml) |
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Ion trapping in kidney defn |
acidification or alkalization of urine can assist in excretion of basic or acidic drugs respectively |
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Acid drugs and treatment |
Phenobarbital, salicylate Treat with bicarb |
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Basic drugs and treatment |
Amphetamine Atropine Meperidine Treat with ammonium chloride or ascrobic acid |
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Some drugs actively secreted here |
Mostly in proximal convoluted tubules |
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Probenecid function |
Saturates transporters so that penecillin isn't excreted Also enhances the excretion of uric acid by saturating transporters that go from tubule to blood |
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How to tell if drug is actively secreted |
If its clearance exceeds GFR |
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When GFR increases to adult levels |
8-12 months of age |
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Drug from slide that should be reduced in neonates |
Aminoglycoside antibiotics |
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Drug clearance does not vary with this |
Body weight or surface area (a one year old won't necessarily have lower clearance values vs. a 10 year old) |
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Cardiovascular nephrotoxic drugs |
Diuretics B1 blockers Vasodilators ACE inhibitors Cyclosporine (CsA) Tacrolimus |
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Drugs causing PCT necrosis |
Aminoglycoside antibiotics (Streptomycin, gentomycin) Antifungals (Amphotericin B) (pore forming) Cisplatin (anti-cancer) Radiocontrast media |
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Drugs causing DCT necrosis |
Aspirin Ibuprofen Diclofenac Ketorolac |
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Tubular obstruction |
Sulfonamides Methotrexate Acyclovir |
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Acute interstitial nephritis |
B-lactam antibiotics Vancomycin Rifampin Sulfonamides Ciprofloxacin NSAIDs Furosemide Thiazides Phenytoin |
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Chronic interstitial nephritis |
Lithium Cyclosprine |
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Acute glomerulonephritis |
Heroin Pamidronate |
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Nephrogenic diabetes insipidus |
Diabetes insipidus that cannot be overcome by vasopressin Lithium Demeclocyline Amphotericin B Foscarnet (treat CMV in AIDS patients) |
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Cyclosporine and tacrolimus nephrotoxicity |
Generates endothelin-1 via increased generation fo TGFB1 Vasoconstricts (These drugs are transplant drugs btw) |
