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Pharm 1-3
Question | Answer |
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Drugs easily displaced by albumin characteristics. | -Bound to albumin they are sequestered and not able to have a pharm effect. -displaced from albumin pharm active. -easily displaced drugs generally have higher "active" concentrations in body. -Albumin most strongly binds hydrophic drugs. |
Drugs that induce P450 characteristics. | Lead to increased rate of metabolism of anything metabolized by P450, including other drugs. -If induced than it more quickly metabolizes the drug inducing it as well as any other drugs processed by it --> LESS pharm active drug than expected. |
Drugs that inhibit P450 characteristics. | Decrease rate of metabolism of itself and other drugs biotransformed by P450 --> greater amount of pharm active drug in the body than expected. |
Drugs that compete for renal transporters characteristics. | Drugs that are normally excreted out of body via renal transporters on renal tubules (proximal convoluted tubules). Nonspecific & limited # of tranporters so pt taking 2+ drugs that both compete will result in higher levels of pharm active drug in body. |
Sulfonamides | Sulfa drugs, ABX Easily displaced from Albumin Inhibits P450 Competes at renal transporters |
Phenylbutazone | Analgesic, anti-inflammatory used for arthritis and gout Easily displaced from albumin Inhibits P450 |
Tolbutamide | hypoglycemic agent, specifically a sulfonylurea used for Type 2 DM. Easily displaced from albumin. |
Coumadin | anticoagulant. Easily displaced from albumin Inhibits P450 |
Alcohol | Ethanol Inhibits P450 |
Barbiturates | Sedative and anti-spasmodic Induces P450 |
Phenytoin | Antileptic. Induces P450 |
Rifampin | ABX, specifically transcription inhibitor. Induces P450 |
Chloramphenicol | ABX, works as protein synthesis inhibitor Inhibits P450 |
Uric Acid | NATURAL product of human body (not parmaceutical). Competes at renal transporters. |
Probenecid | Inhibits renal excretion of uric acid and certain drugs, but increases uric acid secretion if administered at high doses b/c of its other effects on kidney that occur only at high doses. Competes at renal transporters. |
Penicillins | ABX Competes at renal transporters. |
Salicylates | Analgesic, Antipyretic, antiseptic, disinfectant. Competes at renal transporters. |
Thiazides | Diuretic. Competes at renal transporters. |
Methadone | Analgesic and tx for heroin addiction Induces P450. |
Levodopa | stimulates dopamine production for parkinson's dz. Induces P450. |
Oral Contraceptive Pill | Induces P450 |
Isoniazid | Antibacterial used for TB. Inhibits P450. |
Cimetidine | H2 blocker that is used for gastritis and peptic ulcer dz. Inhibits P450. |
Dicumarol | Anticoagulant Inhibits P450. |
Aminoglycosides + Loop diuretics | Accentuated nephrotoxicity and ototoxicity. |
MAO inhibitors + SSRIs | may promote serotonin syndrome. |
MAO Inhibitors + TCAs | may promote serotonin syndrome or severe sympathetic nervous system activation. |
Antiarrhythmics + Fluoroquinolones | may cause QT prolongation and resulting torsade de pointe. |
Cation-containing drugs/Citric Acid + Fluoroquinolones | Severe impairment of fluoroquinolone absorption |
Alcohol/Rifampin + Isoniazid | Liver damage and possible failure. |
Bone marrow toxicity | most chemotherapeutic agents chloramphenicol ganciclovir zidovudine interferon flucytosine carbamazepine |
Hepatotoxicity | all imidazoles interferon nevirapine all HMG CoA inhibitors valproic acid isoniazid |
Nephrotoxicity | aminoglycosides foscarnet cidofovir NSAIDs cyclosporine amphotericin |
Tendon ruptures | quinolones |
DVTs | raloxifene tamoxifen estrogens/progesterones |
orthostatic hypotension | all alpha blockers most TCAs |
hypertensive crisis | MAO inhibitors TCAs *most likely to occur when drugs listed herein are mixed w/one another |
Serotonin Syndrome | MAO inhibitors SSRIs Decongestants w/pseudoephedrine TCAs SNRIs *most likely to occur when drugs listed herein are mixed w/one another. |
Cutaneous flushing | Niacin |
Seizure | Meperidine |
G6PD Eacerbation | any drug has the ability, but especially: Sulfa Drugs Primaquine |
Drug-induced lupus | hydralazine procainamide |
Malignant hyperthermia | halothane |
Non-arteritic anterior ischemic optic neuropathy (NAION) | PDE-5 Inhibitors |
Ototoxicity | Aminoglycosides PDE-5 Inhibitors |
Neural Tube Defects | Carbamazepine (when used by mother during pregnancy). Valproic Acid (when used by mom during pregnancy). |
Ebstein's Anomaly | Lithium (when used by mother during pregnancy). |
Teratogenic | NSAIDs |
Decreased libido and erectile dysfunction | 5-Alpha Reductase Inhibitors |