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21 Cards in this Set
- Front
- Back
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Bile acid sequesterants (2)
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Cholestyramine
Cholistipol |
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side effects of bile acid sequesterants
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GI (const, flatuence, abdom discomfort
Tastes bad Can bind to concomitantly dministered drugs |
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Fibric Acid Derivatives
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Gemfibrozil
Fenofibrate |
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MOA of Fibric Acid Derivatives
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reduces vLDL and increases activity of lipoprotein lipase
Lowers triglycerides and raises HDL |
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Side effects of Fibric acid derivatives
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Rash, GI sympt, myopathy
Arrhythmias Hypokalemia risk of cholesterol gall stones Increase coumadin anticoag Conta: pts with renal or hepatic dysfunc, biliary tract disease |
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Statins (6)
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Pravastatin,
Lovastatin (Mevacor) Simvastatin (Zocor) Fluvastatin (Lescol) Atorvastatin (Lipitor) Cerivastatin (Baycol) Discontinued |
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Statins MOA
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competitively inhibs HMG Co-A reductase
Decrease hepatic cholesterol biosynthesis (hepatic LDL receps up-regulated to increase uptake of circulating LDL) (up-reg LDL receps have half-life of 15-20 hrs) Anti-thrombotic/anti-platelet anti-oxidant restores endothelial dysfnction |
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Do you get less side effects with a smaller dose?
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no.
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Is there evidence supporting a class effect of the HMGs on reducing MI, PTCA/CABG, stroke, or mortality?
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no
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adverse effects of statins
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Liver: transaminase elevations
Myopathy: creatine kinase elevation --> rhabdomyolysis and acute renal failure CYP3A4 inhibs or substrates increase risk of myoopathy |
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Risk factors for statin-induced myopathy
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hepatic dysfunction
renal insuff hypothyroidisn age infection |
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Famous CYP3A4 inhibitors
think (O2CmEGetF*CKD) |
Cimetidine (Tagamet)
Erythromycin Clarithromycin Fluconazole, ketoconazole Diltiazem Grapefruit juice Omeprazole cylcosporin |
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Prodrug
Decreases GI uptake of cholesterol Reduces cholesterol pool in liver which results in increased synthesis of high affinity LDL receptors Lowers serum LDL and triglycerides May increase hepatic toxicity if used with HMG CoA reductase inhibitors |
Ezetimibe (Zetia)
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Decreases LDL production
10-25% reduction in LDL 15-30% increases in HDL Concerns Rash/facial flushing Liver enzymes |
Niacin (Nicotinic Acid)
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Water soluble vitamin B3
Converted to nicotinamide adenine dinucleotide (NAD) Inhibits vLDL secretion which results in reduction of LDL. Also lowers triglycerides and Lp(a) levels |
Niacin (Nicotinic Acid)
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Side effects of Niacin
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Flushing
Tachycardia Dry skin Hyperuricemia Glucose intolerance Hepatic dysfunction |
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Contraindications of Niacin
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Peptic ulcers
Cardiac arrhythmias Liver disease Gout Diabetes mellitus |
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ACEIs and AII Antagonists:
Decreases breakdown of bradykinin, allowing stimulation of NO and ______ |
vasodilation
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________ (6 months) improved endothelial function in hyperlipidemic patients
Not observed with other ACEIs such as enalapril |
Quinapril
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Pathophysiologic Actions of AII
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Vasoconstriction
Growth promotion Induces expression of endothelin Pro-thrombic Promotes oxidative stress 90% of ACE in tissues, 10% in blood |
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Vascular Effects of Estrogen
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Arterial vasodilation
Increases release of NO Increases release of prostacyclin Decreases AII vasoconstriction Decreases cell proliferation Calcium channel antagonism Inhibits platelet aggregation Decreases LDL Increases HDL Decreases inflammation Antioxidant |
