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21 Cards in this Set

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Bile acid sequesterants (2)
Cholestyramine
Cholistipol
side effects of bile acid sequesterants
GI (const, flatuence, abdom discomfort
Tastes bad
Can bind to concomitantly dministered drugs
Fibric Acid Derivatives
Gemfibrozil
Fenofibrate
MOA of Fibric Acid Derivatives
reduces vLDL and increases activity of lipoprotein lipase
Lowers triglycerides and raises HDL
Side effects of Fibric acid derivatives
Rash, GI sympt, myopathy
Arrhythmias
Hypokalemia
risk of cholesterol gall stones
Increase coumadin anticoag
Conta: pts with renal or hepatic dysfunc, biliary tract disease
Statins (6)
Pravastatin,
Lovastatin (Mevacor)
Simvastatin (Zocor)
Fluvastatin (Lescol)
Atorvastatin (Lipitor)
Cerivastatin (Baycol) Discontinued
Statins MOA
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
Do you get less side effects with a smaller dose?
no.
Is there evidence supporting a class effect of the HMGs on reducing MI, PTCA/CABG, stroke, or mortality?
no
adverse effects of statins
Liver: transaminase elevations
Myopathy: creatine kinase elevation --> rhabdomyolysis and acute renal failure
CYP3A4 inhibs or substrates increase risk of myoopathy
Risk factors for statin-induced myopathy
hepatic dysfunction
renal insuff
hypothyroidisn
age
infection
Famous CYP3A4 inhibitors

think (O2CmEGetF*CKD)
Cimetidine (Tagamet)
Erythromycin
Clarithromycin
Fluconazole, ketoconazole
Diltiazem
Grapefruit juice
Omeprazole
cylcosporin
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)
Decreases LDL production
10-25% reduction in LDL
15-30% increases in HDL
Concerns
Rash/facial flushing
Liver enzymes
Niacin (Nicotinic Acid)
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)
Side effects of Niacin
Flushing
Tachycardia
Dry skin
Hyperuricemia
Glucose intolerance
Hepatic dysfunction
Contraindications of Niacin
Peptic ulcers
Cardiac arrhythmias
Liver disease
Gout
Diabetes mellitus
ACEIs and AII Antagonists:
Decreases breakdown of bradykinin, allowing stimulation of NO and ______
vasodilation
________ (6 months) improved endothelial function in hyperlipidemic patients
Not observed with other ACEIs such as enalapril
Quinapril
Pathophysiologic Actions of AII
Vasoconstriction
Growth promotion
Induces expression of endothelin
Pro-thrombic
Promotes oxidative stress
90% of ACE in tissues, 10% in blood
Vascular Effects of Estrogen
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