Anti Hypercholesterolemic Drugs

Drug (Brand — Generic) Class Dose Mechanism Indications Contraindications Common SE Serious AE Nurse's Role
Atorvastatin (Lipitor) Statin (HMG-CoA reductase inhibitor) 10–80 mg PO once daily ↓HMG-CoA reductase → ↓cholesterol synthesis → ↑hepatic LDL receptors → ↓LDL-C Primary hypercholesterolemia, mixed dyslipidemia, ASCVD risk reduction Active liver disease, pregnancy, breastfeeding, hypersensitivity GI upset, headache, myalgias Myopathy/rhabdomyolysis, hepatotoxicity Baseline LFTs, CK if muscle symptoms; teach to report muscle pain/weakness or dark urine; avoid grapefruit; ensure contraception
Rosuvastatin (Crestor) Statin 5–40 mg PO once daily (adjust for renal impairment) Potent HMG-CoA reductase inhibition → large LDL reductions Same as atorvastatin Same as atorvastatin Same as atorvastatin Same as atorvastatin Monitor renal function in elderly and adjust as needed
Simvastatin (Zocor) Statin 10–40 mg PO once daily (usually evening) Same as atorvastatin Same as atorvastatin Same as atorvastatin Same as atorvastatin Same as atorvastatin More drug-interactions (CYP3A4) — many contraindications with strong CYP3A4 inhibitors
Ezetimibe (Zetia) Cholesterol absorption inhibitor 10 mg PO once daily Inhibits NPC1L1 intestinal cholesterol uptake → ↓chylomicron/LDL cholesterol Add-on to statin if LDL goals not met; statin intolerance strategies Active liver disease (when combined with statin) Diarrhea, arthralgia; rare myopathy/hepatitis when combined with statin Myopathy (when combined with statin) Monitor LFTs if combined with statin; counsel on adherence and lifestyle
Fenofibrate (Tricor) Fibrate (PPAR-α agonist) 48–145 mg PO once daily (depending on formulation) ↑lipoprotein lipase activity → ↓TG, ↑HDL Severe hypertriglyceridemia, mixed dyslipidemia Severe hepatic or renal disease, gallbladder disease GI upset, ↑LFTs Myopathy (especially with statins), gallstones Monitor LFTs, creatinine; avoid combination with gemfibrozil if on statin
Niacin (Nicotinic acid) Miscellaneous IR/ER regimens vary (up to ~2000 mg/day under supervision) ↓VLDL production → ↓TG; ↑HDL. Low HDL or hypertriglyceridemia (less used now) Active liver disease, peptic ulcer disease, gout, uncontrolled diabetes. Flushing, pruritus, GI upset. Hepatotoxicity, hyperglycemia, gout exacerbation. Recommend aspirin 30–60 min before to reduce flushing (if not contraindicated); monitor LFTs and glucose.
Cholestyramine (Questran), Colesevelam (Welchol) Bile Acid Sequestrants Cholestyramine powder varies 4–16 g/day; colesevelam 3.75 g/day (tablet or powder). Bind bile acids in gut → ↑conversion of cholesterol to bile acids → ↓LDL. LDL lowering, adjunct therapy. Complete biliary obstruction. Nausea, Constipation, Bloating. Constipation, bloating, reduced absorption of fat-soluble vitamins and some drugs. Mix powder well; separate other oral meds by 2–4 hours; encourage fiber/fluids.

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