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Pharmacologic class: HMG-CoA reductase inhibitor
Therapeutic class: Antihyperlipidemic
Pregnancy risk category X
Inhibits HMG-CoA reductase, an enzyme crucial to cholesterol synthesis. Decreases total cholesterol and low-density lipoprotein (LDL) levels and increases high-density lipoprotein level.
Tablets: 10 mg, 20 mg, 40 mg
Tablets (extended-release): 10 mg, 20 mg, 40 mg, 60 mg
Indications and dosages
➣ To reduce LDL, total cholesterol, triglyceride, and apolipoprotein B levels
Adults: Initially, 20 mg P.O. daily. May be increased, as needed, at 4-week intervals to a maximum of 80 mg/day as a single dose or in divided doses. Or 20 mg P.O. (extended-release) daily. May be increased, as needed, at 4-week intervals to a maximum daily dosage of 60 mg.
➣ Heterozygous familial hypercholesterolemia in boys and postmenarchal girls ages 10 and older who have high LDL and cholesterol levels despite adequate trial of diet therapy
Adolescents ages 10 to 17: 10 to 40 mg P.O. daily, with adjustments made at 4-week intervals
• Severe renal insufficiency
• High-risk patients with diabetic dyslipidemia, familial dysbetalipoproteinemia, familial combined hyperlipidemia, or nephrotic hyperlipidemia
• Hypersensitivity to drug, its components, or angiotensin-converting enzyme inhibitors
• Active hepatic disease or unexplained persistent hepatic enzyme elevation
• Concurrent gemfibrozil or azole antifungal therapy
• Pregnancy or breastfeeding
Use cautiously in:
• cerebral arteriosclerosis, heart disease, renal impairment, severe acute infection, severe hypotension or hypertension, uncontrolled seizures, myopathy, visual disturbances, major surgery, trauma, alcoholism
• severe metabolic, endocrine, or electrolyte problems
• women of childbearing age
• Give daily dose with evening meal.
• Increase dosage at intervals of 4 weeks or longer, as ordered.
• Don't give with grapefruit juice (may increase drug blood level).
☞ Discontinue if alanine aminotransferase (ALT) or aspartate aminotransferase (AST) level exceeds three times the upper limit of normal.
CNS: headache, dizziness, asthenia
EENT: blurred vision, eye irritation
GI: nausea, vomiting, constipation, diarrhea, abdominal pain or cramps, dyspepsia, flatulence
Musculoskeletal: myalgia, cramps, rhabdomyolysis
Skin: pruritus, rash, photosensitivity
Other: hypersensitivity reaction
Drug-drug. Azole antifungals, cyclosporine, erythromycin, folic acid derivatives, gemfibrozil, niacin: increased risk of myopathy and rhabdomyolysis
Bile acid sequestrants: decreased lovastatin blood level
Isradipine: increased lovastatin clearance
Warfarin: increased prothrombin time, bleeding
Drug-diagnostic tests. ALT, AST: increased levels
Drug-food. Grapefruit juice: increased lovastatin blood level
Drug-herbs. Red yeast rice: increased risk of adverse reactions
Chaparral, comfrey, germander, jin bu huan, kava, pennyroyal, St. John's wort: increased risk of hepatotoxicity
• Obtain liver function tests before starting therapy, 6 and 12 weeks after therapy begins or dosage is increased, and periodically thereafter.
• Tell patient to take immediate-release tablets with evening meal or extended-release tablets at bedtime.
• Instruct patient not to break, crush, or chew extended-release tablets.
• Emphasize importance of cholesterol-lowering diet and other therapies, such as exercise and weight control.
☞ Instruct patient to report unexplained muscle pain, tenderness, or weakness, as well as signs or symptoms of hepatotoxicity (fever, malaise, abdominal pain, yellowing of skin or eyes, clay-colored stools, or tea-colored urine).
☞ Advise patient to contact prescriber immediately if she is breastfeeding or suspects pregnancy.
• Tell patient not to use herbs without consulting prescriber.
• Inform patient that drug may cause photosensitivity. Caution him to avoid excessive sun or heat lamp light.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and herbs mentioned above.