No

Antilipemic Agent (HMG-CoA Reductase Inhibitor)

Reduces total LDL serum cholesterol concentrations in primary hypercholesterolemia in conjunction with diet

X

Breast-feeding/lactation: Breast-feeding is not recommended by manufacturer

Hypersensitivity to cerivastatin or any component; active liver disease; unexplained persistent elevations of serum transaminases; pregnancy

Liver function must be monitored by periodic laboratory assessment. Rhabdomyolysis with acute renal failure has occurred. Risk is increased with concurrent use of clarithromycin, danazol, diltiazem, fluvoxamine, indinavir, nefazodone, nelfinavir, ritonavir, verapamil, troleandomycin, cyclosporine, fibric acid derivatives, erythromycin, niacin, or azole antifungals. Weigh the risk versus benefit when combining any of these drugs with cerivastatin. Use with caution in patients who have a history of liver disease and/or consume substantial quantities of alcohol. Temporarily discontinue in any patient experiencing an acute or serious condition predisposing to renal failure secondary to rhabdomyolysis. Has not been evaluated in homozygous familial hypercholesterolemia.

1% to 10%:

Central nervous system: Weakness (3.1%), insomnia (2%), headache (0.4% to 5.7%)

Cardiovascular: Chest pain (2%), peripheral edema (2%)

Gastrointestinal: Abdominal pain (1.4% to 3.4%), diarrhea (1.5% to 3.8%)

Neuromuscular & skeletal: Arthralgia (4.4%), myalgia (2.3%)

Respiratory: Cough (2.4%)

<1% (Including class-related events not necessarily reported with cerivastatin therapy and postmarketing case reports): Myopathy, muscle cramps, increased CPK (>10x normal), rhabdomyolysis, renal failure (secondary to rhabdomyolysis), blurred vision, alteration in taste, impaired extraocular muscle movement, facial paresis, tremor, dizziness, memory loss, vertigo, paresthesia, peripheral neuropathy, peripheral nerve palsy, anxiety, depression, psychic disturbance, hypersensitivity reaction, angioedema, anaphylaxis, rash, systemic lupus erythematosus-like syndrome, polymyalgia rheumatica, dermatomyositis, vasculitis, purpura, thrombocytopenia, leukopenia, hemolytic anemia, positive ANA, increased ESR, eosinophilia, arthritis, urticaria, photosensitivity, fever, chills, flushing, malaise, dyspnea, toxic epidermal necrolysis, erythema multiforme, Stevens-Johnson syndrome, pancreatitis, hepatitis, cholestatic jaundice, fatty liver, cirrhosis, fulminant hepatic necrosis, hepatoma, anorexia, vomiting, alopecia, pruritus, nodules, skin discoloration, dryness of skin/mucous membranes, nail changes, gynecomastia, decreased libido, erectile dysfunction, impotence, cataracts, ophthalmoplegia, elevated transaminases, increased alkaline phosphatase, increased GGT, hyperbilirubinemia, thyroid dysfunction

CYP3A3/4 enzyme substrate

Cholestyramine reduces cerivastatin absorption. Separate administration times by at least 4 hours.

Cholestyramine and colestipol (bile acid sequestrants): Cholesterol-lowering effects are additive.

Clofibrate and fenofibrate may increase the risk of myopathy and rhabdomyolysis.

Gemfibrozil: Increased risk of myopathy and rhabdomyolysis.

Grapefruit juice may inhibit metabolism of cerivastatin via CYP3A3/4; avoid high dietary intakes of grapefruit juice.

Niacin may increase the risk of myopathy and rhabdomyolysis.

As an HMG-CoA reductase inhibitor, cerivastatin competitively inhibits 3-hydroxyl-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the rate-limiting step in cholesterol biosynthesis

Onset of effect: Maximal reductions in ~2 weeks

Distribution: V_d: 0.3 L/kg

Protein binding: >99%

Metabolism: Hepatic; active metabolite, demethylation and hydroxylation

Bioavailability: 60%, no effect with food

Half-life: 2-3 hours

Elimination: 26% renally, as metabolites; 70% in feces

Adults: Oral: 0.3 mg once daily in the evening; may be taken with or without food.

Dosing adjustment in hepatic impairment: Avoidance suggested; no guidelines for dosage reduction available.

Serum total cholesterol, LDL, HDL, triglycerides, apolipoprotein B, diet, weight, LFTs

HMG-CoA reductase inhibitors are effective in secondary prevention of cardiovascular events in patients with hyperlipidemia. In these situations, the target of therapy is a reduction in LDL cholesterol to <100 mg/dL. HMG-CoA reductase inhibitors have also been shown to be effective in primary prevention of coronary artery disease in individuals without established cardiovascular disease but who have multiple risk factors. Selection of lipid-lowering therapy should be based on the patient's lipid profile, concomitant disease states, and the cost of therapy. The benefits of lipid-lowering are also compelling in women and in the elderly. Important side effects relate to elevated liver enzymes and rhabdomyolysis. LFTs need to be monitored at specified intervals.

May cause insomnia

None reported

No information available to require special precautions

No effects or complications reported

Take prescribed dose in the evening (with or without food). You will need laboratory evaluation during therapy. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). May cause headache (mild analgesic may help); drowsiness, dizziness, or blurred vision (use caution when driving or engaging in tasks that require alertness until response to medication is known). Report chest pain; swelling of extremities; weight gain (>5 lb/week); respiratory difficulty; persistent vomiting or abdominal pain; muscle weakness or pain; persistent cough; swelling of mouth, lips, or face; unusual bruising or bleeding; or skin rash. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Do not get pregnant during or for 1 month following therapy. Consult prescriber for instruction on appropriate contraceptive measures. This drug may cause severe fetal defects. Do not breast-feed.

Tablet, as sodium: 0.2 mg, 0.3 mg, 0.4 mg

"Summary of the Second Report of the National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults (Adult Treatment Panel II)," JAMA, 1993, 269(23):3015-23.