Atorvastatin

What it is and how it works

Mechanism of Action Atorvastatin calcium is a selective, competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl-coenzyme A to mevalonate, a precursor of sterols, including cholesterol. In animal models, atorvastatin calcium lowers plasma cholesterol and lipoprotein levels by inhibiting HMG-CoA reductase and cholesterol synthesis in the liver and by increasing the number of hepatic LDL receptors on the cell surface to enhance uptake and catabolism of LDL; atorvastatin calcium also reduces LDL production and the number of LDL particles.

Indications

Therapy with lipid-altering agents should be only one component of multiple risk factor intervention in individuals at significantly increased risk for atherosclerotic vascular disease due to hypercholesterolemia. Drug therapy is recommended as an adjunct to diet when the response to a diet restricted in saturated fat and cholesterol and other nonpharmacologic measures alone has been inadequate. In patients with CHD or multiple risk factors for CHD, atorvastatin calcium tablets can be started simultaneously with diet. Atorvastatin calcium is an HMG-CoA reductase inhibitor indicated as an adjunct therapy to diet to: • Reduce the risk of MI, stroke, revascularization procedures, and angina in adult patients without CHD, but with multiple risk factors . • Reduce the risk of MI and stroke in adult patients with type 2 diabetes without CHD, but with multiple risk factors . • Reduce the risk of non-fatal MI, fatal and non-fatal stroke, revascularization procedures, hospitalization for CHF, and angina in adult patients with CHD .

Dosage and administration (summary)

• Dose range: 10 to 80 mg once daily . • Recommended start dose: 10 or 20 mg once daily . • Patients requiring large LDL-C reduction (>45%) may start at 40 mg once daily . • Pediatric patients with HeFH: starting dose: 10 mg once daily; dose range: 10 to 20 mg/day for patients 10 years to 17 years of age . Hyperlipidemia and Mixed Dyslipidemia The recommended starting dose of atorvastatin calcium tablet is 10 or 20 mg once daily. Patients who require a large reduction in LDL-C (more than 45%) may be started at 40 mg once daily. The dosage range of atorvastatin calcium tablet is 10 to 80 mg once daily.

Contraindications

• Active Liver Disease, Which May Include Unexplained Persistent Elevations in Hepatic Transaminase Levels • Hypersensitivity to Any Component of This Medication • Pregnancy . • Lactation . • Active liver disease, which may include unexplained persistent elevations in hepatic transaminase levels . • Hypersensitivity to any component of this medication . • Pregnancy ( 4 , Error! Hyperlink reference not valid. , Error! Hyperlink reference not valid. ). • Lactation ( 4 , 8.2 ).

Warnings and precautions

Skeletal muscle effects (e.g., myopathy and rhabdomyolysis): Risks increase when higher doses are used concomitantly with cyclosporine and strong CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, HIV protease inhibitors). Predisposing factors include advanced age (> 65), uncontrolled hypothyroidism, and renal impairment. Rare cases of rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported. Advise patients to promptly report to their physician unexplained and/or persistent muscle pain, tenderness, or weakness.

Pregnancy

Pregnancy Risk Summary Atorvastatin calcium tablet is contraindicated for use in pregnant women since safety in pregnant women has not been established and there is no apparent benefit of lipid lowering drugs during pregnancy.

Storage and supply

Storage Store at 20°C to 25°C (68°F to 77°F). .

Source: Atorvastatin Calcium (Atorvastatin Calcium) — US FDA prescribing information, 2022-04-01, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.