What is Atorva E (atorvastatin)?

What is Atorva E (Atorvastatin)?

Atorvastatin (commonly marketed as Lipitor, and likely what "Atorva E" refers to) is an HMG-CoA reductase inhibitor (statin) that lowers cholesterol by inhibiting the rate-limiting enzyme in cholesterol synthesis, thereby reducing LDL cholesterol, triglycerides, and apolipoprotein B while modestly increasing HDL cholesterol. 1

Mechanism of Action

• Atorvastatin selectively and competitively inhibits HMG-CoA reductase, the enzyme that converts 3-hydroxy-3-methylglutaryl-coenzyme A to mevalonate, a precursor of cholesterol 1

• The drug works primarily in the liver by inhibiting cholesterol synthesis and upregulating hepatic LDL receptors on cell surfaces, which enhances LDL uptake and catabolism 1

• Atorvastatin also reduces LDL production and decreases the total number of LDL particles circulating in plasma 1

Pharmacological Properties

• Atorvastatin is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 1-2 hours 1

• The absolute bioavailability is approximately 14% due to extensive first-pass metabolism in the gastrointestinal mucosa and liver, though the systemic availability of HMG-CoA reductase inhibitory activity reaches approximately 30% 1

• The drug is ≥98% bound to plasma proteins with a mean volume of distribution of approximately 381 liters 1

• The mean plasma elimination half-life is approximately 14 hours, but the half-life of inhibitory activity extends to 20-30 hours due to active metabolites 1

• Atorvastatin is extensively metabolized by cytochrome P450 3A4 to ortho- and para-hydroxylated derivatives, with approximately 70% of circulating inhibitory activity attributed to these active metabolites 1

Clinical Efficacy

• Atorvastatin 10-80 mg daily reduces LDL cholesterol by 35-61% and triglycerides by 14-45% in patients with primary hypercholesterolemia 2

• In comparative trials, atorvastatin produces greater reductions in total cholesterol, LDL cholesterol, triglycerides, and apolipoprotein B compared to pravastatin, simvastatin, or lovastatin at equivalent doses 3, 2

• Atorvastatin 10 mg reduces LDL cholesterol by approximately 43-50%, which is significantly more potent than pravastatin 40 mg (34% reduction) 4

• The American College of Cardiology reports that atorvastatin 80 mg achieves LDL cholesterol levels of 62 mg/dL compared to pravastatin 40 mg achieving 95 mg/dL—a 33 mg/dL (35%) difference 4

• In the CARDS trial, atorvastatin 10 mg produced a 37% relative reduction in major cardiovascular events and a 27% reduction in all-cause mortality in patients with type 2 diabetes over 3.9 years 5, 6

• The PROVE-IT trial demonstrated that atorvastatin 80 mg reduced composite cardiovascular endpoints by 16% compared to pravastatin 40 mg in patients with acute coronary syndrome 4

Available Formulations

• Atorvastatin calcium tablets are available for oral administration in 10,20,40, or 80 mg strengths 1

• The tablets contain atorvastatin calcium in propylene glycol solvate form with inactive ingredients including calcium acetate, colloidal silicon dioxide, croscarmellose sodium, hydroxypropyl cellulose, hypromellose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, sodium carbonate, and titanium dioxide 1

Safety Profile

• The most frequently reported adverse events are gastrointestinal effects, similar to other HMG-CoA reductase inhibitors 3, 2

• Atorvastatin 80 mg shows slightly higher transaminase elevations (3.3%) compared to pravastatin 40 mg (1.1%), though these are generally asymptomatic and reversible 4

• Advanced age (≥65 years), renal impairment, and hepatic impairment are risk factors for atorvastatin-associated myopathy and rhabdomyolysis 1

• The drug is contraindicated in patients with acute liver failure or decompensated cirrhosis 1

• Drug interactions occur with potent CYP3A4 inhibitors (itraconazole, erythromycin, grapefruit juice), cyclosporine, gemfibrozil, and niacin, which increase the risk of myopathy and rhabdomyolysis 7, 2

Clinical Indications

• The American Diabetes Association recommends atorvastatin 40-80 mg daily for high-intensity therapy in patients with established cardiovascular disease or high risk 8

• The American Heart Association suggests high-intensity therapy with atorvastatin 40-80 mg once daily to reduce LDL cholesterol by ≥50% from baseline in patients with established cardiovascular disease 8

• Treatment should be indefinite and lifelong in patients with established cardiovascular disease or high risk, as cardiovascular benefits are maximized with continuous long-term treatment 8