-2%
Atorvastatin is a selective inhibitor of HMG-CoA reductase, the key enzyme responsible for cholesterol synthesis in the liver. By inhibiting this enzyme, atorvastatin reduces hepatic cholesterol production and increases LDL receptor activity, leading to enhanced clearance of LDL cholesterol from the bloodstream.
Stacor should not be used in patients with:
- Hypersensitivity to atorvastatin or formulation components
- Active liver disease or persistent elevation of liver enzymes
- History of severe adverse reactions to statins
Stacor is prescribed as an adjunct to dietary modification and lifestyle changes to manage lipid disorders when non-pharmacological measures alone are insufficient. It is used to:
- Lower total cholesterol, LDL-cholesterol, apolipoprotein B (ApoB), and triglycerides
- Treat heterozygous and homozygous familial hypercholesterolemia
- Manage mixed dyslipidemia (Fredrickson Types IIa and IIb)
- Reduce elevated triglyceride levels in hypertriglyceridemia (Fredrickson Type IV)
- Treat dysbetalipoproteinemia (Fredrickson Type III)
- Reduce the risk of ischemic cardiac events in patients with asymptomatic or mild to moderate coronary artery disease and elevated LDL-cholesterol
- Lower cholesterol levels in patients with diabetes mellitus or following renal transplantation
Absorption
Rapidly absorbed after oral administration
Peak plasma levels achieved within 1–2 hours
Absolute bioavailability of parent drug is approximately 14%
Systemic inhibitory activity reaches about 30%
Distribution
Mean volume of distribution: ~381 L
Approximately 98% protein-bound
Limited penetration into red blood cells
Likely excreted into breast milk based on animal studies
Metabolism
Extensively metabolized into active ortho- and para-hydroxylated metabolites
Metabolism primarily via CYP3A4
Active metabolites contribute approximately 70% of HMG-CoA reductase inhibitory activity
Excretion
Eliminated mainly through bile
Plasma half-life of atorvastatin: ~14 hours
Functional inhibitory half-life: 20–30 hours
Less than 2% excreted unchanged in urine