Atorvastatin 80 Mg Tablet

Atorvastatin 80 mg tablets are a high-dose formulation of the popular statin medication, atorvastatin, which is primarily used to lower cholesterol levels in the blood and prevent cardiovascular disease. Atorvastatin belongs to the group of drugs known as HMG-CoA reductase inhibitors or “statins.” It works by reducing the production of “bad” LDL cholesterol in the liver, increasing the removal of LDL cholesterol from the bloodstream, and slightly increasing the levels of “good” HDL cholesterol. This medication is often prescribed to individuals with high cholesterol, those at risk of heart disease, and sometimes to patients who have already experienced a heart attack or stroke to prevent further cardiovascular events.

Indications and Usage

Atorvastatin 80 mg tablets are indicated for:

• Primary Hyperlipidemia: To reduce elevated total cholesterol, LDL-cholesterol, apolipoprotein B, and triglycerides, and to increase HDL-cholesterol in patients with primary hypercholesterolemia (heterozygous familial and nonfamilial) and mixed dyslipidemia.
• Homozygous Familial Hypercholesterolemia: As an adjunct to other lipid-lowering treatments or when such treatments are not appropriate.
• Prevention of Cardiovascular Disease: To reduce the risk of myocardial infarction (MI), stroke, and the need for revascularization procedures and angina in adult patients without clinical evidence of CHD but with multiple risk factors for CHD.

Pharmacology and Pharmacokinetics

Atorvastatin is selectively and competitively inhibition of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl-coenzyme A to mevalonate, a precursor of cholesterol. Like other statins, atorvastatin has a hepatic site of action, reducing intrahepatic cholesterol production, which leads to increased production of LDL receptors on the hepatocyte surface, increased removal of LDL and IDL (intermediate-density lipoprotein) from the bloodstream, and ultimately lowering of circulating LDL and IDL levels.

Following oral administration, atorvastatin is rapidly absorbed, with peak plasma concentrations occurring within 1-2 hours. However, due to extensive first-pass metabolism in the liver, the systemic bioavailability of atorvastatin is approximately 12-14%. Atorvastatin undergoes extensive hepatic metabolism, primarily via the cytochrome P450 3A4 pathway, resulting in two major metabolites: ortho-hydroxyatorvastatin and para-hydroxyatorvastatin.

Safety and Side Effects

While generally well-tolerated, atorvastatin can cause side effects, some of which can be serious. Common side effects include headache, nausea, stomach pain, weakness, and muscle pain. More serious adverse effects can include:

• Muscle Pain and Damage (Myopathy and Rhabdomyolysis): The risk is increased with higher doses and certain genetic conditions.
• Liver Damage: Indicated by elevations in liver enzymes, which necessitate monitoring of liver function tests before and during treatment.
• Increased Risk of Diabetes: Particularly in patients with risk factors for diabetes.

Dosage and Administration

Atorvastatin 80 mg tablets should be taken orally once daily, with or without food. The dosage may need adjustment based on the patient’s response to treatment, especially in patients with renal insufficiency or those taking concomitant medications that may interact with atorvastatin.

Interactions and Contraindications

Atorvastatin can interact with various medications, including other lipid-lowering agents, antifungals, macrolide antibiotics, and immunosuppressants, among others, potentially increasing the risk of muscle toxicity or altering atorvastatin’s efficacy. Contraindications include active liver disease, unexplained elevations of transaminases, and pregnancy and breastfeeding due to potential fetal and neonatal harm.

Conclusion

Atorvastatin 80 mg tablets represent a powerful therapeutic option for managing elevated cholesterol levels and reducing the risk of cardiovascular events. However, their use requires careful consideration of the balance between benefits and risks, especially at high doses. Monitoring of liver enzymes, creatine kinase (CK) levels for potential muscle damage, and regular assessment of lipid profiles are essential components of patient management.