In this article, we will discuss LIPITOR® (Overview). So, let’s get started.
LIPITOR® (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.
• Reduce elevated total-C, LDL-C, apo B, and TG levels and increase HDL-C in adult patients with primary hyperlipidemia (heterozygous familial and non familial) and mixed dyslipidemia.
• Reduce elevated TG in adult patients with hypertriglyceridemia and primary dysbetalipoproteinemia.
• Reduce total-C and LDL-C in patients with homozygous familial hypercholesterolemia (HoFH).
• Reduce clevated total-C. LDL-C, and apo B levels in pediatric patients, 10 years to 17 years of age, with heterozygous familial hypercholesterolemia (HeFH) afier failing an adequate trial of diet therapy.
Mechanism of Action
LIPITOR® 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, LIPITOR® lowers plasma cholesterol and lipoprotein levels by inhibiting HMG-CoA reductase and cholesterolsynthesis in the liver and by increasing the number of hepatic LDL receptors on thecell surface to enhance uptake and catabolismof LDL; LIPITOR® also reduces LDL production and the number of LDL particles.
Pharmacodynamics
LIPITOR®, as well as some of its metabolites, are pharmacologically active in humans. The liver is the primary site of action and the principal site of cholesterol synthesis and LDL clearance. Drug dosage, rather than systemic drug concentration, correlates better with
LDL-C reduction. Individualization of drug dosage should be based on therapeutic response.
Dosage
Hyperlipidemia and Mixed Dyslipidemia
The recommended starting dose of LIPITOR® is 10 or 20 mg once daily. Patients who require a large reduction in LDL-C (more than 45%) my be started at 40 mg once daily. The dosage range of LIPITOR® is 10 to 80 mg once daily LIPITOR® can be administered as a single dose at any time of the day, with or without food. The starting doseand maintenance doses of LIPITOR® should be individualized according to patient characteristics such as goal of therapy and response. After initiation and/or upon titration of LIPITOR®, lipid levels should be analyzed within 2 to 4 weeks and dosage adjusted accordingly.
Heterozygous Familial Hypercholesterolemia in Pediatric Patients (10 Years to 17 Years of Age)
The recommended starting dose of LIPITOR® is 10 mg/day: the usualdose range is 10 to 20 mg orally once daily. Doses should be individualized according to the recommended goal of therapy. Adjustments should be made at intervals of 4 weeks or more.
Homozygous Familial Hypercholesterolemia
The dosage of LIPITOR® in patients with HoFH is 10 to 80 mg daily. LIPITOR should be used as an adjunct to other lipid-lowering treatments (eg. LDL apheresis) in these patients or if such treatments are unavailable.
Concomitant Lipid-Lowering Therapy
LIPITOR® may be used with bile acid res ins. The combination of HMG-CoA reductase inhibitors (statins) and fibrates should generally be used with caution.
Dosage in Patients with Renal Impairment
Renal disease does not affect the plastru concentrations nor LDL-C reduction of LIPITOR®; thus, dosage adjustment in patients with renal dysfunction is not necessary.
Dosage in Patients Taking Cyclosporine, Clarithromycin, Itraconazole, or Certain Protease Inhibitors
In patients taking cyclosporine or the HIV protease inhibitor tipranavir plus ritonaviror the hepatitis C virus (HCV) protease inhibitor glecaprevir plus pibrentasvir, therapy with LIPITOR should be avoided. In patients with HIV taking lopinavir plus ritonavir, use the lowest dose necessary of LIPITOR. In patients taking clarithromycin, itraconazole, elbasvir plus grazoprevir, or in patients with HIV taking a combination of saquinavir plus ritonavir, darunavir plus ritonavir, fosamprenavir, ar losamprunavir plus ritonavir, therapy with LIPITOR® should be limited to 20 mg, and appropriate clinical assessment is recommended to ensure that the lowest dose necessary of LIPITOR is used. In patients taking the HIV protease inhibitor nelfinavir therapy with LIPITOR® should be limited to 40 mg. When co-prescribing atorvastatin with other protease inhibitors appropriate clinical assessment is recommended to ensure that the lowest dose necessary of LIPITOR® is used.
Dosage Forms and Strengths
LIPITOR® tablets are white elliptical, film-coated, and are available in four strengths.
LIPITOR® Tablet Strengths and Identifying Features
Tablet Strength – Identifying Features
10 mg of atorvastatin – “PD 155” on one side and “10” on the other
20 mg of atorvastatin – “PD 156” on one side and “20” on the other
40 mg of atorvastatin – “PD 157” on one side and “40” on the other
80 mg of atorvastatin – “PD 158” on one side and “80” on the other
Contraindications
• Active Liver Disease, which may include unexplained persistent elevations in Hepatic Transaminase Levels
• Hypersensitivity
• Pregnancy
• Lactation