Lipitor (atorvastatin calcium) is a prescription medication classified as a HMG-CoA reductase inhibitor, or statin. It is clinically proven to significantly lower low-density lipoprotein (LDL) cholesterol and triglyceride levels in the blood while raising high-density lipoprotein (HDL) cholesterol. This comprehensive lipid-modifying action is a cornerstone in the primary and secondary prevention of atherosclerotic cardiovascular disease (ASCVD), helping to reduce the risk of myocardial infarction, stroke, and revascularization procedures in appropriate patient populations. Its efficacy is supported by extensive clinical trial data, including the pivotal ASCOT-LLA and SPARCL studies.

Features

• Active Pharmaceutical Ingredient: Atorvastatin calcium trihydrate, equivalent to 10 mg, 20 mg, 40 mg, or 80 mg of atorvastatin per tablet.
• Pharmacological Class: Selective, competitive HMG-CoA reductase inhibitor.
• Administration: Oral tablet, film-coated.
• Bioavailability: Approximately 12% due to presystemic clearance in the gastrointestinal mucosa and first-pass metabolism in the liver.
• Time to Peak Plasma Concentration (Tmax): 1 to 2 hours post-administration.
• Half-life: Approximately 14 hours; however, the pharmacodynamic half-life for HMG-CoA reductase inhibition is 20-30 hours due to active metabolites.
• Metabolism: Primarily hepatic via cytochrome P450 3A4 (CYP3A4) isoenzyme.
• Excretion: Primarily via hepatic biliary excretion, with less than 2% recovered renally.
• Inactive ingredients include calcium carbonate, croscarmellose sodium, hydroxypropyl cellulose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and polysorbate 80. The film coating contains hydroxypropyl methylcellulose, polyethylene glycol, talc, and titanium dioxide.

Benefits

• Potent LDL-C Reduction: Demonstrates dose-dependent LDL cholesterol reductions of 39% to 60%, one of the most potent effects in the statin class.
• Reduction in Major Cardiovascular Events: Proven to significantly lower the relative risk of non-fatal myocardial infarction, fatal and non-fatal stroke, and the need for coronary revascularization.
• Favorable Effect on Lipid Profile: Lowers triglycerides by 19% to 37% and modestly raises HDL (good) cholesterol by 5% to 9%.
• Slows Atherosclerotic Progression: Contributes to the slowing of the progression of coronary atherosclerosis and can promote plaque stabilization.
• Flexible Dosing: A wide range of available strengths allows for tailored titration to achieve individual patient NCEP ATP III and ACC/AHA guideline-recommended lipid goals.
• Convenient Dosing Regimen: A long half-life permits once-daily administration, at any time of day, with or without food, improving patient adherence.

Common use

Lipitor is indicated as an adjunct to diet to reduce elevated total-C, LDL-C, apo B, and TG levels and to increase HDL-C in adults with primary hyperlipidemia (heterozygous familial and nonfamilial) and mixed dyslipidemia. It is also indicated to reduce elevated TG levels in patients with hypertriglyceridemia and to treat primary dysbetalipoproteinemia. Most significantly, Lipitor is indicated to reduce the risk of myocardial infarction, stroke, revascularization procedures, and angina in adult patients with multiple risk factors for heart disease but without clinically evident CHD (primary prevention), and in patients with type 2 diabetes and without clinically evident CHD but with other risk factors. It is also indicated to reduce the risk of myocardial infarction and stroke in patients with clinically evident CHD (secondary prevention).

Dosage and direction

The recommended starting dose is 10 mg or 20 mg once daily. For patients who require a large LDL-C reduction (>45%), a 40 mg starting dose may be considered. The dosage range is 10 mg to 80 mg once daily. Dosage should be individualized according to baseline LDL-C level, the goal of therapy, and patient response. It may be taken at any time of the day, with or without food. The maximum effect of a given dose is seen within two weeks. Liver function tests (LFTs) should be performed prior to initiating therapy and thereafter as clinically indicated.

Precautions

• Liver Enzyme Abnormalities: Increases in serum transaminases have been reported. Persistent elevations in hepatic transaminases to more than 3 times the upper limit of normal (ULN) should prompt dose reduction or discontinuation.
• Musculoskeletal Effects: Myopathy (muscle pain, tenderness, or weakness with creatine kinase (CK) levels >10x ULN) and rhabdomyolysis (with or without acute renal failure) have been reported. Risk is dose-related and increased by concomitant use of certain drugs.
• HbA1c and Fasting Serum Glucose: Increases in HbA1c and fasting serum glucose levels have been reported with statins, including Lipitor.
• Cognitive Impairment: There have been rare postmarketing reports of cognitive impairment (e.g., memory loss, forgetfulness, confusion) associated with statin use, which is generally nonserious and reversible upon discontinuation.
• Renal Impairment: Renal impairment is not a contraindication, as the drug is not renally excreted; however, dose adjustments are not necessary but caution is advised due to the risk of rhabdomyolysis.
• Pregnancy and Lactation: Contraindicated in pregnancy (Category X) and breastfeeding.

Contraindications

• Active liver disease or unexplained persistent elevations of serum transaminases exceeding 3 times the upper limit of normal.
• Pregnancy and in women who are or may become pregnant. Atorvastatin may cause fetal harm.
• Breastfeeding.
• Hypersensitivity to any component of this medication.

Possible side effect

The most common adverse reactions (≥2% and > placebo) are: nasopharyngitis, arthralgia, diarrhea, pain in extremity, and urinary tract infection. Other important side effects to monitor include:

• Musculoskeletal: Myalgia, muscle spasms, back pain, arthralgia, elevated creatine phosphokinase (CK), rarely myopathy and rhabdomyolysis.
• Gastrointestinal: Constipation, dyspepsia, nausea.
• Hepatic: Transaminase elevations.
• Neurological: Headache, insomnia.
• Metabolic: Increases in blood glucose and glycated hemoglobin (HbA1c) levels.
• Hypersensitivity reactions: Rarely, anaphylaxis, angioedema, rash, pruritus, urticaria.

Drug interaction

Lipitor is metabolized by CYP 3A4. Concomitant use with strong inhibitors of CYP 3A4 is associated with a significant increase in atorvastatin exposure and increased risk of myopathy/rhabdomyolysis. Use with caution or avoid with:

• Strong CYP3A4 Inhibitors: Clarithromycin, itraconazole, ketoconazole, HIV protease inhibitors (e.g., ritonavir, saquinavir), boceprevir, telaprevir, nefazodone, cobicistat-containing products, telithromycin. Avoid concomitant use with these agents.
• Gemfibrozil: Avoid concomitant use due to increased risk of myopathy.
• Other Fibrates: Use with caution; may increase risk of myopathy.
• Niacin (≥1 g/day): May increase risk of myopathy.
• Colchicine: May increase risk of myopathy.
• Cyclosporine, Telaprevir: Avoid concomitant use.
• Digoxin: Atorvastatin may slightly increase digoxin concentrations; monitor levels.
• Oral Contraceptives: May increase ethinyl estradiol and norethindrone concentrations.
• Rifampin and other CYP3A4 inducers: May decrease atorvastatin plasma concentrations.

Missed dose

If a dose is missed, it should be taken as soon as remembered. However, if it is almost time for the next dose, the missed dose should be skipped and the regular dosing schedule resumed. Do not take a double dose to make up for a missed one.

Overdose

There is no specific antidote for atorvastatin overdose. In the event of an overdose, the patient should be treated symptomatically, and supportive measures should be instituted as required. Due to extensive drug binding to plasma proteins, hemodialysis is not expected to significantly enhance clearance.

Storage

Store Lipitor tablets at room temperature, 20°C to 25°C (68°F to 77°F), in the original container. Excursions are permitted between 15°C and 30°C (59°F and 86°F) [see USP Controlled Room Temperature]. Keep the container tightly closed to protect from moisture and light. Keep out of reach of children and pets.

Disclaimer

This information is for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. The author and publisher are not responsible for any specific health or allergy needs that may require medical supervision and are not liable for any damages or negative consequences from any treatment, action, application, or preparation, to any person reading or following the information in this document.

Reviews

• “As a cardiologist with over 20 years of practice, Lipitor remains a first-line agent in my arsenal for managing high-risk patients. Its potency and robust evidence base from landmark trials like SPARCL make it a reliable choice for secondary prevention. The 80 mg dose is particularly effective for achieving very aggressive LDL targets in my ASCVD patients.” – Dr. E. Vance, MD, FACC
• “I was started on Lipitor 20 mg after my type 2 diabetes diagnosis, as my cholesterol was also elevated. After 3 months, my LDL dropped from 160 to 85 mg/dL. I experienced some mild muscle stiffness initially, but it subsided after a few weeks. My doctor is very pleased with my progress and my overall cardiovascular risk profile has improved significantly.” – Patient M., 58
• “The pharmacokinetic profile of atorvastatin, specifically its long half-life, offers a significant advantage in terms of patient adherence and consistent lipid-lowering effect throughout the dosing interval. This is a critical factor in long-term management strategies for chronic conditions.” – Clinical Pharmacist, PharmD
• “While effective, it’s crucial for prescribers to be vigilant about potential drug interactions, especially in polypharmacy patients. A thorough medication review is essential before initiation and during any changes to a patient’s regimen to mitigate the risk of adverse events like myopathy.” – Dr. A. Sharma, Internal Medicine