Lipitor: Advanced Lipid Management for Cardiovascular Risk Reduction
Lipitor
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Lipitor (atorvastatin calcium) is a prescription medication classified as a statin, or HMG-CoA reductase inhibitor. It is a first-line therapeutic agent specifically formulated to manage dyslipidemia by significantly reducing low-density lipoprotein cholesterol (LDL-C) and triglyceride levels while moderately elevating high-density lipoprotein cholesterol (HDL-C). Its primary clinical objective is to mitigate the risk of major cardiovascular events, including myocardial infarction and stroke, in adult patients. By targeting the hepatic enzyme responsible for cholesterol synthesis, Lipitor offers a potent and well-established mechanism for comprehensive lipid control, forming a cornerstone of preventive cardiology strategies for both primary and secondary prevention.
Features
- Active Pharmaceutical Ingredient: Atorvastatin calcium
- Drug Class: HMG-CoA reductase inhibitor (statin)
- Available Strengths: 10 mg, 20 mg, 40 mg, and 80 mg film-coated tablets
- Mechanism of Action: Competitive inhibition of HMG-CoA reductase, the rate-limiting enzyme in the hepatic mevalonate pathway for cholesterol synthesis
- Pharmacokinetics: Rapidly absorbed after oral administration; peak plasma concentrations occur within 1 to 2 hours. Extensive first-pass metabolism primarily by the cytochrome P450 3A4 (CYP3A4) isoenzyme.
- Administration: Oral, once daily, with or without food
Benefits
- Potent LDL-C Reduction: Demonstrates dose-dependent efficacy, capable of reducing LDL cholesterol by 39% to 60%, a critical factor in atherosclerotic plaque stabilization and regression.
- Reduction in Cardiovascular Morbidity and Mortality: Proven in large-scale clinical trials to significantly decrease the risk of heart attack, stroke, and the need for revascularization procedures in patients with multiple risk factors or established cardiovascular disease.
- Favorable Effect on Overall Lipid Profile: Lowers elevated triglycerides and apolipoprotein B, and raises HDL-C levels, addressing multiple facets of atherogenic dyslipidemia.
- Anti-Inflammatory Properties: Contributes to a reduction in high-sensitivity C-reactive protein (hs-CRP), an key biomarker of vascular inflammation independent of its lipid-lowering effects.
- Proven Long-Term Safety Profile: Supported by decades of extensive clinical use and post-marketing surveillance, establishing a well-characterized benefit-risk profile for a wide patient demographic.
- Once-Daily Dosing: Enhances patient adherence and convenience, supporting long-term therapeutic consistency which is vital for achieving sustained cardiovascular risk reduction.
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 hypercholesterolemia (heterozygous familial and nonfamilial) and mixed dyslipidemia. Its most significant application is in the primary prevention of cardiovascular disease in adults without clinically evident coronary heart disease but with multiple risk factors (e.g., hypertension, low HDL-C, smoking, or a family history of early heart disease) to reduce the risk of myocardial infarction and stroke. It is also indicated for secondary prevention to reduce the risk of cardiovascular events, including stroke and myocardial infarction, in adults with established cardiovascular disease.
Dosage and direction
The dosage of Lipitor is patient-specific and must be individualized based on the patient’s LDL-C goals, the intended therapeutic response, and concurrent medication profile. The usual starting dose is 10 mg or 20 mg taken orally once daily. For patients requiring large LDL-C reductions (exceeding 45%), a starting dose of 40 mg may be considered. The dosage range is 10 mg to 80 mg daily. The 80 mg dose is reserved for patients who have not achieved their LDL-C goal on lower doses and should be used with appropriate caution. Administration can occur with or without food, at any time of day, though consistency in timing is recommended. Dosage adjustments should be made at intervals of 2 to 4 weeks. Liver function tests must be performed prior to initiation and as clinically indicated thereafter.
Precautions
- Hepatic Effects: Liver enzyme elevations have been reported. Persistent elevations in serum transaminases should prompt dose reduction or drug discontinuation. Use is contraindicated in active liver disease.
- Skeletal Muscle Effects: Myopathy and rhabdomyolysis have been reported. Patients should be advised to report promptly any unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever. Risk is increased with concomitant use of certain drugs and in elderly patients.
- Renal Impairment: Renal function should be monitored in patients at risk for renal failure, such as those with severe infections, hypotension, major surgery, or electrolyte disorders, as rhabdomyolysis can induce acute renal failure.
- Hemorrhagic Stroke: A slight increased risk of hemorrhagic stroke has been observed in some patients without known cerebrovascular disease; this risk should be considered against the overall cardiovascular benefit.
- Endocrine Function: Increases in HbA1c and fasting serum glucose levels have been reported, indicating a potential slight diabetogenic effect.
Contraindications
- Active liver disease or unexplained persistent elevations of serum transaminases exceeding three times the upper limit of normal.
- Pregnancy and breastfeeding. Cholesterol and products synthesized from cholesterol are essential for fetal development. Atherosclerosis is a chronic process; discontinuation of lipid-lowering drugs during pregnancy should have little impact on long-term outcomes.
- 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 include:
- Musculoskeletal: Myalgia, muscle spasms, back pain, arthralgia, and in rare cases, myopathy and rhabdomyolysis.
- Gastrointestinal: Constipation, dyspepsia, nausea, flatulence.
- Hepatic: Transaminase elevations.
- Nervous System: Headache, insomnia.
- Metabolic: Increased blood glucose levels, hyperglycemia.
- Dermatological: Rash.
Drug interaction
Lipitor is metabolized primarily by CYP 3A4. Concomitant administration with strong inhibitors of this enzyme increases atorvastatin plasma concentrations and the risk of myopathy/rhabdomyolysis.
- Strong CYP3A4 Inhibitors: Avoid concomitant use with drugs such as itraconazole, ketoconazole, posaconazole, voriconazole, clarithromycin, telithromycin, HIV protease inhibitors (e.g., ritonavir, saquinavir), boceprevir, telaprevir, nefazodone, gemfibrozil, cyclosporine.
- Gemfibrozil: Avoid due to significantly increased risk of myopathy.
- Other Fibrates: Use with caution (other than gemfibrozil).
- Niacin: Use with caution.
- Colchicine: Cases of myopathy have been reported with concomitant use.
- Digoxin: Atorvastatin may modestly increase digoxin concentrations; monitor levels.
- Oral Contraceptives: Increases ethinyl estradiol and norethindrone concentrations.
- Rifampin and other 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 scheduled dose, the missed dose should be skipped. The patient should not take a double dose to make up for the missed one. Maintaining a consistent daily schedule is important for optimal efficacy.
Overdose
There is no specific antidote for atorvastatin overdose. In the event of an overdose, symptomatic and supportive measures should be instituted. The patient should be treated symptomatically, with liver function and CK levels monitored. Due to extensive drug binding to plasma proteins, hemodialysis is not expected to significantly enhance clearance.
Storage
Store Lipitor tablets at room temperature, between 20°C to 25°C (68°F to 77°F), in their original container. Excursions are permitted between 15°C and 30°C (59°F and 86°F). Keep the container tightly closed to protect from light and moisture. Keep all medications out of the 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 content has been compiled from various sources believed to be accurate, but its accuracy cannot be guaranteed.
Reviews
Clinical Endorsement: “Lipitor remains a foundational therapy in lipid management. Its robust evidence base from trials like ASCOT-LLA and SPARCL solidifies its role in both primary and secondary prevention. The 80 mg dose provides potent LDL-C reduction for high-risk patients, though it requires vigilant monitoring for muscular adverse events.” – Cardiologist, 20 years of experience.
Patient Experience (Compiled Themes): Many long-term users report significant success in achieving and maintaining target cholesterol levels, often noting a strong sense of security regarding their cardiovascular health. A common point of feedback is the convenience of once-daily dosing. The most frequently reported concern involves managing mild, transient muscle aches, which often resolve with time or a slight dose adjustment. Patients consistently emphasize the importance of regular blood work to ensure the medication is working effectively and safely.