1. Atorvastatin Calcium
2. Pharmacological Class: HMG-CoA Reductase Inhibitor (Lipophilic Statin); Lipid-Lowering & Plaque-Stabilising Agent • 3. Therapeutic Category: Cardiovascular & Antithrombotic Medicines (Ch 03)
4. Clinical Overview & Verified Formulation Identity
Atorvastatin Calcium
Code: [3.16] | Stable ID: TIP-MED-000016
Representative Indian Market Examples (Edition 2.7 Ch 03 [3.16], p. 28): Atorva (Zydus), Storvas (Sun Pharma), Lipitor (Pfizer), Tonact (Lupin), Lipikind (Mankind), Aztor (Sun) — Strengths & Forms: Oral Film-Coated Tablets: 5 mg, 10 mg, 20 mg, 40 mg, 80 mg
Oral Film-Coated Tablets: 5 mg, 10 mg, 20 mg, 40 mg, 80 mg
Route: Oral / Parenteral / Topical as specified by formulation
Schedule H Prescription Drug • NLEM 2022 Core Essential Medicine
True
5 & 6. Mechanism of Action & Pharmacodynamics
Competitively inhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme converting HMG-CoA to mevalonate in hepatic cholesterol synthesis. Depletion of intracellular hepatocyte sterols activates SREBP-2, upregulating hepatic surface LDL receptors and lowering plasma LDL-C by 35%–55%.
8. Therapeutic Indications
- Primary and secondary prevention of atherosclerotic cardiovascular disease (ASCVD, post-MI, post-PCI, stroke)
- Primary hypercholesterolaemia (heterozygous/homozygous familial) and mixed dyslipidaemia
- Diabetic dyslipidaemia in adults aged 40–75 years
10. Dosage and Administration (Educational Reference Summary)
Administration & Timing: Oral; can be taken at any time of day (morning or bedtime) with or without food due to its 20–30 hr active metabolite half-life.
11 & 13. Contraindications, Precautions and Warnings
- Active liver disease or unexplained persistent serum transaminase elevation >3x ULN
- Pregnancy and breastfeeding
- Concomitant strong CYP3A4 / OATP1B1 inhibitors (Cyclosporine, Gemfibrozil, Tipranavir/Ritonavir)
Contraindicated in active acute liver disease or unexplained persistent transaminase elevations (>3x ULN).
7, 12, 14–18. Detailed Pharmacokinetics, Interactions, Special Populations & Counselling
7 & 16. Pharmacokinetics (ADME) & Renal / Hepatic Considerations
7. Pharmacokinetics (Absorption, Distribution, Metabolism, Excretion): Absorption, distribution, metabolism, and excretion follow class pharmacokinetic profile; verify patient renal/hepatic function.
16a. Renal Considerations: No dose adjustment required in chronic kidney disease (<2% renal excretion); preferred statin alongside Rosuvastatin in CKD.
16b. Hepatic Considerations: Contraindicated in active acute liver disease or unexplained persistent transaminase elevations (>3x ULN).
12 & 14. Adverse Effects & Drug Interactions
- Statin-associated muscle symptoms (myalgia, cramps; rare CPK >10x ULN myopathy or rhabdomyolysis <0.1%)
- Asymptomatic reversible elevation of hepatic transaminases (ALT/AST)
- Modest dose-dependent increase in incident Type 2 Diabetes / HbA1c (~0.1–0.2%; CV benefit outweighs risk)
- Clarithromycin, Itraconazole, Protease Inhibitors (CYP3A4 inhibition): markedly increases Atorvastatin AUC and rhabdomyolysis risk (limit dose <=20 mg)
- Gemfibrozil (OATP1B1 & glucuronidation inhibition): contraindicated due to severe myopathy risk (Fenofibrate preferred if fibrate required)
- Grapefruit juice (>1.2 L/day): inhibits enteric CYP3A4 and elevates statin exposure
15, 17 & 18. Special Populations, Clinical Monitoring & Patient Counselling
15. Use in Special Populations (Pregnancy, Lactation, Paediatrics, Geriatrics): Evaluate maternal-foetal benefit-risk ratio, paediatric mg/kg ceiling, and geriatric renal function prior to prescribing.
17. Clinical & Laboratory Monitoring: Monitor clinical response, baseline renal/hepatic parameters, and relevant serum biomarkers.
18. Patient Counselling & Storage:- May be taken at any consistent time of day (unlike short-acting Simvastatin which must be taken at night).
- Report unexplained severe muscle pain, tenderness, weakness, or dark cola-coloured urine promptly.
- Continue diet and physical activity alongside statin therapy.
Storage & Dispensing Notes: Store below 25–30°C protected from moisture.
Visual Pharmacology Illustration (PLATE-8.10)
19. Authoritative References & Source Traceability
Primary Reference Record: Indian Pharmacopoeia (IP 2026) • NLEM 2022 (MoHFW) • CDSCO Approved Prescribing Information
Verification Portals: Indian Pharmacopoeia Commission (IPC) • CDSCO (India Jurisdiction) • NCBI Bookshelf • DailyMed (US FDA Label Reference)
Last Reviewed Date: 2026-11-08 • Related Study Guide: Essential Hypertension Clinical Management →