1. Clinical & Scientific Overview
Amlodipine (as Amlodipine Besylate) (TIP-MED-000001, Reference Code [3.1]) is classified under
Cardiovascular & Antithrombotic Medicines (Ch 03) as a Dihydropyridine Calcium Channel Blocker (CCB); Arterial Vasodilator.
Within the Indian regulatory and compendial framework, it is governed under Schedule H (Drugs Rules, 1945 — Prescription Only).
Stamlo (Dr. Reddy's), Amlogard (Pfizer), Amlopres (Cipla), Amlokind (Mankind)
Oral Uncoated Tablets: 2.5 mg, 5 mg, 10 mg (Racemic Amlodipine); S-Amlodipine Tablets: 2.5 mg, 5 mg
3. Mechanism of Action & Pharmacodynamics
Binds selectively to vascular smooth muscle L-type voltage-gated calcium channels (Cav1.2), inhibiting transmembrane calcium influx and producing peripheral arterial vasodilation with minimal negative inotropic or AV-nodal conduction effect.
4. Therapeutic Indications & Evidence-Supported Uses
- Essential hypertension (first-line monotherapy or combination therapy)
- Chronic stable angina pectoris and vasospastic (Prinzmetal) angina
5. Educational Dosage Context, Formulations & Administration
Educational Dosing & Regimen Summary: Educational Reference Summary: Typically initiated at 2.5 mg to 5 mg orally once daily; titrated to a maximum of 10 mg once daily based on blood pressure response over 7–14 days (elderly or hepatic impairment: 2.5 mg once daily).
Administration & Meal Timing: Once daily (morning or evening), independent of meals. Intrinsic plasma elimination half-life is 30–50 hours, maintaining 24-hour trough blood pressure control even if a dose is slightly delayed.
6. Pharmacokinetics, Metabolism & Renal/Hepatic Adjustment
Absorption, distribution, metabolism, and excretion follow class pharmacokinetic profile; verify patient renal/hepatic function.
Extensively metabolised by hepatic CYP3A4; initiate at 2.5 mg once daily and titrate slowly in severe hepatic insufficiency (Child-Pugh C).
No dose adjustment required in renal impairment (including CKD Stages 3–5); Amlodipine is not dialysable.
Extensively metabolised by hepatic CYP3A4; initiate at 2.5 mg once daily and titrate slowly in severe hepatic insufficiency (Child-Pugh C).
7. Contraindications, Precautions & High-Risk Warnings
- Severe systemic hypotension or cardiogenic shock
- Severe aortic stenosis (hemodynamically unstable outflow obstruction)
- Known hypersensitivity to dihydropyridine derivatives
Key Clinical Precautions: Extensively metabolised by hepatic CYP3A4; initiate at 2.5 mg once daily and titrate slowly in severe hepatic insufficiency (Child-Pugh C).
8. Adverse Effects Profile
- Dose-dependent bilateral ankle/pedal oedema (due to pre-capillary arteriolar dilation without matching post-capillary venular dilation — responds to ACEi/ARB addition rather than loop diuretics)
- Facial flushing, headache, dizziness, palpitations
- Gingival hyperplasia (with long-term use; advise oral hygiene)
- Monitor for severe hypersensitivity, organ toxicity, or dose-limiting adverse events.
9. Major Drug–Drug, Drug–Food & Drug–Herb Interactions
- Simvastatin: Co-administration with Amlodipine increases simvastatin systemic exposure; cap simvastatin dose at 20 mg/day to prevent myopathy/rhabdomyolysis.
- Strong CYP3A4 Inhibitors (Clarithromycin, Itraconazole, Ketoconazole): Increase plasma Amlodipine levels by up to 60%; monitor for hypotension and pedal oedema.
- CYP3A4 Inducers (Rifampicin, Phenytoin, Carbamazepine): Reduce Amlodipine plasma concentrations; monitor blood pressure control.
10. Clinical Monitoring, Patient Counselling & Storage
Clinical & Laboratory Monitoring: Monitor clinical response, baseline renal/hepatic parameters, and relevant serum biomarkers.
Pharmacist Patient Counselling Points:
- Take once daily at the same time each day, with or without food.
- Report persistent ankle or foot swelling; do not abruptly discontinue antihypertensive therapy without medical guidance.
- Rise slowly from sitting or lying positions during the first week to minimise postural dizziness.
Storage, Stability & Dispensing Safeguards: Store below 30°C protected from light and moisture. Verify strength carefully (2.5 mg vs 5 mg vs 10 mg) and check whether prescribed as plain Amlodipine or an FDC (e.g., Amlodipine + Telmisartan or Amlodipine + Atenolol).
11. Visual Pharmacology & Mechanism Diagram (svg-v339-01-adme-12-step-journey)
12. Authoritative References, Regulatory Sources & Editorial Disclaimer
Primary Compendial & Guideline Reference: Indian Pharmacist Desk Reference — Professional Edition 2.7 (2026–27) by Tejas Nartam; NFI 7th Ed (2026); NLEM 2022.
Official Verification Portals: Indian Pharmacopoeia Commission (IPC) & National Formulary of India (NFI) • Central Drugs Standard Control Organization (CDSCO) • Ministry of Health & Family Welfare — NLEM 2022 • NCBI Bookshelf / StatPearls Pharmacology Reference • DailyMed (US FDA Official Prescribing Reference)
Last Medically & Pharmaceutically Reviewed: 2026-11-10 • Verification Status: VERIFIED_EDUCATIONAL_CONTENT
Educational & Clinical Disclaimer: This reference profile is published solely for pharmacy education, academic study, and professional clinical reference. It does not substitute for patient-specific clinical judgement, qualified specialist oncology/medical supervision, or official CDSCO/IP prescribing information. Never self-medicate with prescription, Schedule H/H1/X, NDPS, or oncology medicines.