Amlodipine (as Amlodipine Besylate)
Dihydropyridine Calcium Channel Blocker (CCB); Arterial Vasodilator • Schedule H (Drugs Rules, 1945 — Prescription Only)
Level 1 — Quick Professional Summary (At a Glance)
Amlodipine (as Amlodipine Besylate)
Monograph Code: [3.1] | Stable ID: TIP-MED-000001
Stamlo (Dr. Reddy's), Amlogard (Pfizer), Amlopres (Cipla), Amlokind (Mankind)
Dihydropyridine Calcium Channel Blocker (CCB); Arterial Vasodilator
Cardiovascular & Antithrombotic Medicines (Ch 03)
Oral Uncoated Tablets: 2.5 mg, 5 mg, 10 mg (Racemic Amlodipine); S-Amlodipine Tablets: 2.5 mg, 5 mg
Route: Oral / Parenteral / Topical as specified by formulation
9–10. 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.
12. Therapeutic Indications
- Essential hypertension (first-line monotherapy or combination therapy)
- Chronic stable angina pectoris and vasospastic (Prinzmetal) angina
13 & 16. Contraindications, Precautions & Warnings
- Severe systemic hypotension or cardiogenic shock
- Severe aortic stenosis (hemodynamically unstable outflow obstruction)
- Known hypersensitivity to dihydropyridine derivatives
Extensively metabolised by hepatic CYP3A4; initiate at 2.5 mg once daily and titrate slowly in severe hepatic insufficiency (Child-Pugh C).
14. Dosage & Administration Context (Educational Reference Summary)
Administration & 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.
Level 2 — Detailed Pharmacology, PK, Interactions & Special Populations
11 & 19. Pharmacokinetics (ADME), Renal & Hepatic Considerations
Pharmacokinetic Profile: Absorption, distribution, metabolism, and excretion follow class pharmacokinetic profile; verify patient renal/hepatic function.
Renal Considerations: No dose adjustment required in renal impairment (including CKD Stages 3–5); Amlodipine is not dialysable.
Hepatic Considerations: Extensively metabolised by hepatic CYP3A4; initiate at 2.5 mg once daily and titrate slowly in severe hepatic insufficiency (Child-Pugh C).
15 & 17. Adverse Effects & Clinically Significant Drug Interactions
- 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)
- 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.
18, 20, 21 & 22. Special Populations, Monitoring, Counselling & Storage
Pregnancy, Lactation, Paediatric & Geriatric Use: Evaluate maternal-foetal benefit-risk ratio and age-appropriate organ function before prescribing.
Clinical & Laboratory Monitoring: Monitor clinical response, baseline renal/hepatic parameters, and relevant serum biomarkers.
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 & Dispensing Governance: 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).
Visual Pharmacology Mechanism Diagram (PLATE-8.10)
23. Traceable Source References & Jurisdiction
Primary Reference Record: Indian Pharmacist Desk Reference — Professional Edition 2.7 (2026–27) by THE INDIAN PHARMACIST Editorial Reference; NFI 7th Ed (2026); NLEM 2022.
Authoritative Verification Portals: Indian Pharmacopoeia Commission (IPC) • CDSCO (India Jurisdiction) • NCBI Bookshelf • DailyMed (US FDA Label Reference)
Last Checked Date: 2026-11-08 • Related Study Guide: Essential Hypertension Clinical Management →