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CANONICAL MONOGRAPH [3.1] • ID: TIP-MED-000001

1. Amlodipine (as Amlodipine Besylate)

2. Pharmacological Class: Dihydropyridine Calcium Channel Blocker (CCB); Arterial Vasodilator • 3. Therapeutic Category: Cardiovascular & Antithrombotic Medicines (Ch 03)

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4. Clinical Overview & Verified Formulation Identity

Generic Name & Identifier:
Amlodipine (as Amlodipine Besylate)
Code: [3.1] | Stable ID: TIP-MED-000001
Verified Indian Market Brands / Status:
Stamlo (Dr. Reddy's), Amlogard (Pfizer), Amlopres (Cipla), Amlokind (Mankind)
9. Dosage Forms & Strengths:
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
Indian Regulatory Schedule & NLEM Status:
Schedule H (Drugs Rules, 1945 — Prescription Only)
True

5 & 6. 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.

8. Therapeutic Indications

10. Dosage and Administration (Educational Reference Summary)

Dosing & Clinical Context: 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 & 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.

11 & 13. Contraindications, Precautions and Warnings

🚫 11. Contraindications:
  • Severe systemic hypotension or cardiogenic shock
  • Severe aortic stenosis (hemodynamically unstable outflow obstruction)
  • Known hypersensitivity to dihydropyridine derivatives
⚠️ 13. Precautions and Warnings:

Extensively metabolised by hepatic CYP3A4; initiate at 2.5 mg once daily and titrate slowly in severe hepatic insufficiency (Child-Pugh C).

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 renal impairment (including CKD Stages 3–5); Amlodipine is not dialysable.

16b. Hepatic Considerations: Extensively metabolised by hepatic CYP3A4; initiate at 2.5 mg once daily and titrate slowly in severe hepatic insufficiency (Child-Pugh C).

12 & 14. Adverse Effects & Drug Interactions
12. Adverse Effects:
  • 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)
14. Drug 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.
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:
  • 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 Notes: 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 Illustration (PLATE-8.10)

ANTIHYPERTENSIVE PHARMACOLOGY: RAAS CASCADE, CALCIUM CHANNELS & NEPHRON SITES RENIN–ANGIOTENSIN–ALDOSTERONE SYSTEM (RAAS) 1. Juxtaglomerular Renin Release ← [Blocked by β1-Blockers: Metoprolol, Bisoprolol] 2. Angiotensinogen (Liver) → Angiotensin I (Decapeptide) 3. ACE Inhibitors (Ramipril, Enalapril, Perindopril) Block ACE: • Prevents Angiotensin I → Angiotensin II (↓ Vasoconstriction & ↓ Aldosterone) • Prevents Bradykinin breakdown (↑ NO/PGI2 vasodilation; Dry Cough ADR) 4. Angiotensin Receptor Blockers — ARBs (Telmisartan, Losartan, Olmesartan): • Selectively block AT1 Receptor (Gq) → Vasodilation & Efferent arteriole dilation • Does NOT inhibit bradykinin degradation (Minimal cough) 5. Mineralocorticoid Antagonists (Spironolactone, Eplerenone): Block Aldosterone Contraindicated in Pregnancy (ACEi/ARB Fetotoxicity) & Bilateral Renal Artery Stenosis Never combine ACEi + ARB (ONTARGET Trial: ↑ Hyperkalaemia & AKI) VASCULAR CALCIUM CHANNELS & DIURETIC TARGETS Dihydropyridine CCBs (Amlodipine, Cilnidipine, Nifedipine): • Block vascular smooth muscle L-type Ca2+ channels (Cav1.2) → Arterial dilation • Cilnidipine also blocks sympathetic N-type Ca2+ channels (↓ pedal oedema) Non-Dihydropyridine CCBs (Verapamil, Diltiazem): • Block SA/AV nodal & myocardial Ca2+ channels (↓ HR, ↓ AV conduction) • Avoid combining Verapamil/Diltiazem with Beta-Blockers (Heart block risk) Thiazide & Thiazide-Like Diuretics (Chlorthalidone, Indapamide, HCTZ): • Inhibit Na+/Cl- cotransporter (NCC) in Distal Convoluted Tubule • Monitor Electrolytes: Hypokalaemia, Hyponatraemia, Hyperuricaemia Central Sympatholytics & Pregnancy Hypertension: • First-line in Pregnancy: Labetalol (α1/β-blocker), Nifedipine SR, Methyldopa (α2-agonist)
Figure 8.10: Integrated cardiovascular site-of-action map for antihypertensive drug classes: ACE Inhibitors, ARBs, Dihydropyridine vs Non-Dihydropyridine CCBs, Thiazide/Loop/K+-Sparing Diuretics, and Beta-Blockers.

19. Authoritative References & Source Traceability

Primary Reference Record: Indian Pharmacist Desk Reference — Professional Edition 2.7 (2026–27) by Tejas Nartam; NFI 7th Ed (2026); NLEM 2022.

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 →