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CANONICAL MONOGRAPH [3.3] • ID: TIP-MED-000003

1. Losartan Potassium

2. Pharmacological Class: Angiotensin II Receptor Blocker (ARB; selective AT1 antagonist) • 3. Therapeutic Category: Cardiovascular & Antithrombotic Medicines (Ch 03)

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4. Clinical Overview & Verified Formulation Identity

Generic Name & Identifier:
Losartan Potassium
Code: [3.3] | Stable ID: TIP-MED-000003
Verified Indian Market Brands / Status:
Losar (Unichem), Losacar (Zydus), Repace (Sun Pharma), Tozaar (Torrent)
9. Dosage Forms & Strengths:
Oral Film-Coated Tablets: 25 mg, 50 mg, 100 mg
Route: Oral / Parenteral / Topical as specified by formulation
Indian Regulatory Schedule & NLEM Status:
Schedule H Prescription Drug (To be sold by retail on the prescription of a Registered Medical Practitioner only — Drugs Rules 1945)
True

5 & 6. Mechanism of Action & Pharmacodynamics

Blocks AT1 receptor-mediated vasoconstriction and aldosterone secretion; converted via hepatic CYP2C9/CYP3A4 to active carboxylic acid metabolite E-3174 (10–40x more potent) + unique URAT1-mediated uricosuric effect

8. Therapeutic Indications

10. Dosage and Administration (Educational Reference Summary)

Dosing & Clinical Context: General Adult Reference: Initially 50 mg once daily (25 mg OD in intravascular volume depletion or hepatic impairment); may increase to 100 mg once daily or 50 mg twice daily. Follow physician prescription.
Administration & Timing: With or without food (typically after breakfast). | Once daily in the morning, or divided twice daily (morning and evening) if 50 mg BD is prescribed for smoother 24-hour BP control.

11 & 13. Contraindications, Precautions and Warnings

🚫 11. Contraindications:
  • Contraindicated in pregnancy, lactation, and bilateral renal artery stenosis. Requires CYP2C9 conversion to its active E-3174 metabolite for full potency.
⚠️ 13. Precautions and Warnings:

Renal: No initial dose reduction required unless volume-depleted, but requires close monitoring of creatinine and K+ as eGFR declines; suspend during acute dehydrating illness ('Sick Day Rule'). Hepatic: Plasma concentrations doubled in cirrhosis—initiate at 25 mg once daily.

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: Renal: No initial dose reduction required unless volume-depleted, but requires close monitoring of creatinine and K+ as eGFR declines; suspend during acute dehydrating illness ('Sick Day Rule'). Hepatic: Plasma concentrations doubled in cirrhosis—initiate at 25 mg once daily.

16b. Hepatic Considerations: Renal: No initial dose reduction required unless volume-depleted, but requires close monitoring of creatinine and K+ as eGFR declines; suspend during acute dehydrating illness ('Sick Day Rule'). Hepatic: Plasma concentrations doubled in cirrhosis—initiate at 25 mg once daily.

12 & 14. Adverse Effects & Drug Interactions
12. Adverse Effects:
  • Dizziness, nasal congestion, fatigue, mild hyperkalaemia, transient musculoskeletal ache.
  • Severe hyperkalaemia, acute renal failure in renal artery stenosis, rare angioedema, hepatotoxicity.
14. Drug Interactions:
  • Potassium-sparing diuretics (Spironolactone, Eplerenone), K+ supplements, or salt substitutes (LoSalt) -> severe hyperkalaemia
  • NSAIDs -> blunted antihypertensive effect and acute kidney injury ('Triple Whammy' with diuretic)
  • Lithium -> reversible lithium toxicity
  • CYP2C9 inducers (Rifampicin) reduce active E-3174 metabolite and lower BP efficacy; Fluconazole inhibits conversion to E-3174 (clinical significance: monitor BP response over 1–2 weeks)
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:
  • Patient Counselling Checklist: Highlight that losartan uniquely lowers serum uric acid mildly by inhibiting renal URAT1 reabsorption, making it particularly advantageous in hypertensive patients prone to gout. Maintain adequate hydration during initial weeks.
  • Meal & Clock Timing Instruction: With or without food (typically after breakfast). (Once daily in the morning, or divided twice daily (morning and evening) if 50 mg BD is prescribed for smoother 24-hour BP control.)
  • Missed Dose Protocol: Take as soon as remembered unless within 6–8 hours of the next scheduled dose. Do not double the dose.
  • Geriatric Dispensing Pearl: Shorter half-life than telmisartan (parent drug ~2 h, active metabolite ~6–9 h); some elderly patients experience evening BP breakthrough on once-daily dosing and may be prescribed 25–50 mg BD. Initiate at 25 mg in patients >75 years or on diuretics.

Storage & Dispensing Notes: Store below 25°C–30°C in original moisture- and light-resistant packaging out of reach of children. Available forms: Oral Film-Coated Tablets: 25 mg, 50 mg, 100 mg

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) • Ch 03 [3.3] (p. 22)

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 →