Losartan Potassium
Angiotensin II Receptor Blocker (ARB; selective AT1 antagonist) • Schedule H Prescription Drug (To be sold by retail on the prescription of a Registered Medical Practitioner only — Drugs Rules 1945)
Level 1 — Quick Professional Summary (At a Glance)
Losartan Potassium
Monograph Code: [3.3] | Stable ID: TIP-MED-000003
Losar (Unichem), Losacar (Zydus), Repace (Sun Pharma), Tozaar (Torrent)
Angiotensin II Receptor Blocker (ARB; selective AT1 antagonist)
Cardiovascular & Antithrombotic Medicines (Ch 03)
Oral Film-Coated Tablets: 25 mg, 50 mg, 100 mg
Route: Oral / Parenteral / Topical as specified by formulation
9–10. 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
12. Therapeutic Indications
- Hypertension (especially with concurrent hyperuricaemia/gout or left ventricular hypertrophy)
- diabetic nephropathy with proteinuria in Type 2 DM
- heart failure (when ACE inhibitors are not tolerated)
13 & 16. Contraindications, Precautions & Warnings
- Contraindicated in pregnancy, lactation, and bilateral renal artery stenosis. Requires CYP2C9 conversion to its active E-3174 metabolite for full potency.
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.
14. Dosage & Administration Context (Educational Reference Summary)
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.
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: 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.
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.
15 & 17. Adverse Effects & Clinically Significant Drug Interactions
- Dizziness, nasal congestion, fatigue, mild hyperkalaemia, transient musculoskeletal ache.
- Severe hyperkalaemia, acute renal failure in renal artery stenosis, rare angioedema, hepatotoxicity.
- 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)
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:- 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 Governance: 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 Mechanism Diagram (PLATE-8.10)
23. Traceable Source References & Jurisdiction
Primary Reference Record: Indian Pharmacist Desk Reference — Professional Edition 2.7 (2026–27) • Ch 03 [3.3] (p. 22)
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 →