1. Generic & Brand Names
Generic: Losartan Potassium
Brands: Cozaar® (global), Losacar® (India), Repace®
Combinations:
With diuretic: Hyzaar® (losartan + hydrochlorothiazide)
With amlodipine: Amturnide® (losartan + amlodipine + HCTZ)
2. Drug Class & Mechanism
Class: Angiotensin II Receptor Blocker (ARB)
Mechanism:
Blocks AT₁ receptors → prevents angiotensin II-induced:
Vasoconstriction
Aldosterone release
Cardiac remodeling
↑ Bradykinin levels (less than ACEi) → lower cough risk
Onset: 6 hours; Peak effect: 3-6 weeks
3. FDA-Approved Uses
| Condition | Key Benefits |
|---|---|
| Hypertension (HTN) | First-line monotherapy or combo |
| Diabetic Nephropathy | ↓ Proteinuria, slows CKD progression |
| Stroke Prevention | In HTN patients with LVH (LIFE trial) |
| Off-label: | Heart failure (if ACEi intolerant) |
4. Dosing Regimens
| Indication | Starting Dose | Target Dose | Max Dose |
|---|---|---|---|
| HTN | 50 mg daily | 50-100 mg daily | 100 mg |
| Diabetic Nephropathy | 50 mg daily | 100 mg daily | 100 mg |
| LVH (Stroke Prevention) | 50 mg daily | 100 mg daily | 100 mg |
| Key Notes: |
Take with/without food
Full effect in 3-6 weeks (titrate monthly)
Renal Adjustment: No change needed
5. Side Effects
| Common (>5%) | Serious (<1%) |
|---|---|
| Dizziness | Hyperkalemia (K⁺ >5.5 mEq/L) |
| Fatigue | Acute Kidney Injury |
| Back pain | Angioedema (rare) |
| No dry cough (vs. ACEi) | Hepatotoxicity |
6. Black Box Warnings & Contraindications
🚫 Absolute Contraindications:
Pregnancy (Category D: fetal injury/death)
Bilateral renal artery stenosis
Concomitant aliskiren in diabetes
High-Risk Groups:
Renal impairment: Monitor K⁺/creatinine
Volume depletion: Risk of hypotension
7. Nephroprotective Effects
| Parameter | Impact |
|---|---|
| Proteinuria | ↓ 30-40% in diabetic nephropathy |
| eGFR Decline | Slows by 2-4 mL/min/year |
| Mechanism | ↓ Intraglomerular pressure |
| Evidence: RENAAL trial - ↓ ESRD risk by 28% in type 2 diabetics |
8. Critical Drug Interactions
| Medication | Risk | Action |
|---|---|---|
| NSAIDs | ↑ AKI/hyperkalemia risk | Avoid combo; use acetaminophen |
| Potassium Supplements | ↑ Hyperkalemia risk | Monitor K⁺ weekly |
| Lithium | ↑ Lithium levels → toxicity | Avoid combo |
| Aliskiren | ↑ AKI/hyperkalemia/hypotension | Contraindicated in diabetes |
9. Special Populations
| Group | Recommendation |
|---|---|
| Pregnancy | Discontinue immediately if pregnancy detected |
| Elderly | Start 25 mg daily (↑ hypotension risk) |
| Renal Impairment | Monitor K⁺/creatinine at 1-2 weeks |
| Hepatic Impairment | ↓ Dose 50% (Child-Pugh ≥B) |
10. Clinical Pearls
✅ Advantages:
First-line for HTN + diabetes/proteinuria
Better tolerability vs. ACEi (no cough)
Uricosuric effect (↓ serum uric acid)
❌ Limitations:Less HF mortality benefit vs. ACEi
Weak antihypertensive as monotherapy (combine with CCB/thiazide)
Losartan vs. Other ARBs
| Parameter | Losartan | Valsartan | Telmisartan |
|---|---|---|---|
| Half-life | 6-9 hours | 6 hours | 24 hours |
| Dosing | QD | QD-BID | QD |
| Proteinuria Reduction | +++ | ++ | ++++ |
| Cost | $ (generic) | $$ | $$$ |
Patient Counseling
"Take daily – even if feeling well."
"Avoid NSAIDs (ibuprofen, naproxen) – use Tylenol® for pain."
"Report immediately:
Dizziness/fainting (hypotension)
Swelling of face/lips (angioedema)
Muscle weakness (hyperkalemia)"
"Use contraception – stop drug if pregnancy suspected."
"Check BP weekly – bring log to appointments."
⚠️ Pregnancy Warning:
Category D – causes fetal harm (2nd/3rd trimester)
Switch to methyldopa/nifedipine if planning pregnancy
Prescribing Status: First-line for HTN with diabetes/CKD per ADA/KDIGO guidelines.
Cost: Generic <$0.10/dose.
Sources: ADA Standards of Care (2024), KDIGO 2022 CKD Guidelines, LIFE Trial (Lancet).
Comments
Post a Comment