Evidence suggests ARBs should be first line for CV indications over ACE inhibitors (Chen et al. Hypertension 2021). Which ARBs should you choose when prescribing?
| When? | Which one to give? | Which one to avoid? | |
|---|---|---|---|
| Clinical condition of concern | First ARBs of choice | ARBs with potentially beneficial effects | ARBs with potentially negative effect |
| Cardiovascular prevention | Telmisartan [10–12] | Losartan [13] | |
| Heart failure | Valsartan [14] Candesartan [15, 16] Losartan [17–19] |
||
| Myocardial infarction | Valsartan [20, 21] | Telmisartan [10, 22] | |
| Stroke | Losartan [23] | Telmisartan [24, 25] Candesartan [27] Eprosartan [28] |
|
| Atrial fibrillation | Telmisartan [34–36] | Losartan [29, 33] Candesartan [30] Valsartan [31, 32] |
|
| Diabetes mellitus | Telmisartan [47, 50, 54, 55] Valsartan [47, 53, 55] |
Losartan [47, 53] Irbesartan [47] Candesartan [47, 53] |
Olmesartan [47] |
| Diabetic nephropathy | Losartan [60] Irbesartan [61, 62] |
Telmisartan [63] Valsartan [64–66] Candesartan [67] |
Olmesartan [68–70] |
| Metabolic syndrome | Telmisartan [72, 75, 77–79] | Valsartan [81, 82] | |
| Hyperuricemia | Losartan [89–91] | Irbesartan [93] | Candesartan [89–91] |
| Erectile dysfunction | Valsartan [101–104] Losartan [105, 106] Irbesartan [106, 108] |
||
| Cognitive decline | Candesartan [116] Irbesartan [116] Losartan [116] Valsartan [116] Eprosartan [121] Telmisartan [122] |
||
Pharmacology
| ARBs | Half-life (h) | Tmax (h) | Bioavailability | Route of elimination: renal (R) biliary/fecal (B) |
Food Interaction | Drug Interactionsϕ | CYP metabolism |
|---|---|---|---|---|---|---|---|
| Losartan* | 2 | 1–1.5 | 33% | 35% R; 60% B | Yes∞ | Rifampin, fluconazole | 2C9, 3A4 |
| Candesartan cilexetil | 9 | 2–5ε | 42% | 33% R; 67% B | No | None | 2C9 (negligible) |
| Eprosartan | 5–9 | 1–3 | 63% | 7% R; 90% B | Yes¶ | None | No |
| Irbesartan | 11–15 | 1.3–3 | 60–80% | 20% R; 80% B | No | 2C9, 3A4 (negligible) | |
| Telmisartan | 24 | 0.5–1 | 43% | <1% R; >97% B | No | Digoxin | No |
| Valsartan | 6 | 2–4 | 23% (capsule) 50% (solution) |
13% R; 83% B | Yes§ | None | 2C9 (weak) |
| Olmesartan medoxomil | 12–14 | 1.7–2.5 | 26% | 35–50%R; 50–65% B | No | None | No |
| Azilsartan medoxomil | 12 | 1.5–3 | 60% | 42% urine; 55% B | No | None | 2C9, CYP2B6 (negligible), CYP2C8 (negligible) |
References
- https://medsask.usask.ca/documents/drug-shortages-pdfs/arb-comparison-.v22.pdf
- Dézsi CA. The Different Therapeutic Choices with ARBs. Which One to Give? When? Why? Am J Cardiovasc Drugs. 2016;16:255-266. doi:10.1007/s40256-016-0165-4
- Abraham HMA, White CM, White WB. The Comparative Efficacy and Safety of the Angiotensin Receptor Blockers in the Management of [[Hypertension]] and Other Cardiovascular Diseases. Drug Saf. 2015;38(1):33-54. doi:10.1007/s40264-014-0239-7