EPROSARTAN MESYLATE
Clinical safety rating: avoid
Contraindicated (not allowed)
Eprosartan mesylate is an angiotensin II receptor antagonist (ARB) that selectively blocks the binding of angiotensin II to the AT1 receptor, thereby inhibiting the vasoconstrictor and aldosterone-secreting effects of angiotensin II.
| Metabolism | Eprosartan is not significantly metabolized by the cytochrome P450 system; it undergoes minimal hepatic metabolism primarily via glucuronidation and is excreted unchanged in bile and urine. |
| Excretion | Primarily biliary/fecal (≈90% as unchanged drug); renal elimination accounts for ≈7% (mostly unchanged). |
| Half-life | Terminal elimination half-life is about 5–9 hours. Clinical context: supports once-daily dosing for hypertension. |
| Protein binding | High (≈98%) primarily to albumin. |
| Volume of Distribution | ≈13 L (0.13 L/kg for 70 kg adult), indicating limited extravascular distribution. |
| Bioavailability | Oral: approximately 13% (low due to first-pass metabolism; food does not affect absorption). |
| Onset of Action | Oral: 1–2 hours (peak antihypertensive effect occurs within 3–6 hours). |
| Duration of Action | 24 hours (supports once-daily dosing; sustained blood pressure reduction over 24 hours). |
Oral, 600 mg once daily. May increase to 800 mg once daily if inadequate response.
| Dosage form | TABLET |
| Renal impairment | CrCl 30-60 mL/min: maximum 600 mg once daily. CrCl <30 mL/min: not recommended (no data). |
| Liver impairment | Mild to moderate hepatic impairment (Child-Pugh A-B): maximum 600 mg once daily. Severe impairment (Child-Pugh C): not recommended. |
| Pediatric use | Safety and efficacy not established; no approved dosing. |
| Geriatric use | No specific adjustment required; start at low end of dosing range due to potential renal decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
NSAIDs may diminish the antihypertensive effect Lithium levels may be increased Use in pregnancy can cause injury and death to the developing fetus.
| Breastfeeding | Data are insufficient; eprosartan is excreted in low amounts in human milk (M/P ratio unknown). Given potential for infant renal effects, breast-feeding is not recommended. Consider alternative agents. |
| Teratogenic Risk | First trimester: Fetal exposure may carry risk of oligohydramnios and fetal harm based on angiotensin receptor blocker (ARB) class effects, though specific data for eprosartan are limited; use is generally avoided. Second and third trimesters: Fetal toxicity is well-documented, including oligohydramnios, renal dysfunction, skull ossification defects, and anuria; ARBs are contraindicated in pregnancy. |
■ FDA Black Box Warning
Fetal toxicity: drugs acting directly on the renin-angiotensin system can cause injury and death to the developing fetus. Discontinue as soon as possible once pregnancy is detected.
| Common Effects | Dizziness |
| Serious Effects |
["Pregnancy","Hypersensitivity to eprosartan or any component of the formulation"]
| Precautions | ["Fetal/neonatal morbidity and mortality","Hypotension in volume-depleted patients","Renal function impairment","Hyperkalemia"] |
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| Fetal Monitoring | Maternal: Blood pressure, renal function (serum creatinine, BUN), serum electrolytes (potassium). Fetal: Serial ultrasound for amniotic fluid volume, fetal growth, renal anatomy; consider fetal echocardiography in second trimester. |
| Fertility Effects | Animal studies at high doses showed adverse effects on fertility (impaired spermatogenesis and reduced conception rates). Human data limited; ARBs may theoretically interfere with renin-angiotensin system in reproductive tissues. |