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). |
| Molecular Weight | 520.63 |
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 | Avoid; associated with fetal renal impairment and oligohydramnios. |
| 2nd trimester | Contraindicated; risk of fetal hypotension, anuria, and renal failure. |
| 3rd trimester | Contraindicated; potential for neonatal renal dysfunction and skull hypoplasia. |
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.
| Placental transfer | Crosses placenta; demonstrated in animal studies. |
| Breastfeeding | No human data; consider risk of infant hypotension; use with caution. |
| Lactation Rating |
■ 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 |
Hypersensitivity to eprosartanPregnancyHistory of angioedema with ARBsSevere hepatic impairmentCo-administration with aliskiren in diabetes
| Precautions | Fetal/neonatal morbidity and mortality, Hypotension in volume-depleted patients, Renal function impairment, Hyperkalemia |
| Food/Dietary | Eprosartan can be taken with or without food. High-fat meals may slightly reduce the rate of absorption, but the overall extent of absorption is not significantly affected. Avoid excessive alcohol consumption as it may increase the risk of hypotension. No specific food restrictions are necessary, but maintain a consistent diet regarding salt and fluid intake, especially if on concurrent diuretics. Avoid potassium-rich foods and salt substitutes in large amounts unless cleared by a physician. |
Loading safety data…
| L3: Limited Data |
| 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. |
| 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. |
| Clinical Pearls | Eprosartan mesylate is an angiotensin II receptor blocker (ARB) used for hypertension. It has a high affinity for AT1 receptors with no agonistic activity. Unlike some ARBs, eprosartan is not prodrug and does not require hepatic activation. Monitor renal function and electrolytes, especially in patients with renal artery stenosis, heart failure, or on diuretics. Avoid use in pregnancy; discontinue as soon as pregnancy is detected. Eprosartan has a relatively short half-life (5-9 hours) compared to other ARBs, requiring twice-daily dosing. It may cause less cough than ACE inhibitors. Can be taken without regard to meals. |
| Patient Advice | Take eprosartan exactly as prescribed, usually twice daily with or without food. · Do not stop taking this medication suddenly without consulting your doctor. · Avoid becoming pregnant; use effective contraception while on this medication. If you become pregnant, stop the drug and call your doctor immediately. · This medication can cause dizziness or lightheadedness, especially when first starting or if dehydrated. Rise slowly from sitting or lying positions. · Inform your doctor if you experience symptoms such as fainting, irregular heartbeat, or swelling of the face, lips, or throat. · Avoid potassium supplements or salt substitutes containing potassium without consulting your doctor. · Drink plenty of fluids to avoid dehydration, but do not overhydrate without medical advice. · Do not take this medication if you have diabetes and are taking aliskiren (a direct renin inhibitor). · Store at room temperature away from moisture and heat. |