TEVETEN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TEVETEN (TEVETEN).
Selective angiotensin II receptor type 1 (AT1) antagonist, blocking the vasoconstrictor and aldosterone-secreting effects of angiotensin II.
| Metabolism | Primarily metabolized by glucuronidation (UGT1A3, UGT2B7); minimal CYP450 metabolism. |
| Excretion | Renal (approximately 60% as unchanged drug) and biliary/fecal (approximately 40%). |
| Half-life | Terminal elimination half-life is approximately 7-8 hours in patients with normal renal function, supporting once-daily dosing. |
| Protein binding | Approximately 99% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Approximately 0.3 L/kg, indicating distribution mainly in extracellular fluid. |
| Bioavailability | Oral: approximately 15-20% due to extensive first-pass metabolism; absorption is not significantly affected by food. |
| Onset of Action | Oral: 1-2 hours for reduction in blood pressure; peak effect at 4-6 hours. |
| Duration of Action | Approximately 24 hours, allowing once-daily dosing; sustained effect over 24 hours at steady state. |
400-800 mg orally once daily; can be divided twice daily if needed for adequate blood pressure control.
| Dosage form | TABLET |
| Renal impairment | CrCl 30-59 mL/min: no adjustment; CrCl <30 mL/min: 200-400 mg once daily; hemodialysis: not studied, use with caution. |
| Liver impairment | No adjustment required for mild to moderate impairment; not studied in severe impairment (Child-Pugh C). |
| Pediatric use | Safety and efficacy not established in pediatric patients <18 years. |
| Geriatric use | No specific adjustment needed, but start at lower end of dosing range (400 mg once daily) due to potential renal impairment and increased sensitivity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TEVETEN (TEVETEN).
| Breastfeeding | Eprosartan is excreted in rat milk at concentrations approximately 2.4 times higher than maternal plasma. No data exist on its excretion in human breast milk. Due to the potential for adverse effects in nursing infants, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother. The M/P ratio in humans is unknown. |
| Teratogenic Risk | Drugs acting directly on the renin-angiotensin system (RAS) can cause fetal and neonatal morbidity and death when used in pregnancy. First-trimester exposure is associated with a low risk of congenital anomalies, but second- and third-trimester exposure is associated with oligohydramnios, fetal renal dysfunction, skull ossification defects, and neonatal hypotension, anuria, and renal failure. TEVETEN (eprosartan mesylate) is an angiotensin II receptor blocker, and its use is contraindicated in pregnancy, especially during the second and third trimesters. |
■ FDA Black Box Warning
None
| Serious Effects |
["Concomitant use with aliskiren in patients with diabetes mellitus (type 2) or moderate to severe renal impairment (eGFR <60 mL/min/1.73 m²)","Hypersensitivity to eprosartan or any component","Pregnancy (especially second and third trimesters)"]
| Precautions | ["Avoid use in pregnancy (fetal toxicity/neonatal morbidity/mortality)","Hypotension in volume-depleted patients (e.g., diuretic therapy, dialysis)","Hyperkalemia in patients with renal impairment or potassium-sparing diuretics/supplements","Acute renal failure in patients with bilateral renal artery stenosis or solitary kidney","Monitor renal function and serum potassium periodically"] |
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| Fetal Monitoring | Monitor maternal blood pressure and renal function. In cases of inadvertent fetal exposure, perform serial ultrasound examinations to assess amniotic fluid volume and fetal renal function. Monitor neonates for hypotension, oliguria, and hyperkalemia after birth. |
| Fertility Effects | No specific studies have been conducted on the effects of eprosartan on human fertility. In preclinical studies, there were no adverse effects on fertility in male and female rats at doses up to 1000 mg/kg/day (approximately 370 times the maximum recommended human dose on a mg/m² basis). |