TEVETEN
Clinical safety rating
cautionComprehensive 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. |
| Molecular Weight | 404.46 |
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 | Teratogenic effects in animal studies; avoid in first trimester due to potential fetal renal toxicity and oligohydramnios. |
| 2nd trimester | Contraindicated in second trimester due to risk of fetal renal dysfunction, oligohydramnios, and skull ossification defects. |
| 3rd trimester | Contraindicated in third trimester due to high risk of fetal and neonatal morbidity, including renal failure, hypotension, and death. |
Clinical note
Comprehensive clinical and safety monograph for TEVETEN (TEVETEN).
| Placental transfer | Crosses placenta; detected in fetal circulation. Risks of oligohydramnios and fetal renal impairment increase with gestational age. |
| Breastfeeding | Excretion into human milk unknown; avoid breastfeeding due to potential adverse effects on infant renal function. Consider alternative antihypertensives. |
| Lactation Rating | L5 (Contraindicated) or 'Avoid'. |
| 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. |
| 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). |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to eprosartan or any componentConcomitant use with aliskiren in diabetic patientsPregnancy (second and third trimester)History of angioedema with ACE inhibitors (caution)Severe renal impairment (eGFR < 30 mL/min/1.73 m²) not on dialysis
| 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 |
| Food/Dietary | No specific food interactions. Avoid excessive potassium intake (e.g., potassium-rich foods like bananas, oranges, tomatoes, spinach) as TEVETEN may increase serum potassium. No restrictions with alcohol, but limit intake as it may lower blood pressure and increase side effects. Grapefruit juice has no known interaction. |
| Clinical Pearls | TEVETEN (eprosartan mesylate) is an angiotensin II receptor blocker (ARB) with a high affinity for the AT1 receptor. It has a dose-dependent antihypertensive effect. Avoid use in pregnancy; discontinue as soon as pregnancy is detected. Monitor renal function and serum potassium in patients with renal impairment, diabetes, or those on potassium-sparing diuretics. May cause angioedema, though rare. Use with caution in patients with unilateral or bilateral renal artery stenosis due to risk of acute renal failure. |
| Patient Advice | Take TEVETEN exactly as prescribed, usually once daily, with or without food. · Do not stop taking this medication without consulting your doctor, as it may worsen your condition. · Avoid becoming pregnant while on TEVETEN; use effective contraception and inform your doctor immediately if you think you are pregnant. · Report any signs of angioedema (swelling of face, lips, throat, difficulty breathing) or fainting to your doctor immediately. · Inform all healthcare providers that you are taking TEVETEN, especially before surgery or any procedure requiring anesthesia. · Stay hydrated, but do not use potassium supplements or salt substitutes containing potassium without medical advice. · Monitor your blood pressure regularly as directed and keep a log to share with your doctor. |
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