TEVETEN HCT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TEVETEN HCT (TEVETEN HCT).
TEVETEN HCT combines eprosartan mesylate, an angiotensin II receptor antagonist, and hydrochlorothiazide, a thiazide diuretic. Eprosartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively antagonizing the AT1 receptor. Hydrochlorothiazide inhibits the sodium-chloride symporter in the distal convoluted tubule, increasing excretion of sodium, chloride, and water, thereby reducing plasma volume.
| Metabolism | Eprosartan is primarily metabolized by glucuronidation (UGTs) and is not significantly metabolized by CYP450 enzymes. Hydrochlorothiazide is not metabolized and is excreted unchanged in urine. |
| Excretion | Eprosartan: renal (70% unchanged, 10% as metabolite), biliary/fecal (20%); Hydrochlorothiazide: renal (≥95% unchanged). |
| Half-life | Eprosartan: 5-9 hours; Hydrochlorothiazide: 6-15 hours; allows once-daily dosing. |
| Protein binding | Eprosartan: 98% (albumin); Hydrochlorothiazide: 40-68% (albumin). |
| Volume of Distribution | Eprosartan: 0.15 L/kg (limited tissue distribution); Hydrochlorothiazide: 3-4 L/kg (wide distribution). |
| Bioavailability | Eprosartan: 13% (oral); Hydrochlorothiazide: 65-75% (oral). |
| Onset of Action | Eprosartan: 1-2 hours (oral); Hydrochlorothiazide: 2 hours (oral). |
| Duration of Action | Eprosartan: 24 hours; Hydrochlorothiazide: 6-12 hours; clinical effect persists 24 hours with combination. |
| Molecular Weight | 520.5 |
One tablet orally once daily, containing eprosartan 600 mg and hydrochlorothiazide 12.5 mg or 25 mg, with or without food. Maximum dose: eprosartan 600 mg/hydrochlorothiazide 25 mg per day.
| Dosage form | TABLET |
| Renal impairment | Contraindicated in severe renal impairment (CrCl <30 mL/min). For CrCl 30-60 mL/min, no dose adjustment required but use with caution. For CrCl <30 mL/min, not recommended. |
| Liver impairment | No specific dose adjustment for mild to moderate hepatic impairment (Child-Pugh A or B). Use with caution in severe hepatic impairment (Child-Pugh C); not studied. |
| Pediatric use | Safety and effectiveness in pediatric patients (<18 years) have not been established. Not recommended. |
| Geriatric use | Start with the lower dose (eprosartan 600 mg/hydrochlorothiazide 12.5 mg) due to increased risk of orthostatic hypotension, electrolyte imbalance, and renal impairment. Monitor renal function and electrolytes frequently. |
| 1st trimester | Contraindicated; risk of teratogenicity, including oligohydramnios and fetal renal dysfunction. |
| 2nd trimester | Contraindicated; exposure in second trimester associated with oligohydramnios, fetal hypotension, and renal failure. |
| 3rd trimester | Contraindicated; exposure in third trimester increases risk of neonatal hypotension, anuria, and hyperkalemia. |
Clinical note
Comprehensive clinical and safety monograph for TEVETEN HCT (TEVETEN HCT).
| Placental transfer | Both eprosartan and hydrochlorothiazide cross the placenta. Eprosartan crosses in limited amounts; hydrochlorothiazide readily crosses with measurable fetal concentrations. |
| Breastfeeding | Eprosartan is minimally excreted into breast milk (low relative infant dose), but hydrochlorothiazide may suppress lactation. Use with caution in breastfeeding women, especially when nursing preterm or jaundiced infants. |
■ FDA Black Box Warning
None
| Serious Effects |
AnuriaHypersensitivity to eprosartan or hydrochlorothiazidePregnancySevere renal impairment (CrCl <30 mL/min)History of angioedema with ARB
| Precautions | Fetal/neonatal morbidity and mortality when used in pregnancy (second and third trimesters), Hypotension in volume-depleted patients, Impaired renal function, including acute renal failure, Electrolyte imbalances (hyperkalemia, hyponatremia, hypomagnesemia, hypochloremic alkalosis), Exacerbation of renal impairment in bilateral renal artery stenosis, Sulfonamide allergy (hydrochlorothiazide is a sulfonamide derivative) |
| Food/Dietary | Avoid high-potassium foods (e.g., bananas, oranges, spinach, potatoes) if serum potassium is elevated or if taking potassium supplements. Avoid alcohol, which may increase orthostatic hypotension. Take with food to reduce gastric irritation. |
Loading safety data…
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | First trimester: Potential risk based on drugs acting on renin-angiotensin system (RAS); fetal renal development may be affected. Second and third trimesters: Known to cause fetal renal dysfunction, oligohydramnios, skull ossification defects, and neonatal hypotension. Contraindicated after first trimester. |
| Fetal Monitoring | Monitor maternal blood pressure, renal function, serum electrolytes, and urine output. Fetal ultrasound for amniotic fluid volume, renal anatomy, and growth. Neonatal assessment for hypotension, hyperkalemia, and renal function post-delivery if exposed in utero. |
| Fertility Effects | No data on fertility impact in humans. Animal studies with eprosartan show no effects on fertility. Hydrochlorothiazide has not been associated with fertility impairment. |
| Clinical Pearls | TEVETEN HCT contains eprosartan mesylate (an ARB) and hydrochlorothiazide (a thiazide diuretic). Onset of ARB component is delayed; full antihypertensive effect may take 2-4 weeks. Monitor serum potassium, especially in elderly, diabetics, or those on NSAIDs, potassium supplements, or potassium-sparing diuretics. Contraindicated in anuria, hypersensitivity to sulfonamide-derived drugs (hydrochlorothiazide), and pregnancy (Category D in second and third trimesters). |
| Patient Advice | Take exactly as prescribed, usually once daily, with or without food; try to take at the same time each day. · May cause dizziness or lightheadedness, especially during first few days; avoid driving until you know how it affects you. · Do not use salt substitutes containing potassium without consulting your doctor. · Stay hydrated, especially in hot weather or during exercise; notify your doctor if you experience excessive dehydration, vomiting, or diarrhea. · If you become pregnant or plan to become pregnant, stop taking this drug and contact your doctor immediately. · Do not stop taking this medication abruptly; it can cause a rapid increase in blood pressure. |