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eprosartan (Teveten)

 

Classes: ARBs

Dosing and uses of Teveten (eprosartan)

 

Adult dosage forms and strengths

tablet

  • 400mg
  • 600mg

 

Hypertension

Initial: 600 mg PO qDay, in patients without intravascular volume depletion

Maintenance: 400-800 mg/day PO qDay OR divided q12hr PO (twice daily may improve effect)

See also combo with hydrochlorothiazide (Teveten HCT)

Generally adjust qMonth; more aggressively in high-risk patients

 

Renal Impairment

Dose adjustment not necessary; carefully monitor patient; not to exceed 600 mg/day

 

Hepatic Impairment

Dose adjustment not necessary; carefully monitor patient; not to exceed 600 mg/day

 

Additional Information

Similar dosing has been used in diabetic nephropathy, and CHF

 

Pediatric dosage forms and strengths

Safety and efficacy not established

 

Geriatric dosage forms and strengths

 

Hypertension

Initial: 600 mg PO qDay, in patients without intravascular volume depletion

Maintenance: 400-800 mg/day PO qDay OR divided q12hr PO (twice daily may improve effect)

See also combo with hydrochlorothiazide (Teveten HCT)

Generally adjust qMonth; more aggressively in high-risk patients

 

Teveten (eprosartan) adverse (side) effects

1-10%

Upper respiratory infection (8%)

Cough (4%)

Abdominal pain (2%)

Fatigue (2%)

 

Frequency not defined

Facial edema

Dizziness

Headache

Neutropenia

Back pain

Myalgia

 

Warnings

Black box warnings

Discontinue as soon as possible when pregnancy is detected; affects renin-angiotensin system causing oligohydramnios, which may result in fetal injury and/or death

 

Contraindications

Hypersensitivity

Pregnancy (2nd/3rd trimesters): significant risk of fetal/neonatal morbidity and mortality

Bilateral renal artery stenosis

Do not coadminister with aliskiren in patients with diabetes

 

Cautions

Angioedema, hypovolemia, hyperkalemia, surgery, and anesthesia

Discontinue STAT if pregnant: potential risk of congenital malformations (see Contraindications and Black box warnings)

Risk of hypotension, especially if hypovolemic/hyponatremic, or on concomitant diuretics or dialysis

Dual blockade of the renin angiotensin system with ARBs, ACE inhibitors, or aliskiren associated with increased risk for hypotension, hyperkalemia, and renal function changes (including acute renal failure) compared to monotherapy

Risk of anaphylactoid reactions and/or angioedema

Increased risk of renal dysfunction with CHF

Renal/hepatic impairment

 

Pregnancy and lactation

Pregnancy category: C (1st trimester); D (2nd & 3rd trimesters). During the second and third trimesters of pregnancy, these drugs have been associated with fetal injury that includes hypotension, neonatal skull hypoplasia, anuria, reversible or irreversible renal failure, and death

Lactation: excretion in milk unknown/not recommended

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Teveten (eprosartan)

Mechanism of action

Angiotensin II blocker; displaces angiotensin II from AT1 receptor and may lower blood pressure by antagonizing AT1-induced vasoconstriction, aldosterone release, catecholamine release, arginine vasopressin release, water absorption, and hypertrophic responses

May induce more complete inhibition of renin-angiotensin system compared with ACE inhibitors; does not affect response to bradykinin

Inhibits the pressor effects of an angiotensin II infusion in a dose-related manner

 

Pharmacokinetics

Half-Life: 5-9 hr

Onset: 4 hr

Peak Plasma Time: 4 hr

Bioavailability: 13%, food & age increases absorption

Protein Bound: 98%

Vd: 3.8 L

Metabolism: Partially conjugated with glucuronic acid in liver

Metabolites: Acyl glucuronide metabolite (inactive)

Excretion: Feces (90%), urine (7%)

Clearance

  • Total Body: 48.5 L/hr
  • Renal: 39-45 mL/min