EPROSARTAN

Fetal Risk Summary

Eprosartan is a selective angiotensin II receptor antagonist that is used, either alone or in combination with other antihypertensive agents, for the treatment of hypertension. Eprosartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by preventing angiotensin II from binding to AT1 receptors.

Reproduction studies have been conducted in rats and rabbits (1). No teratogenic effects were observed in either species, but dose-related toxicity occurred in pregnant rabbits. In pregnant rats, no adverse effects on the fetus or on the postnatal development and maturation of offspring were observed at oral doses up to approximately 0.6 times the human exposure (based on area under the plasma concentration curve) at the maximum recommended human dose or 800 mg/day (MRHD). Similarly, a dose approximately 0.8 times the MRHD did not result in fetal or maternal toxicity in pregnant rabbits. Increasing the dose to approximately 2.7 times the MRHD in pregnant rabbits, however, caused both maternal (reduced body weight, decreased food consumption, and death) and embryo/fetal (resorptions, abortions, and litter loss) toxicity (1).

It is not known if eprosartan crosses the human placenta. The molecular weight (about 521) is low enough that passage to the fetus should be expected.

No reports describing the use of eprosartan during human pregnancy have been located. The antihypertensive mechanisms of action of eprosartan and angiotensin converting enzyme (ACE) inhibitors are very close. That is, the former selectively blocks the binding of angiotensin II to AT1 receptors, whereas the latter blocks the formation of angiotensin II itself. Therefore, use of this drug during the 2nd and 3rd trimesters may cause teratogenicity and severe fetal and neonatal toxicity that is identical to that seen with ACE inhibitors (e.g., see Captopril or Enalapril). Fetal toxic effects may include anuria, oligohydramnios, fetal hypocalvaria, intrauterine growth retardation, prematurity, and patent ductus arteriosus. Anuria-associated oligohydramnios may produce fetal limb contractures, craniofacial deformation, and pulmonary hypoplasia. Severe anuria and hypotension, that is resistant to both pressor agents and volume expansion, may occur in the newborn following in utero exposure to eprosartan. Newborn renal function and blood pressure should be closely monitored.

[*Risk factor DM if used in 2nd or 3rd trimesters.]

Breast Feeding Summary

No reports describing the use of eprosartan during human lactation have been located. The drug is excreted into animal milk (1). The molecular weight (about 521) is low enough that excretion into breast milk should also be expected. The effects of this exposure on a nursing infant are unknown. The American Academy of Pediatrics, however, considers ACE inhibitors, a closely related group of antihypertensive agents, to be compatible with breast feeding (see Captopril and Enalapril).

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