Enalapril, after hydrolysis to enalaprilat, inhibits angiotensin-converting enzyme (ACE) in human subjects and animals. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II. Angiotensin II also stimulates aldosterone secretion by the...
The mean percentage conversion of enalapril to enalaprilat ranged from 64.7% for children ages 1 to 24 months to 74.6% for children ages 6 to < 12 years. The median effective half-life for accumulation ranged from 14.6 hours in children ages 12 to < 16 years to 16.3 hours in children ...
inhibitor. The compound has been used to study diabetic angiopathy in diabetic rats and inhibition of ACE in hog plasma (I50=1.2nM). ACE inhibitors disturb the enin-angiotensin- aldosterone system. Additional ACE inhibitors include: Enalapril, Enalaprilat dihydrate, Enalaprilat , and Enalapril-d5 Ma...
Enalapril (MK-421) is a prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications. It is rapidly metabolized in the liver to enalaprilat following oral administration. Enalapril (MK-421) is a potent, competitive inhibitor of ACE, the enzyme responsible for the...
Enalaprilat: Injection: 1.25 mg/mL (1, 2 mL); containsbenzyl alcohol Hypertension: Infant and child: PO:0.08 mg/kg/24 hr up to 5 mg/24 hr once daily; increase PRN over 2 wk. Max. dose (higher doses have not been evaluated): 0.58 mg/kg/24 hr up to 40 mg/24 hr ...
enalaprilat Vasotec IV Pharmacologic class: Angiotensin-converting enzyme (ACE) inhibitor Therapeutic class: Antihypertensive Pregnancy risk category C (first trimester), D (second and third trimesters) FDA Box Warning • When used during second or third trimester of pregnancy, drug can cause fetal...
It is rapidly metabolized in the liver to enalaprilat following oral administration. Enalapril (MK-421) is a potent, competitive inhibitor of ACE, the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of...
4]. It acts as a competitive inhibitor for ACE preventing conversion of angiotensin I to angiotensin II which acts as a vasoconstrictor material and stimulates the secretion of aldosterone. The binding of the enalaprilat to the enzyme forms a complex with slow dissociation rate which leads to ...
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The steady-state intestinal extraction ratio of enalapril was small (0.04 +/- 0.066) compared to that for the liver (0.74 +/- 0.06), indicating that the liver was responsible for most of the hydrolytic conversion of enalapril to its pharmacologically active diacid metabolite, enalaprilat. More...