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Vasotec (ENALAPRILAT)
Vasotec (generic name: ENALAPRILAT) is a enalaprilat Small molecule drug developed by Biovail Labs Intl. It is currently FDA-approved (first approved 1988) for Asymptomatic left ventricular systolic dysfunction, Congestive heart failure, Hypertensive disorder.
Vasotec works by blocking the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor.
Vasotec (enalaprilat) is a small molecule drug developed by Biovail Labs Intl that targets the angiotensin-converting enzyme (ACE) to treat asymptomatic left ventricular systolic dysfunction, congestive heart failure, and hypertensive disorders. It was FDA approved in 1988 and is now off-patent with multiple generic manufacturers. Vasotec works by blocking the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor, thereby reducing blood pressure and improving heart function. The drug has a half-life of 39 hours and 40% bioavailability. It is no longer under patent protection.
At a glance
| Generic name | ENALAPRILAT |
|---|---|
| Sponsor | Biovail Labs Intl |
| Drug class | enalaprilat |
| Target | Angiotensin-converting enzyme |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | FDA-approved |
| First approval | 1988 |
Mechanism of action
Mechanism of Action. Intravenous enalaprilat, or oral enalapril, after hydrolysis to enalaprilat, inhibits ACE in human subjects and animals. ACE is peptidyl dipeptidase that catalyzes the conversion of angiotensin to the vasoconstrictor substance, angiotensin II. Angiotensin II also stimulates aldosterone secretion by the adrenal cortex. Inhibition of ACE results in decreased plasma angiotensin II, which leads to decreased vasopressor activity and to decreased aldosterone secretion. Although the latter decrease is small, it results in small increases of serum potassium. In hypertensive patients treated with enalapril alone for up to 48 weeks, mean increases in serum potassium of approximately 0.2 mEq/L were observed. In patients treated with enalapril plus thiazide diuretic, there was essentially no change in serum potassium. (See PRECAUTIONS.) Removal of angiotensin II negative feedback on renin secretion leads to increased plasma renin activity.ACE is identical to kininase, an enzym
Approved indications
- Asymptomatic left ventricular systolic dysfunction
- Congestive heart failure
- Hypertensive disorder
Boxed warnings
- USE IN PREGNANCY When used in pregnancy during the second and third trimesters, ACE inhibitors can cause injury and even death to the developing fetus. When pregnancy is detected, enalaprilat injection should be discontinued as soon as possible. See WARNINGS, Fetal/Neonatal Morbidity and Mortality .
Common side effects
- Hypotension
- Syncope
- Hyperkalemia
- Minor increases in blood urea nitrogen and serum creatinine
- Hemoglobin decrease
- Hematocrit decrease
- Anemia
- Neutropenia
- Thrombocytopenia
- Bone marrow depression
- Muscle cramps
- Vertigo
Key clinical trials
- Study of Hydroxychloroquine in Patients With X-linked Alport Syndrome in China (CHXLAS) (PHASE2)
- Mortality Control Program for Economically Productive Age Group in Tribal Area of Melghat. (PHASE4)
- Genetic Determinants of ACEI Prodrug Activation (PHASE4)
- The COVID-RASi Trial (COVID-19) (PHASE3)
- Nifedipine and Enalapril vs Nifedipine and Labetalol for the Treatment of Postpartum Hypertension Study (NA)
- Mineralocorticoid Receptor, Coronary Microvascular Function, and Cardiac Efficiency in Hypertension (PHASE4)
- Association of Angiotensin-Converting Enzyme Inhibitors and Angiotensin Receptor Blockers With Post-Stroke Pneumonia: A Real-World Retrospective Cohort Study
- Efficacy and Safety of Sacubitril/Valsartan Compared With Enalapril on Morbidity, Mortality, and NT-proBNP Change in Patients With CCC (PHASE4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Vasotec CI brief — competitive landscape report
- Vasotec updates RSS · CI watch RSS
- Biovail Labs Intl portfolio CI
Frequently asked questions about Vasotec
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Related
- Drug class: All enalaprilat drugs
- Target: All drugs targeting Angiotensin-converting enzyme
- Manufacturer: Biovail Labs Intl — full pipeline
- Therapeutic area: All drugs in Cardiovascular
- Indication: Drugs for Asymptomatic left ventricular systolic dysfunction
- Indication: Drugs for Congestive heart failure
- Indication: Drugs for Hypertensive disorder
Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing