Enalaprilat

Intravenous enalaprilat, or oral enalapril, after hydrolysis to enalaprilat, inhibits ACE in human subjects and animals. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II.

• Enalaprilat injection is indicated for the treatment of hypertension when oral therapy is not practical. Enalaprilat injection has been studied with only one other antihypertensive agent, furosemide, which showed approximately additive effects on blood pressure.ICD-10: I10

• Enalaprilat injection is contraindicated in patients who are hypersensitive to any component of this product and in patients with a history of angioedema related to previous treatment with an angiotensin-converting enzyme inhibitor and in patients with hereditary or idiopathic angioedema.contraindicated

FOR INTRAVENOUS ADMINISTRATION ONLY The dose in hypertension is 1.25 mg every six hours administered intravenously over a five minute period. A clinical response is usually seen within 15 minutes. Peak effects after the first dose may not occur for up to four hours after dosing. The peak effects of the second and subsequent doses may exceed those of the first. No dosage regimen for enalaprilat injection has been clearly demonstrated to be more effective in treating hypertension than 1.25 mg every six hours. However, in controlled clinical studies in hypertension, doses as high as 5 mg every six hours were well tolerated for up to 36 hours. There has been inadequate experience with doses greater than 20 mg per day. In studies of patients with hypertension, enalaprilat has not been administered for periods longer than 48 hours. In other studies, patients have received enalaprilat for as long as seven days. The dose for patients being converted to enalaprilat injection from oral therapy for hypertension with enalapril maleate is 1.25 mg every six hours. For conversion from intravenous to oral therapy, the recommended initial dose of oral enalapril maleate, is 5 mg once a day with subsequent dosage adjustments as necessary. Patients On Diuretic Therapy For patients on diuretic therapy the recommended starting dose for hypertension is 0.625 mg administered intravenously over a five minute period; also see below, Patients at Risk of Excessive Hypotension. A clinical response is usually seen within 15 minutes.

Hypotension Excessive hypotension is rare in uncomplicated hypertensive patients but is a possible consequence of the use of enalaprilat especially in severely salt/volume depleted persons such as those treated vigorously with diuretics or patients on dialysis. Patients at risk for excessive hypotension, sometimes associated with oliguria and/or progressive azotemia, and rarely with acute renal failure and/or death, include those with the following conditions or characteristics: heart failure, hyponatremia, high dose diuretic therapy, recent intensive diuresis or increase in diuretic dose, renal dialysis, or severe volume and/or salt depletion of any etiology. It may be advisable to eliminate the diuretic, reduce the diuretic dose or increase salt intake cautiously before initiating therapy with enalaprilat injection in patients at risk for excessive hypotension who are able to tolerate such adjustments (see PRECAUTIONS, Drug Interactions ; ADVERSE REACTIONS , and DOSAGE AND ADMINISTRATION ). In patients with heart failure, with or without associated renal insufficiency, excessive hypotension has been observed and may be associated with oliguria and/or progressive azotemia, and rarely with acute renal failure and/or death. Because of the potential for an excessive fall in blood pressure especially in these patients, therapy should be followed closely whenever the dose of enalaprilat is adjusted and/or diuretic is increased.

Enalaprilat has been found to be generally well tolerated in controlled clinical trials involving 349 patients (168 with hypertension, 153 with congestive heart failure and 28 with coronary artery disease). The most frequent clinically significant adverse experience was hypotension (3.4 percent), occurring in eight patients (5.2 percent) with congestive heart failure, three (1.8 percent) with hypertension and one with coronary artery disease. Other adverse experiences occurring in greater than one percent of patients were: headache (2.9 percent) and nausea (1.1 percent). Adverse experiences occurring in 0.5 to 1 percent of patients in controlled clinical trials included: myocardial infarction, fatigue, dizziness, fever, rash and constipation. Angioedema : Angioedema has been reported in patients receiving enalaprilat, with an incidence higher in black than in non-black patients. Angioedema associated with laryngeal edema may be fatal. If angioedema of the face, extremities, lips, tongue, glottis and/or larynx occurs, treatment with enalaprilat should be discontinued and appropriate therapy instituted immediately (see WARNINGS ). Cough: See PRECAUTIONS, Cough . Enalapril Maleate Since enalapril is converted to enalaprilat, those adverse experiences associated with enalapril might also be expected to occur with enalaprilat injection. The following adverse experiences have been reported with enalapril and, within each category, are listed in order of decreasing severity.

Pregnancy Pregnancy Categories C (first trimester) and D (second and third trimesters) See WARNINGS, Fetal/Neonatal Morbidity and Mortality.

Metabolism

and Metabolism Following intravenous administration of a single dose, the serum concentration profile of enalaprilat is polyexponential with a prolonged terminal phase, apparently representing a small fraction of the administered dose that has been bound to ACE. The amount bound does not increase with dose, indicating a saturable site of binding.

In clinical studies, some hypertensive patients received a maximum dose of 80 mg of enalaprilat intravenously over a fifteen minute period. At this high dose, no adverse effects beyond those as associated with the recommended dosages were observed. A single intravenous dose of ≤4,167 mg/kg of enalaprilat was associated with lethality in female mice. No lethality occurred after an intravenous dose of 3,472 mg/kg. The most likely manifestation of overdosage would be hypotension, for which the usual treatment would be intravenous infusion of normal saline solution. Enalaprilat may be removed from general circulation by hemodialysis and has been removed from neonatal circulation by peritoneal dialysis (see WARNINGS, Anaphylactoid reactions during membrane exposure ).

• Aug 22, 2000ANDAANDA075578Dr Reddys
• Dec 23, 2008ANDAANDA078687Hikma Farmaceutica

1. 1Heart Rate Decreased197.7%
2. 2Blood Pressure Systolic Abnormal187.3%
3. 3Blood Pressure Systolic Increased187.3%
4. 4Joint Swelling187.3%
5. 5Oxygen Saturation Decreased187.3%
6. 6Blood Pressure Diastolic Decreased176.9%
7. 7Nausea176.9%
8. 8Fall156.1%
9. 9Hypertension156.1%
10. 10Drug Hypersensitivity145.7%
11. 11Intestinal Perforation145.7%
12. 12Angioedema135.3%
13. 13Arthralgia135.3%
14. 14Dyspnoea135.3%
15. 15Acute Kidney Injury124.9%

Recent PubMed references pinned to Enalaprilat as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• A green HPLC-UV method for the simultaneous analysis of enalapril, enalaprilat and diketopiperazine in pharmaceutical formulations.
  Analytical methods : advancing methods and applications · 2025 · Fracetti MM, Chellini PR, de Oliveira MAL, et al.
  PMID 41186323DOI 10.1039/d5ay01199j
• Population Pharmacokinetic Analysis of Enalapril and Enalaprilat in Newly Treated Children with Heart Failure: Implications for Safe Dosing of Enalapril (LENA Studies).
  Clinical pharmacokinetics · 2025 · Steichert M, Cawello W, Laeer S, et al.
  PMID 40461938DOI 10.1007/s40262-025-01520-5
• Target Reserve and Turnover Parameters Determine Rightward Shift of Enalaprilat Potency From its Binding Affinity to the Angiotensin Converting Enzyme.
  Journal of pharmaceutical sciences · 2024 · Nguyen VA, Zhang L, Kagan L, et al.
  PMID 37871777DOI 10.1016/j.xphs.2023.10.025
• Cardiopulmonary Actions of Intravenously Administered Enalaprilat in Trauma Patients: Retraction.
  Critical care medicine · 2023
  PMID 37589532DOI 10.1097/CCM.0000000000005907
• Enalaprilat as a new means of preventing the development of retinopathy of prematurity.
  Biomeditsinskaia khimiia · 2023 · Katargina LA, Chesnokova NB, Pavlenko TA, et al.
  PMID 37132491DOI 10.18097/PBMC20236902097
• The Influence of Structural Variants of the CES1 Gene on the Pharmacokinetics of Enalapril, Presumably Due to Linkage Disequilibrium with the Intronic rs2244613.
  Genes · 2022 · Ikonnikova A, Kazakov R, Rodina T, et al.
  PMID 36553492DOI 10.3390/genes13122225
• Lack of an Effect of Polysorbate 80 on Intestinal Drug Permeability in Humans.
  Pharmaceutical research · 2022 · Metry M, Krug SA, Karra VK, et al.
  PMID 35672541DOI 10.1007/s11095-022-03312-z
• Effects of soluble guanylate cyclase stimulator on renal function in ZSF-1 model of diabetic nephropathy.
  PloS one · 2022 · Hu L, Chen Y, Zhou X, et al.
  PMID 35085251DOI 10.1371/journal.pone.0261000

The 10 most recently updated of 177 ClinicalTrials.gov registrations naming Enalaprilat as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Treating Metabolic Acidosis in Chronic Kidney Disease to Prevent Adverse Kidney and Cardiovascular Outcomes
  Completed · Interventional · 108 enrolled · Donald Wesson
  NCT06545461updated 2026-06-12
• Nifedipine and Enalapril vs Nifedipine and Labetalol for the Treatment of Postpartum Hypertension Study
  Recruiting · Interventional · 200 enrolled · The Cleveland Clinic
  NCT07363343updated 2026-06-12
• Efficacy and Safety of Sacubitril/Valsartan Compared With Enalapril on Morbidity, Mortality, and NT-proBNP Change in Patients With CCC
  Completed · Phase 4 · Interventional · 922 enrolled · Novartis Pharmaceuticals
  NCT04023227updated 2026-05-11
• Rapid and Simultaneous Initiation of Four Guideline-Directed CKD Therapies (RAPID-CKD)
  Not yet recruiting · Phase 4 · Interventional · 64 enrolled · Baylor Research Institute
  NCT07547878updated 2026-05-08
• Impact of Medically Supervised Performance-Enhancing Substances (PES) on Elite Athletes
  Enrolling by invitation · Interventional · 60 enrolled · Enhanced Emirates Limited
  NCT07568574updated 2026-05-06
• The Assessment of Partial Guideline-Directed Medical Therapy Down Titration in Heart Failure in Remission.
  Recruiting · Phase 4 · Interventional · 100 enrolled · Ziekenhuis Oost-Limburg
  NCT07513883updated 2026-04-07
• Mineralocorticoid Receptor, Coronary Microvascular Function, and Cardiac Efficiency in Hypertension
  Recruiting · Phase 4 · Interventional · 75 enrolled · Brigham and Women's Hospital
  NCT05593055updated 2026-04-06
• Study of Hydroxychloroquine in Patients With X-linked Alport Syndrome in China (CHXLAS)
  Completed · Phase 2 · Interventional · 50 enrolled · Shanghai Children's Hospital
  NCT04937907updated 2026-03-02
• Mortality Control Program for Economically Productive Age Group in Tribal Area of Melghat.
  Completed · Phase 4 · Interventional · 72,564 enrolled · MAHAN Trust
  NCT07436104updated 2026-02-27
• Genetic Determinants of ACEI Prodrug Activation
  Completed · Phase 4 · Interventional · 21 enrolled · University of Michigan
  NCT03051282updated 2026-02-18

Frequently asked questions

How does Enalaprilat work?

Intravenous enalaprilat, or oral enalapril, after hydrolysis to enalaprilat, inhibits ACE in human subjects and animals. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II.

What is Enalaprilat used for?

According to FDA labeling, Enalaprilat carries indications including: Enalaprilat injection is indicated for the treatment of hypertension when oral therapy is not practical. Enalaprilat injection has been studied with only one other antihypertensive agent, furosemide, which showed approximately additive effects on blood pressure.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Enalaprilat?

Enalaprilat is classified as Angiotensin-converting Enzyme Inhibitors, Decreased Blood Pressure, Decreased Bradykinin Degradation, Decreased Intravascular Volume, Decreased Mineralocorticoid Secretion, Decreased Renal K+ Excretion, Increased Renal Na+ Excretion, Renal Arterial Vasodilation.

What are the contraindications for Enalaprilat?

Enalaprilat labeling lists contraindications including: Enalaprilat injection is contraindicated in patients who are hypersensitive to any component of this product and in patients with a history of angioedema related to previous treatment with an angiotensin-converting enzyme inhibitor and in patients with hereditary or idiopathic angioedema.. Always consult the full prescribing information and a clinician.