Enalapril converting enzyme

Folic acid deficiency Hyperthermia Phenylketonuria Rheumatic disease Virilizing tumors Drugs and chemicals Androgenic chemicals Angiotensin-converting enzyme inhibitors Captopril, enalapril Antibiotics... 

Angiotensm-converting enzyme (ACE) inhibitors— for example, captopril (Capoten), enalapril (Vasotec), and lismopril (Prinivil)... 

Captopril, enalapril Angiotensin converting enzyme Hypertension... 

Figure 3.4 Interactions of (A) substrate, (B) captopril, and (C) enalaprilate with the active site of angiotensin converting enzyme.

Enalaprilat and SQ27,519 are angiotensin-converting enzyme (ACE) inhibitors with poor oral absorption. Enalapril and fosinopril are dipeptide and amino acid derivatives of enalaprilat and SQ27,519, respectively [51] (Fig. 10). Both prodrugs are converted via deesterification to the active drug by hepatic biotransformation. In situ rat perfusion of enalapril indicated a nonpassive absorption mechanism via the small peptide carrier-mediated transport system. In contrast to the active parent, enalapril renders enalaprilat more peptide-like, with higher apparent affinity for the peptide carrier. The absorption of fosinopril was predominantly passive. Carrier-mediated transport was not demonstrated, but neither was its existence ruled out. 

DI Friedman, GL Amidon. Passive and carrier-mediated intestinal absorption components of two angiotensin converting enzyme (ACE) inhibitor prodrugs in rats Enalapril and fosinopril. Pharm Res 6(12) 1043-1047, 1989. 

Captopril 678 and enalapril 679 are potent angiotensin converting enzyme (ACE) inhibitors used as antihypertensives. Molecular manipulation based on the enzyme model led to the discovery of some perspective bicyclic structures, for example, cilazapril 680 and compound 681, highly active antihypertensives in vivo. Compound 681 belongs to the most potent conformationally restricted ACE inhibitors and is often used as a model for molecular modeling studies <1996JA8231>. 

Minsker, D., Bagdon, W., MacDonald, J., Robertson, R. and Bokelman, D. (1990). Matemo-toxicity and fetotoxicity of an angiotensin-converting enzyme inhibitor, enalapril, in rabbits. Fund. Appl. Toxicol. 14 461-479. 

Peptidyl-dipeptidase A (angiotensin-I converting enzyme, ACE, EC 3.4.15.1) plays a pivotal role in the control of blood pressure [80]. It has been established that its active site contains an essential Zn-atom that functions like that of carboxypeptidase A [2], ACE is inhibited by peptides having a proline or aromatic amino acid at the C-terminal position. These observations as well as the similarities with the active site of carboxypeptidase A have allowed a rational design of effective inhibitors of ACE (e.g., captopril (3.4) and enalapril (3.5)) used in the treatment of hypertension [81]. 

All angiotensin-converting enzyme inhibitors including enalapril, may precipitate a hypoglycaemic attack in a diabetic patient because they may potentiate the effect of sulphonylureas. 

Diclofenac is a non-steroidal anti-inflammatory drug. NSAIDs interact with both angiotensin-converting enzyme inhibitors, such as enalapril, and beta-adrenoceptor blockers, such as atenolol, resulting in antagonism to the hypotensive reaction, leading to a hypertensive reaction. NSAIDs interact with... 

Moreover, whether or not hypertension is caused by an elevated level of renin or other reasons, angiotensin-converting enzyme inhibitors lower both systolic and diastolic arterial pressure in hypertensive patients, and their effects are enhanced by diuretics. Angiotensin-converting drugs of this series (captopril, enalapril) are effective antihypertensive drugs used both independently and in combination with other drugs to treat all types of hypertension as well as to treat cardiac insufficiency. 

Like captopril, enalapril selectively suppresses the rennin-angiotensin-aldosterone system, inhibits angiotensin-converting enzyme, and prevents conversion of angiotensin I into angiotensin 11. 

Enalapril Angiotensin-converting enzyme 2 Chemical synthesis... 

P.K. Shiromani and J.F. Bavitz, Effect of moisture on the physical and chemical stability of granulations and tablets of the angiotensin converting enzyme inhibitor, enalapril maleate. Drug Dev. Ind. Pharm., 12 (1986) 2467. 

Angiotensin converting ENZYME (ACE) inhibitors captopril cilazapril enalapril maleate fosinopril sodium lisinopril... 

Enalapril maleate is an orally active angiotensin converting enzyme (ACE) inhibitor, it lowers peripheral vascular resistance without causing an increase in heart rate. The maleate salt (enalapril) allows better absorption after oral administration. It is an ideal drug for hypertensive patients who are intolerant to beta-blocker therapy. It also shows promise in the treatment of congestive heart failure. Following oral adminishation, enalapril is rapidly absorbed and hydrolysed to... 

Enalapril is an oral prodrug that is converted by hydrolysis to a converting enzyme inhibitor, enalaprilat, with effects similar to those of captopril. Enalaprilat itself is available only for intravenous use, primarily for hypertensive emergencies. Lisinopril is a lysine derivative of enalaprilat. Benazepril, fosinopril, moexipril, perindopril, quinapril, ramipril, and trandolapril are other long-acting members of the class. All are prodrugs, like enalapril, and are converted to the active agents by hydrolysis, primarily in the liver. 

Drug Class Angiotensin-converting enzyme [ACE] inhibitors Suffix -pril Common Examples Captopril, enalapril Primary Indication or Desired Effect (Chapter in Parentheses) Antihypertensive [21], congestive heart failure [24]... 

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