Captopril converting enzyme inhibitors

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

Most ACE inhibitors are prodrugs, with the exceptions of captopril, lisinopril, and ceranapril. Prodrugs exert improved oral bioavailability, but need to be converted to active compounds in the liver, kidney, and/or intestinal tract. In effect, converting enzyme inhibitors have quite different kinetic profiles with regard to half time, onset and duration of action, or tissue penetration. 

The answer is b. (1 Iardman, pp 750-751) Angiotensin converting enzyme inhibitors, especially captopril, can cause alteration or loss of taste sensation... 

Captopril by decreasing heart rate and contraction Angiotensin converting enzyme inhibitor, decreases arterial... 

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. 

Captopril enhances cardiac output in patients with congestive heart failure by inducing a reduction in ventricular afterload and preload. Converting enzyme inhibitors have been shown to decrease the mass and wall... 

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. 

Peptides with C-terminal phosphonates, initially reported to have antibacterial properties, have also been found to possess inhibitory properties toward serine proteases)28 The synthesis of peptide phosphonates (Section 15.1.8) usually requires protection of the phos-phonic moiety as a diester, followed by selective deprotection in the final stage. The importance of peptide thiols (Section 15.1.9) is exemplified by captopril, an orally active angiotensin converting enzyme inhibitor used as a treatment for hypertension)29 These peptide thiols are prepared by the reaction of sulfanylalkanoyl amino acids with a-amino esters followed by deprotection of carboxy and sulfanyl groups. Other peptide thiols have been reported to be inhibitors of zinc metalloproteases, collagenases, and aminopeptidases. 

Parenteral 40, 80, 160 mg/mL for IV injection 80, 160, 320 mg/dL in 5% dextrose for IV infusion Angiotensin-Converting Enzyme Inhibitors Labeled for Use in Congestive Heart Failure Captopril (generic, Capoten)... 

Angiotensin peptides - the angiotensin converting enzyme inhibitor (ACE), captopril, has anxiolytic activity in both experimental and clinical studies. It has recently been shown that the angiotensin 1 receptor antagonist, losartin, has anxiolytic properties whereas the angiotensin 2 antagonists are inactive. 

Clinical effects Angiotensin-converting enzyme inhibitors improve symptoms, New York Heart Association (NYHA) functional class, and exercise capacity in patients with HF The Captopril Multicenter Research Group (6) showed that captopril treatment improved the NYHA class in 61% of patients compared with only 24% of patients taking placebo over a 12-week period, Treadmill exercise time improved throughout the 12 weeks of the study in 24% of captopril-treated patients, but in none of the placebo-treated patients. 

Human PepTl was initially cloned from intestine (92) and was found to be localized to the brush border of intestinal epithelial cells (93) and in SI segment of apical proximal tubules (94). PepTl transports (3-lactam antibiotics (95), antiviral drugs such as valacyclovir and valganciclovir (96), and the angiotensin converting enzyme inhibitor captopril (97). Polymorphisms have been reported, however little is known regarding their functional consequences (64). 

Pandey S, Anand-Srivastava MB. 1996. Modulation of G-protein expression by the angiotensin converting enzyme inhibitor captopril in hearts from spontaneously hypertensive rats relationship with adenylyl cyclase. Am J Hypertens 9 833-837. 

Today, captopril (Capoten ) ranks among the most frequently used drugs in the treatment of hypertension. Enalapril (Xanef ) has been commercially available since 1985 as a second ACE inhibitor. The discovery of captopril started an avalanche of research into the synthesis of angiotensin-converting enzyme inhibitors. Some new developments should be mentioned at this point ... 

It is advisable to avoid using certain drugs in patients with advanced liver disease. For example, angiotensin-converting enzyme inhibitors and nonsteroidal anti-inflammatory drugs should be avoided because of their potential to cause acute renal failure. Paradoxically, administration of captopril... 

An increased risk of severe and early but reversible neutropenia has been found in patients taking angiotensin-converting enzyme inhibitors (enalapril and captopril) with interferon alfa (404). 

Case, D. B., Atlas, S. A., Laragh, J. H., Sealey, J. E., Sullivan, P. A., McKinstry, D. N. Clinical experience with blockade of the renin-angi-otensin-aldosterone system by an oral converting-enzyme inhibitor (SQ 14,225, captopril) in hypertensive patients. Prog. Cardiovasc. Dis. 1978,21,195-206. 

Angiotensin-converting enzyme inhibitors (captopril and derivatives)... 

Rostoker G, Maadi AB, Remy P, et al. Low-dose angiotensin-converting-enzyme inhibitor captopril to reduce proteinuria in adult idiopathic membranous nephropathy A prospective study of long-term treatment. Nephrol Dial Transplant 1995 10 25-29. 

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