Lisinopril converting enzyme

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. 

As angiotensin-converting enzyme inhibitors influence protein excretion in renal disease, Gansevoort et al. (G2) and Keilani et al. (K10) investigated serum Lp(a) concentrations in patients treated with Lisinopril resp. fosinopril and detected a reduction. 

Sources (1) Natesh R, Schwager SL, Sturrock ED, Acharya KR. Crystal structure of the human angiotensin-converting enzyme-lisinopril complex, Nature 421 551-554 (2003). Used with permission. (2) Turk B. Targeting proteases, successes, failures and future prospects. Nature Reviews Drug Discovery 5 785-799 (2006). 

Fig. 14. Active site (a) of the angiotensin converting enzyme (ACE) with Lisinopril inhibitor bound to zinc(II) (PDB-Code 1086) (101), (b) of the lethal factor of Bacillus anthracis (PDB-Code 1J7N) (103).

Zestril contains lisinopril, an angiotensin-converting enzyme inhibitor. Angiotensin-converting enzyme inhibitors tend to retain potassium, thereby counteracting the potassium loss caused by the thiazide diuretic bendroflumethiazide. 

Concomitant administration of methotrexate and Voltarol, a proprietary preparation of diclofenac, a non-steroidal anti-inflammatory drug, may result in accumulation of methotrexate as its excretion is reduced. The use of diclofenac and diuretics such as bendroflumethiazide may increase the risk of nephrotoxicity. Concomitant use of alcohol and an angiotensin-converting enzyme inhibitor such as lisinopril (Zestril) may result in an enhanced hypotensive effect. Alcohol and the benzodiazepine diazepam (Valium) may result in enhanced sedation. 

Lisinopril is an angiotensin-converting enzyme (ACE) inhibitor and ACE inhibitors should be avoided during pregnancy. ACE inhibitors may adversely affect fetal and neonatal blood pressure control and renal function. They may also cause neonatal skull defects. 

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

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. 

Angiotensin-converting enzyme (ACE) inhibitors, such as benazepril (Lotensin), enalapril (Vasotec), fosinopril (Monopril), lisinopril (Prinivil, Zestril), quinapril (Accupril), and ramipril (Altace). 

Packer M, Poole-Whson PA, Armstrong PW, Cleland JG, Horowitz JD, Massie BM, Ryden L, Thygesen K, Uretsky BF. Comparative effects of low and high doses of the angiotensin-converting enzyme inhibitor, lisinopril, on morbidity and mortality in chronic heart failure. ATLAS Study Group. Circulation 1999 100(23) 2312-18. 

Friedman DI, Amidon GL. Intestinal absorption mechanism of dipeptide angiotensin converting enzyme inhibitors of the lysyl-proline type lisinopril and SQ 29,852. J Pharm Sci 1989 78(12) 995-8. 

HJ Leis, G Fauler, G Raspotnig, W Windischhofer. Quantitative determination of the angiotensin-converting enzyme inhibitor lisinopril in human plasma by stable isotope dilution gas chromatography/negative ion chemical ionization mass spectrometry. Rapid Commun Mass Spectrom 12 1591—1594, 1998. 

Lisinopril is an angiotensin I-converting enzyme (ACE) inhibitor. It competitively inhibits ACE, prevents angiotensin I conversion to angiotensin II, and is a potent vasoconstrictor that also stimnlates aldosterone secretion. Results are a decrease in sodinm and fluid retention, a decrease in BP, and increase in dinresis. It is indicated in the treatment of hypertension treatment of heart failure not responding to dinretics and digitalis and treatment of acute MI within 24 honrs in hemodynamically stable patients. 

Lisinopril/hydrochlorothiazide is antihypertensive combination. Lisinopril competitively inhibits angiotensin I-converting enzyme and prevents angiotensin I conversion to angiotensin n, reversing the potassium loss associated with the diuretic. Hydrochlorothiazide increases chloride, sodium, and water excretion by interfering with transport of sodium ions across renal tubular epithehum. They are indicated in the treatment of hypertension. 

Wong, Y.-c. Charles, B.G. Determination of the angiotensin-converting enzyme inhibitor lisinopril in urine using solid-phase extraction and reversed-phase high-performance liquid chromatography. J.Chromatogr.B, 1995, 673, 306-310... 

Angiotensin-Converting Enzyme Inhibitors Six ACE inhihilots-captopril (Capoten), enalapril (VASOTEC), ramipril (altace), lisinopril (prinivil, zestril), quinapril (accupril), and/oi-inopril (monopril)—are currently EDA-approved for the treatment of heart failure. Data from... 

Angiotensin-converting enzyme inhibitor prototype used in HTN, diabetic nephropathy, and CHF. Tox hyperkalemia, fetal renal damage, cough ( sore throat ). Other prils benzepril, enalapril. lisinopril, quinapril. 

Lisinopril (Zestril) is an angiotensin-converting enzyme inhibitor used for the treatment of hypertension, alone or in combination with thiazide diuretics. Reported data are (Ritschel and Kearns, 2004) ... 

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