Benazepril HCl

Benazepril hydrochloride, an angiotensin converting enzyme inhibitor, which is a medication used to treat high blood pressure.

A randomized, double-blind trial comparing the effects of amlodipine besylate/benazepril HCl vs amlodipine on endothelial function and blood pressure.[Pubmed:17028482]

J Clin Hypertens (Greenwich). 2006 Oct;8(10):692-8.

Evidence suggests that renin-angiotensin-aldosterone system inhibition ameliorates endothelial dysfunction. The authors examined the effect of amlodipine besylate/Benazepril HCl combination treatment compared with amlodipine besylate monotherapy in modulating endothelial dysfunction. This multicenter, double-blind, 12-week study randomized 70 hypertensive subjects with at least one other endothelial dysfunction risk factor to amlodipine besylate/Benazepril HCl (5/20 mg/d force-titrated to 5/40 mg/d) or amlodipine besylate monotherapy (5 mg/d force-titrated to 10 mg/d). Both the combination and monotherapy produced significant median increases from baseline in percentage flow-mediated vasodilation (2.0% and 1.2%, respectively) and percentage change in percent flow-mediated vasodilation (25% and 16%, respectively). These improvements were numerically larger with combination treatment, but between-group differences did not achieve statistical significance. Reductions in systolic and diastolic blood pressure were significantly greater (P=.0452/P=.0297) with combination treatment (-18.6/-12.3 mm Hg) than with monotherapy (-14.8/-9.1 mm Hg). A highly positive correlation between change in systolic blood pressure and change in percent of flow-mediated vasodilation was demonstrated only for combination treatment.

Formal synthesis of the ACE inhibitor benazepril x HCl via an asymmetric aza-Michael reaction.[Pubmed:17971736]

Molecules. 2006 Aug 23;11(8):641-8.

A formal enantioselective synthesis of benazepril.HCl (4), an anti- hypertensive drug, is reported. Our synthesis employed an asymmetric aza-Michael addition of L-homophenylalanine ethyl ester (LHPE, 1) to 4-(2-nitrophenyl)-4-oxo- but-2-enoic acid methyl ester (6) as the key step to prepare (2S,3'S)-2-(2-oxo-2,3,4,5- tetrahydro-1H-benzo[b]azepin-3-ylamino)-4-phenylbutyric acid ethyl ester (8), which is the key intermediate leading to benazepril x HCl (4).

Adherence to antihypertensive therapy with fixed-dose amlodipine besylate/benazepril HCl versus comparable component-based therapy.[Pubmed:14688505]

Congest Heart Fail. 2003 Nov-Dec;9(6):324-32.

Adhering to medication regimens has the potential to significantly improve clinical outcomes for persons with high blood pressure. A patient-related factor likely to affect adherence to treatment is the convenience of the prescribed drug regimen. The authors hypothesized that medication adherence would be superior and cost benefits would accrue in subjects who receive a once-daily, single-capsule, fixed-dose combination product for blood pressure control, compared with subjects who receive a similar regimen of separate components. A managed care organization that provides benefits for members enrolled in various health plans provided the data for this retrospective analysis. The database was used to assess medication adherence patterns for two groups of hypertensive subjects. Group 1 included subjects who had been prescribed the single-capsule, fixed-dose combination of amlodipine besylate/Benazepril HCl. Group 2 comprised subjects who had been prescribed a regimen including an angiotensin-converting enzyme inhibitor and a dihydropyridine calcium channel blocker as separate drugs. Adherence was measured by the medication possession ratio, and medical resource utilization by the two groups was assessed during the study period. Group 1 (n=2754) and Group 2 (n=2978) were balanced with regard to age (mean, 53 years; range, 18-64 years) and sex (men, 50%; women, 50%). The overall medication possession ratio for Group 1 was significantly higher than that for Group 2 (80.8% vs. 73.8%; p<0.001). The average annual cost of cardiovascular-related care per subject was significantly lower in Group 1 compared with Group 2 (p<0.001). Subjects receiving the once-daily, single-capsule, fixed-dose combination of amlodipine/Benazepril HCl demonstrated significantly better medication adherence and required fewer medical resources than did subjects receiving an angiotensin-converting enzyme inhibitor and a dihydropyridine calcium channel blocker as separate components.

Kinetics of the acidic and enzymatic hydrolysis of benazepril HCl studied by LC.[Pubmed:11682216]

J Pharm Biomed Anal. 2002 Jan 1;27(1-2):107-16.

A reversed-phase high-performance liquid chromatographic (HPLC) method was developed and validated for the kinetic investigation of the chemical and enzymatic hydrolysis of benazepril hydrochloride. Kinetic studies on the acidic hydrolysis of benazepril hydrochloride were carried out in 0.1 M hydrochloric acid solution at 50, 53, 58 and 63 degrees C. Benazepril hydrochloride appeared stable in a pH 7.4 phosphate buffered solution at 37 degrees C and showed susceptibility to undergoing in vitro enzymatic hydrolysis with porcine liver esterase (PLE) in a pH 7.4 buffered solution at 37 degrees C. Benazeprilat appeared to be the major degradation product in both (chemical and enzymatic) studies of hydrolysis. Statistical evaluation of the proposed HPLC methods revealed their good linearity and reproducibility. Relative standard deviation (R.S.D.) was less than 4.76, while detection limits for benazepril hydrochloride and benazeprilat were 13.0 x 10(-7) and 9.0 x 10(-7) M, respectively. Treatment of the kinetic data of the acidic hydrolysis was carried out by non-linear regression analysis and k values were determined. The kinetic parameters of the enzymatic hydrolysis were determined by non-linear regression analysis of the data using the equation of Michaelis-Menten.