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Experimental glomerulonephritis results in hypertension that is sensitive to salt. Nevertheless, salt retention alone cannot explain the increase in blood pressure. Angiotensin antagonistic therapy reduces hypertension caused by puromycin amino nucleosides (PAN). We investigated the hypothesis that PAN modifies renal vascular reactivity through processes dependent on angiotensin. Long-Evans rats were given an intraperitoneal injection of either puromycin (150 mg/kg) or saline (controls). Group 1 was fed a normal sodium diet (NSD, n = 9). Group 2 was given 30 mg/L of quinapril (Q) in addition to NSD (NSD + Q; n = 6). Group 3 received a high sodium diet (HSD, n = 7), and Group 4 received HSD + Q (n = 7). Systolic blood pressure (SBP), plasma creatinine, proteinuria, and sodium balance were monitored for 12 days. On day 15, renal vascular reactivity was assessed by administering increasing doses of angiotensin II, acetylcholine (ACh), and sodium nitroprusside (SNP) directly into the renal artery. SBP progressively increased in all PAN groups. This increase in SBP was greater in the HSD groups and was not significantly altered by Q treatment. SBP increased by 22 ± 4% (NSD), 51 ± 5% (NSD + Q), 81 ± 10% (HSD), and 65 ± 8% (HSD + Q). The renal blood flow of PAN rats did not return to baseline despite their normal renal vasoconstrictor responses to angiotensin II. Additionally, they showed reduced renal vasodilator responses to SNP and Ach. The vasodilator responses to both vasodilators were surprisingly unaffected by the inhibition of the angiotensin-converting enzyme (ACE). Renal vasodilator responses to both endothelium-dependent and independent variables were reduced in early PAN-induced hypertension. We found that the angiotensin-mediated mechanism is not responsible for this altered renal vasoreactivity. [ABSTRACT FROM AUTHOR]

The study presents an approach for formulation of 3D printed fast dissolving tablets using binder jetting technology. [Display omitted] Increasing access to additive manufacturing technologies utilising easily available desktop devices opened novel ways for formulation of personalized medicines. It is, however, challenging to propose a flexible and robust formulation platform which can be used for fabrication of tailored solid dosage forms composed of APIs with different properties (e.g., hydrophobicity) without extensive optimization. This manuscript presents a strategy for formulation of fast dissolving tablets using binder jetting (BJ) technology. The approach is demonstrated using two model APIs: hydrophilic quinapril hydrochloride (QHCl, logP = 1.4) and hydrophobic clotrimazole (CLO, logP = 5.4). The proposed printing method uses inexpensive, well known, and easily available FDA approved pharmaceutical excipients. The obtained model tablets had uniform content of the drug, excellent mechanical properties, and highly porous structure resulting in short disintegration time and fast dissolution rate. The tablets could be scaled and obtained in predesigned shapes and sizes. The proposed method may find its application in the early stages of drug development where high flexibility of the formulation is required and the amount of available API is limited. [ABSTRACT FROM AUTHOR]

The objective of the present study is to create a new approach to design and evaluate mucoadhesive microspheres for oral controlled release. The quinapril hydrochloride microspheres with a coat consisting of alginate polymer i.e. sodium alginate in combination of mucoadhesive mineral origin chitin molecule polymer chitosan and galactomannan polymer i.e. guargum were prepared by an ionic gelation process. The microspheres were evaluated for morphological character, particle size, micromeritic properties, percentage entrapment efficiency, Swelling Index, in-vitro wash-off test, in-vitro release studies and in vivo mucoadhesion behavior in albino rabbits. The result of mucoadhesive microspheres were identified spherical and have free flowing properties. The percent of drug loading efficiency was 89.9 to 95.6%. The microspheres showed good mucoadhesive property during the in vitro wash-off test. The drug quinapril hydrochloride released from polymer matrix mucoadhesive system from these was slow and extended over 12 h duration on the composition of coat. Mucoadhesive microspheres provide the capability to adhere on the mucosal tissue of stomach. Quinapril Hydrochloriderelease mucoadhesive pulsatile multiunit dosage forms was found to be slow and extended period of time. The drug discharge ratio was dependent on the composition of polymer and stirring speed used during the formulation. The release of drug was prolonged through the matrix system produced after swelling of polymeric composition of coat within mucoadhesive polymers and sustained drug release up to 12 h duration. The result concluded that prepared mucoadhesive microspheres best suited for oral controlled release of quinapril hydrochloride for the management of hypertension via oral route. [ABSTRACT FROM AUTHOR]

Type 2 diabetes management usually requires polytherapy, which increases the risk of drug-to-drug interactions. Among the multiple diabetes comorbidities, hypertension is the most prevalent. This study aimed to investigate the binding interactions between the model protein, bovine albumin, and the hypoglycemic agent gliclazide (GLICL) in the presence of typical hypotensive drugs: quinapril hydrochloride (QUI), valsartan (VAL), furosemide (FUR), amlodipine besylate (AML), and atenolol (ATN). Spectroscopic techniques (fluorescence quenching, circular dichroism) and thermodynamic experiments were employed. The binding of the gliclazide to the albumin molecule was affected by the presence of an additional drug ligand, which was reflected by the reduced binding constant of the BSA–DRUG–GLICL system. This may indicate a possible GLICL displacement and its enhanced pharmacological effect, as manifested in clinical practice. The analysis of the thermodynamic parameters indicated the spontaneity of the reaction and emphasized the role of hydrogen bonding and van der Waals forces in these interactions. The secondary structure of the BSA remained almost unaffected.

Various methods have been developed in recent years to determine the active ingredients of drugs used in the treatment of hypertension. In this study, active agents such as quinapril and hydrochlorothiazide were examined with UV/VIS and HPLC methods and to ensure accuracy and precision, studies are supported by PLS and PCR chemometric analyzes. After UV / VIS studies, recovery values of quinapril and hydrochlorothiazide as a result of PCR analysis were 100.56% and 99.85%, respectively; standard deviations are 0.512 and 0.027; As a result of PLS analysis, recovery values were 99.18% and 99.75%, respectively; and the standard deviations were calculated as 0.334 and 0.289. After HPLC studies, the recovery values of quinapril and hydrochlorothiazide as a result of PCR analysis were 100.01% and 99.78%, respectively; the standard deviations are 0.170 and 0.241; As a result of PLS studies, recovery values were 100.57% and 100.51%, respectively; and the standard deviations were found to be 0.462 and 0.706. In this study, the efficacy of UV/VIS and HPLC methods in the simultaneous determination of the drug active substances were examined chemometrically and it is concluded that these methods can be used in studies related to the quality and target suitability of hypertension drugs composed of quinapril and hydrochlorothiazide. [ABSTRACT FROM AUTHOR]

Mitral valve (MV) disease is the most important valvular condition affecting athletic performance in horses. Twenty and 22 years old Thoroughbred Stallions used for breeding had suffered from increased respiratory and heart rate, poor performance and incomplete ejaculate release during covering, since three months ago. Cardiac examination projected irregular cardiac rhythm after a halt and an early-mid-systolic murmur.

Aim. To assess effects of quinapril on the regulatory-adaptive status (RAS) in patients with chronic heart failure (CHF) NYHA class 1 and arterial hypertension (HT). Material and methods. Patients (n=49) with CHF NYHA class I and HT stage I–II (25 men and 24 women, aged 52.5±8.4 years) were included into an open noncomparative study. A cardio-respiratory synchronization (CRS) test, 6 minute walk test, treadmill test with evaluation of the maximal oxygen uptake during exercise, ambulatory blood pressure monitoring, echocardiography , determination of N-terminal prohormone of brain natriuretic peptide (NT-proBNP) plasma level were performed at baseline and after 6 months of quinapril therapy. Results. The quinapril treatment (average daily dose 17.3±7.9 mg) improved myocardium structural and functional parameters, increased the exercise tolerance, reduced neurohumoral activity , improved the RAS according to CRS test: increase in synchronization range of cardiorespiratory cycles per minute from 8.0±2.1 to 11.0±2.5 (Δ27.3%; p

Background: Left ventricular (LV) global longitudinal strain (GLS) has been proposed as an early imaging biomarker of cardiac mechanical dysfunction., Objective: To assess the impact of angiotensin-converting enzyme (ACE) inhibitor treatment of hypertensive heart disease on LV GLS and mechanical function., Methods: The spontaneously hypertensive rat (SHR) model of hypertensive heart disease ( n  = 38) was studied. A subset of SHRs received quinapril (TSHR, n  = 16) from 3 months (mo). Wistar Kyoto rats (WKY, n  = 13) were used as controls. Tagged cardiac MRI was performed using a 4.7 T Varian preclinical scanner., Results: The SHRs had significantly lower LV ejection fraction (EF) than the WKYs at 3 mo (53.0 ± 1.7% vs. 69.6 ± 2.1%, P  < 0.05), 14 mo (57.0 ± 2.5% vs. 74.4 ± 2.9%, P  < 0.05) and 24 mo (50.1 ± 2.4% vs. 67.0 ± 2.0%, P  < 0.01). At 24 mo, ACE inhibitor treatment was associated with significantly greater LV EF in TSHRs compared to untreated SHRs (64.2 ± 3.4% vs. 50.1 ± 2.4%, P  < 0.01). Peak GLS magnitude was significantly lower in SHRs compared with WKYs at 14 months (7.5% ± 0.4% vs. 9.9 ± 0.8%, P  < 0.05). At 24 months, Peak GLS magnitude was significantly lower in SHRs compared with both WKYs (6.5 ± 0.4% vs. 9.7 ± 1.0%, P  < 0.01) and TSHRs (6.5 ± 0.4% vs. 9.6 ± 0.6%, P  < 0.05)., Conclusions: ACE inhibitor treatment curtails the decline in global longitudinal strain in hypertensive rats, with the treatment group exhibiting significantly greater LV EF and GLS magnitude at 24 mo compared with untreated SHRs., (Copyright © 2023 Wolters Kluwer Health, Inc. All rights reserved.)

A novel electrochemiluminescence (ECL) sensor with composite consisted of silica-sol, Zinc oxide nanoparticles (ZnO NPs), polyvinylpyrrolidone (PVP) and tris(2, 2′-bipyridine) ruthenium (II) was constructed. A new method for simultaneous determination of quinapril hydrochloride (QHCl) and its metabolite quinaprilat hydrochloride (QTHCl) in human plasma was developed using the ECL sensor coupled with capillary electrophoresis (CE). ECL intensities of QHCl and QTHCl increased dramatically when the ECL sensor was used as working electrode. The running buffer contains 14 mmol/L phosphate (pH 8.0) and 20% n-propyl alcohol. Under optimized experimental conditions, the linearity ranges of the method are 0.007–8.0 μg/mL for QHCl and 0.009–8.3 μg/mL for QTHCl. The detection limits of QHCl and QTHCl (S/N=3) are 3.6 ng/mL and 3.9 ng/mL, respectively. The method was applied for the simultaneous determination of QHCl and QTHCl in human plasma with satisfactory results. [ABSTRACT FROM AUTHOR]

Presents a case of treating hypertension stage II, 2 nd degree, risk 3 (high) in a patient of 54 years on an outpatient basis. For antihypertensive therapy was chosen fixed combination of quinapril 20 mg + hydrochlorothiazide 12.5 mg (Akkuzid) 1 times a day. Assigned therapy has several solutions to achieve the urgent tasks: to reach target blood pressure (BP) during the entire two weeks, to maintain the target blood pressure level throughout the observation period (24 weeks) to achieve regression of left ventricular hypertrophy. Effectiveness of prescribed therapy served as the main reason for high patient complains of treatment.

The study involved 100 people (50 men and 50 women) aged 32 to 68 years. The first group consisted of 53 patients with chronic heart failure class II and III stage of hypertensive disease (29 men and 24 women, age 52,9±10,7 y. o.), treated with sustained-release metoprolol succinate (betaloc ZOK of «AstraZeneca», Sweden production, of 97,3±9,5 mg/day doze). The second group included 47 patients with chronic heart failure class II and III stage of hypertensive disease (21 men and 26 women, age 57,5±5,7 y. o.), receiving quinapril (accupro of «Pfizer», USA production in 24,7±13,4 mg daily doze. Treadmill activity with measuring of the maximum oxygen consumption on effort, 24-hour blood pressure monitoring, echocardiography and NT-proBNP testing, сardio-respiratory synchronism trial was carried out initially and after six months of therapy. Beta-blocker and angiotensine converting enzyme inhibitor are equally reducing blood pressure, are not identical in influencing the in statedly-adaptive status patients and the latter can be preferred.

100 patients with CHF functional class (FC) I against the background of hypertensive disease of stage II with regular left ventricular (LV) ejection fraction (EF) (LVEF≥55%) took part in the research and were randomized into two groups. Group 1 consisted of 51 patients (54,2±22,9 years old) and received metoprolol succinate (Betalok ZOK, «AstraZeneca», Sweden) in a dosage of 78,1±19,3 mg per day. Group 2 consisted of 49 patients (55,4±23,1 years old) and received Quinapril (Accupro, «Pfizer», USA) in a dosage of 17,3± 7,7 mg per day. Initially and 6 months into therapy, the following tests were done: VO2max treadmill test, echocardiography, 6-minute walk test, NT-proBNP test. In order to objectively quantitatively determine regulatory adaptive status (RAS), a cardiorespiratory synchronism test was done. Results of the research showed that both medications improved indices of diastolic function of the LV, however only Quinapril effectively changed its structural and geometric parameters and systolic function. Exercise tolerance increased, NT-proBNP level decreased, VO2max increased, RAS improved only with Quinapril treatment. Therefore Quinapril has the advantage over metoprolol succinate in patients with CHF FC I and regular LVEF against the background of HD of stage II.

Background/Aims: Diabetic nephropathy remains a major clinical problem. The effects of prorenin might be adverse, but the literature data are controversial. We compared the renal effects of the (pro)renin receptor ((P)RR) blockade and angiotensin converting enzyme (ACE) inhibition on the progression of diabetic nephropathy in rats. Methods: Diabetes (DM) was induced by ip. streptozotocin administration in adult male Sprague-Dawley rats, followed by eight weeks of treatment with the (P)RR blocker "handle region" decoy peptide (HRP, 0,1 mg/kg/day) or with the ACE inhibitor Quinapril (Q, 50 mg/kg/day) and grouped as follows: 1. Control (n=10); 2. DM (n=8); 3. DM+HRP (n=6); 4. DM+Q (n=10); 5. DM+Q+HRP (n=10). Renal functional parameters, histology and gene expressions were evaluated. Results: HRP reduced glomerulosclerosis and podocyte desmin expression, but did not affect proteinuria and tubular ERK(1/2) phosphorylation. Both Q and Q+HRP treatment reduced proteinuria, glomerular and tubular damage, tubular TGF-β1 expression and ERK(1/2) phosphorylation to the same extent. Conclusion: The effects of HRP were partially beneficial on diabetic kidney lesions as HRP reduced damage but did not improve tubular damage and failed to reduce ERK(1/2) phosphorylation in rats. The combination of HRP with Quinapril had no additive effects over Quinapril monotherapy on the progression of diabetic nephropathy. [ABSTRACT FROM AUTHOR]

Aim. To evaluate the effect of quinapril on diabetic cardiovascular autonomic neuropathy (CAN) and peripheral neuropathy (DPN). Patients and Methods. Sixty-three consecutive patients with diabetes mellitus [43% males, 27 with type 1 DM, mean age 52 years (range 22–65)], definite DCAN [abnormal results in 2 cardiovascular autonomic reflex tests (CARTs)], and DPN were randomized to quinapril 20 mg/day (group A, n=31) or placebo (group B, n=32) for 2 years. Patients with hypertension or coronary heart disease were excluded. To detect DPN and DCAN, the Michigan Neuropathy Screening Instrument Questionnaire and Examination (MNSIQ and MNSIE), measurement of vibration perception threshold with biothesiometer (BIO), and CARTs [R-R variation during deep breathing [assessed by expiration/inspiration ratio (E/I), mean circular resultant (MCR), and standard deviation (SD)], Valsalva maneuver (Vals), 30 : 15 ratio, and orthostatic hypotension (OH)] were used. Results. In group A, E/I, MCR, and SD increased (p for all comparisons < 0.05). Other indices (Vals, 30 : 15, OH, MNSIQ, MNSIE, and BIO) did not change. In group B, all CART indices deteriorated, except Vals, which did not change. MNSIQ, MNSIE, and BIO did not change. Conclusions. Treatment with quinapril improves DCAN (mainly parasympathetic dysfunction). Improved autonomic balance may improve the long-term outcome of diabetic patients. [ABSTRACT FROM AUTHOR]

Aim. To identify the optimal therapeutic strategy in Functional Class (FC) I–II chronic heart failure (CHF), in accordance with the effects of different drug classes on the regulatory and adaptive status (RAS). Material and methods. The study included 200 patients with FC I–II CHF, who were randomised into two groups. The first group included 104 patients (mean age 52,8±1,9 years) who received metoprolol succinate extended-release in the mean daily dose of 87,7±7,6 mg. The second group included 96 patients (mean age 55,0±1,4 years) receiving quinapril in the mean daily dose of 21,0±5,5 mg. At baseline and 6 months later, 24-hour blood pressure monitoring, the cardio-respiratory synchronism test, treadmill test with the VO2 max assessment, echocardiography, and the measurement of the plasma levels of N-terminal pro-brain natriuretic peptide (NT-proBNP) were performed. Results. Both medications improved the parameters of left ventricular (LV) diastolic function. However, only quinapril effectively improved LV structure, geometry, and systolic function. Only in the quinapril group, exercise capacity and stress test VO2 max increased, while the reduction in NT-proBNP levels, together with the improvement in RAS parameters, was more pronounced. Conclusion. Compared to metoprolol succinate, quinapril demonstrated more pronounced positive effects on cardiac structure and function, as well as on RAS parameters, in patients with FC I–II CHF.

Aim.To identify the optimal treatment tactics in patients with Functional Class (FC) II chronic heart failure (CHF) (NYHA classification) and essential arterial hypertension (EAH), via investigating the effects of different medication classes on regulatory and adaptive status (RAS). Material and methods.The study included 100 patients with FC II CHF and Stage II EAH, who were randomised into 2 groups. Group I included 53 patients (mean age 52,9±2,3 years) receiving metoprolol succinate (mean dose 97,3±9,5 mg/d). Group II included 47 patients (mean age 57,5±1,3 years) administered quinapril (mean dose 24,7±6,3 mg/d). At baseline and after 6 months of therapy, the following procedures were performed: treadmill test with VO2max assessment; echocardiography; 24-hour blood pressure monitoring; N-terminal pro-brain natriuretic peptide (NT-proBNP) level measurement; and cardio-respiratory synchronism test. Results.While both medications improved left ventricular (LV) diastolic function, only quinapril demonstrated beneficial effects on LV structure, geometry, and systolic function. Only in Group II, exercise capacity and VO2max increased, RAS improved, and NT-proBNP levels decreased to a greater extent. Conclusion.Quinapril was more effective than metoprolol succinate in the treatment of patients with FC II CHF and Stage II EAH.

The aim of the study was to assess the effectiveness of Accupro (Quinapril; 40 mg/d), as monotherapy and basis medication of combined therapy, in the treatment of arterial hypertension (AH) among patients with metabolic syndrome (MS). After 8 weeks of Accupro monotherapy (40 mg/d), target levels of blood pressure (BP) were achieved in 68% of the patients. BP normalization correlated with endothelial function improvement. Accupro therapy (40 mg/d) was also well tolerated. Accupro (40 mg/d) could be recommended as an effective and safe basis medication for combined antihypertensive therapy in patients with AH and MS.

The review presents current experimental and clinical evidence on organo-protective effects of an ACE inhibitor quinapril. These effects are dependent on I/D polymorphism of ACE gene. The data available are consistent that quinapril could modulate this genetic risk factor, highly prevalent in Russian patients.

We aimed to investigate the effects of nebivolol and quinapril treatments on P-wave duration and dispersion in hypertensive patients. Hypertensive patients who were in sinus rhythm were assigned to the two treatment groups and received either 20 mg quinapril/day or 5 mg nebivolol/day. P-Wave dispersion (PWD) was measured at baseline and after four weeks of treatment and defined as the difference between the maximum (Pmax) and the minimum (Pmin) P-wave duration. The study group consisted of 54 patients (Mean age: 53 ± 9 years, 46% women) with 27 patients in each group. At 4-week follow up both treatment groups showed a significant reduction (p0.05). In conclusion, short-term treatment with nebivolol and quinapril produces a similar but significant reduction in Pmax and PWD in hypertensive patients. This effect is independent of blood pressure and heart rate changes.

Aim. To investigate antihypertensive efficacy, effects on endothelial, diastolic function of the left ventricule and metabolism of combination of ACE inhibitor quinapril (accupro) with diuretic indapamide SR in patients with hypertension of the second-third degree and type 2 diabetes mellitus (DM) and free of DM. Material and methods. Outpatient treatment was given to 60 patients with AH (mean age 55.3 ± 9.6 years) in combination with mild or moderate DM (group 1) and free of DM (group 2). The patients were observed for 12 weeks. Clinical and biochemical blood tests, ECG, echo-CG, measurements of blood pressure were made in all the patients. Results. Quinapril course (mean dose 23.3 ± 9.8 mg/day) in combination with indapamide (1.5 mg/day) produced a complete hypotensive effect in group 1 (23 patients,76.7%), in group 2 - 25 (83.3%). DM patients demonstrated reduction of fasting and postprandial glycemia and cholesterol, time of isovolumic relaxation reduced in group 1 by 9.1%, in group 2 by 19.8% (p < 0.01). Left ventricular diastolic function improved, endothelium-dependent vasodilation in diabetics rose by 40%, non-endothelium-dependent - by 21.8%, in hypertensive patients free of DM - by 51.9 and 43.2%, respectively. Conclusion. Combination of quinapril with indapamide produces a significant antihypertensive effect in patients with AH of degree II-III associated with type 2 DM, improves carbohydrate and lipid metabolism, left ventricular diastolic function.

Aim. To assess the effectiveness of non-pharmaceutical body weight (BW) reduction and its influence on clinical quinapril effectiveness in patients with arterial hypertension (AH) and obesity.Material and methods. Fifty AH patients - men and women aged 34-71 years (mean age 50,8+1,78 years) were examined. Physical examination, anthropometry, measurement of body mass index (BMI) and blood pressure (BP) by Korotkoff method, 24-hour BP monitoring (BMP) and visceral fat measurement with OMRON BF 302 device were performed.Results. In all participants, significant reduction in office BP (p