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Fosinopril (FOS) is an angiotensin-converting enzyme inhibitor that can decrease angiotensin II (Ang II) formation, thereby reducing systemic vasoconstriction. This study investigated the impact of FOS on vascular smooth muscle cell (VSMC) phenotypic transformation in hypertension. Experiments using western blotting revealed that FOS inhibits the Ang II-induced downregulation of α-SMA and SM22α and the upregulation of OPN in VSMCs. In addition, CCK8 assays, EdU staining, and Transwell assays demonstrated that FOS reduces Ang II-induced increases in VSMC cell viability, proliferation, migration, and MMP2 and MMP9 expression. Moreover, immunofluorescence and ELISA experiments showed that FOS suppresses Ang II-induced increases in ROS levels, NAD(P)H activity, and NOX2 and NOX4 expression in VSMCs. Western blotting also indicated that FOS inhibits Ang II-induced increases in TGF-β1 and p-Smad2/3 expression in VSMCs. Finally, FOS mitigates Ang II-induced VSMC proliferation, phenotypic transformation, migration, and oxidative stress by inhibiting the TGF-β1/Smad signaling pathway. In conclusion, these results suggest that FOS could be effective in managing vascular diseases, including hypertension.

Effective and safe therapies for the treatment of diseases caused by intraerythrocytic parasites are impeded by the rapid emergence of drug resistance and the lack of novel drug targets. One such disease is human babesiosis, which is a rapidly emerging tick-borne illness caused by Babesia parasites. In this study, we identified fosinopril, a phosphonate-containing, FDA-approved Angiotensin Converting Enzyme (ACE) inhibitor commonly used as a prodrug for hypertension and heart failure, as a potent inhibitor of B. duncani parasite development within human erythrocytes. Cell biological and mass spectrometry analyses revealed that the conversion of fosinopril to its active diacid molecule, fosinoprilat, is essential for its antiparasitic activity. We show that this conversion is mediated by a parasite-encoded esterase, BdFE1, which is highly conserved among apicomplexan parasites. Parasites carrying the L238H mutation in the active site of BdFE1 failed to convert the prodrug to its active moiety and became resistant to the drug. Our data set the stage for the development of this class of drugs for therapy of vector-borne parasitic diseases.

ObjectiveFosinopril and amlodipine are commonly prescribed as first-line pharmacotherapeutic agents for pediatric hypertension, but there is a lack of comparative studies regarding the efficacy of these two drugs. We aimed to evaluate and compare the efficacy of fosinopril and amlodipine monotherapy in pediatric primary hypertension.MethodsThis was a single-center, bidirectional observational study. A total of 175 children and adolescents with primary hypertension receiving antihypertensive monotherapy from July 2020 to February 2023 were enrolled. According to antihypertensive drugs, they were divided into the fosinopril group (n = 96) and the amlodipine group (n = 79). Subgroup analysis was performed to compare the efficacy of the two groups in terms of blood pressure (BP) control rates and reductions following a 4-week treatment.ResultsAfter 4 weeks of treatment, both groups achieved significant reductions in systolic BP (SBP) and diastolic BP (DBP) by more than 18 mmHg and 6 mmHg, respectively, with BP control rates of 61.5% in the fosinopril group and 59.5% in the amlodipine group, revealing no significant differences in the antihypertensive efficacy between the two groups except for DBP control rate (FDR adjusted P > 0.05). Further subsequent subgroup analyses revealed that the reductions in SBP and DBP in the fosinopril group were significantly greater than those in the amlodipine group in patients of females and hypo-HDL-cholesterolemia (FDR adjusted P 0.05).ConclusionsFosinopril and amlodipine monotherapy were both effective in pediatric primary hypertension during a short-term follow-up. Fosinopril may be particularly effective in reducing BP in hypertensive patients of females, central obesity, IR, and hypo-HDL-cholesterolemia. These findings indicate that optimizing antihypertensive medication selection based on the individualized characteristics of children with hypertension may improve the efficacy of antihypertensive treatment.

Abstract Background With the expanded utilization of transcatheter aortic valve implantation (TAVI) to younger and lower surgical risk patients with severe aortic stenosis (AS), optimal medical therapy after TAVI procedure has become the main concern. Renin-angiotensin system inhibitors (RASi) are widely utilized in the area of cardiovascular disease including heart failure and myocardial infarction and revealed the ability to reverse left ventricular (LV) remodeling. Interests have, thus, been drawn in investigating whether the prescription of RASi after the TAVI procedure can prevent or reverse cardiac remodeling and improve long-term clinical outcomes. No recommendation regarding the prescription of RASi after TAVI is proposed yet due to the lack of evidence from randomized controlled trials, especially in the Chinese population. We, therefore, designed this randomized controlled trial to explore the effect of adding fosinopril to standard care in patients who underwent a successful TAVI procedure on the LV remodeling. Methods A total of 200 post-TAVI patients from seven academic hospitals across China will be recruited and randomized with a ratio of 1:1 to receive standard care or standard care plus fosinopril. Follow-up visits will take place at 30 days, 3 months, 6 months, 12 months, and 24 months from randomization to assess the clinical symptoms, any adverse events, cardiac function, and quality of life. Cardiac magnetic resonance will be performed at baseline and repeated at the 24-month follow-up visit to assess LV remodeling. Discussion This study will provide evidence regarding medical therapy for AS patients who underwent TAVI and filling the gap in the Chinese population. Trial registration Chinese Clinical Trial Registry ChiCTR2100042266 . Registered on 17 January 2021

The aim of the study was to evaluate the effectiveness of the integrated use of propranolol with heparin and percutaneous coronary intervention (PCI); propranolol with tenecteplase, syto-mask in combination with PCI and separately only PCI for hemodynamics, cardiohemodynamics and the clinical course in the acute period, as well as in the observation of MI. The results of complex drug and mechanical revascularization are compared. Materials and research methods. 63 patients with acute coronary syndrome (ACS) were examined: myocardial infarction non elevation ST segment, at the age from 30 to 70 years (56.7 ± 1.20), which were divided into 3 groups of 21 people by randomization. In the 1st group, they were treated with heparin, propranolol with Cito- Mak, kardiotekct, preduktal MR35mq, BLAII and PCI; in the 2nd group, methylase (tenecteplase) and propranolol were administered, fozinopril was given, and PCI was performed after 24 hours; in the 3rd group only PCI was produced. Using echocardiography and Doppler echocardiography, the values the end systolic volume (ESV), end diastolic volume (EDV), ejection fraction (EF), stroke index (SI), cardiac index (CI), and the index of the disturbance of local left ventricular contractility (LVC) and also established the dynamics of systolic and diastolic blood pressure, the clinical course of OKMI in the observation period. Results and discussion. Administration of heparin, propranolol kardiotekst, Cito- Mak infusion, preduktal MR35 mq and AIIbl oral administration and transdermal coronary intervention (PCI) administration after 24 hours accelerate stabilization of central hemodynamics. The reduced ESV, EDV, IALC and decreased, degree improves left ventricular systolic function, increases PV. There was no restenosis, recurrence of MI and mortality. In one patient, on 5 days, was recorded DOS. During treatment with fozinopril, propranolol with heparin and PCI, central hemodynamics are systolic function (group 1). At the same time, in 2 patients, on day 3 and 3, was recorded DOS, in 1 - recurrence of MI. When only PCI was performed, 4 patients developed recurrence of MI, 4 had restenosis, 2 had AHF, and 2 died. Conclusions. The result of this work shows that the integrated use of drug therapy with percutaneous coronary intervention allows you to get a prognostically positive result in contrast to using only PCI. [ABSTRACT FROM AUTHOR]

Aim. Еvaluate the influence of combination therapy with fosinopril or zofenopril on the regulatory-adaptive status (RAS) of patients with diastolic chronic heart failure (CHF). Material and methods. The study includes 80 patients with CHF I-II functional class according to the classification of the New York heart Association with left ventricle ejection fraction ≥50% because of hypertensive disease (HD) of III stage, who were randomized into two groups for treatment with fosinopril (14.7±4.2 mg/day, n=40) or zofenopril (22.5±7.5 mg/day, n=40). As part of combination pharmacotherapy, patients were included nebivolol (7.1±2.0 mg/day and 6.8±1.9 mg/day), in the presence of indications, atorvastatin and acetylsalicylic acid in the intestinal shell were prescribed. Initially and after six months, the following was done: a quantitative evaluation of the RAS (by cardio-respiratory synchronism test), echocardiography, tredmil-test, six-minute walking test, determination of the N-terminal precursor of the natriuretic brain peptide level in blood plasma and subjective evaluation of quality of life. Results. Therapy, using fosinopril, in comparison with zofenopril, more improved RAS (by 66.5%, p

Aim. To determine effectiveness of combination therapy with lisinopril and fosinopril in patients with chronic heart failure (CHF) with preserved left ventricular ejection fraction (LV EF), considering its impact on the regulatory and adaptive capabilities organism. Materials and methods. 80 patients were examined with CHF II functional class with preserved systolic function of the left ventricle (left ventricular ejection fraction ≥50%) (classification of the New York Heart Association) in the presence of hypertension disease (HD) III stage and/or ischemic heart disease (IHD). Randomly divided into two equal groups. In the first group was appointed for treatment with lisinopril (the average dose was 14.0±3.8 mg/day), in the second group - fosinopril (the average dose - 14.7±4.2 mg/day). All patients were prescribed nebivolol (7.1±2.2 mg/day and 6.8±2.1 mg/day). Depending on the concomitant pathology were appointed acetylsalicylic acid in the intestinal shell (100 mg/day, n=9 and 100 mg/day, n=10) and atorvastatin (15.3±4.9 mg/day, n=15 and 16.5±4.8 mg/day, n=17). Initially and after six months later of combined pharmacotherapy studied: a quantitative assessment of regulatory and adaptive capabilities of the organism, echocardiography, treadmill test, six-minute walk test, determination in blood plasma of the N-terminal precursor of the natriuretic brain peptide level, all-day monitoring of blood electrocardiograms and pressure. The quality of life was also assessed using a questionnaire. Results. Both treatment regimens of patients equally improved the structural and functional parameters of the heart, reduced neurohumoral activity, optimized heart rate and pulse. In this case, treatment with fosinopril is more pronounced positively regulatory-adaptive capacity and tolerance to physical load, and also there was an improvement in the quality of life. Conclusion. In patients with CHF with preserved LV EF, in the presence of HD and/or IHD combined pharmacotherapy with fosinopril in comparison with lisinopril probably is preferable due to the more pronounced increase in regulatory and adaptive capabilities.

Aim. Сompare the effectiveness of combination therapy with lisinopril and fosinopril in patients with diastolic chronic heart failure (CHF) in the presence of hypertension disease (HD), considering its impact on the regulatory adaptive status (RAS). Materials and methods. The study take parted 69 patients with CHF II functional class according to the classification of the New York Heart Association in the presence of HD III stage with preserved systolic function of the left ventricle (left ventricular ejection fraction ≥50%), who were randomized into two groups for treatment with lisinopril (13.7±3.7 mg/day, n=34) or fosinopril (14.5±4.1 mg/day, n=35). As part of combination pharmacotherapy, patients were included nebivolol (7.2±2.4 mg/day and 7.0±2.2 mg/day), and acetylsalicylic acid when required (100 mg/day, n=8 and 100 mg/day, n=7), atorvastatin (15.7±4.9 mg/day, n=14 and 16.9±4.6 mg/day, n=16) respectively. Initially and after six months, the following was done: a quantitative evaluation of the RAS (by cardio-respiratory synchronism test), echocardiography, holter monitoring of blood electrocardiograms, all-day monitoring of pressure, treadmill test, determination of the N-terminal precursor of the natriuretic brain peptide level in blood plasma, six-minute walking test, subjective evaluation of quality of life. Results. Both combined pharmacotherapy schemes comparably improved structural and functional state of the heart, neurohumoral activation and optimized blood pressure. However, in this case, the use of fosinopril, in comparison with lisinopril, positively affected on RAS, increased exercise tolerance and improved quality of life more. Conclusion. In patients with diastolic CHF in the presence of HD III stage as part of the combination therapy, the use of fosinopril, in comparison with lisinopril, may be preferable because of a more pronounced positive effect on RAS.

The article exemplified the successful experience of using combination therapy consisting of fosinopril, an angiotensin-converting enzyme inhibitor, and diltiazem, a non-dihydropyridine calcium antagonist, in a patient with a history of arterial hypertension, sinus tachycardia and bronchial asthma. The authors proved the high antihypertensive efficacy and safety of the therapy, its favourable effect on the daily profile of blood pressure and heart rate, and strong organ-protective properties, the ability to reduce the degree of left ventricular hypertrophy and microalbuminuria level.

We studied hypotensive effects, as well as short-term, daily and long-term variability of arterial pressure against the background of treatment with angiotensin-transforming ferment inhibitor and angiotensin-ferment blockers II in patients with arterial hypertension in comorbidity with chronic obstructive pulmonary disease.

The article is devoted to the diagnosis and management of patients with myocarditis, and its role in the development of chronic heart failure (CHF). It also determined the role of specific therapy and approaches to the treatment of CHF in patients with this pathology.

This article discusses clinicopharmacological niches of fosinopril, one of the most popular ACE inhibitors in daily outpatient practice. The authors cover aspects, where fosinopril has advantages over other ACE inhibitors and angiotensin II receptor blockers (sartans) from the point of view of therapy, cardiology and clinical pharmacology. The theses taken as a basis of the article are confirmed by the authors, who named and reviewed the leading clinical trials of fosinopril and its potentially possible combinations with diuretics and calcium channel blockers. The article also covers issues and satellite phenomena of “vascular” comorbidity in patients with arterial hypertension, chronic heart failure and chronic kidney disease; describes the mechanisms of their development and mutual aggravation; examines the points of administration and the evidence for the efficacy and safety of fosinopril in this cohort of patients. One of the main theses of this article is the importance of organ-protection (-cardio, -nefro, -angio). The main directions and postulates of its implementation are provided using the example of ACE inhibitors.

The article briefly describes the inhibitor of angiotensin converting enzyme (ACEI) - fosinopril, calcium channel blocker - diltiazem and antiplatelet agent- acetylsalicylic acid (ASA). The mechanism of their action and possible side effects are given. The authors of the article described in detail the antihypertensive drug from the group ACEI - fosinopril, antiplatelet agent - ASA and non-hydropyridine calcium channel blocker - diltiazem. The results of multicenter randomized trials of ASA, fosinopril in patients with arterial hypertension, ischemic heart disease, nephropathy and heart failure are presented. The article presents a clinical example that demonstrates the selection of the optimal drugs for the treatment of the combined pathology of the heart and kidneys, and also provides an evidence base for the efficacy and safety of fosinopril and ASA preparations. Presented drugs (ASA, fosinopril, diltiazem) are highly effective in all categories of patients with CVD and can be recommended for wider clinical use.

Objective: To explore whether Panax notoginseng saponins (PNS) exhibits heart protective effect in myocardial infarction (MI) rats and to identify the potential signaling pathways involved. Methods: MI rats induced by ligating the left anterior descending (LAD) coronary artery were assigned to sham coronary artery ligation or coronary artery ligation. Totally 36 Sprague-Dawley rats were randomly divided into sham group (distilled water, n=9), MI group (distilled water, n=9), PNS group (PNS, 40 mg/kg daily, n=9) and fosinopril group (FIP, 1.2 mg/kg daily, n=9) according to a random number table. The left ventricular morphology and function were conducted by echocardiography. Histological alterations were evaluated by the stainings of HE and Masson. The serum levels of C reactive protein (CRP), tumor necrosis factor α (TNF-α), growth differentiation factor-15 (GDF-15) and the ratio of metalloproteinase-9 (MMP-9) and tissue inhibitor of MMP-9 (TIMP-1) were determined by ELISA. The levels of activating transcription factor 3 (ATF3), mitogen-activated protein kinase kinase 3 (MAP2K3), p38 mitogen-activated protein kinase (p38 MAPK), phosphorylation of p38 MAPK (p-p38 MAPK), transforming growth factor-β (TGF-β1), collagen I, nuclear factor kappa B p65 (NFκB p65), phosphorylation of NFκB p65 (p-NFκB p65), and phosphorylation of inhibitory kappa Bα (p-Iκ Bα) in hearts were measured by Western blot and immunohistochemical staining, respectively. Results: PNS improved cardiac function and fibrosis in MI rats (P<0.05). The serum levels of CRP, TNF-α, GDF-15 and the ratio of MMP9/TIMP1 were reversed by PNS in MI rats. The expressions of TGF-β1, collagen I, MAP2K3, p38 MAPK, p-p38 MAPK, NFκB p65, p-NFκB p65, and p-IκBα were down-regulated, while ATF3 increased with the treatment of PNS (P<0.05). Conclusions: PNS may improve cardiac function and fibrosis in MI rats via regulating ATF3/MAP2K3/p38 MAPK and NFκB signaling pathways. These results suggest the potential of PNS in preventing the development of ventricular remodeling in MI rats. [ABSTRACT FROM AUTHOR]

Objective: evaluate antihypertensive and vasoprotective effects of fosinopril in patients with arterial hypertension with a high and very high risk of cardiovascular complications. Material and methods. The open study included 26 Grade 2 hypertensive patients with high and very high cardiovascular risk. Among them were 13 (50%) women, 13 (50%) men, the average age of which was 58.1 ± 10.3 years. Initially, all patients received hydrochlorothiazide diuretic therapy at a dose of 12.5 mg per day and various ACE inhibitors, but target blood pressure levels were not achieved. Fosinopril, an angiotensin converting enzyme (ACE) inhibitor (Monopril, VALEANT LLC, Russia), was administered to correct blood pressure for all patients instead of ACE inhibitors which they received earlier. The patients underwent a complete clinical and instrumental examination. The emphasis was placed on the study of the endothelial function by instrumental and laboratory methods. A test with endothelium-dependent vasodilatation (EDVD) was performed using method D. Celermajer; the total concentration of nitrate- and nitrite ions (NO2, NO3) in the blood serum was determined by the colorimetric method. The results of the examination were compared before administration of the drug and after 4 weeks of treatment. Results. 22 patients (85%) could achieve the target level of blood pressure (less than 140/90 mm Hg) after 8 weeks of fosinopril treatment. Daily monitoring of blood pressure showed a significant decrease in the variability of both systolic (SBP) and diastolic blood pressure (DBP). Initially, the dilatation reaction of the brachial artery was reduced in all patients and averaged to 6.8 ± 1.9%. The level of NO2 was 18.1 ± 0.9 μmol/l, NO3 – 28.8 ± 0.3 μmol/l. After 4 weeks of treatment, the EDVD increased to 7.5 ± 2.9%. The level of NO2 was 19.3 ± 0.4 μmol/l, NO3 – 38.75 ± 0.54 μmol/l. Conclusion. Fosinopril, an ACE inhibitor, had a pronounced antihypertensive effect, and improved endothelial function in patients with hypertension with a high and very high risk of cardiovascular complications after 4 weeks of treatment.

Arterial hypertension (AH) complicates the course of diabetes mellitus (DM) of both the 1st and 2nd type. In patients with diabetes type 1, the main cause of AH is diabetic nephropathy. In diabetes type 2, on the other hand, essential hypertension is diagnosed in 70-80% of cases. The choice of antihypertensive therapy in patients with diabetes is not easy; when selecting the best anti-hypertensive drug for a diabetes patient, the associated vascular complications should always be considered. Angiotensin-convertingenzyme inhibitors are the most common treatment of hypertension in diabetic patients. Damage of the nervous system - diabetic polyneuropathy (DPN) – is a key element in the clinical picture of diabetes. In the treatment of DPN, activation of neural regeneration (reinnervation) and pain management are crucial. Neurotropic B vitamins with multimodal effect play a key role in this.

Cardiovascular diseases (CVD) remain the main cause of mortality in the world. [1] At the same time, arterial hypertension (AH) is one of the most common CV pathologies, which, according to foreign researchers, affects about 30–45% of the general population [2] and about 40–47% of the population according to Russian studies. [3] The experts forecast that by 2030 the prevalence of hypertension will increase by approximately 10%. [4]

Aim. To study the therapeutic equivalence of original and generic fosinopril in patients with arterial hypertension (HT) of 1-2 degrees, and to evaluate the cost effectiveness of original drug substitution with generic. Material and methods. Patients (n=36) with HT of 1-2 degree aged 41-82 years and disease duration up 3 to 22 years included in an open, crossover , randomized trial. All patients had two courses of treatment: with generic (Fosicard) and the original drug (Monopril); sequence of courses was determined by randomization. Wash-out period (10-14 days) preceded each course. Treatment duration was 6 weeks; drugs were administered QD; initial dose - 10 mg/day. Blood pressure (BP) and heart rate (HR) were evaluated at the end of the wash-out period, and in 2, 4 and 6 weeks of therapy. In case of ineffective BP control (>140/90 mm Hg) hydrochlorothiazide 12.5 mg was added initially and dose fosinopril was increased up to 20 mg/day next. Results. Patients in groups were comparable by basic clinical parameters. Both fosinopril based drugs have comparable antihypertensive effect. Differences between their effect on systolic and diastolic BP as well as HR at all steps of treatment were not significant. The individual analysis revealed a tendency to more pronounced Monopril antihypertensive effect compared with Fosicard, but the differences were not significant. An average dose of Monopril was 11.8±3.9 mg/day , and Fosicard — 13.2±4.7 mg/day (p=0.13); the rate of monotherapy with both drugs of fosinopril at dose of 10 mg/day was similar (in 41% and 44% of patients, respectively); the rate of combined therapies with various composition differed insignificantly. Reduction in BP

Aim. To compare the effect of fosinopril and atenolol on synchronization of heart 0.1 Hz-rhythms and blood microcirculatory.Material and methods. 63 patients at the age of 47±8 with hypertension (HT) of grade 1-2 were enrolled in the study. 0.1 Hz-oscillations in heart rate variability (HRV) and in filling of microcirculatory bed were registered during passive tilt test under spontaneous breathing. The duration of each stage of test was 10 min. Synchronization was estimated as a phase difference between 0.1 Hz-rhythms of heart rate and filling of microcirculatory bed. Frequency values of HRV spectrum in LF- and HF-ranges were also assessed.Results. Fosinopril and atenolol showed comparable effect on blood pressure (BP) reduction. Atenolol decreased in heart rate significantly. Treatment with either fosinopril or atenolol in patients with significant vegetative dysfunction resulted in repair of functional interaction between heart 0.1 Hz-regulation and microcirculatory bed. Functional dissociation of 0.1 Hz-regulation mechanisms was observed under the treatment with fosinopril or atenolol in patients with initially sufficient interaction.Conclusions. Fosinopril and atenolol influenced similarly on heart 0.1 Hz-mechanisms and microcirculation autonomic regulation in patients with HT. Atenolol is a drug of choice in patients with sympathicotony. Both drugs should be administered in according with an individual level of 0.1-Hz rhythms synchronization assessed before start of the treatment.

Aim. To study dynamics of the indices of heart rate variability (HRV) and heart remodeling in response on combined therapy with fosinopril and simvastatin in postmenopausal metabolic syndrome (MS). Material and methods. 95 women were dynamically examined (before and after 12 months of therapy with fosinopril and simvastatin) to assess heart rhythm variability (time and spectral domains) and remodeling with Holter ECG monitoring and echocardiography. Results. Fosinopril has resulted in blood pressure decrease, reduction in heart remodeling andmyocardial heterogeneity , which accompanied HRV rise with increase in parasympathetic activity. Simvastatin potentiated fosinopril positive effects on left ventricular hypertrophy , myocardial electric heterogeneity and autonomic modulation due to its prominent hypolipidemic and pleiotropic effect. Conclusion. In patients with postmenopausal MS medicines, which modified different elements of MS (ACE inhibitor and statin), not only have antihypertensive and hypolipidemic action, but also reduce the heart remodeling and improve the autonomic nervous system balance.

Aim. To estimate effects of fosinopril and atenolol on autonomic regulation of heart in patients with arterial hypertension (HT) on the basis of spectral characteristics of heart rate variability (HRV).Material and methods. 49 patients (46±7 y.o.) with untreated or inadequately treated HT without end organ damages and associated clinical conditions were involved in the study. Heart rhythm was registered during passive orthostatic test with spontaneous breath within 10 min for each stage of the test. HRV was estimated by parametrical method based on autoregression model. Frequency power of HRV spectrum (ms2 ) in high-frequency (HF: 0,15-0,4 Hz) and low-frequency (LF: 0,04-0,15 Hz) ranges was calculated as well as the total power of a spectrum (ТР).Results. Fosinopril and atenolol reduced in blood pressure levels similarly, atenolol as well reduced in heart rate. Fosinopril and atenolol changed power of LF-range in comparable decreasing manner in upright position. Fosinopril therapy resulted in the same changes with power of HF-range. Atenolol increased power of HF-range in horizontal position and had no effect in upright position. There were not dynamic in TP during treatments.Conclusion. Fosinopril and atenolol have similar effects on the central mechanisms of autonomic heart regulation and HRV, though atenolol effect on sympathetic-parasympathetic balance is more prominent.

In Russia, cardiovascular diseases account for 57% of deaths in the overall mortality. Arterial hypertension (AH) is one of the main risk factors (RF) for cardiovascular diseases (along with dyslipidemia, smoking, metabolic syndrome, diabetes mellitus, alcohol abuse, etc.). AH is the largest contributor to cardiovascular morbidity and mortality, and a very common disease in Russia (about 40% of the adult Russian population suffer from hypertension).

The review article dials with the characteristics of fosinopriltherapeutic features, apparently associated with the fact that it contains phosphorus. It has special specter possessing the numerous of organotropic effects and good tolerability and safety, allowing tochange the drug tofosinoprilin patients,who has dry cough, and have been treated using different ACE inhibitors. We discuss the possible prospects of drugs appointment in case of unconventional diseasesfor ACE inhibitors application.

Effective and safe therapies for the treatment of diseases caused by intraerythrocytic parasites are impeded by the rapid emergence of drug resistance and the lack of novel drug targets. One such disease is human babesiosis, which is a rapidly emerging tick-borne illness caused by Babesia parasites. In this study, we identified fosinopril, a phosphonate-containing, FDA-approved angiotensin converting enzyme (ACE) inhibitor commonly used as a prodrug for hypertension and heart failure, as a potent inhibitor of Babesia duncani parasite development within human erythrocytes. Cell biological and mass spectrometry analyses revealed that the conversion of fosinopril to its active diacid molecule, fosinoprilat, is essential for its antiparasitic activity. We show that this conversion is mediated by a parasite-encoded esterase, BdFE1, which is highly conserved among apicomplexan parasites. Parasites carrying the L238H mutation in the active site of BdFE1 failed to convert the prodrug to its active moiety and became resistant to the drug. Our data set the stage for the development of this class of drugs for the therapy of vector-borne parasitic diseases., Competing Interests: Conflict of interest The authors declare that they have no conflicts of interest with the contents of this article., (Copyright © 2023 The Authors. Published by Elsevier Inc. All rights reserved.)

The mouth dissolving film overcomes the shortfalls of conventional quick dispersing/dissolving intraoral tablets. Fosinopril is an angiotensin converting enzyme (ACE) inhibitor used for the treatment of hypertension and some types of chronic heart failure. It undergoes extensive hepatic first pass metabolism, with bioavailability being only 36%. In the present investigation, an attempt was made to formulate fast dissolving film of fosinopril sodium by Solvent casting method using various film forming polymers such as HPMC 5cps, HPMC E-3, HPMC E-15 each being varied at three different concentration(6%,8%,10%). Drug-excipient compatibility studies were carried out by FTIR spectroscopy and DSC. in order to establish compatibility between drug and excipients The results revealed that the drug and excipients were satisfactorily compatible, without any significant changes in the chemical nature of the drug. Prepared films were subjected to different evaluation parameters such as folding endurance, physical appearance, %moisture absorption, drug content uniformity, in vitro disintegration time, in vitro dissolution studies and stability studies. All the formulations show name accurred compliance with pharmacopoeial standards. The stability study shows that no significant changes in films after one month study. Results revealed that the formulations F1 containing 6% HPMC 5cps showed better release property, low disintegration time, good folding endurance and good physical appearance compared to other formulations, so it was selected as the best formulation. [ABSTRACT FROM AUTHOR]

Hepatocellular carcinoma (HCC) is a major global health problem. Therapeutic interventions of HCC are still limited because of its complicated molecular pathogenesis. Many reports showed that renin-angiotensin system (RAS) contributes to the development of different types of malignancies. Therefore, the present study aimed to examine the effect of RAS inhibition using perindopril (1 mg/kg), fosinopril (2 mg/kg), or losartan (10 mg/kg) on diethylnitrosamine-induced HCC compared to sorafenib (30 mg/kg). The administration of RAS inhibitors resulted in improved liver function and histologic picture with a reduction in AFP levels. These effects found to be mediated through inactivation of NFкB pathway by the inhibition of NFĸB p65 phosphorylation at the Ser536 residue and inhibition of the phosphorylation-induced degradation of NFĸBia. Consequently, expression levels of cyclin D1 mRNA were significantly lowered. In addition, NFкB-induced TNF-α and TGF-β1 levels were reduced leading to lower levels of MMP-2 and VEGF. We concluded that RAS inhibition either through inhibiting the ACE or the blockade of AT1R has the same therapeutic benefit and that the tissue affinity of the ACEIs has no impact on its anti-tumor activity. These results suggest that ACEIs and ARBs can serve as promising candidates for further clinical trials in the management of HCC. [ABSTRACT FROM AUTHOR]

Abstract: The intermolecular interaction of fosinopril, an angiotensin converting enzyme inhibitor with bovine serum albumin (BSA), has been investigated in physiological buffer (pH 7.4) by multi‐spectroscopic methods and molecular docking technique. The results obtained from fluorescence and UV absorption spectroscopy revealed that the fluorescence quenching mechanism of BSA induced by fosinopril was mediated by the combined dynamic and static quenching, and the static quenching was dominant in this system. The binding constant, Kb, value was found to lie between 2.69 × 103 and 9.55 × 103 M−1 at experimental temperatures (293, 298, 303, and 308 K), implying the low or intermediate binding affinity between fosinopril and BSA. Competitive binding experiments with site markers (phenylbutazone and diazepam) suggested that fosinopril preferentially bound to the site I in sub‐domain IIA on BSA, as evidenced by molecular docking analysis. The negative sign for enthalpy change (ΔH0) and entropy change (ΔS0) indicated that van der Waals force and hydrogen bonds played important roles in the fosinopril‐BSA interaction, and 8‐anilino‐1‐naphthalenesulfonate binding assay experiments offered evidence of the involvements of hydrophobic interactions. Moreover, spectroscopic results (synchronous fluorescence, 3‐dimensional fluorescence, and Fourier transform infrared spectroscopy) indicated a slight conformational change in BSA upon fosinopril interaction. [ABSTRACT FROM AUTHOR]