Dipeptidyl peptidase‐4 inhibitor improves cardiac function by attenuating adverse cardiac remodelling in rats with chronic myocardial infarction
New Findings What is the central question of this study? Although cardioprotective effects of dipeptidyl peptidase‐4 (DPP‐4) inhibitors have been demonstrated, their cardiac effects in chronic myocardial infarction (MI) are unclear. We determined the effects of a DPP‐4 inhibitor on cardiac function and remodelling in rats with chronic MI. What is the main finding and its importance? We demonstrated, for the first time, that DPP‐4 inhibitor, but not metformin, exerted similar efficacy in improving cardiac function and attenuating cardiac fibrosis compared with enalapril in rats with chronic MI. These findings rev...
Source: Experimental Physiology - May 13, 2015 Category: Physiology Authors: Tharnwimol Inthachai, Suree Lekawanvijit, Sirinart Kumfu, Nattayaporn Apaijai, Wanpitak Pongkan, Siriporn C. Chattipakorn, Nipon Chattipakorn Tags: Research Paper Source Type: research
Enalapril Normalizes Endothelium-Derived Hyperpolarizing Factor-Mediated Relaxation in Mesenteric Artery of Adult Hypertensive Rats Prenatally Exposed to Testosterone.
Abstract Prenatal exposure to elevated testosterone levels induces adult life hypertension associated with selective impairments in endothelium-derived hyperpolarizing factor (EDHF)-mediated relaxation in mesenteric arteries. We tested whether the angiotensin-converting enzyme inhibitor enalapril restores EDHF function through regulating the activities of small (Kcnn3) and intermediate (Kcnn4) conductance calcium-activated potassium channels in the mesenteric arteries. Pregnant Sprague-Dawley rats were injected with vehicle or testosterone propionate (0.5 mg/kg/day from Gestation Day 15-19, subcutaneously), and th...
Source: Biology of Reproduction - May 13, 2015 Category: Reproduction Medicine Authors: More AS, Mishra J, Hankins GD, Yallampalli C, Sathishkumar K Tags: Biol Reprod Source Type: research
Blocking VEGF/Caveolin-1 signaling contributes to renal protection of fasudil in streptozotocin-induced diabetic rats.
CONCLUSION: Fasudil exerts protective actions in STZ-induced diabetic nephropathy by blocking the VEGFR2/Src/caveolin-1 signaling pathway and fibronectin upregulation. Thus, VEGFR2 may be a potential therapeutic target for the treatment of diabetic nephropathy. PMID: 25937636 [PubMed - as supplied by publisher] (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - May 4, 2015 Category: Drugs & Pharmacology Authors: Jin J, Peng C, Wu SZ, Chen HM, Zhang BF Tags: Acta Pharmacol Sin Source Type: research
Systematic Review Of The Societal Cost And Economic Burden Associated With Chronic Heart Failure
The objective of this study was to systematically identify and quantify the non-health sector costs for adults with CHF and in caregivers to patients with CHF. (Source: Value in Health)
Source: Value in Health - May 1, 2015 Category: Global & Universal Authors: F. Allen, R. Haroun, D. King Source Type: research
Effect of carboxylesterase 1 c.428G > A single nucleotide variation on the pharmacokinetics of quinapril and enalapril
CONCLUSIONSThe CES1 c.428G > A SNV decreased enalaprilat concentrations likely by reducing the hydrolysis of enalapril, but had no observable effect on the pharmacokinetics of quinapril. This article is protected by copyright. All rights reserved. (Source: British Journal of Clinical Pharmacology)
Source: British Journal of Clinical Pharmacology - April 28, 2015 Category: Drugs & Pharmacology Authors: E. Katriina Tarkiainen, Aleksi Tornio, Mikko T. Holmberg, Terhi Launiainen, Pertti J. Neuvonen, Janne T. Backman, Mikko Niemi Tags: Pharmacogenetics Source Type: research
Effect of enalapril maleate on ghrelin levels in metabolic syndrome in rats
In conclusion, ghrelin levels in MetS groups were significantly lower than control group, and thus Enalapril treatment improves components of MetS and has direct effects on serum ghrelin levels that are independent of MetS. (Source: Peptides)
Source: Peptides - April 24, 2015 Category: Biochemistry Source Type: research
A note on (+)-catechin
This article is interesting and the authors should be complimented for the significant amount of work they have done. The purpose of this letter is to call attention to the need for some clarification on (+)-catechin. The authors write “Our findings suggest that CTN has renoprotective properties comparable with ACEi, and coadministration of CTN and enalapril might be useful in reducing albumin excretion as well as improving endothelial function. (Source: Nutrition Research)
Source: Nutrition Research - April 24, 2015 Category: Nutrition Authors: Christophe Wiart Tags: Letter to the Editor Source Type: research
Design, synthesis and evaluation of novel 2-butyl-4-chloroimidazole derived peptidomimetics as Angiotensin Converting Enzyme (ACE) inhibitors.
Abstract A series of novel 2-butyl-4-chloro-1-methylimidazole derived peptidomimetics were designed, synthesized and evaluated for their Angiotensin Converting Enzyme (ACE) inhibitor activity. 2-Butyl-4-chloro-1-methylimidazole-5-carboxylic acid 2 obtained after oxidation of respective carboxaldehyde 1, was condensed with various amino acid methyl esters 3a-k to give imidazole-amino acid conjugates 4a-k in very good yields. Ester hydrolysis of 4a-k with aqueous LiOH gave the desired peptidomimetics 5a-k. Screening all the new compounds 4a-k and 5a-k using ACE inhibition assay, resulted five compounds 4i, 4k, 5e, 5...
Source: Bioorganic and Medicinal Chemistry - April 16, 2015 Category: Chemistry Authors: Jallapally A, Addla D, Bagul P, Sridhar B, Banerjee SK, Kantevari S Tags: Bioorg Med Chem Source Type: research
Current Challenges in the Management of Heart Failure.
Abstract The management of chronic heart failure (HF) with low ejection fraction (EF) has changed considerably over the past 30 years: the introduction of angiotensin-converting enzyme inhibitors (ACEIs), β-blockers, angiotensin-receptor blockers, mineralocorticoid-receptor antagonists and recently, the Ifblocker, ivabradine, has led to a significant reduction in overall mortality and HF mortality. Recently, a trial testing a dual inhibitor blocking the angiotensin-II receptor and neprylisin, the enzyme responsible for B-type natriuretic peptide degradation, showed that this complex molecule improved clinical...
Source: Circulation Journal - April 14, 2015 Category: Cardiology Authors: Komajda M Tags: Circ J Source Type: research
[In Context] News in brief
Folic acid can reduce risk of first stroke, according to the results of a double-blind trial. 20 702 people with hypertension without a history of stroke or myocardial infarction enrolled in the China Stroke Primary Prevention Trial were randomly assigned to receive either combined enalapril 10 mg and folic acid 0·8 mg or enalapril 10 mg alone. The trial was terminated early, after a median of 4·5 years, when benefits of the combined treatment were identified: there was a significant reduction in risk of first stroke in the folic acid-enalapril group (hazard ratio 0·79, 95% CI 0·68–0&mid...
Source: Lancet Neurology - April 13, 2015 Category: Neurology Tags: In Context Source Type: research
LCZ696 (Angiotensin-Neprilysin Inhibition): The New Kid on the Heart Failure Block?
This article provides an extensive review of the mechanism of action, pharmacokinetic properties, clinical efficacy, safety, and tolerability of LCZ696. (Source: Journal of Pharmacy Practice)
Source: Journal of Pharmacy Practice - April 12, 2015 Category: Drugs & Pharmacology Authors: Pham, A. Q., Patel, Y., Gallagher, B. Tags: Continuing Education Article Source Type: research
The effects of anti‐hypertensives and type 2 diabetes on salivary flow and total antioxidant capacity
ConclusionsEnalapril is not xerogenic but is antioxidant, which moderately reduces the risk of xerogenic effect development even in the presence of DM type 2. However, metoprolol and drug combinations exhibit xerogenic effect. In DM type 2, xerogenic effect of all drugs was pronounced except of metoprolol. (Source: Oral Diseases)
Source: Oral Diseases - April 6, 2015 Category: ENT & OMF Authors: LJ Djukić, J Roganović, MD Brajović, D Bokonjić, D Stojić Tags: Original Article Source Type: research
LCZ696: The Next Step in Improving RAS Inhibition?
Abstract LCZ696 is a single molecule which combines the angiotensin receptor blocker valsartan with the neprilysn inhibitor sacubitril (AHU377). In the recently published PARADIGM-HF trial, LCZ696 proved superior to enalapril in reducing overall mortality, heart failure hospitalizations, and other endpoints in patients with systolic dysfunction heart failure. Increases in counter-regulatory natriuretic peptides which oppose sodium retention, vasoconstriction, and the deleterious structural changes which follow neurohormonal activation are thought to account for these improved outcomes. In two large hypertension s...
Source: Current Hypertension Reports - April 1, 2015 Category: Primary Care Source Type: research
Cranial vena cava syndrome secondary to cryptococcal mediastinal granuloma in a cat.
Abstract The successful management of cranial vena cava syndrome with suspected secondary chylothorax due to mediastinal cryptococcal granuloma in a 4-year-old male domestic shorthair cat is described. Treatment included long-term antifungal medication, short-term corticosteroids, intermittent thoracocentesis, rutin, octreotide, and enalapril. PMID: 25829555 [PubMed - in process] (Source: The Canadian Veterinary Journal)
Source: The Canadian Veterinary Journal - April 1, 2015 Category: Veterinary Research Authors: Letendre JA, Boysen S Tags: Can Vet J Source Type: research
Valsartan/Sacubitril Reduces Mortality More Than Enalapril 10 mg Twice Daily in Patients With Heart Failure.
PMID: 25884751 [PubMed - as supplied by publisher] (Source: American Family Physician)
Source: American Family Physician - April 1, 2015 Category: Primary Care Authors: Ebell MH Tags: Am Fam Physician Source Type: research
Why Can dl-Sotalol Prolong the QT Interval In Vivo Despite Its Weak Inhibitory Effect on hERG K(+) Channels In Vitro? Electrophysiological and Pharmacokinetic Analysis with the Halothane-Anesthetized Guinea Pig Model.
Abstract In order to bridge the gap of action of dl-sotalol between the human ether-a-go-go-related gene (hERG) K(+) channel inhibition in vitro and QT-interval prolongation in vivo, its electropharmacological effect and pharmacokinetic property were simultaneously studied in comparison with those of 10 drugs having potential to prolong the QT interval (positive drugs: bepridil, haloperidol, dl-sotalol, terfenadine, thioridazine, moxifloxacin, pimozide, sparfloxacin, diphenhydramine, imipramine and ketoconazole) and four drugs lacking such property (negative drugs: enalapril, phenytoin, propranolol or verapamil) w...
Source: Cardiovascular Toxicology - March 31, 2015 Category: Cardiology Authors: Katagi J, Nakamura Y, Cao X, Ohara H, Honda A, Izumi-Nakaseko H, Ando K, Sugiyama A Tags: Cardiovasc Toxicol Source Type: research
Not Just Chlorthalidone: Evidence-Based, Single Tablet, Diuretic Alternatives to Hydrochlorothiazide for Hypertension
Abstract Accounting for 15 % of deaths worldwide, hypertension is often treated with hydrochlorothiazide (HCTZ) (50 million prescriptions annually). HCTZ has a
Source: Current Hypertension Reports - March 28, 2015 Category: Primary Care Source Type: research
Dynamic drug-induced organic mitral regurgitation during exercise echocardiography following chronic exposure to ergotamine
A 67-year-old woman with a history of hypertension and migraine had been hospitalized 9 months ago for unexplained acute pulmonary oedema with evidence of preserved LV ejection fraction and mild to moderate mitral regurgitation (MR). Coronary angiography was normal, she was in sinus rhythm and blood pressure was normal. She had been exposed continuously to ergotamine (gynergene) for migraine prophylaxis for 30 years (1 to 3 mg of ergotamine). Despite treatment by enalapril and furosemide introduced for heart failure, the patient remained in NYHA functional class III with evidence of preserved LV ejection fraction, mild MR ...
Source: International Journal of Cardiology - March 22, 2015 Category: Cardiology Authors: Sylvestre Maréchaux, Yassine Ben Brahim, Pierre Vladimir Ennezat, François Delelis, Christophe Tribouilloy Tags: Letter to the Editor Source Type: research
Angiotensin receptor-neprilysin inhibitors in heart failure: a shifting paradigm
Commentary on: McMurray JJ, Packer M, Desai AS, et al.; PARADIGM-HF Investigators and Committees. Angiotensin–neprilysin inhibition versus enalapril in heart failure. N Engl J Med 2014;371:993–1004. Context ACE inhibitors prolong survival in patients with heart failure with reduced ejection fraction (HFrEF) and have served as the backbone of heart failure management for over two decades.1 Natriuretic peptides (NPs) are hormones responsible for maintaining sodium and fluid homoeostasis; their release is triggered by increased myocardial filling pressures. NP benefits include direct vasodilation, increased glomer...
Source: Evidence-Based Medicine - March 17, 2015 Category: Internal Medicine Authors: Vardeny, O. Tags: Clinical trials (epidemiology), Epidemiologic studies, Immunology (including allergy), Drugs: cardiovascular system, Drugs: CNS (not psychiatric), Hypertension, Dermatology, Arrhythmias Therapeutics/Prevention Source Type: research
Endothelin A Receptor Antagonist, Atrasentan, Attenuates Renal and Cardiac Dysfunction in Dahl Salt-Hypertensive Rats in a Blood Pressure Independent Manner
In this study, we investigated whether atrasentan, an ETA receptor antagonist, has renal and cardiovascular effects independent of RAS inhibition. Male Dahl salt sensitive (DSS) rats, at six weeks of age, received water with or without different doses of atrasentan and/or enalapril under high salt (HS) diet or normal diet (ND) for 6 weeks. At the end of 12th week, atrasentan at a moderate dose significantly attenuated proteinuria and serum creatinine without reducing mean arterial pressure (MAP), thereby preventing cardiac hypertrophy and improving cardiac function. ACE inhibitor enalapril at a dose that did not significan...
Source: PLoS One - March 16, 2015 Category: Biomedical Science Authors: Mohammed A. Samad et al. Source Type: research
Folate Supplements for Stroke Prevention Targeted Trial Trumps the Rest
The effect of folate supplementation on cardiovascular disease has been studied in many observational studies and randomized trials and has been a topic of debate for a number of years. In this issue of JAMA, Huo and colleagues provide results from their important clinical trial of folic acid therapy for primary prevention of stroke. In a carefully designed and executed randomized trial, 20 702 adults with hypertension were randomized to receive enalapril alone (n = 10 354) or enalapril combined with 0.8 mg folic acid (n = 10 348). As recommended by the data and safety monit...
Source: JAMA - Journal of the American Medical Association - March 15, 2015 Category: Journals (General) Source Type: research
Efficacy of Folic Acid Therapy in Primary Prevention of Stroke Among Adults With Hypertension in China The CSPPT Randomized Clinical Trial
Conclusions and RelevanceAmong adults with hypertension in China without a history of stroke or MI, the combined use of enalapril and folic acid, compared with enalapril alone, significantly reduced the risk of first stroke. These findings are consistent with benefits from folate use among adults with hypertension and low baseline folate levels.Trial Registrationclinicaltrials.gov Identifier: NCT00794885 (Source: JAMA - Journal of the American Medical Association)
Source: JAMA - Journal of the American Medical Association - March 15, 2015 Category: Journals (General) Source Type: research
The effect of enalapril on furosemide‐activated renin–angiotensin–aldosterone system in healthy dogs
This study was designed to evaluate the efficacy of enalapril in suppressing ACE activity and furosemide‐induced circulating RAAS activation. Failure to do so would suggest that this failure may be a drug class effect. We hypothesized that enalapril would suppress ACE activity and furosemide‐induced circulating RAAS activation. Sixteen healthy hound dogs. The effect of furosemide (2 mg/kg PO, q12 h; Group F) and furosemide plus enalapril (0.5 mg/kg PO, q12 h; Group FE) on circulating RAAS was determined by plasma ACE activity, 4–6 h post‐treatment, and urinary A:C on days −1, &min...
Source: Journal of Veterinary Pharmacology and Therapeutics - March 15, 2015 Category: Veterinary Research Authors: A. C. Lantis, M. K. Ames, S. Werre, C. E. Atkins Tags: Short Communication Source Type: research
Neprilysin inhibition to treat heart failure: a tale of science, serendipity, and second chances
This review describes the role of neprilysin (also known as neutral endopeptidase or enkephalinase) in the degradation of natriuretic and other vasoactive peptides, including bradykinin and adrenomedullin. The initial development of neprilysin inhibitors, then angiotensin converting enzyme‐neprilysin inhibitors and, most recently, the angiotensin receptor neprilysin inhibitor (ARNI) LCZ696 (sacubitril valsartan) as an extension of the nurohumoral basis for the treatment of heart failure is also summarised. Finally, the implications of the compelling benefits of LCZ696 compared with enalapril in the Prospective comparison...
Source: European Journal of Heart Failure - March 9, 2015 Category: Cardiology Authors: John J.V. McMurray Tags: Review Source Type: research
Study CAMBIMED: Effects of changes in medication appearance on safety of antihypertensive and hypolipidemic treatments in chronic patients older than 65 years in primary health care
DiscussionFor drugs of the same active ingredient, the effect that different package appearances and presentation may have on the safety of patients undergoing chronic treatments is unknown under the new legislative framework. There are various initiatives that promote the iso-appearance of drugs: “If they are the same, make them look the same”. It is to be expected that older, multi-medicated patients with chronic pathologies will be the ones under a greater risk of suffering from this problem. (Source: BMC Public Health)
Source: BMC Public Health - March 4, 2015 Category: Consumer Health News Authors: Jesús Arancon-MongeAlicia de-Castro-CuencaÁngel Serrano-VázquezLuz Campos-DíazMontserrat Díaz-ErasoIsabel del Cura-GonzálezElena Polentinos-CastroRicardo Rodríguez-BarrientosAutores Colaboradores: GRUPO CAMBIMED Source Type: research
Cost–Utility of Angiotensin-Converting Enzyme Inhibitor-Based Treatment Compared With Thiazide Diuretic-Based Treatment for Hypertension in Elderly Australians Considering Diabetes as Comorbidity
The objective of this study was to examine the cost-effectiveness of angiotensin-converting enzyme inhibitor (ACEI)-based treatment compared with thiazide diuretic-based treatment for hypertension in elderly Australians considering diabetes as an outcome along with cardiovascular outcomes from the Australian government's perspective. We used a cost–utility analysis to estimate the incremental cost-effectiveness ratio (ICER) per quality-adjusted life-year (QALY) gained. Data on cardiovascular events and new onset of diabetes were used from the Second Australian National Blood Pressure Study, a randomized clinical tria...
Source: Medicine - March 1, 2015 Category: Internal Medicine Tags: Article: Economic Evaluation Study Source Type: research
Dipeptidyl peptidase‐4 inhibitor improves cardiac function via attenuating adverse cardiac remodeling in rats with chronic myocardial infarction
This article is protected by copyright. All rights reserved (Source: Experimental Physiology)
Source: Experimental Physiology - March 1, 2015 Category: Physiology Authors: Tharnwimol Inthachai, Suree Lekawanvijit, Sirinart Kumfu, Nattayaporn Apaijai, Wanpitak Pongkun, Siriporn C. Chattipakorn, Nipon Chattipakorn Tags: Research Paper Source Type: research
Absorption and cleavage of enalapril, a carboxyl ester prodrug, in the rat intestine: In vitro, in situ intestinal perfusion, and portal vein cannulation models
This article is protected by copyright. All rights reserved. (Source: Biopharmaceutics and Drug Disposition)
Source: Biopharmaceutics and Drug Disposition - March 1, 2015 Category: Drugs & Pharmacology Authors: Vinay K. Holenarsipur, Nilesh Gaud, Jaydeep Sinha, Sankara Sivaprasad, Priyadeep Bhutani, Murali Subramanian, Sheelendra Pratap Singh, Rambabu Arla, Sundeep Paruchury, Tarun Sharma, Punit Marathe, Sandhya Mandlekar Tags: Original Paper Source Type: research
Insulin Receptor Substrate-2 (Irs2) in Endothelial Cells Plays a Crucial Role in Insulin Secretion
Endothelial cells are considered to be essential for normal pancreatic β-cell function. The current study attempted to demonstrate the role of insulin receptor substrate-2 (Irs2) in endothelial cells with regard to insulin secretion. Endothelial cell–specific Irs2 knockout (ETIrs2KO) mice exhibited impaired glucose-induced, arginine-induced, and glucagon-induced insulin secretion and showed glucose intolerance. In batch incubation and perifusion experiments using isolated islets, glucose-induced insulin secretion was not significantly different between the control and the ETIrs2KO mice. In contrast, in perfusion...
Source: Diabetes - February 24, 2015 Category: Endocrinology Authors: Hashimoto, S.; Kubota, N.; Sato, H.; Sasaki, M.; Takamoto, I.; Kubota, T.; Nakaya, K.; Noda, M.; Ueki, K.; Kadowaki, T. Tags: Islet Studies Source Type: research
Adverse Drug Reaction reports for cardiometabolic drugs from sub‐Saharan Africa: A study in VigiBase
Conclusions‘In recent years the number of Adverse Drug Reactions (ADRs) reported in Sub Saharan Africa (SSA) has sharply increased. The data showed the well‐known population‐based differential ADR profile of ACE‐inhibitors in the SSA population.’This article is protected by copyright. All rights reserved. (Source: Tropical Medicine and International Health)
Source: Tropical Medicine and International Health - February 21, 2015 Category: Tropical Medicine Authors: Derbew Fikadu Berhe, Kristina Juhlin, Kristina Star, Kidanemariam G/Michael Beyene, Mukesh Dheda, Flora M Haaijer‐Ruskamp, Katja Taxis, Peter GM Mol Tags: Original Article Source Type: research
Drug therapy for patients with systolic heart failure after the PARADIGM-HF trial: in need of a new paradigm of LCZ696 implementation in clinical practice
In the PARADIGM-HF trial, the novel drug LCZ696 is more effective than enalapril for heart failure; Gerasimos Filippatos et al discuss the clinical applications and highlight the PARAGON-HF trial that is addressing the effect of LCZ696 in patient subgroups. (Source: BMC Medicine)
Source: BMC Medicine - February 18, 2015 Category: Internal Medicine Authors: Gerasimos FilippatosDimitrios FarmakisJohn ParissisJohn Lekakis Source Type: research
In HF, angiotensin-neprilysin inhibition reduced mortality and HF hospitalization compared with enalapril.
PMID: 25686189 [PubMed - in process] (Source: Annals of Internal Medicine)
Source: Annals of Internal Medicine - February 17, 2015 Category: Internal Medicine Authors: Schmitt BP Tags: Ann Intern Med Source Type: research
Soluble Neprilysin Is Predictive of Cardiovascular Death and Heart Failure Hospitalization in Heart Failure Patients
This study sought to assess the presence of circulating soluble neprilysin in a real-life cohort of HF patients and correlate neprilysin levels with outcomes.MethodsCirculating soluble neprilysin was measured with a modified sandwich immunoassay in consecutive ambulatory patients with HF who were followed up for 4.1 years. Associations between neprilysin level and a composite endpoint that included cardiovascular death or HF hospitalization were explored.ResultsMedian neprilysin concentration in 1,069 patients was 0.642 ng/ml (median quartile 1 to 3: 0.385 to 1.219). Neprilysin weakly but significantly correlated with age ...
Source: Journal of the American College of Cardiology - February 17, 2015 Category: Cardiology Source Type: research
Vitamin D receptor agonist VS-105 improves cardiac function in the presence of enalapril in 5/6 nephrectomized rats
Vitamin D receptor (VDR) agonists (VDRAs) are commonly used to manage hyperparathyroidism secondary to chronic kidney disease (CKD). Patients with CKD experience extremely high risks of cardiovascular morbidity and mortality. Clinical observations show that VDRA therapy may be associated with cardio-renal protective and survival benefits in patients with CKD. The 5/6 nephrectomized (NX) Sprague-Dawley rat with established uremia exhibits elevated serum parathyroid hormone (PTH), hypertension, and abnormal cardiac function. Treatment of 5/6 NX rats with VS-105, a novel VDRA (0.05 and 0.5 μg/kg po by gavage), once daily f...
Source: AJP: Renal Physiology - February 15, 2015 Category: Urology & Nephrology Authors: Wu-Wong, J. R., Chen, Y.-w., Wessale, J. L. Tags: ARTICLES Source Type: research
A putative placebo analysis of the effects of LCZ696 on clinical outcomes in heart failure
Aims Although active-controlled trials with renin–angiotensin inhibitors are ethically mandated in heart failure with reduced ejection fraction, clinicians and regulators often want to know how the experimental therapy would perform compared with placebo. The angiotensin receptor-neprilysin inhibitor LCZ696 was compared with enalapril in PARADIGM-HF. We made indirect comparisons of the effects of LCZ696 with putative placebos. Methods and results We used the treatment-arm of the Studies Of Left Ventricular Dysfunction (SOLVD-T) as the reference trial for comparison of an ACE inhibitor to placebo and the Candesartan ...
Source: European Heart Journal - February 14, 2015 Category: Cardiology Authors: McMurray, J., Packer, M., Desai, A., Gong, J., Greenlaw, N., Lefkowitz, M., Rizkala, A., Shi, V., Rouleau, J., Solomon, S., Swedberg, K., Zile, M. R., Andersen, K., Arango, J. L., Arnold, M., Belohlavek, J., Bohm, M., Boytsov, S., Burgess, L., Cabrera, W. Tags: Heart failure/cardiomyopathy Source Type: research
Prospective randomized study of the tolerability and efficacy of combination therapy for hypertensive chronic kidney disease: results of the PROTECT-CKD study
Abstract Background We conducted a randomized, open-label trial to determine which of the antihypertensive drugs was most beneficial for CKD patients with hypertension in spite of treatment with an angiotensin receptor blocker (ARB). Methods Patients 20–75 years of age who had CKD according to the definition in the K/DOQI Guidelines and hypertension (systolic blood pressure ≥130 mmHg and/or diastolic blood pressure ≥80 mmHg) with the usual dose of an ARB were randomly assigned to receive losartan 50 mg plus 5 mg of th...
Source: Clinical and Experimental Nephrology - February 14, 2015 Category: Urology & Nephrology Source Type: research
Profibrosing Effect of Angiotensin Converting Enzyme Inhibitors in Human Lung Fibroblasts
The objective of this study is to determine the effect of two angiotensin-converting enzyme inhibitors (ACEi) (Enalapril and Captopril), an angiotensin-II receptor inhibitor (Losartan) and a renin inhibitor (Aliskiren) on renin, TGF-β1 and collagen expressions in human lung fibroblast cultures through real-time PCR and ELISA. Materials and Methods Normal commercial fibroblasts (CCD25) were exposed to 10−6 M of enalapril, captopril, losartan, or aliskiren for 6 h. Subsequently, media were recovered and proteins were concentrated; RNA was extracted from the cells. ...
Source: Lung - February 6, 2015 Category: Respiratory Medicine Source Type: research
Comparing individual angiotensin-converting enzyme inhibitors with losartan in the risk of hospitalization for pneumonia and related mortality: a nationwide cohort study
Conclusions: Treatment with ACE inhibitors is not associated with a lower risk of pneumonia incidence and mortality as compared with losartan. (Source: Journal of Hypertension)
Source: Journal of Hypertension - January 30, 2015 Category: Cardiology Tags: ORIGINAL PAPERS: Therapeutic aspects Source Type: research
Angiotensin Converting Enzyme Inhibitors (ACEI) and doxorubicin pharmacokinetics in women receiving adjuvant breast cancer treatment
PurposeDoxorubicin (DOX) chemotherapy can cause cardiac complications. Angiotensin converting enzyme inhibitors (ACEI) may protect against these complications. We performed a pharmacokinetics (PK) study to determine whether DOX levels are altered in the presence of ACEI. Methods: In this randomized, cross-over, single-blinded drug-drug interaction study, 19 women with breast cancer prescribed DOX and cyclophosphamide every 14?days received one cycle of DOX chemotherapy with ACEI enalapril 10?mg daily and another cycle of DOX with placebo. Blood samples for DOX and doxorubicinol were drawn at baseline, 0.5, 1.0, 2.0, 4.0, 2...
Source: Epidemiologic Perspectives and Innovations - January 23, 2015 Category: Epidemiology Authors: Anne BlaesDaniel DuprezTodd DeforRyan ShanleyHeather BeckwithTufia HaddadDavid PotterDouglas YeeKinjal SanghaviPamala Jacobson Source Type: research
Nemaline myopathy and heart failure: Role of ivabradine; a case report
Conclusions: HF is a rare feature of NM, but it can negatively influence prognosis. Conventional HF therapy and/or heart transplant are the only reasonable strategy in these patients. Ivabradine is a useful, effective and safe drug for therapy in NM patients with HF and should be considered when resting HR remains high despite beta-blockers' full titration or beta-blockers' underdosing due to intolerance or side effects. (Source: BMC Cardiovascular Disorders)
Source: BMC Cardiovascular Disorders - January 19, 2015 Category: Cardiology Authors: Filippo SarulloGiuseppe VitaleAntonino Di FrancoSilvia SarulloYlenia SalernoLaura VassalloEmanuela BavieraStefania MaraziaGiorgio MandalàGaetano Lanza Source Type: research
Enalapril treatment increases T cell number and promotes polarization towards M1-like macrophages locally in diabetic nephropathy.
ahl A Abstract Diabetic nephropathy (DN) is a serious complication of longstanding diabetes affecting up to 30% of all diabetes patients and is the main cause of end-stage kidney disease globally. Current standard treatment e.g. ACE-inhibitors like enalapril merely offers a delay in the progression leading to DN. Herein, we describe in two preclinical models evidence to local effects on the inflammatory signatures after intervention treatment with enalapril which provides enhanced understanding of the mechanism of ACE inhibitors. Enalapril transiently reduced albuminuria in both the db/db and the STZ-induced DN mo...
Source: International Immunopharmacology - January 15, 2015 Category: Allergy & Immunology Authors: Cucak H, Nielsen Fink L, Højgaard Pedersen M, Rosendahl A Tags: Int Immunopharmacol Source Type: research
Visceral angioedema: an under-recognized complication of angiotensin-converting enzyme inhibitors.
We describe a patient in whom the diagnosis was delayed for> 2 years. A 60-year-old woman with hypertension on treatment with enalapril presented with complaints of abdominal pain and diarrhea for 2 days. Physical examination was significant for diffuse abdominal tenderness and hypotension. Laboratory data were normal except for leukocytosis and elevated creatinine. Computed tomography (CT) of the abdomen showed diffuse small bowel wall thickening. ACEI-induced visceral angioedema was considered, enalapril was discontinued and supportive care was provided. Patient's symptoms and CT appearance improved 48 and 72 hours, r...
Source: Postgraduate Medicine - January 14, 2015 Category: Internal Medicine Tags: Postgrad Med Source Type: research
Effect of ACE inhibitors and AT 1 receptor antagonists on pentylenetetrazole-induced convulsions in mice
Abstract Experimental data show that some angiotensin-converting enzyme (ACE) inhibitors and angiotensin AT1 receptor antagonists that are normally used as antihypertensive drugs can exert anticonvulsant-like activity against audiogenic seizures. In the current study, a number of ACE inhibitors (captopril, enalapril, cilazapril, perindopril and zofenopril) and AT1 antagonists (losartan, telmisartan and candesartan) were examined against pentylenetetrazole (PTZ)-induced seizures in mice. Captopril (50 mg/kg) administered intraperitoneally significantly raised the PTZ threshold (p
Source: Neurological Sciences - January 9, 2015 Category: Neurology Source Type: research
Enalapril induced normocomplementemic urticarial vasculitis
Savita Koregol, Varna Naidu, Sudhakar Rao, BS AnkadIndian Journal of Dermatology, Venereology, and Leprology 2015 81(1):73-74 (Source: Indian Journal of Dermatology, Venereology and Leprology)
Source: Indian Journal of Dermatology, Venereology and Leprology - January 6, 2015 Category: Dermatology Authors: Savita KoregolVarna NaiduSudhakar RaoBS Ankad Source Type: research
The effects of antihypertensives and type 2 diabetes on salivary flow and total antioxidant capacity
ConclusionsEnalapril is not xerogenic but is antioxidant, which moderately reduces the risk of xerogenic effect development even in the presence of DM type 2. However, metoprolol and drug combinations exhibit xerogenic effect. In DM type 2 xerogenic effect of all drugs was pronounced except of metoprolol.This article is protected by copyright. All rights reserved. (Source: Oral Diseases)
Source: Oral Diseases - January 1, 2015 Category: ENT & OMF Authors: LJiljana Djukić, Jelena Roganović, Milan Danilo Brajović, Dubravko Bokonjić, Dragica Stojić Tags: Original Article Source Type: research
Use of Different types of Angiotensin Converting Enzyme Inhibitors and Mortality in Systolic Heart Failure
Angiotensin converting enzyme-inhibitors (ACEIs) are the first-line treatment for patients with heart failure (HF) with reduced ejection fraction (EF). The benefit of ACEIs in HF is regarded as a class effect and different types of agents are used interchangeably. However, evidence on the comparable effectiveness of different ACEIs is scarce. We conducted a registry-based cohort study to assess all-cause mortality associated with the use of enalapril, perindopril, and trandolapril, as compared with ramipril, in patients with systolic HF. (Source: International Journal of Cardiology)
Source: International Journal of Cardiology - December 27, 2014 Category: Cardiology Authors: Henrik Svanström, Björn Pasternak, Mads Melbye, Anders Hviid Source Type: research
Efficacy of angiotensin–neprilysin inhibition versus enalapril in patient with heart failure with a reduced ejection fraction
(Source: Internal and Emergency Medicine)
Source: Internal and Emergency Medicine - December 24, 2014 Category: Emergency Medicine Source Type: research
Comparative proteomic analysis of rat left ventricle in a subtotal nephrectomy model
Conclusion Our studies provide a repertoire of potential biomarkers related to cardiac hypertrophy in CKD. There are still residual disturbed molecules/pathways despite ACEi intervention. Further studies are warranted to investigate these potential novel targets to alleviate CKD-related cardiomyopathy. (Source: Journal of the Chinese Medical Association)
Source: Journal of the Chinese Medical Association - December 21, 2014 Category: Journals (General) Source Type: research
Combination of ACE inhibitor with nicorandil provides further protection in chronic kidney disease
In conclusion, nicorandil may synergize with enalapril to provide superior protection in chronic kidney disease. (Source: AJP: Renal Physiology)
Source: AJP: Renal Physiology - December 15, 2014 Category: Urology & Nephrology Authors: Shiraishi, T., Tamura, Y., Taniguchi, K., Higaki, M., Ueda, S., Shima, T., Nagura, M., Nakagawa, T., Johnson, R. J., Uchida, S. Tags: TRANSLATIONAL PHYSIOLOGY Source Type: research
Single-pill combination therapy in the initial treatment of marked hypertension: a propensity-matched analysis.
Conclusions: Single-pill fixed-dose combination therapies are highly effective and safe in the study settings. Best clinical and echocardiographic outcomes were noted among patients receiving E/L, R/H and P/A. PMID: 25496379 [PubMed - as supplied by publisher] (Source: Clinical and Experimental Hypertension)
Source: Clinical and Experimental Hypertension - December 12, 2014 Category: Cardiology Authors: Angeloni E, Vitaterna A, Lombardo P, Pirelli M, Refice S Tags: Clin Exp Hypertens Source Type: research