Inhibitory effects of antihypertensive drugs on human cytochrome P450 2J2 activity: Potent inhibition by azelnidipine and manidipine.
Abstract
The inhibitory effects of antihypertensive drugs (dihydropyridine calcium channel blockers, angiotensin II receptor blockers, and angiotensin-converting enzyme inhibitors) on cytochrome P450 2J2 (CYP2J2) activity were examined. Amlodipine, azelnidipine, barnidipine, benidipine, cilnidipine, efonidipine, felodipine, manidipine, nicardipine, nifedipine, nilvadipine, nisoldipine, nitrendipine, telmisartan, delapril, and quinapril inhibited luciferin-2J2/4F12 O-dealkylase activity of recombinant human CYP2J2 in a concentration-dependent manner (IC50 = 0.116-9.19 μM). Kinetic analyses of the inh...
Source: Chemico-Biological Interactions - April 5, 2019 Category: Molecular Biology Authors: Ikemura N, Yamaori S, Kobayashi C, Kamijo S, Murayama N, Yamazaki H, Ohmori S Tags: Chem Biol Interact Source Type: research
Experimental autoimmune myocarditis in rats and therapeutic histamine H1 - H4 receptor inhibition.
Authors: Stasiak A, Gola J, Kraszewska K, Mussur M, Kobos J, Mazurek U, Stark H, Fogel WA
Abstract
Myocarditis, a life threatening disease, is still not adequately treated. Histamine plays an important role in physiology and pathophysiology of cardiovascular system. All four histamine receptors (H1R - H4R), are present in the heart. Experimental autoimmune myocarditis (EAM) was used to investigate which histamine receptor had a greater impact on the disease's progression. EAM was evoked in Lewis rats by porcine myosin immunization. Mepyramine, ranitidine and ciproxifan were used to inhibit H1R, H2R and H3R...
Source: Journal of Physiology and Pharmacology - March 23, 2019 Category: Drugs & Pharmacology Tags: J Physiol Pharmacol Source Type: research
Comparative effectiveness of generic and brand-name medication use: A database study of US health insurance claims
ConclusionsIn this study, we observed that use of generics was associated with comparable clinical outcomes to use of brand-name products. These results could help in promoting educational interventions aimed at increasing patient and provider confidence in the ability of generic medicines to manage chronic diseases. (Source: PLoS Medicine)
Source: PLoS Medicine - March 12, 2019 Category: Internal Medicine Authors: Rishi J. Desai Source Type: research
Beneficial effect of combined spironolactone and quinapril treatment on thrombosis and hemostasis in 2K1C hypertensive rats.
Abstract
A strong correlation between raised aldosterone levels and increased risk of thrombotic disorders has been provided. Clinical studies have demonstrated the benefits of the addition of the aldosterone receptor antagonist to the standard therapy with angiotensin-converting enzyme inhibitor in the reduction of cardiovascular events in patients. We suggest that the benefits of this dual renin-angiotensin-aldosterone system (RAAS) blockade may be related to the drug's effects on the hemostatic and oxidative balance. Thus, we investigated the effect of combined spironolactone (SPIRO) and quinapril (QUIN...
Source: J Physiol Pharmacol - April 1, 2018 Category: Drugs & Pharmacology Authors: Gromotowicz-Poplawska A, Stankiewicz A, Mikita J, Aleksiejczuk M, Marcinczyk N, Szemraj J, Chabielska E Tags: J Physiol Pharmacol Source Type: research
The effect of antihypertensive treatment on arterial stiffness and serum concentration of selected matrix metalloproteinases.
CONCLUSIONS: In patients with arterial hypertension, beside age and systolic blood pressure, the determinants of arterial stiffness include serum MMP-3 concentration. For drugs compared in the study with the same hypotensive effect obtained, the arterial stiffness reduction effect is not dependent on the drug used. Systolic blood pressure is one of the independent factors responsible for the reduction of arterial stiffness in the course of antihypertensive treatment.
PMID: 28721143 [PubMed] (Source: Archives of Medical Science)
Source: Archives of Medical Science - July 20, 2017 Category: General Medicine Tags: Arch Med Sci Source Type: research
The Effect of Combined Treatment with the (Pro)Renin Receptor Blocker HRP and Quinapril in Type 1 Diabetic Rats
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.Kidney Blood Press Res 2017;42:109 –122 (Source: Kidney and Blood Pressure Research)
Source: Kidney and Blood Pressure Research - March 30, 2017 Category: Urology & Nephrology Source Type: research
Rapid analysis of drug dissolution by paper spray ionization mass spectrometry
Publication date: 20 March 2017 Source:Journal of Pharmaceutical and Biomedical Analysis, Volume 136 Author(s): Yang Liu, Ning Liu, Ya-nan Zhou, Lan Lin, Lan He With a great quantity of solid dosage tested by dissolution technology, developing a rapid and sensitive method to access the content of drug within dissolution media is highly desired by analysts and scientists. Traditionally, dissolution media is not compatible with mass spectrometry since the inorganic salts in the media might damage the mass spectrometer. Here, paper spray ionization mass spectrometry (PSI-MS), one of the ambient mass spectrometry techno...
Source: Journal of Pharmaceutical and Biomedical Analysis - January 6, 2017 Category: Drugs & Pharmacology Source Type: research
Treatment for hereditary angioedema with normal C1 ‐INH and specific mutations in the F12 gene (HAE‐FXII)
We report our experience treating HAE‐FXII with discontinuation of potential trigger factors and drug therapies. The study included 72 patients with HAE‐FXII. Potential triggers included estrogen‐containing oral contraceptives (eOC), hormonal replacement therapy, or angiotensin‐converting enzyme inhibitors. Drug treatment comprised plasma‐derived C1 inhibitor (pdC1‐INH) for acute swelling attacks and progestins, tranexamic acid, and danazol for the prevention of attacks. Discontinuation of eOC was effective in 25 (89.3%) of 28 women and led to a reduction in the number of attacks (about 90%). After ending hormo...
Source: Allergy - November 30, 2016 Category: Allergy & Immunology Authors: K. Bork, K. Wulff, G. Witzke, J. Hardt Tags: Brief Communication Source Type: research
Treatment of hereditary angioedema with normal C1 ‐INH and specific mutations in the F12 gene (HAE‐FXII)
ConclusionsFor patients with HAE‐FXII various treatment options are available which completely or at least partially reduce the number or duration of attacks.This article is protected by copyright. All rights reserved. (Source: Allergy)
Source: Allergy - November 5, 2016 Category: Allergy & Immunology Authors: K. Bork, K. Wulff, G. Witzke, J. Hardt Tags: Brief Communication Source Type: research
Quinapril decreases antifibrinolytic and prooxidative potential of propofol in arterial thrombosis in hypertensive rats
Angiotensin converting enzyme inhibitors and propofol both exert hypotensive action and may affect hemostasis. We investigated the influence of quinapril and propofol on hemodynamics and hemostasis in renal-hypertensive rats with induced arterial thrombosis. Two-kidney, one clip hypertensive rats were treated with quinapril (3.0 mg/kg for 10 days), and then received propofol infusion (15 mg/kg/h) during ongoing arterial thrombosis. The hemodynamic and hemostatic parameters were assayed. Quinapril exerted a hypotensive effect increasing after propofol infusion. Quinapril showed an antithrombotic effect with the platelet adh...
Source: Journal of the Renin-Angiotensin-Aldosterone System : JRAAS - May 10, 2016 Category: Biomedical Science Authors: Wojewodzka-Zelezniakowicz, M., Kisiel, W., Kramkowski, K., Gromotowicz-Poplawska, A., Zakrzeska, A., Stankiewicz, A., Kolodziejczyk, P., Szemraj, J., Ladny, J. R., Chabielska, E. Tags: Original Article Source Type: research
Modulation of acute transient exercise-induced hypertension after oral administration of four angiotensin-converting enzyme inhibitors in normotensive horses
In conclusion, administration of PO benazepril at a dose of 0.5 mg/kg modulated physiological hypertension induced by exercise in horses that were otherwise normotensive. (Source: The Veterinary Journal)
Source: The Veterinary Journal - October 23, 2015 Category: Veterinary Research Source Type: research
β-blocker Therapy is Not Associated with Reductions in Angina or Cardiovascular Events After Coronary Artery Bypass Graft Surgery: Insights from the IMAGINE Trial
Conclusions
β-blocker therapy after CABG is not associated with reductions in angina or cardiovascular events in low-risk patients with preserved LVEF, and may not be systematically indicated in such patients. (Source: Cardiovascular Drugs and Therapy)
Source: Cardiovascular Drugs and Therapy - June 14, 2015 Category: Cardiology Source Type: research
Application of quantitative NMR for purity determination of standard ACE inhibitors
This study investigated the accuracy of the quantitative NMR method for purity determination of ACE inhibitors reference standards and the discovery of two pairs of new diastereoisomers. Six types of ACE inhibitors, imidapril hydrochloride, benazepril hydrochloride, lisinopril, enalapril maleate, quinapril hydrochloride, and captopril were quantificated and validated for the qNMR method by discussing factors that affect parameters of the qNMR experiment, internal standards, integration, pH-effect, and uncertainty. The results were compared with data obtained by the mass balance method. The study found that maleic acid infl...
Source: Journal of Pharmaceutical and Biomedical Analysis - June 12, 2015 Category: Drugs & Pharmacology 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
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, 4...
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
