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Carvedilol - DOAJ

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Last Updated: 10 January 2023

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Effect of P-glycoprotein Inhibitor (Carvedilol) on Developmental Outcome Methotrexate are Given Alone and in Combination of Pregnant Rats

During pregnancy and breastfeeding cycles, dosing in male and 2 weeks in female rats was divided randomly into four groups orally administered 0. 72 mg/kg methotrexate, combined doses carvedilol+methotrexate, and distilled water for 2 months in male and two weeks. The results of fertility index tests in Cv-TG, MTX-TG, and Cv+MTX-TG were markedly lower than those in the control group, with lower gestation index in MTX-TG and Cv+MTX-TG reported in MTX-TG and Cv-MTX-TG significantly lower than those in Cv-TG and Cv+MTX-TG and Cv-MTX-TG and Cv+MTX-TG as a In both the fetus and pups of Cv+MTX-TG group's present findings, it is suggested that blocking P-gp by carvedilol could raise the placental passage and rise methotrexate concentration in fetal and pupsu2019 tissue as a result of increased toxic exposure of methotrexate.

Source link: https://doi.org/10.30539/ijvm.v46i2.1410


Validation of a quantitative multiplex LC-MS/MS assay of carvedilol, enalaprilat, and perindoprilat in dried blood spots from heart failure patients and its cross validation with a plasma assay

Adherence to medications is a determinant of heart disease-related illnesses such as heart failure and heart failure. Dried blood spots are commonly used for drug testing due to less stringent transportation and storage requirements. Objects: To quantitatively validate a LC-MS/MS system for simultaneous quantification of carvedilol, enalaprilat, and perindoprilat in DBS, assay assay, and determine the likelihood of using the method as an adherence determination assay. From a pharmacokinetic pilot study, To verify the assay more clinically by establishing correlation and agreement between plasma and DBS samples. Enalaprilat's full range of dosages of the pharmacokinetic pilot study may be quantified for enalaprilat, but not for carvedilol and perindoprilat. For more than 67 percent of samples for all analytes, the difference between the observed and calculated plasma concentrations was less than 20% of their mean. DBS and plasma concentrations can be used interchangeably, owing to the equivalence between measured and predicted plasma concentrations.

Source link: https://doi.org/10.1016/j.jmsacl.2022.12.003


Central composite design for the development of carvedilol-loaded transdermal ethosomal hydrogel for extended and enhanced anti-hypertensive effect

The central composite scheme may be used to enhance ethosomal formulation. The in-vitro drug development showed steady delivery of carvedilol from ethosomes and ethosomal hydrogel. The ethosomal gel showed increased penetration of carvedilol throughout the skin relative to free carvedilol-loaded hydrogel. In addition, ethosomal hydrogels in rats showed a gradual decrease in blood pressure for 24 h in rats. Conclusions: Central Composite Designed can be used for successful refinement of carvedilol-loaded ethosomes formulation, as well as the most promising transdermal delivery system for carvedilol. In addition, the carvedilol-loaded ethosomal gel can extend the anti-hypertensive action of carvedilol for a longer time than free carvedilol, demonstrating its therapeutic value in future clinics.

Source link: https://doi.org/10.1186/s12951-021-00833-4


Formulation and Characterization of Carvedilol Leciplex for Glaucoma Treatment: In-Vitro, Ex-Vivo and In-Vivo Study

After 30 min and the duration of the trial lasted for 24 hours, Carvedilol leciplex's intraocular pressure dropped to a normal range in ocular hypertensive rabbits after 30 minutes, while the carvedilol solution returned IOP to a healthy level after 60 min and duration of the trial lasted for 6 h.

Source link: https://doi.org/10.3390/pharmaceutics10040197


Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol

Although Carvedilol developed 1:1 inclusion complexes, those with RAMEB appear to be more effective than those with u03b3CD. RAMEB's complexity added to the drug's photochemical stability in a diluted solution, contributing to the drug's photochemical stability.

Source link: https://doi.org/10.3390/pharmaceutics13111746


Formulation and Characterization of Acetazolamide/Carvedilol Niosomal Gel for Glaucoma Treatment: In Vitro and In Vivo Study

Acetazolamide is a diuretic used in glaucoma treatment and has several side effects; it is also used in kidney diuretics; it is also used in skin cancer therapy. Two different ratios were created and tested on Sixty's niosome formulations containing Span 20, Span 60, Tween 20, and Tween 60 with two different ratios. After 1 h and sustained vigor for four days, the combined formula was exposed to an in vivo investigation of intraocular pressure in ocular hypertensive rabbits for 60 h. The improved glaucomatous eye retinal atrophy was shown by histological analysis of rabbit eyeballs treated with the chosen treatment.

Source link: https://doi.org/10.3390/pharmaceutics13020221


Topical Delivery of Carvedilol Loaded Nano-Transfersomes for Skin Cancer Chemoprevention

In vitro and in vivo, the u03b2-blocker carvedilol has been shown to prevent skin carcinogenesis. Mouse epidermal JB6 P+ cells at non-toxic levels were inhibited by EGF-mediated neoplastic transformation of mouse epidermal JB6 P+ cells at non-toxic levels, but only in mice with high concentrations caused cytotoxicity in JB6 P+ and human keratinocytes HaCaT. Comparing to the free drug, F18 was released through the dialysis membrane and permeated through the porcine ear skin at a slower rate, but the skin's epidermis and dermis were depositing the drug. According to these results, transfersome is a promising topical delivery system for preventing ultraviolet-induced skin damage and carcinogenesis.

Source link: https://doi.org/10.3390/pharmaceutics12121151


Doxazosin and Carvedilol Treatment Improves Hepatic Regeneration in a Hamster Model of Cirrhosis

An important goal in the treatment of liver cirrhosis is proper regulation of fibrosis' mechanisms. Consequently, u03b1/u03b2 adrenoblockers have been used as an alternative therapy for persistent liver lesions such as fibrosis and/or cirrhosis, as well as potential liver transplantation. During tissue repair in a hamster model of liver cirrhosis, We herein investigated the effects of doxazosin and carvedilol treatments. Tissue samples were analyzed by H&E and PAS to determine tissue damage, and Sirius red to determine collagen fiber content. TIMP-2 decreased and MMP-13 increased in animals treated with adrenoblockers with respect to the group with cirrhosis. Furthermore, the concentrations of u03b1-SMA and TGF-u03b2 decreased with both drugs relative to placebo, p 0. 05. Hence, doxazosin and carvedilol could be used to treat hepatic cirrhosis in hamsters as a result of collagen depletion in the hepatic parenchyma.

Source link: https://doi.org/10.1155/2018/4706976


Heart rate reduction as a marker to optimize carvedilol treatment and enhance myocardial recovery in pediatric dilated cardiomyopathy

Introduction: An elevated heart rate is correlated with an elevated risk of death or cardiac transplant in children with dilated cardiomyopathy. This is a multicenter retrospective review of all children with DCM between 2013 and 2020, with LVEF 40% and treated with carvedilol. The relationship between HRR and LVEF, left ventricular end-diastolic and end-systolic diameter, was determined before and after HRR with carvedilol was determined using regression analysis. 100 patients were enrolled. HRR reported a dramatic decrease in LVESd and LVEF recovery up to 15% at the three-year follow-up. It is also shown that HRR can be used as a diagnostic marker to diagnose HF in children.

Source link: https://doi.org/10.3389/fphys.2022.1001752


UHPLC Enantiomer Resolution for the ɑ/β-Adrenoceptor Antagonist R/S -Carvedilol and Its Major Active Metabolites on Chiralpak IB N-5

Carvedilolamine, a racemic lipophilic aryloxy propanolamine, acts as a targeted u03b1 1 -adrenoreceptor antagonist and a nonselective u03b1 1 -adrenoreceptor antagonist. Desmethyl carvedilol, 4u2032-hydroxy carvedilol, and 5u2032-hydroxy carvedilol are three primary metabolites that are most prevalent in CAR metabolism: desmethyl carvedilol, 4u2032-hydroxy carvedilol, 4u2032-hydroxy carvedilol and 5u2032-hydroxy carvedilol are three key metabolites. On a suitable chiral stationary phase, the current study seeks to determine the response surface for the parent CAR's enantiomer separation as well as the key metabolites. In a first screening phase, an experimental design was used, followed by central-composite layout for delimitation of the four enantiomeric pairs in least run time. In order to select the most significant quality attributes, the effect of chromatographic variables on critical peaks resolution and adjusted retention time was investigated. The validated assay was applied to plasma samples from cardiovascular patients treated with rac -CAR.

Source link: https://doi.org/10.3390/molecules27154998

* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions

* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions