Carvedilol ((2RS)-1-(9H-carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]propan-2-ol), a β1-, β2-, and α1-adrenoreceptor blocker drug with antioxidant and antiproliferative effects, is indicated for treatment of hypertension, stable angina pectoris, and congestive heart failure. A profile of this drug substance is provided in this chapter and includes physical characteristics of Carvedilol (e.g., UV-vis, IR, NMR, and mass spectra). Details regarding the stability of Carvedilol in the solid state and solution phase are presented and methods of analysis (compendial and literature) are summarized. Furthermore, an account of the pharmacokinetics (ADME) and synthesis of Carvedilol are presented.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/B978-0-12-407691-4.00004-6 | DOI Listing |
Pharmaceutics
December 2024
Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia.
Background/objectives: Selective laser sintering (SLS) is one of the most promising 3D printing techniques for pharmaceutical applications as it offers numerous advantages, such as suitability to work with already approved pharmaceutical excipients, the elimination of solvents, and the ability to produce fast-dissolving, porous dosage forms with high drug loading. When the powder mixture is exposed to elevated temperatures during SLS printing, the active ingredients can be converted from the crystalline to the amorphous state, which can be used as a strategy to improve the dissolution rate and bioavailability of poorly soluble drugs. This study investigates the potential application of SLS 3D printing for the fabrication of tablets containing the poorly soluble drug carvedilol with the aim of improving the dissolution rate of the drug by forming an amorphous form through the printing process.
View Article and Find Full Text PDFAntioxidants (Basel)
December 2024
Graduate Institute of Biomedical Sciences, College of Medicine, Chang Gung University, Taoyuan City 33302, Taiwan.
Hypoxia/reoxygenation (HR) often occurs under cardiac pathological conditions, and HR-induced oxidative stress usually leads to cardiomyocyte damage. Carvedilol, a non-selective β-blocker, is used clinically to treat cardiac ischemia diseases. Moreover, Carvedilol has also been reported to have an antioxidant ability by reducing lipid peroxidation.
View Article and Find Full Text PDFJ Med Case Rep
January 2025
Department of Hepatic Biliary Pancreatic Medicine, First Hospital of Jilin University, 1 Xinmin Avenue, Changchun, 130021, China.
Background: Dyskeratosis congenita is a rare genetic disease due to telomere biology disorder and characterized by heterogeneous clinical manifestations and severe complications. "Porto-sinusoidal vascular disease" has been recently proposed, according to new diagnostic criteria, to replace the term "idiopathic non-cirrhotic portal hypertension." TERT plays an important role in telomeric DNA repair and replication.
View Article and Find Full Text PDFBMC Cardiovasc Disord
January 2025
Department of Clinical Pharmacy, School of Pharmacy, College of Medicine and Health Sciences, Wollo University, Dessie, Ethiopia.
Background: Evidence-based beta-blockers are essential in managing heart failure with reduced ejection fraction (HFrEF) and are known to improve cardiovascular outcomes. Despite robust nascent guideline recommendations, studies indicate that beta-blockers are often underutilized or administered below target doses. This shivery issue is particularly relevant in Ethiopia, where comprehensive evaluations of beta-blocker utilization and dosing practices are limited.
View Article and Find Full Text PDFJ Cardiovasc Pharmacol
January 2025
Division of Clinical Physiology, Department of Cardiology, Faculty of Medicine, University of Debrecen, Debrecen, Hungary.
Positive inotropic responses upon administration of milrinone, an inhibitor of the phosphodiesterase enzyme (PDE), involve a well-pronounced positive chronotropic effect. Here we tested whether milrinone evokes this chronotropic response solely by PDE inhibition or by a concerted action that involve additional pharmacological targets. Milrinone stimulated increases in heart rate were studied in right atrial preparations of guinea pig in the presence or absence of inhibitors of putative ancillary molecular pathways or ion channels: i.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!