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Related Concept Videos

Adrenergic Antagonists: Pharmacological Actions of β-Receptor Blockers01:27

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β-receptor blockers significantly impact the cardiovascular system by counteracting catecholamine-induced sympathetic responses. These medications decrease heart rate, contractility, and cardiac output, potentially leading to cardiac depression, life-threatening bradycardia, and death. Therapeutically, β-blockers function as mild antihypertensives and are utilized in treating angina pectoris and cardiac arrhythmias. However, nonselective β-blockers inhibit β2-receptors in...
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β receptors are classified into three subclasses: β1, β2, and β3. β1 receptors are primarily located in the heart and kidneys. When they get activated, they increase heart rate, contractility, and renin release. This process enhances blood pressure and aids in stress management. In contrast, β2 receptors are situated mainly in the lungs, blood vessels, and skeletal muscles. Upon activation, they trigger smooth muscle relaxation, causing bronchodilation and...
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β-adrenergic antagonists, or β-blockers, modulate the sympathetic nervous system by targeting β-adrenoceptors and inhibiting catecholamine-mediated sympathetic responses. β-blockers differ in their adrenoceptor subtype affinity, lipophilicity, and α-blocking capabilities. The history of β-blocker development began with the prototype, dichloroisoprenaline, which exhibited partial agonist activity. As a result, propranolol was developed as a pure antagonist but...
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Adrenergic Antagonists: ɑ and β-Receptor Blockers

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Third-generation β-blockers, such as labetalol and carvedilol, represent a significant advancement in managing cardiovascular conditions. Unlike conventional β-blockers, which can induce peripheral vasoconstriction, third-generation drugs block α1 adrenoceptors. This promotes vasodilation through several mechanisms, such as increased nitric oxide production, inhibition of calcium ion entry, opening of potassium ion channels, and antioxidant action. Labetalol, for instance, is...
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Heart Failure Drugs: β-Blockers01:22

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β-adrenergic antagonists, commonly known as β-blockers, block the effects of sympathetic neurotransmitters such as noradrenaline (NA) and adrenaline (ADR). They have several beneficial effects in heart failure treatment. They reduce heart rate, the force of contraction, and cardiac muscle relaxation. They also slow the atrial-ventricular conduction rate and raise the threshold for arrhythmias. The concentration of β-blockers determines their effects on bronchodilation,...
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Antihypertensive Drugs: Action of β1 Blockers01:17

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β1-receptors are primarily located in the heart and kidneys. In cardiac myocytes, these receptors interact with neurotransmitters released by the sympathetic nervous system during heightened activity or danger. As a result, β1-receptors get activated, initiating a series of biochemical processes. Excessive activation of beta receptors due to chronic stress can abnormally increase heart rate and contractility, resulting in high blood pressure or hypertension. To counteract this,...
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Bisoprolol: A comprehensive profile.

Ahmed H Bakheit1, Raisuddin Ali2, Ali D Alshahrani3

  • 1Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia; Department of Chemistry, Faculty of Science and Technology, Al-Neelain University, Khartoum, Sudan.

Profiles of Drug Substances, Excipients, and Related Methodology
|January 19, 2021
PubMed
Summary

This study provides a comprehensive profile of Bisoprolol, detailing its physicochemical properties, analytical methods, and structural characteristics. It also covers thermal analysis and recent pharmacokinetic analysis techniques for this important cardiovascular drug.

Keywords:
BisoprololDescriptionMethod of analysisPharmacokineticsPhysical characteristicsStabilitySynthesisUses

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Area of Science:

  • Pharmaceutical Sciences
  • Analytical Chemistry

Background:

  • Bisoprolol is a widely used beta-blocker for cardiovascular conditions.
  • A thorough understanding of its properties is crucial for quality control and drug development.

Purpose of the Study:

  • To present a detailed profile of Bisoprolol.
  • To outline its physicochemical properties, analytical methods, and structural characterization.

Main Methods:

  • Physicochemical characterization (pKa, solubility, X-ray diffraction).
  • Analytical method development and validation (spectroscopic, chromatographic, CE).
  • Thermal analysis (DSC, TGA) and structural confirmation (FTIR, NMR).

Main Results:

  • Comprehensive data on Bisoprolol's properties, including melting point and hydration states.
  • Established methods for its identification and quantification.
  • Mass fragmentation pattern and pharmacokinetic analysis techniques reported.

Conclusions:

  • The study offers a complete monograph for Bisoprolol.
  • Provides essential data for researchers and pharmaceutical industries.
  • Highlights advanced analytical techniques for Bisoprolol assessment.