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Chapter 10
Adrenoceptor Antagonist Drugs;Review: The Major effects of
AdrR activation;;Adrenoceptor Antagonist (Blocker) Drugs:
Competitive or petitive blockers
Bind to adrRs
Inactive or partially active adrRs
Classification:
α adrenoceptor antagonists
β adrenoceptor antagonists
α and β adrenoceptor antagonists;α-antagonists;Mechanism of Action;Pharmacologic Effects and clinical application;Dilate small artery venule?Peripheral resistance↓?BP↓? Orthostatic hypotension
2. Baroreflex ?HR↑(tachycardia);A. Hypertensive emergencies;Other Effects of α1-blockers;
Urinary Obstruction (Major application)
Used to improve urine flow of BPH patients
Prazosin,?doxazosin, and?tamsulosin (preferred)
;What Is benign prostatic hyperplasia (BPH)?
a non-cancerous enlargement of the prostate
;Contract smooth muscle of tract
→↓resistance to the flow of urine;Subtype-selective?α1A,D-receptor antagonists may have improved?efficacy and safety, such as?tamsulosin?with minor effects on blood pressure at a low dose.?;α2 blocker;Applications of α2?Blockers;α2 blocker;The effects of α-antagonism on dog’s BP change induced by Epinephrine.
;A. Pheochromocytoma (Major application);What’s pheochromocytoma?
A ?neuroendocrine tumor?of the?medulla?of the?adrenal glands?or sympathetic ganglion cells
Catecholamines↑
Symptoms:hypertension, headaches, palpitations, and increased sweating.;;Agents;Structure of several α-receptor–blocking drugs.;Comparison of α Adrenergic Receptor Antagonists;Agents;Agents;Summary of α-receptor antagonists;β-antagonists;James W. Black held his Nobel Lecture on 8 December 1988, at Karolinska Institutet, Stockholm. He was presented by Professor Folke Sj?qvist of the Karolinska Institutet, due to the contribution of “Drugs from Emasculated Hormones: The Principles of Syntopic Antagonism”. In this research, he made a series of beta antagonists, including propranolol.;β agonist;Mode of actions;Pharmacologic effects ;with caution in patients with asthm
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