浙江大学医学院：《药理学》课程教学资源（PPT讲稿）肾上腺素受体拮抗药 Adrenoceptor Antagonists

Part 5 Adrenoceptor Antagonists 1. at receptor antagonists 2. B receptor antagonists 3. a, B receptor antagonists

Part 5 Adrenoceptor Antagonists 1.  receptor antagonists 2.  receptor antagonists 3. ,  receptor antagonists

13585 12850 160 200 190/124 16082 175/110 13590 210 Epinephrine before phentolamine 12585 100/35 HR 210 Epinephrine after phentolamine Top: Effects of phentolamine, an areceptor-blocking drug, on blood pressure in an anesthetized dog. Epinephrine reversal is demonstrated by tracings showing the response to epinephrine before (middle)and after(bottom) phentolamine. All drugs given intravenously. (BP, blood pressure HR, heart rate. Epinephrine reversal(肾上腺素作用的翻转)

Epinephrine reversal （肾上腺素作用的翻转）

1. at receptor antagonists 0 1-1 a1, O, receptor antagonists a Short-acting Phentolamine酚妥拉明 CH3 N——CH2 HO

1.  receptor antagonists 1-1 1 , 2 receptor antagonists Short-acting Phentolamine 酚妥拉明 N N CH3 HO N CH2 H

1. at receptor antagonists 口1.1 Pharmacolog u() Vasodilatation Blocking a, receptor; direct action u(2)Stimulating heart Reflex; blocking a, receptor w Ne release T 3)Cholinergic and histamine -like eflects Contraction of GI smooth muscles, 0 Gastric acid secretion T

1.1 Pharmacology (1) Vasodilatation Blocking 1 receptor; direct action (2) Stimulating heart Reflex；blocking 2 receptor ～NE release  (3) Cholinergic and histamine-like effects Contraction of GI smooth muscles, Gastric acid secretion  1.  receptor antagonists

1. at receptor antagonists 日1.2 Clinical uses u(1) Peripheral vascular diseases Acrocyanosis, Raynaud's disease d(2) Local vasoconstrictor extravasation

1.2 Clinical uses (1) Peripheral vascular diseases Acrocyanosis, Raynaud’s disease (2) Local vasoconstrictor extravasation 1.  receptor antagonists

1. at receptor antagonists u(3)Shock cardiac output个; 0 redistribution of blood flow. shift of fluid from interstitial compartment to vascular compartment; u pulmonary pressure u should be used after fully adequate replacement of intravascular fluid

(3) Shock cardiac output ; redistribution of blood flow; shift of fluid from interstitial compartment to vascular compartment; pulmonary pressure ; should be used after fully adequate replacement of intravascular fluid 1.  receptor antagonists

1. at receptor antagonists d() Acute myocardial infarction and congestive heart failure after-oad↓; cardiac output个 2. CAPACITANCE Venules 3. PUMP OUTPUT CNS Sympathetic nerves 4. VOLUME 1. RESISTANCE Kidneys Arterioles Re Aldosterone-+- Angiotensin

(4) Acute myocardial infarction and congestive heart failure after-load  ； cardiac output  1.  receptor antagonists

1. at receptor antagonists u(5) Pheochromocytoma pre-and post-operation uses a diagnosis (6) Others: impotency(阳痿)

(5) Pheochromocytoma pre- and post-operation uses diagnosis (6) Others: impotency (阳痿) 1.  receptor antagonists

1. at receptor antagonists u 1.3 Adverse effects a(1)Postural hypotension u(2) Reflex heart stimulation u tachycardia, arrhythmia, angina pectoris u 3)GI reactions u(4)Other central depression

1.3 Adverse effects (1) Postural hypotension (2) Reflex heart stimulation tachycardia, arrhythmia, angina pectoris (3) G.I. reactions (4) Other central depression 1.  receptor antagonists

1. at receptor antagonists T0 lazoline妥拉唑啉 weak effects more severe adverse eftects

Tolazoline 妥拉唑啉 weak effects more severe adverse effects 1.  receptor antagonists