上海交通大学：《药理学 Pharmacology》课程教学资源（讲义课件）ADRENOCEPTOR ANTAGONIST DRUGS

SECTION II AUTONOMIC DRUGS CHAPTER 11 ADRENOCEPTOR ANTAGONIST DRUGS

SECTION II AUTONOMIC DRUGS CHAPTER 11 ADRENOCEPTOR ANTAGONIST DRUGS

Adrenoceptor: a-adrenoceptor, a:agonist:phenylephrine;antagonist:prazosin VSM;(+Radial M.of iris;heart;liver a2:agonist:clonidine;antagonist:yohimbine VSM;platelet;fat cell;pre-synaptic receptor B-adrenoceptor, B1:agonist:dobutamine;antagonist:metoprolol heart kidney B2:agonist:tebutaline;antagonist:butoxamine smooth M;skeletal M;liver B3:agonist:propranolol;antagonist:NA fat tissue

Adrenoceptor: -adrenoceptor, including: - 1 : agonist: phenylephrine; antagonist: prazosin VSM; (+) Radial M. of iris; heart; liver - 2 : agonist: clonidine; antagonist: yohimbine VSM; platelet; fat cell; pre-synaptic receptor -adrenoceptor, including: - 1 : agonist: dobutamine; antagonist: metoprolol heart & kidney - 2 : agonist: tebutaline; antagonist: butoxamine smooth M; skeletal M; liver - 3 : agonist: propranolol; antagonist: NA fat tissue

TOPIC1 Alpha adrenergic receptor antagonists

TOPIC1 Alpha adrenergic receptor antagonists

Alpha adrenergic receptor antagonists - phentolamine 【Mechanism】 Pentolamine has similar affinity for both and o,receptors.It is a competitive antagonist.It has wide spectrum of pharmacological specificities. Short-term blocker

Alpha adrenergic receptor antagonists -- phentolamine 【 Mechanism 】 Pentolamine has similar affinity for both 1 and 2 receptors. It is a competitive antagonist. It has wide spectrum of pharmacological specificities. Short-term  blocker

Alpha adrenergic receptor antagonists phentolamine Effects on cardiovascular system a.Vasodilation:decrease peripheral resistance b.Cardiac stimulation:increase cardiac output.reflex sympathetic nerve stimulation

Alpha adrenergic receptor antagonists -- phentolamine Effects on cardiovascular system a. Vasodilation: decrease peripheral resistance b. Cardiac stimulation: increase cardiac output. reflex sympathetic nerve stimulation

Alpha adrenergic receptor antagonists- phentolamine 【therapeutic uses.】 a.pheochromocytoma b.Hypertensive emergency C. peripheral vascular disease:vasospasm of Raynaud's disease and frostbite d.Local vasoconstrictor excess

Alpha adrenergic receptor antagonists -- phentolamine 【therapeutic uses 】 a. pheochromocytoma b. Hypertensive emergency c. peripheral vascular disease: vasospasm of Raynaud's disease and frostbite d. Local vasoconstrictor excess

Alpha adrenergic receptor antagonists phenoxybenzamine Irreversibly block a and a receptors.Long-term a blocker. 【pharmacological properties】 attenuates catecholamine-induced vasoconstriction 【therapeutic uses】 pheochromocytoma peripheral vascular disease: Septic shock

Alpha adrenergic receptor antagonists -- phenoxybenzamine • Irreversibly block 1 and 2 receptors. Long-term  blocker. 【pharmacological properties 】 • attenuates catecholamine-induced vasoconstriction 【therapeutic uses 】 • pheochromocytoma • peripheral vascular disease: • Septic shock

TOPIC2 Beta adrenergic receptor antagonists

TOPIC2 Beta adrenergic receptor antagonists

B-Blocker B-Receptor blocks receptor 100ml Stroke volume 1 sec B-Blockade β1-Stmulation A.B-Sympatholytics:effect on cardiac function

a B2 a B2 B2-BlockadeB2-Stimulation B2-Blockade ±P2-Stimuletion B.B-Sympatholytics:effect on bronchial and vascular tone