3α、β-RantagonistsLabetalol（拉贝洛尔.pptVIP

Chapter 9 adrenoceptor blocking drugs (Adrenoceptor antagonists) α-R antagonists β-R antagonists α、β-R antagonists Section 1 α-R antagonists α1, α2-R antagonists α1-R antagonists α2-R antagonists Basic actions of α-R antagonists 1.CVS effects (1)α1-R antagonistic effects: Endogenous CA blockage: BP↓ (Postural hypotension) Exogenous CA blockage: “adrenaline reversal” (2) α2-R antagonistic effects: presynaptic ?2 antagonism –NE release ↑ CNS ?2 antagonism -sympathetic activity ↑ Basic actions of α-R antagonists 2.other effects (1) Prostate and bladder sphincter α1-R antagonism: dilation (2) insular α2-R antagonism: insulin ↑ Classification Ⅰ. α1, α2-R antagonists 1.short-term acting: phentolamine (酚妥拉明), tolazoline (妥拉唑啉) 2. long-term acting: phenoxybenzamine(酚苄明) Ⅱ. α1-R antagonists: prazosin(哌唑嗪) Ⅲ. α2-R antagonists: yohimbine(育亨宾)  α1, α2-R antagonistsphentolamine (酚妥拉明, regitine,立其丁) competitive α-R antagonists pharmacological actions 1.vessels : dilation; BP ↓ Mechanism: (1) direct action (2) ?1-R blockade: “adrenaline reversal” pharmacological actions 2.heart: excitation, CO ↑ HR ↑ Mechanism: (1) BP ↓?excite heart (2) ?2-R blockade 3.other effects: cholinergic action histamine-like action clinical uses 1. peripheral vasospasmatic disorders: eg. Raynaud’s syndrome, 雷诺氏综合征 2. local vasoconstrictor excess (eg, NA) 3. shock : a. dilate vessel ? peripheral resistance↓ (肺血管) b. excite heart ? Co↑ c. pulse pressure↑ ?improve viscera hemoperfusion, relief microcirculation disturbance Phentolamine+ NE 4. CHF and AMI Pathophysiology: Cardia insufficiency ? arteriovenous reflex contraction Phentolamine: dilate vessel?cardiac load↓ ?Co↑ 5. diagnosis and treatment of pheochromocytoma 6. others: male sexual dysfuction 甲磺酸酚妥拉明分散片（伟哥） adverse reactions 1.cardiovas