Adrenergic antagonists Chapter 11 Adrenergic antagonists 肾上腺素受体拮抗剂剂

Subtypes and effects of adrenergic receptors Presynaptic membrane α2 receptor inhibiting the release of NA β receptor promoting the release of NA α 1受体 Promoting the contracting of the vascular smooth muscle in skin, mucosa [mjuː‘kəʊsə] 粘膜, and kidney β受体 β1 receptor excitation of the heart β2受体 Relaxing the smooth muscle of bronchus [‘brɒŋkəs] 支气管 Relaxing the smooth muscle of coronary artery, and blood vessels in skeletal muscle Negative feedback Positive feedback Pupil 瞳孔 dilation  Postsynaptic membrane

α-receptor antagonists Phentolamine [fen'tɔləmi:n] 酚妥拉明 Effects 1 Decreasing blood pressure based on vasodilation effect; 2 Cardiac stimulation based on depressor reflex减压反射: heart contractility ↑, heart rate ↑, cardiac output↑

3 Cholinergic [,kəʊlɪ‘nɜːdʒɪk] 拟胆碱的 effects: Increasing glandular secretion; promoting the contracting of smooth muscle. 4 Histamine like effects: Increasing gastric acid secretion; lead to skin flush

Uses: 1 Peripheral vascular diseases: Raynaud’s syndrome 雷诺氏综合征, thromboangiitis [,θrɔmbəu,ændʒi'aitis]血栓血管炎; 2 Local vasoconstrictor血管收缩剂 excess; 3 Shock； 4 Pheochromocytoma [fi:əkrəuməsai'təumə]嗜铬细胞瘤; 5 Congestive heart failure.

Adverse effects 1 Postural hypotension (体位性低血压); 2 Tachycardia; 3 Nasal [‘neɪz(ə)l]鼻的 congestion (鼻粘膜充血) ; 4 Gastrointestinal stimulation.

Prazosin ['prezosɪn]哌唑嗪 Effects: Block 1 receptor Uses: Hypertension Side effects: Postural hypotension, tachycardia, nasal congestion, drowsiness (['draʊzɪnɪs] 嗜睡)

-adrenoceptor blocking drugs (-adrenoceptor antagonists) 1 2 receptor blockade effects (1) Heart: 1 blockade→HR↓, heart conductivity↓, contractility↓, CO↓; (2) 2 blockade→ vasoconstriction↑; (3) 2 blockade→ bronchoconstriction [,brɔŋkəukən'strikʃən]支气管狭窄; (4) Renin secretion↓

2 Intrinsic sympathomimetic [,sɪmpəθəʊmɪ‘metɪk]拟交感的 activity; 3 Membrane stabilizing activity

Uses: 1 Cardiac arrhythmias; 2 Angina [æn‘dʒaɪnə] pectoris [’pektəris] 心绞痛 3 Hypertension 4 Hyperthyroidism [,haipə'θairɔidizəm]甲亢

Adverse effects Contraindication: 1 Induction or exacerbation [ek,sæsə‘beɪʃən] 恶化of asthma; 2 Inhibition of cardiac function; 3 Withdraw syndrome. Contraindication: Asthma Serious heart failure

Typical drugs Propranolol [prəu'prænə,lɔl]普萘诺尔； Metoprolol [mɪ'tɔprəlɔl] 美托洛尔

大纲要求 1．掌握普萘洛尔的作用、用途、不良反应、禁忌症。 2．熟悉美托洛尔的作用特点。 3．了解吲哚洛尔的作用特点，α受体阻断药的作用、用途、不良反应。

Glossary Depressor reflex Gastric acid Syndrome Congestive heart failure Postural hypotension Drowsiness Angina pectoris