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Adrenergic antagonists
Chapter 11 Adrenergic antagonists 肾上腺素受体拮抗剂剂
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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
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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↑
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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
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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.
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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.
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Prazosin ['prezosɪn]哌唑嗪
Effects: Block 1 receptor Uses: Hypertension Side effects: Postural hypotension, tachycardia, nasal congestion, drowsiness (['draʊzɪnɪs] 嗜睡)
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-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↓
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2 Intrinsic sympathomimetic [,sɪmpəθəʊmɪ‘metɪk]拟交感的 activity;
3 Membrane stabilizing activity
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Uses: 1 Cardiac arrhythmias;
2 Angina [æn‘dʒaɪnə] pectoris [’pektəris] 心绞痛 3 Hypertension 4 Hyperthyroidism [,haipə'θairɔidizəm]甲亢
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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
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Typical drugs Propranolol [prəu'prænə,lɔl]普萘诺尔;
Metoprolol [mɪ'tɔprəlɔl] 美托洛尔
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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。
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Glossary Depressor reflex Gastric acid Syndrome Congestive heart failure Postural hypotension Drowsiness Angina pectoris
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