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

2. 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

3. 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↑

5. 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

6. 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.

7. 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.

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

9. -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↓

10. 2 Intrinsic sympathomimetic [,sɪmpəθəʊmɪ‘metɪk]拟交感的 activity;
3 Membrane stabilizing activity

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

12. 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

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

14. 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。

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