微 信 题 库 搜 索
精品课程
热门课程
>
外科 妇产科 儿科
内科学 生理学 更多
药学专业
药理学 中药学 药物化学
生药学 卫生毒理学 更多
中医专业
中医基础理论 中医学 更多
口腔专业
口腔内科 口腔外科 更多
 医学全在线 > 精品课程 > 药理学 > 南华大学 > 正文
药理学授课教案-第四篇 心血管系统药理:第二十三章 肾素-血管紧张素系统药理
来源:南华大学资源网 更新:2013/9/10 字体:

生命科学与技术学院

教 案 首 页

教研室:药理学  教师姓名:欧和生

课 程名 称

药理学

授课专业及班次

临床医学专业

授课内 容

肾素-血管紧张素系统药理

授课方式

授课时数

理论讲授

2学时

1. 熟悉肾素-血管紧张素系统对心血管系统的生理机制。
2. 掌握ACEI和血管紧张素II受体I型阻滞剂的药理作用及其机制。
3. 掌握卡托普利氯沙坦的药理作用、临床应用及主要不良反应。

重点

1. ACEI和血管紧张素II受体I型阻滞剂的药理作用及其机制。

2. 托普利和氯沙坦等药物的药理作用、临床应用。

难点

肾素-血管紧张素系统对心血管系统调节的生理机制及药物作用机制。

授课内容及时间分配

1.   Renin-Aangiotensin-System (20 分钟)

2.   Angiotensin converting enzyme inhibitors (ACEI) (45分钟)

3.   The blockade of angiotension II receptor (20 分钟)

4.   小结、布置思考题、安排下次课内容 (5分钟)

教具教材

多媒体加版书

教材:杨宝峰 主编:药理学 人民卫生出版社,北京,2003年

1.  周宏灏主编:药理学 科学出版社,北京,2003年

2.  Pharmacology : 天津医科大学药理教研室主编,1999年

3.  H.P. Rang, M.M Dale, J.M. Ritter P.K. Moore. Pharmacology ( the fifth edition). 2003.


Part 1  Renin-Aangiotensin-System

 

Introduction

1.Element of RAS (renin, angiotensinogen,angiotensin, ACE, ATR)

Renin is an enzyme that acts on angiotensinogen to catalyze the formation of the decapeptide angiotensin I.

Angiotensin I is then cleaved by ACE to yield the octapeptide angiotensin II.

ATR: AT1R, AT2R

2.The regulation effect of RAS on blood pressure

The renin-angiotensinsystem is an important participant in both the short-and long-term regulationof arterial blood pressure.

Angiotensin II acts in several ways to increase totalperipheral resistance and thereby contributes to the short-term regulation ofarterial blood pressure. Perhaps the more important is the ability of angiotensin II to inhibit excretion of Na+ and water by thekidneys.

Angiotensin II – induced changes in renal functionplay an important role in long-term stabilization of arterial blood pressure.

Part 2  Angiotensinconverting enzyme inhibitors (ACEI)

1.Pharmacological effects

(1) Inhibit the formation of Ang II.

 (2) Maintain the activity of brandykinin (BK).

 (3) Protection of endothelium andanti-atherosclerosis

 (4) Anti-iscamiaand protection of myocardial cell

 (5) Increase the sensitivity of insulin

(6) Inhibit the pathological cardiovascular remodeling

2. Clinical uses

(1) Hypertension

(2) CHF and myocardial infarction

(3) DMEM and nephropathy

3. Untoward effects

(1) Hypotension: occurring in the first use.

(2) Cough: of 6 ~ 12%

(3) Hyperkalemia

(4) Low blood sugar

(5) Renal function trauma

(6) Affection of the development of fetus and newborn.

(7) Neuro Oedema.

(8) Malfunction of taste, tetter (thedrugs with –SH).

4.The drugs of ACEI.

. Captopril

Pharmacological Action :

 i  Directly inhibited ACE. (IC50:23 ~ 35 nmol /L), The depressor effect associated with the activitystate of RAS.

ii   The protection of heart is relatedto abolishing of ROS, such as iscamia.

Pharmacokinetics

o  Absorption : Po, F=75%. Taction :30 min. Tmax=1h.

o  Distribution: extensivelydistributed in body , Pb=30%.

o  Metabolism: oxygen in –SH.

o  Excretion: from kidney: 40-50%in parent drug and the others in metabolites.

Clinical uses

o  Hypertension: single or combination.

o  CHF

o  Cardiac infarct.

o  DMEM-nephropathy (only captopril).

Untoward effects

Apart fromthe common side effect, cough is usually complaint.

Enalapril

o  Action : the action of inhibition of ACE is 10 times stronger than captopril.

o  The absorption is not affectedby food. Po. TP=4-6h.  Tmaintain=24h,q.d.

o  Metabolism: enalaprilat(MK22)

o  Distribution extensively inbody. T1/2: 11h.

o  Excretion from kidney.

o  Uses: hypertensionwww.med126.com/sanji/ and CHF.

o  Aside effect: cough ,hypotension, hyperkalemiaetc.

Fosinopril

o  Prodrug (poo-): fosinoprilacid is the activity chemical.

o  Tp=3-6 h

o  Pb=95%

o&www.med126.com/kuaiji/nbsp; T1/2=12h

o  Distribution : heart and brain(much)

o  Excretion: from liver and kidney,  no toxicityaccumulation for light malfunction of kidney.

o  No use:lactation

Lisinopril

benazepril

Part 3  The blockade of angiotension II receptor

losartan、valsartan、erbesartan、candesartan、tasosartan、eprosartan、telmisartan

1. Pharmacological effects and mechanism

 (1) Block the AT1R   vasodilatation 

     Aldostrone  Hypotension

 


(2) Block theAT1R Renin  AngII AT2RBK-NO 

Vasodilatation, regression of remodeling Hypotension.

Losartan

1.Pharmacological effects

(1)AT1R: Losartan block AT1R>AT2R (2-3万倍).   EXP3174 >losartanin  blocking  AT1R  (10- 40 times)

(2)Vasodilate renalartery, decrease reabsorption of water and Na+in renal tube.

(3)Protect kidney:Hypertension,DM and failure of kidney.

(4)Inhibit vascular remodeling.

2. Clinical uses

 (1) Hypertension

 (2)CHF

3. Untoward effects: less than ACEI, avoid use with low efficacy diuretics.

Part 4 Howabout combination of AT1Ranta and ACEI

  1. Increase effects(cure in hypertension, CHF), decrease disadvantage of the two class drugs.

  2. Have not found anyadverse effects

Questions:

1. Describe the advantages anddisadvantages of AT1R and ACEI in therapeutics of hypertension.

2. what is thecommon side effect of Captopril?

相关文章
 临床检验基础参考文献:第十七章各系统脱落
 医学微生物学教学图片资源:图片12
 卫生统计学电子教材:第三章
 护理学基础参考文献:参考网站
 内科学授课教案:肺血栓栓塞症教案
 内科学图片库:肠、腹膜结核升结肠溃疡、糜
   触屏版       电脑版       全站搜索       网站导航   
版权所有:医学全在线(m.med126.com)
网站首页
频道导航
医学论坛
返回顶部