1、Antihypertensive drugs,hypertension,Mean arterial blood pressure is higher than the normal range, in the case of not taking blood pressure drugs ： Systolic blood pressure 18.7kPa(140mmHg)and（or） Diastolic blood pressure 12.0kPa(90mmHg) Divided into primary hypertension （90%95%） And secondary hyperte

2、nsion,complications,Heart failure Coronary heart disease (CHD) Cerebrovascular accident Renal failure,Antihypertensive drugs,Reasonable application of antihypertensive drugs,Control of blood pressure,Delay the formation and development of atherosclerosis,Reduce the complications such as brain, heart

3、 and kidney,Reduce the mortality rate, prolong life,Blood pressure,- The factors influencing blood pressure ： Cardiac output :heart rate, myocardial contraction force, change of blood volume, etc.; Peripheral resistance: the length of the blood vessels and blood viscosity, blood vessels, radius, etc

4、. - Nerve - fluid system on blood pressure regulation 。,1.Nervous regulation: the sympathetic nervous system,Peripheral neurotransmitter release,The postsynaptic membrane receptor,Second, humoral regulation: renin angiotensin aldosterone system,Kidney adjacent ball Beside the machine,-R blockers,ren

5、in,Angiotensin original,angiotensin,invertase,ACEI,angiotensin ,Small artery contraction,losartan,Aldosterone secretion,Water sodium retention,diuretic,(thiazides),Classification,Diuretic The sympathetic nervous depressants (1) central blood pressure medication (2) the ganglion block (3) noradrenali

6、ne can nerve endings block (4) the adrenaline receptor blockers Affect the renin - angiotensin system medicine A gleam of antihypertensives: diuretic, calcium antagonist medicine, beta receptor blockers and ACEI,Diuretic,On the basis of (a line) blood pressure medication Effect in the thiazide diure

7、tic is most commonly used, antihypertensive effect is mild, persistent, long-term application of no significant resistance Features: Antihypertensive effect is weak, by an average of 10% 2 3 weeks after the majority of patients in medical work Can be used for various high blood pressure (basic blood

8、 pressure medication) Mild - alone, medium and severe - share Can make the elderly hypertension patients complicated with stroke, the incidence of left heart failure and mortality is left,Hydrochlorothiazide,Early antihypertensive mechanism With sodium diuresis, reduce the extracellular fluid and bl

9、ood volume Long-term antihypertensive mechanism Diuretic row sodium to Na + left aortic smooth muscle cell, cell Na + / Ca2 + exchange left - intracellular Ca2 + left, reduce vascular smooth muscle of norepinephrine (NE) reactivity,disadvantages :,- Blood K+、Na+、Mg2+ - Blood total cholesterol, trigl

10、yceride, low density lipoprotein cholesterol (hdl-c) - Blood uric acid - Blood renin - Glucose tolerance (disabled) for diabetes patients Effective diuretic (furosemide) used in hypertensive crisis and poor associated with chronic renal hypertension patients.,Hypertensive crisis Patients with high b

11、lood pressure in the short term, the blood pressure increased significantly, and appear have a headache, be agitated, palpitation, sweating, nausea, vomiting, or pale flush, blurred vision and other signs. Mechanism: hyperthyroidism and circulating catecholamines increased sympathetic nervous activi

12、ty,Clinical application,A gleam of medication Application of the treatment for mild hypertension separately With other antihypertensive drug treatment, severe hypertension,Effect of diuresis medicine of compound preparations with other drugs,Compound antihypertension tablet: give up ping, hydralazin

13、e, hydrochlorothiazide Compound apocynum tablet: guanidine b organism, hydralazine, hydrochlorothiazide Jane chrysanthemum antihypertension tablet: clonidine, hydrochlorothiazide Compound captopril tablets, enalapril and hydrochlorothiazide Constant dropping pills: clonidine, hydralazine, hydrochlor

14、othiazide,Calcium antagonist medicine,Block L voltage dependent calcium channel - left intracellular Ca2 + diastolic small artery Nifedipine group, horizon, lacidipine flat, amlodipine,Nifedipine,【 Step-down characteristics 】 1 Buck degree was positively correlated with the original high blood press

15、ure, with normal blood pressure has no obvious antihypertensive effect ； 2 Oral absorption is good, work fast: sublingual administering 1-5 minutes work - in the treatment of variant angina pectoris, hypertensive crisis. Oral 30 to 60 minutes work - treatment of mild and moderate hypertension ； 3 Ca

16、n cause reflective heart rate share Receptor blockers.,Clinical application,Light, medium and severe hypertension treatment,Nitrendipine,Selectively ACTS on the peripheral vascular, blocking its internal flow of calcium ions, relaxing smooth muscle, the dilate blood vessels and step-down Warm and la

17、sting antihypertensive effect, applicable to various types of high blood pressure,Lacidipine,Is a potent calcium antagonists, significantly and the effect of selective calcium ion channels in vascular smooth muscle. Its main role is to expand peripheral artery, reduce peripheral vascular resistance

18、and to lower blood pressure Resistance to atherosclerosis Used for mild and moderate hypertension Name of commodity: lacidipine,Amlodipine,More gentle, smooth effect lasting, convenience of once-daily dosage, 24 hours of stability control of high blood pressure and angina pectoris, good safety and t

19、olerability Similar drugs, only it can be used by patients with congestive heart failure safety Also has the role of atherosclerosis,Adrenaline receptor blockers, Receptor blockers ：prazosin、terazosin、doxazosin Receptor blockers ：prapranolol、atenolol、labetalol、carbedilol,Mechanism of action,Nonselec

20、tive beta receptor blockers, mostly related with the beta blocker: Heart: myocardial contraction force is abate, slow heart rate, cardiac output decreases Kidney: reduce renin secretion, inhibit RAS on blood pressure regulation The sympathetic nerve endings presynaptic membrane: inhibition of positi

21、ve feedback, NA secretion decline Central (hypothalamus and medulla oblongata) : excitatory neuron activity is abate, peripheral sympathetic nerve tension by, vascular resistance decreased Increase the top ring element synthesis,Clinical application,Suitable for various high blood pressure With high

22、 cardiac output or plasma renin levels has good effect on the high side of hypertensive patients, especially suitable for hypertensive patients with coronary heart disease, cerebrovascular disease Diuretic or pooling vasodilators can enhance curative effect,atenolol,Selective beta 1 receptor blocker

23、s, lack of internal to the sympathetic activity Oral is used to treat various degree of high blood pressure, antihypertensive effect a longer duration,labetalol,、 Receptor blockers Applicable to various degrees of hypertension and hypertensive emergency, gestational hypertension, pheochromocytoma, h

24、igh blood pressure when anesthesia or surgery,carvedilol）,、 Receptor blockers Used in the treatment of mild and moderate hypertension with renal insufficiency, diabetes, high blood pressure patients,Renin angiotensin system depressants,ACEI： Captopril etc. AT1 - resistance ： Chlorine sand, valsartan

25、, etc,【 Antihypertensive mechanism 】 1.AngII Generate and function 。 Arteriovenous diastolic Peripheral resistance Blood pressure ； Block the release of aldosterone water sodium retention ； 2. Inhibition of slow excitation peptide degradation Slow excitation peptide concentrations in the blood : pro

26、duce NO、PG2 Etc. 血管擴(kuò)張血壓,Angiotensin converting enzyme inhibitors ACEI,captopril （ A sulfhydryl propionic acid pulp ）,【 Function characteristics 】 1 orally active, work fast, antihypertensive effect of medium strong; 2 without reflective heart rate, long-term use without resistance, not easy to cause

27、 the electrolyte disorders; Three pairs of renal hypertensive effect is good, can treat refractory heart failure,【 application 】 Each period high blood pressure. Important first-line drugs. Especially suitable for complicated with diabetes and insulin resistance and left ventricular hypertrophy, hea

28、rt failure, acute myocardial infarction patients with high blood pressure,Angiotensin receptor blockers ARB AT1 receptor: vascular smooth muscle, cardiac muscle, brain, kidney and secretion of aldosterone Adrenal zona cells - has regulating effect to the stability of the cardiovascular function. los

29、artan 【 Antihypertensive mechanism 】 Selective blocking AT1 receptor: blocking angiotensin mediated blood vessels Shrinkage, aldosterone release and promote vascular smooth muscle proliferation and effect Peripheral resistance Promoting uric acid excretion, inhibiting renal tubule of uric acid absor

30、ption, short,【 Clinical application of 】 Each period high blood pressure Step-down features: The oral work fast 2. The role to maintain for a long time: 24 h smooth step-down, 3 6 weeks for maximum effect 【 side effect 】 relatively less ACEI: Attracted less dry cough and angioneurotic oedema; But st

31、ill can cause low blood pressure and high potassium. For patients with pregnancy. Promoting uric acid excretion, inhibiting renal tubule of uric acid absorption, short,Pharmacological effects,Diastolic small artery smooth muscle, reduce the peripheral vascular resistance, lower blood pressure With h

32、eart rate slows, decreased cardiac output Inhibit the secretion of gastrointestinal tract and movement and the protection of gastric mucosa Buck with sedation Reduce intraocular pressure, do not affect the pupil and the adjustment of the lens,Pharmacological action and mechanism,Activate I1-imidazol

33、ine receptor， Make the peripheral sympathetic activity decline, vasodilation, blood pressure drops The excited central postsynaptic membrane receptor alpha 2 Lower levels of plasma renin and aldosterone Inhibit the secretion of gastrointestinal tract and movement and the protection of gastric mucosa

34、 Static note clonidine can produce booster for a short period of time (associated with peripheral alpha 2 receptor excited), followed by a long period of time the step-down (central role). Oral with the central role of the dominant, the booster effect is not obvious,Clonidine,Process in the body Abs

35、orption: oral absorption Distribution: easy through the blood brain barrier, plasma protein combined rate of 30% Metabolism: 50% in intrahepatic metabolism Discharge: metabolic product and prototype by renal excretion,Clinical application,First-line treatment invalid moderately high blood pressure,

36、with thiazide diuretic or other antihypertensive agents share can improve the curative effect Renal hypertension Patients with high blood pressure of peptic ulcer Primary open-angle glaucoma,Adverse reactions,Dry mouth, sleepiness, constipation, impotence, can happen occasionally bradycardia Water s

37、odium retention Drug withdrawal syndrome: a long-term drug withdrawal may suddenly appear have a headache, tremor, abdominal pain, sweating, heart palpitations and blood pressure surge. And long-term medication made the alpha 2 weeks the presynaptic membrane receptor sensitivity, negative feedback e

38、ffect is reduced, sudden withdrawal, increased sympathetic nervous function is associated with increased NE release. Recovery for medicine or alpha receptor blockers (e.g., phentolamine) can alleviate. Withdrawal should be gradually reduced,The other central blood pressure medication,methyldopa A me

39、dium to strong step-down, cardiovascular and output, less influence renal blood flow Suitable for renal hypertension and moderate hypertensive patients with poor kidney function, often with thiazide diuretic share moxonidine For Il receptor affinity is high, and the receptor is strong, biological t1

40、/2 longer, once a day dosing Suitable for patients with mild and moderate hypertension On the central and peripheral alpha 2 receptor function is weak, the calm, dry mouth greatly reduce adverse reactions,Vasodilation medicine,Directly to relax vascular smooth muscle, decrease peripheral resistance

41、and blood pressure to drop Long-term use antihypertensive vasodilators has the following disadvantages Can theexcited sympathetic nerve, reflective increase cardiac output, heart rate speed up Increase of renin and aldosterone secretion, leading to water and sodium retention A long time with easy to

42、lerance With a diuretic or adrenaline receptor blockers share can enhance curative effect, reduce adverse reactions,Sodium nitroprusside,Antihypertensive effects associated with an increased NO - GC - cGMP, can dilate blood vessels and inhibit platelet aggregation Of arterioles and venules vascular

43、smooth muscle were diastolic function, antihypertensive effect strong, rapid and short Mainly used in the treatment of hypertensive crisis. Also used in congestive heart failure, acute myocardial infarction and controlling hypertension during anesthesia Because of excessive step-down can cause nause

44、a, vomiting, sweating, restlessness, palpitations and headache,Ganglion block medicine mecamylamine 【 Function characteristics 】 Antihypertensive effect strong, quickly; 2. Has inhibitory effect on both sympathetic and parasympathetic, adverse reactions, and the heavier, orthostatic hypotension; The

45、 parasympathetic ganglion block symptoms. 3. Hypertensive crisis.,Prazosin,Process in the body Absorption: good oral absorption, first eliminate the obvious, bioavailability of 60% Distribution: the combination of plasma protein rate was 97% Metabolism: liver metabolism Discharge: most bile excretio

46、n, by a small number of urine,Pharmacological effects and mechanism of action,Alpha 1 receptors on postsynaptic membrane of vascular smooth muscle are highly selective blocking effect Step-down features: A medium to strong antihypertensive effect Dont affect kidney function, improve the level of ren

47、in Long-term use can improve lipid metabolism Block 1 receptor alpha, relieve dysuria prostate patients,Clinical application,Can be separately used treatment of mild and moderate hypertension For elderly patients with hypertension combined prostatic hypertrophy, can improve the symptoms of dysuria S

48、evere hypertension share diuretic and beta receptor blockers can enhance step-down effect,Adverse reactions,First agent phenomenon: some patients for the first time 0.5 1 hour after the treatment can appear orthostatic hypotension, dizziness, sweating, heart palpitations and reaction Long-term use can cause water sodium retention, diuresis medicine can m