抗高血壓藥-英文版課件

1、 Antihypertensive drugs Antihypertensive drugshypertensionMean 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%）

2、And secondary hypertensionhypertensionMean arterial bloo complicationsHeart failureCoronary heart disease (CHD)Cerebrovascular accidentRenal failure complicationsHeart failureAntihypertensive drugsReasonable application of antihypertensive drugsControl of blood pressureDelay the formation and develo

3、pment of atherosclerosisReduce the complications such as brain, heart and kidneyReduce the mortality rate, prolong lifeAntihypertensive drugsReasonabBlood pressure - The factors influencing blood pressure ： Cardiac output :heart rate, myocardial contraction force, change of blood volume, etc.;Periph

4、eral resistance: the length of the blood vessels and blood viscosity, blood vessels, radius, etc.- Nerve - fluid system on blood pressure regulation 。Blood pressure - The factors imain centreganglionVascular smooth muscleclonidine-methyldopaEplerenonemecamylamineReserpineguanethidinepropranolol1praz

5、osin1 labetalolhydralazine sodium nitroprussidenifedipineminoxidil1.Nervous regulation: the sympathetic nervous systemPeripheral neurotransmitter releaseThe postsynaptic membrane receptormain centreganglionVascular smSecond, humoral regulation: renin angiotensin aldosterone systemKidney adjacent bal

6、lBeside the machine -R blockersreninAngiotensin originalangiotensininvertaseACEIangiotensin Small artery contractionlosartanAldosterone secretionWater sodium retentiondiuretic(thiazides)Second, humoral regulation: KiClassificationDiureticThe sympathetic nervous depressants(1) central blood pressure

7、medication(2) the ganglion block(3) noradrenaline can nerve endings block(4) the adrenaline receptor blockersAffect the renin - angiotensin system medicineA gleam of antihypertensives: diuretic, calcium antagonist medicine, beta receptor blockers and ACEIClassificationDiureticDiureticOn the basis of

8、 (a line) blood pressure medicationEffect in the thiazide diuretic is most commonly used, antihypertensive effect is mild, persistent, long-term application of no significant resistanceFeatures:Antihypertensive effect is weak, by an average of 10%2 3 weeks after the majority of patients in medical w

9、orkCan be used for various high blood pressure (basic blood pressure medication)Mild - alone, medium and severe - shareCan make the elderly hypertension patients complicated with stroke, the incidence of left heart failure and mortality is leftDiureticOn the basis of (a linHydrochlorothiazideEarly a

10、ntihypertensive mechanismWith sodium diuresis, reduce the extracellular fluid and blood volumeLong-term antihypertensive mechanismDiuretic row sodium to Na + left aortic smooth muscle cell, cell Na + / Ca2 + exchange left - intracellular Ca2 + left, reduce vascular smooth muscle of norepinephrine (N

11、E) reactivityHydrochlorothiazideEarly antihdisadvantages : - Blood K+、Na+、Mg2+ - Blood total cholesterol, triglyceride, low density lipoprotein cholesterol (hdl-c) - Blood uric acid - Blood renin - Glucose tolerance (disabled) for diabetes patientsEffective diuretic (furosemide) used in hypertensive

12、 crisis and poor associated with chronic renal hypertension patients.disadvantages : - Blood Hypertensive crisis Patients with high blood pressure in the short term, the blood pressure increased significantly, and appear have a headache, be agitated, palpitation, sweating, nausea, vomiting, or pale

13、flush, blurred vision and other signs.Mechanism: hyperthyroidism and circulating catecholamines increased sympathetic nervous activityHypertensive crisisClinical applicationA gleam of medicationApplication of the treatment for mild hypertension separatelyWith other antihypertensive drug treatment, s

14、evere hypertensionClinical applicationA gleam ofEffect of diuresis medicine of compound preparations with other drugsCompound antihypertension tablet: give up ping, hydralazine, hydrochlorothiazideCompound apocynum tablet: guanidine b organism, hydralazine, hydrochlorothiazideJane chrysanthemum anti

15、hypertension tablet: clonidine, hydrochlorothiazideCompound captopril tablets, enalapril and hydrochlorothiazideConstant dropping pills: clonidine, hydralazine, hydrochlorothiazideEffect of diuresis medicine ofCalcium antagonist medicine Block L voltage dependent calcium channel - left intracellular

16、 Ca2 + diastolic small arteryNifedipine group, horizon, lacidipine flat, amlodipineCalcium antagonist medicine BlNifedipine【 Step-down characteristics 】1 Buck degree was positively correlated with the original high blood pressure, with normal blood pressure has no obvious antihypertensive effect ；2

17、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 Can cause reflective heart rate share Receptor blockers.Nifedipine【 Step-down

18、characteClinical applicationLight, medium and severe hypertension treatmentClinical applicationLight, medNitrendipineSelectively ACTS on the peripheral vascular, blocking its internal flow of calcium ions, relaxing smooth muscle, the dilate blood vessels and step-downWarm and lasting antihypertensiv

19、e effect, applicable to various types of high blood pressureNitrendipineSelectively ACTS oLacidipineIs 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 resi

20、stance and to lower blood pressureResistance to atherosclerosisUsed for mild and moderate hypertensionName of commodity: lacidipine LacidipineIs a potent calcium AmlodipineMore gentle, smooth effect lasting, convenience of once-daily dosage, 24 hours of stability control of high blood pressure and a

21、ngina pectoris, good safety and tolerabilitySimilar drugs, only it can be used by patients with congestive heart failure safetyAlso has the role of atherosclerosisAmlodipineMore gentle, smooth Adrenaline receptor blockers Receptor blockers ：prazosin、terazosin、doxazosin Receptor blockers ：prapranolol

22、、atenolol、labetalol、carbedilolAdrenaline receptor blockersMechanism of actionNonselective beta receptor blockers, mostly related with the beta blocker:Heart: myocardial contraction force is abate, slow heart rate, cardiac output decreasesKidney: reduce renin secretion, inhibit RAS on blood pressure

23、regulationThe sympathetic nerve endings presynaptic membrane: inhibition of positive feedback, NA secretion declineCentral (hypothalamus and medulla oblongata) : excitatory neuron activity is abate, peripheral sympathetic nerve tension by, vascular resistance decreasedIncrease the top ring element s

24、ynthesisMechanism of actionNonselectivClinical applicationSuitable for various high blood pressureWith high 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 dise

25、aseDiuretic or pooling vasodilators can enhance curative effectClinical applicationSuitable fatenololSelective beta 1 receptor blockers, lack of internal to the sympathetic activityOral is used to treat various degree of high blood pressure, antihypertensive effect a longer durationatenololSelective

26、 beta 1 receplabetalol、 Receptor blockersApplicable to various degrees of hypertension and hypertensive emergency, gestational hypertension, pheochromocytoma, high blood pressure when anesthesia or surgerylabetalol、 Receptor blockerscarvedilol）、 Receptor blockersUsed in the treatment of mild and mod

27、erate hypertension with renal insufficiency, diabetes, high blood pressure patientscarvedilol）、 Receptor blockeRenin angiotensin system depressants ACEI： Captopril etc. AT1 - resistance ： Chlorine sand, valsartan, etc ACEI： Captopril etc.【 Antihypertensive mechanism 】 1.AngII Generate and function 。

28、 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 : produce NO、PG2 Etc. 血管擴張血壓 Angiotensin converting enzyme inhibitors ACE

29、I captopril （ A sulfhydryl propionic acid pulp ）【 Antihypertensive mechanism 】【 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 the electrolyte disorders;Three pairs of

30、 renal hypertensive effect is good, can treat refractory heart failure【 Function characteristics 】【 application 】 Each period high blood pressure. Important first-line drugs.Especially suitable for complicated with diabetes and insulin resistance and left ventricular hypertrophy, heart failure, acut

31、e myocardial infarction patients with high blood pressure【 application 】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. losar

32、tan【 Antihypertensive mechanism 】Selective blocking AT1 receptor: blocking angiotensin mediated blood vesselsShrinkage, aldosterone release and promote vascular smooth muscle proliferation and effect Peripheral resistance Promoting uric acid excretion, inhibiting renal tubule of uric acid absorption

33、, shortAngiotensin receptor blocker【 Clinical application of 】Each period high blood pressureStep-down features:The oral work fast2. The role to maintain for a long time: 24 h smoothstep-down, 3 6 weeks for maximum effect【 side effect 】 relatively less ACEI:Attracted less dry cough and angioneurotic

34、 oedema;But still can cause low blood pressure and high potassium. For patients with pregnancy.Promoting uric acid excretion, inhibiting renal tubule of uric acid absorption, short抗高血壓藥_英文版課件Pharmacological effects Diastolic small artery smooth muscle, reduce the peripheral vascular resistance, lowe

35、r blood pressureWith heart rate slows, decreased cardiac outputInhibit the secretion of gastrointestinal tract and movement and the protection of gastric mucosaBuck with sedationReduce intraocular pressure, do not affect the pupil and the adjustment of the lensPharmacological effects DiastPharmacolo

36、gical action and mechanismActivate I1-imidazoline receptor， Make the peripheral sympathetic activity decline, vasodilation, blood pressure dropsThe excited central postsynaptic membrane receptor alpha 2Lower levels of plasma renin and aldosteroneInhibit the secretion of gastrointestinal tract and mo

37、vement and the protection of gastric mucosaStatic 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

38、 obviousPharmacological action and mecClonidineProcess in the bodyAbsorption: oral absorptionDistribution: easy through the blood brain barrier, plasma protein combined rate of 30%Metabolism: 50% in intrahepatic metabolismDischarge: metabolic product and prototype by renal excretionClonidineProcess

39、in the bodyClinical applicationFirst-line treatment invalid moderately high blood pressure, with thiazide diuretic or other antihypertensive agents share can improve the curative effectRenal hypertensionPatients with high blood pressure of peptic ulcerPrimary open-angle glaucomaClinical applicationF

40、irst-lineAdverse reactionsDry mouth, sleepiness, constipation, impotence, can happen occasionally bradycardiaWater sodium retentionDrug withdrawal syndrome: a long-term drug withdrawal may suddenly appear have a headache, tremor, abdominal pain, sweating, heart palpitations and blood pressure surge.

41、 And long-term medication made the alpha 2 weeks the presynaptic membrane receptor sensitivity, negative feedback effect is reduced, sudden withdrawal, increased sympathetic nervous function is associated with increased NE release. Recovery for medicine or alpha receptor blockers (e.g., phentolamine

42、) can alleviate. Withdrawal should be gradually reducedAdverse reactionsDry mouth, slThe other central blood pressure medicationmethyldopaA medium to strong step-down, cardiovascular and output, less influence renal blood flowSuitable for renal hypertension and moderate hypertensive patients with po

43、or kidney function, often with thiazide diuretic sharemoxonidineFor Il receptor affinity is high, and the receptor is strong, biological t1/2 longer, once a day dosingSuitable for patients with mild and moderate hypertensionOn the central and peripheral alpha 2 receptor function is weak, the calm, d

44、ry mouth greatly reduce adverse reactionsThe other central blood pressuVasodilation medicineDirectly to relax vascular smooth muscle, decrease peripheral resistance and blood pressure to dropLong-term use antihypertensive vasodilators has the following disadvantagesCan theexcited sympathetic nerve,

45、reflective increase cardiac output, heart rate speed upIncrease of renin and aldosterone secretion, leading to water and sodium retentionA long time with easy toleranceWith a diuretic or adrenaline receptor blockers share can enhance curative effect, reduce adverse reactionsVasodilation medicineDire

46、ctly Sodium nitroprussideAntihypertensive effects associated with an increased NO - GC - cGMP, can dilate blood vessels and inhibit platelet aggregationOf arterioles and venules vascular smooth muscle were diastolic function, antihypertensive effect strong, rapid and shortMainly used in the treatmen

47、t of hypertensive crisis. Also used in congestive heart failure, acute myocardial infarction and controlling hypertension during anesthesiaBecause of excessive step-down can cause nausea, vomiting, sweating, restlessness, palpitations and headacheSodium nitroprussideAntihypertGanglion block medicine

48、mecamylamine 【 Function characteristics 】Antihypertensive effect strong, quickly;2. Has inhibitory effect on both sympathetic and parasympathetic, adverse reactions, and the heavier, orthostatic hypotension; The parasympathetic ganglion block symptoms.3. Hypertensive crisis.Ganglion block medicinePr

49、azosinProcess in the bodyAbsorption: good oral absorption, first eliminate the obvious, bioavailability of 60%Distribution: the combination of plasma protein rate was 97%Metabolism: liver metabolismDischarge: most bile excretion, by a small number of urinePrazosinProcess in the bodyPharmacological e

50、ffects and mechanism of actionAlpha 1 receptors on postsynaptic membrane of vascular smooth muscle are highly selective blocking effectStep-down features:A medium to strong antihypertensive effectDont affect kidney function, improve the level of reninLong-term use can improve lipid metabolismBlock 1

51、 receptor alpha, relieve dysuria prostate patientsPharmacological effects and meClinical applicationCan be separately used treatment of mild and moderate hypertensionFor elderly patients with hypertension combined prostatic hypertrophy, can improve the symptoms of dysuriaSevere hypertension share di

52、uretic and beta receptor blockers can enhance step-down effectClinical applicationCan be sepAdverse reactionsFirst agent phenomenon: some patients for the first time 0.5 1 hour after the treatment can appear orthostatic hypotension, dizziness, sweating, heart palpitations and reactionLong-term use can cause water sodium retention, diuresis medicine can maint