抗高血压药-英文版课件.ppt

1、 Antihypertensive drugsAntihypertensive drugshypertensionhypertensionMean arterial blood pressure is Mean arterial blood pressure is higher than the normal range,in higher than the normal range,in the case of not taking blood the case of not taking blood pressure drugs pressure drugs：Systolic blood

2、pressure Systolic blood pressure 18.7kPa(140mmHg)and18.7kPa(140mmHg)and（oror）Diastolic blood pressure Diastolic blood pressure 12.0kPa(90mmHg)12.0kPa(90mmHg)Divided into primary hypertension Divided into primary hypertension（90%95%90%95%）And secondary hypertension And secondary hypertension complica

3、tions complicationsHeart failureCoronary heart disease(CHD)Cerebrovascular accidentRenal failureAntihypertensive Antihypertensive drugsdrugsReasonable application of Reasonable application of antihypertensive drugsantihypertensive drugsControl of Control of blood blood pressurepressureDelay the Dela

4、y the formation formation and and developmendevelopment of t of atheroscleatherosclerosisrosisReduce Reduce the the complicatcomplications such ions such as brain,as brain,heart and heart and kidneykidneyReduce the Reduce the mortality mortality rate,rate,prolong prolong lifelifeBlood pressureBlood

5、pressure -The factors influencing blood The factors influencing blood pressure 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.-Nerve-fluid system on blood p

6、ressure Nerve-fluid system on blood pressure regulation regulation。main centreganglionVascular smooth muscleclonidine-methyldopaEplerenonemecamylamineReserpineguanethidine propranolol 1prazosin 1 labetalolhydralazine sodiumnitroprussidenifedipineminoxidil1.Nervous regulation:the sympathetic nervous

7、1.Nervous regulation:the sympathetic nervous systemsystemPeriphePeripheral ral neurotrneurotransmittansmitter er releasereleaseThe The postsynappostsynaptic tic membrane membrane receptorreceptorSecond,humoral regulation:Second,humoral regulation:renin angiotensin aldosterone systemrenin angiotensin

8、 aldosterone systemKidney adjacent Kidney adjacent ballballBeside the Beside the machinemachine -R-R blockersblockersreninreninAngiotensiAngiotensin originaln originalangiotensinangiotensininvertaseinvertaseACEIACEIangiotensinangiotensin Small artery contractionSmall artery contractionlosartanlosart

9、anAldosterone secretionAldosterone secretion Water sodium retentionWater sodium retentiondiureticdiuretic(thiazides)ClassificationClassificationDiureticDiureticThe sympathetic nervous depressantsThe sympathetic nervous depressants(1)central blood pressure medication(1)central blood pressure medicati

10、on(2)the ganglion block(2)the ganglion block(3)noradrenaline can nerve endings block(3)noradrenaline can nerve endings block(4)the adrenaline receptor blockers(4)the adrenaline receptor blockersAffect the renin-angiotensin system medicineAffect the renin-angiotensin system medicineA gleam of antihyp

11、ertensives:diuretic,calcium A gleam of antihypertensives:diuretic,calcium antagonist medicine,beta receptor blockers antagonist medicine,beta receptor blockers and ACEIand ACEIDiureticDiureticOn the basis of(a line)blood pressure medicationEffect in the thiazide diuretic is most commonly used,antihy

12、pertensive 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 workCan be used for various high blood pressure(basic blood pressure medication)Mild-alone,medium an

13、d severe-shareCan make the elderly hypertension patients complicated with stroke,the incidence of left heart failure and mortality is leftHydrochlorothiazideHydrochlorothiazideEarly antihypertensive mechanismWith sodium diuresis,reduce the extracellular fluid and blood volumeLong-term antihypertensi

14、ve mechanismDiuretic row sodium to Na+left aortic Diuretic row sodium to Na+left aortic smooth muscle cell,cell Na+/Ca2+smooth muscle cell,cell Na+/Ca2+exchange left-intracellular Ca2+exchange left-intracellular Ca2+left,reduce vascular smooth muscle of left,reduce vascular smooth muscle of norepine

15、phrine(NE)reactivitynorepinephrine(NE)reactivitydisadvantages disadvantages:-Blood K Blood K+、NaNa+、MgMg2+2+-Blood total cholesterol,Blood total cholesterol,triglyceride,low density lipoprotein triglyceride,low density lipoprotein cholesterol(hdl-c)cholesterol(hdl-c)-Blood uric acid Blood uric acid

16、-Blood renin Blood renin -Glucose tolerance(disabled)for Glucose tolerance(disabled)for diabetes patientsdiabetes patientsEffective diuretic(furosemide)Effective diuretic(furosemide)used in used in hypertensive crisis and poor associated with hypertensive crisis and poor associated with chronic rena

17、l hypertension patients.chronic renal hypertension patients.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 flush,blurred vision and other signs.Mech

18、anism:hyperthyroidism and circulating catecholamines increased sympathetic nervous activityClinical applicationClinical applicationA gleam of medicationApplication of the treatment for mild hypertension separatelyWith other antihypertensive drug treatment,severe hypertensionEffect of diuresis medici

19、ne of compound Effect of diuresis medicine of compound preparations with other drugspreparations with other drugsCompound antihypertension tablet:give up Compound antihypertension tablet:give up ping,hydralazine,hydrochlorothiazideping,hydralazine,hydrochlorothiazideCompound apocynum tablet:guanidin

20、e b Compound apocynum tablet:guanidine b organism,hydralazine,hydrochlorothiazideorganism,hydralazine,hydrochlorothiazideJane chrysanthemum antihypertension tablet:Jane chrysanthemum antihypertension tablet:clonidine,hydrochlorothiazideclonidine,hydrochlorothiazideCompound captopril tablets,enalapri

21、l and Compound captopril tablets,enalapril and hydrochlorothiazidehydrochlorothiazideConstant dropping pills:clonidine,Constant dropping pills:clonidine,hydralazine,hydrochlorothiazidehydralazine,hydrochlorothiazideCalcium antagonist medicineCalcium antagonist medicine Block L voltage dependent calc

22、ium channel-left intracellular Ca2+diastolic small arteryNifedipine group,horizon,lacidipine Nifedipine group,horizon,lacidipine flat,amlodipineflat,amlodipineNifedipineNifedipine【Step-down characteristics Step-down characteristics】1 1 Buck degree was positively correlated with the original high blo

23、od pressure,with normal blood pressure has no obvious antihypertensive effect；2 2 Oral absorption is good,work fastOral 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

24、and moderate hypertension；3 3 Can cause reflective heart rate Can cause reflective heart rate shareshare Receptor blockers.Receptor blockers.Clinical applicationClinical applicationLight,medium and severe Light,medium and severe hypertension treatmenthypertension treatmentNitrendipineNitrendipineSel

25、ectively ACTS on the peripheral vascular,blocking its internal flow of calcium ions,relaxing smooth muscle,the dilate blood vessels and step-downWarm and lasting antihypertensive effect,applicable to various types of high blood pressureLacidipineLacidipineIs a potent calcium antagonists,significantl

26、y and the effect of selective calcium ion channels in vascular smooth muscle.Its main role is to expand peripheral artery,reduce peripheral vascular resistance and to lower blood pressureResistance to atherosclerosisUsed for mild and moderate hypertensionName of commodity:lacidipine AmlodipineAmlodi

27、pineMore gentle,smooth effect lasting,convenience of once-daily dosage,24 hours of stability control of high blood pressure and angina pectoris,good safety and tolerabilitySimilar drugs,only it can be used by patients with congestive heart failure safetyAlso has the role of atherosclerosisAdrenaline

28、 receptor blockers Receptor blockers Receptor blockers：prazosinprazosin、terazosinterazosin、doxazosindoxazosin Receptor blockers Receptor blockers：prapranololprapranolol、atenololatenolol、labetalollabetalol、carbedilolcarbedilolMechanism of actionNonselective beta receptor blockers,mostly related with

29、the beta blocker:Heart:myocardial contraction force is abate,slow heart rate,cardiac output decreasesKidney:reduce renin secretion,inhibit RAS on blood pressure regulationThe sympathetic nerve endings presynaptic membrane:inhibition of positive feedback,NA secretion declineCentral(hypothalamus and m

30、edulla oblongata):excitatory neuron activity is abate,peripheral sympathetic nerve tension by,vascular resistance decreasedIncrease the top ring element synthesisClinical applicationSuitable for various high blood pressureWith high cardiac output or plasma renin levels has good effect on the high si

31、de of hypertensive patients,especially suitable for hypertensive patients with coronary heart disease,cerebrovascular diseaseDiuretic or pooling vasodilators can enhance curative effectatenololatenololSelective beta 1 receptor blockers,lack of internal to the sympathetic activityOral is used to trea

32、t various degree of high blood pressure,antihypertensive effect a longer durationlabetalollabetalol、Receptor blockersApplicable to various degrees of hypertension and hypertensive emergency,gestational hypertension,pheochromocytoma,high blood pressure when anesthesia or surgerycarvedilolcarvedilol）、

33、Receptor blockersUsed in the treatment of mild and moderate hypertension with renal insufficiency,diabetes,high blood pressure patientsRenin angiotensin system depressants ACEIACEI：Captopril etc.AT1-resistance：Chlorine sand,valsartan,etc【Antihypertensive mechanism】1.1.AngIIAngII Generate and functio

34、n Generate and function。Arteriovenous diastolic Arteriovenous diastolic Peripheral resistance Peripheral resistance Blood pressure Blood pressure；Block the release of aldosterone water sodium Block the release of aldosterone water sodium retention retention；2.2.Inhibition of slow excitation peptide

35、Inhibition of slow excitation peptide degradation degradation Slow excitation peptide concentrations in the blood Slow excitation peptide concentrations in the blood:produce produce NONO、PG2PG2 Etc.血管扩张血管扩张血血压压 Angiotensin converting enzyme inhibitors ACEIACEI captopril captopril（A sulfhydryl propio

36、nic 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 the electrolyte disorders;Three pairs of renal hypertensive effect is good,can treat refractory heart failure【

37、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,acute myocardial infarction patients with high blood pressureAngiotensin receptor blockers ARB AT1 receptor:v

38、ascular smooth muscle,cardiac muscle,brain,kidney and secretion of aldosterone Adrenal zona cells-has regulating effect to the stability of the cardiovascular function.losartan losartan【Antihypertensive mechanism】Selective blocking AT1 receptor:blocking angiotensin mediated blood vesselsShrinkage,al

39、dosterone release and promote vascular smooth muscle proliferation and effect Peripheral resistance Promoting uric acid excretion,inhibiting renal tubule of uric acid absorption,short【Clinical application of】Each period high blood pressureStep-down features:1.The oral work fast2.The role to maintain

40、 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 oedema;But still can cause low blood pressure and high potassium.For patients with pregnancy.Promoting uric acid excretion,inhibiting renal tubule of uric ac

41、id absorption,shortPharmacological effectsPharmacological effects Diastolic small artery smooth muscle,reduce the peripheral vascular resistance,lower blood pressureWith heart rate slows,decreased cardiac outputInhibit the secretion of gastrointestinal tract and movement and the protection of gastri

42、c mucosaBuck with sedationReduce intraocular pressure,do not affect the pupil and the adjustment of the lensPharmacological action and Pharmacological action and mechanismmechanismActivate Activate I I1 1-imidazoline receptor-imidazoline receptor，Make the Make the peripheral sympathetic activity dec

43、line,peripheral sympathetic activity decline,vasodilation,blood pressure dropsvasodilation,blood pressure dropsThe excited central postsynaptic membrane receptor alpha 2Lower levels of plasma renin and aldosteroneInhibit the secretion of gastrointestinal tract and movement and the protection of gast

44、ric 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 obviousClonidineClonidineProcess in t

45、he 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 excretionClinical applicationClinical applicationFirst-line treatment invalid moderately hi

46、gh 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 glaucomaAdverse reactionsDry mouth,sleepiness,constipation,impotence,can happen occasionally bradycardi

47、aWater 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.And long-term medication made the alpha 2 weeks the presynaptic membrane receptor sensitivity,negative feedback e

48、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 reducedThe other central blood pressure medicationmethyldopamethyldopaA me

49、dium to strong step-down,cardiovascular and output,less influence renal blood flowSuitable for renal hypertension and moderate hypertensive patients with poor kidney function,often with thiazide diuretic sharemoxonidinemoxonidineFor Il receptor affinity is high,and the receptor is strong,biological

50、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,dry mouth greatly reduce adverse reactionsVasodilation medicineDirectly to relax vascular smooth muscle,decrease peripheral resistance and bl