抗高血压药-整理英文版课件.ppt

1、 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%）And secondary hypertension co

2、mplicationsHeart failureCoronary heart disease(CHD)Cerebrovascular accidentRenal failureAntihypertensive drugsReasonable application of antihypertensive drugsControl of blood pressureDelay the formation and development of atherosclerosisReduce the complications such as brain,heart and kidneyReduce t

3、he mortality rate,prolong lifeBlood 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.-Nerve-fluid system on blood pres

4、sure regulation。main centreganglionVascular smooth muscleclonidine-methyldopaEplerenonemecamylamineReserpineguanethidine propranolol 1prazosin 1 labetalolhydralazine sodiumnitroprussidenifedipineminoxidil1.Nervous regulation:the sympathetic nervous systemPeripheral neurotransmitter releaseThe postsy

5、naptic membrane receptorSecond,humoral regulation:renin angiotensin aldosterone systemKidney adjacent ballBeside the machine-R-R blockersreninAngiotensin originalangiotensininvertaseACEIangiotensin Small artery contractionlosartanAldosterone secretionWater sodium retentiondiuretic(thiazides)Classifi

6、cationDiureticThe sympathetic nervous depressants(1)central blood pressure 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 rece

7、ptor blockers and ACEIDiureticOn the basis of(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 afte

8、r the majority of patients in medical workCan 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 leftHydrochlorothiazideEarly

9、 antihypertensive 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(NE)reactivityd

10、isadvantages:-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 crisis and poor associated with chronic renal hypertension

11、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.Mechanism:hyperthyroidism and circulating catecholamine

12、s increased sympathetic nervous activityClinical applicationA gleam of medicationApplication of the treatment for mild hypertension separatelyWith other antihypertensive drug treatment,severe hypertensionEffect of diuresis medicine of compound preparations with other drugsCompound antihypertension t

13、ablet:give up ping,hydralazine,hydrochlorothiazideCompound apocynum tablet:guanidine b organism,hydralazine,hydrochlorothiazideJane chrysanthemum antihypertension tablet:clonidine,hydrochlorothiazideCompound captopril tablets,enalapril and hydrochlorothiazideConstant dropping pills:clonidine,hydrala

14、zine,hydrochlorothiazideCalcium antagonist medicine Block L voltage dependent calcium channel-left intracellular Ca2+diastolic small arteryNifedipine group,horizon,lacidipine flat,amlodipineNifedipine【Step-down characteristics】1 Buck degree was positively correlated with the original high blood pres

15、sure,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 Can cause refl

16、ective heart rate share Receptor blockers.Clinical applicationLight,medium and severe hypertension treatmentNitrendipineSelectively 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

17、e effect,applicable to various types of high blood pressureLacidipineIs 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 and to lower blood pressure

18、Resistance to atherosclerosisUsed for mild and moderate hypertensionName of commodity:lacidipine AmlodipineMore 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

19、 be used by patients with congestive heart failure safetyAlso has the role of atherosclerosisAdrenaline receptor blockers Receptor blockers：prazosin、terazosin、doxazosin Receptor blockers：prapranolol、atenolol、labetalol、carbedilolMechanism of actionNonselective beta receptor blockers,mostly related wi

20、th 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 an

21、d medulla 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

22、 side of hypertensive patients,especially suitable for hypertensive patients with coronary heart disease,cerebrovascular diseaseDiuretic or pooling vasodilators can enhance curative effectatenololSelective beta 1 receptor blockers,lack of internal to the sympathetic activityOral is used to treat var

23、ious degree of high blood pressure,antihypertensive effect a longer durationlabetalol、Receptor blockersApplicable to various degrees of hypertension and hypertensive emergency,gestational hypertension,pheochromocytoma,high blood pressure when anesthesia or surgerycarvedilol）、Receptor blockersUsed in

24、 the treatment of mild and moderate hypertension with renal insufficiency,diabetes,high blood pressure patientsRenin angiotensin system depressants ACEI：Captopriletc.AT1-resistance：Chlorinesand,valsartan,etc【Antihypertensivemechanism】1.AngII Generate and function。Arteriovenous diastolic Peripheral r

25、esistance 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、PG2Etc.血管扩张血管扩张血压血压 AngiotensinconvertingenzymeinhibitorsACEI captopril（Asulfhydrylpropionicacidpulp）【Fu

26、nction 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【application】Eachp

27、eriodhighbloodpressure.Importantfirst-linedrugs.Especiallysuitableforcomplicatedwithdiabetesandinsulinresistanceandleftventricularhypertrophy,heartfailure,acutemyocardialinfarctionpatientswithhighbloodpressureAngiotensinreceptorblockersARB AT1receptor:vascularsmoothmuscle,cardiacmuscle,brain,kidneya

28、ndsecretionofaldosteroneAdrenalzonacells-hasregulatingeffecttothestabilityofthecardiovascularfunction.losartan【Antihypertensivemechanism】SelectiveblockingAT1receptor:blockingangiotensinmediatedbloodvesselsShrinkage,aldosteronereleaseandpromotevascularsmoothmuscleproliferationandeffect Peripheralresi

29、stancePromotinguricacidexcretion,inhibitingrenaltubuleofuricacidabsorption,short【Clinicalapplicationof】EachperiodhighbloodpressureStep-downfeatures:1.Theoralworkfast2.Theroletomaintainforalongtime:24hsmoothstep-down,36weeksformaximumeffect【sideeffect】relativelylessACEI:Attractedlessdrycoughandangion

30、euroticoedema;Butstillcancauselowbloodpressureandhighpotassium.Forpatientswithpregnancy.Promotinguricacidexcretion,inhibitingrenaltubuleofuricacidabsorption,shortPharmacological effects Diastolic small artery smooth muscle,reduce the peripheral vascular resistance,lower blood pressureWith heart rate

31、 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 action and mechanismActivate I1-imidazoline receptor，Mak

32、e 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 movement and the protection of gastric mucosaStatic note clonidine

33、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 obviousClonidineProcess in the bodyAbsorption:oral absorptionDistribu

34、tion:easy through the blood brain barrier,plasma protein combined rate of 30%Metabolism:50%in intrahepatic metabolismDischarge:metabolic product and prototype by renal excretionClinical applicationFirst-line treatment invalid moderately high blood pressure,with thiazide diuretic or other antihyperte

35、nsive 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 bradycardiaWater sodium retentionDrug withdrawal syndrome:a long-term d

36、rug 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 effect is reduced,sudden withdrawal,increased sympathetic nerv

37、ous 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 medicationmethyldopaA medium to strong step-down,cardiovascular and output,less influence renal

38、 blood flowSuitable for renal hypertension and moderate hypertensive patients with poor 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 hyperte

39、nsionOn 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 blood pressure to dropLong-term use antihypertensive vasodilators has the following

40、 disadvantagesCan theexcited sympathetic nerve,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,reduc

41、e adverse reactionsSodium 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 t

42、reatment 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 headacheGanglion block medicinemecamylamine【Function charact

43、eristics】1.Antihypertensiveeffectstrong,quickly;2.Hasinhibitoryeffectonbothsympatheticandparasympathetic,adversereactions,andtheheavier,orthostatichypotension;Theparasympatheticganglionblocksymptoms.3.Hypertensivecrisis.Prazosin Process in the bodyAbsorption:good oral absorption,first eliminate the

44、obvious,bioavailability of 60%Distribution:the combination of plasma protein rate was 97%Metabolism:liver metabolismDischarge:most bile excretion,by a small number of urinePharmacological effects and mechanism of actionAlpha 1 receptors on postsynaptic membrane of vascular smooth muscle are highly s

45、elective 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 receptor alpha,relieve dysuria prostate patientsClinical applicationCan be separately used treatment of mild an

46、d moderate hypertensionFor elderly patients with hypertension combined prostatic hypertrophy,can improve the symptoms of dysuriaSevere hypertension share diuretic and beta receptor blockers can enhance step-down effectAdverse reactionsFirst agent phenomenon:some patients for the first time 0.5 1 hou

47、r after the treatment can appear orthostatic hypotension,dizziness,sweating,heart palpitations and reactionLong-term use can cause water sodium retention,diuresis medicine can maintain its antihypertensive effectreserpine【Antihypertensive mechanism】Reducecatecholaminetransmitterinthestorageandreleas

48、eAndthesympatheticnerveendings(peripheralandcentraladrenergic)vesiclemembraneAminepumpcombination,catecholamineneurotransmitter(NA,5-HT)synthesis,storage,reuptakeleft,thedepletionoftheneurotransmitters,thesympatheticnerveconductionleft-vasodilation,BPleftCentralinhibition,composed,stableeffect.Pheny

49、lephrine can nerve endings blockerFeatures:effectiveslow,gentleandlasting【Clinical application】1light,moderatetohighbloodpressure,ithasbeenlessusedalone2manicpsychosis【Adverse reactions】The parasympathetic nerve excitement symptoms:nausea,vomiting,intestinal cramps and diarrhea,peptic ulcer 2 2 Cent

50、ral inhibition:calm,lethargy,depression。Potassium channels are openPromote the KATP open The cell membrane hyperpolarization The inflow Ca Thenewconceptofhighbloodpressuremedication1.Theeffectivetreatmentandlifelongtreatment2.Protecttargetorgans3.Smoothstep-down4.CombinationtherapyThe main points1.D