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1、Antihypertensive drugs,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 s
2、econdary hypertension,hypertensionMean arterial bloo,complications,Heart failureCoronary heart disease(CHD)Cerebrovascular accidentRenal failure,complicationsHeart failure,Antihypertensive drugs,Reasonable application of antihypertensive drugs,Control of blood pressure,Delay the formation and develo
3、pment of atherosclerosis,Reduce the complications such as brain,heart and kidney,Reduce the mortality rate,prolong life,Antihypertensive drugsReasonab,Blood pressure,-The factors influencing blood pressure:Cardiac output:heart rate,myocardial contraction force,change of blood volume,etc.;Peripheral
4、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 i,1.Nervous regulation:the sympathetic nervous system,Peripheral neurotransmitter release,The postsynaptic membrane receptor,main centr
5、eganglionVascular sm,Second,humoral regulation:renin angiotensin aldosterone system,Kidney adjacent ballBeside the machine,-R blockers,renin,Angiotensin original,angiotensin,invertase,ACEI,angiotensin,Small artery contraction,losartan,Aldosterone secretion,Water sodium retention,diuretic,(thiazides)
6、,Second,humoral regulation:Ki,Classification,DiureticThe 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:diureti
7、c,calcium antagonist medicine,beta receptor blockers and ACEI,ClassificationDiuretic,Diuretic,On 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:An
8、tihypertensive 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 and severe-shareCan make the elderly hypertension patients complicated with stroke,the incidence of
9、left heart failure and mortality is left,DiureticOn the basis of(a lin,Hydrochlorothiazide,Early 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+exc
10、hange left-intracellular Ca2+left,reduce vascular smooth muscle of norepinephrine(NE)reactivity,HydrochlorothiazideEarly antih,disadvantages:,-Blood K+、Na+、Mg2+-Blood total cholesterol,triglyceride,low density lipoprotein cholesterol(hdl-c)-Blood uric acid-Blood renin-Glucose tolerance(disabled)for
11、diabetes patientsEffective diuretic(furosemide)used in hypertensive 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,
12、be agitated,palpitation,sweating,nausea,vomiting,or pale flush,blurred vision and other signs.Mechanism:hyperthyroidism and circulating catecholamines increased sympathetic nervous activity,Hypertensive crisis,Clinical application,A gleam of medicationApplication of the treatment for mild hypertensi
13、on separatelyWith other antihypertensive drug treatment,severe hypertension,Clinical applicationA gleam of,Effect of diuresis medicine of compound preparations with other drugs,Compound antihypertension tablet:give up ping,hydralazine,hydrochlorothiazideCompound apocynum tablet:guanidine b organism,
14、hydralazine,hydrochlorothiazideJane chrysanthemum antihypertension tablet:clonidine,hydrochlorothiazideCompound captopril tablets,enalapril and hydrochlorothiazideConstant dropping pills:clonidine,hydralazine,hydrochlorothiazide,Effect of diuresis medicine of,Calcium antagonist medicine,Block L volt
15、age dependent calcium channel-left intracellular Ca2+diastolic small arteryNifedipine group,horizon,lacidipine flat,amlodipine,Calcium antagonist medicine Bl,Nifedipine,【Step-down characteristics】1 Buck degree was positively correlated with the original high blood pressure,with normal blood pressure
16、 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 reflective heart rate share Recepto
17、r blockers.,Nifedipine【Step-down characte,Clinical application,Light,medium and severe hypertension treatment,Clinical applicationLight,med,Nitrendipine,Selectively ACTS on the peripheral vascular,blocking its internal flow of calcium ions,relaxing smooth muscle,the dilate blood vessels and step-dow
18、nWarm and lasting antihypertensive effect,applicable to various types of high blood pressure,NitrendipineSelectively ACTS o,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
19、,reduce peripheral vascular resistance and to lower blood pressureResistance to atherosclerosisUsed for mild and moderate hypertensionName of commodity:lacidipine,LacidipineIs a potent calcium,Amlodipine,More gentle,smooth effect lasting,convenience of once-daily dosage,24 hours of stability control
20、 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 atherosclerosis,AmlodipineMore gentle,smooth,Adrenaline receptor blockers,Receptor blockers:prazosin、terazosin、doxazosin Rece
21、ptor blockers:prapranolol、atenolol、labetalol、carbedilol,Adrenaline receptor blockers,Mechanism of action,Nonselective 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
22、RAS on blood pressure 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
23、 ring element synthesis,Mechanism of actionNonselectiv,Clinical application,Suitable 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,cere
24、brovascular diseaseDiuretic or pooling vasodilators can enhance curative effect,Clinical applicationSuitable f,atenolol,Selective 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 duration
25、,atenololSelective beta 1 recep,labetalol,、Receptor blockersApplicable to various degrees of hypertension and hypertensive emergency,gestational hypertension,pheochromocytoma,high blood pressure when anesthesia or surgery,labetalol、Receptor blockers,carvedilol),、Receptor blockersUsed in the treatmen
26、t of mild and moderate hypertension with renal insufficiency,diabetes,high blood pressure patients,carvedilol)、Receptor blocke,Renin angiotensin system depressants,ACEI:Captopril etc.AT1-resistance:Chlorine sand,valsartan,etc,ACEI:Captopril etc.,【Antihypertensive mechanism】1.AngII Generate and funct
27、ion。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.血管扩张血压,Angiotensin converting enzyme inhibitors ACEI,cap
28、topril(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 renal hyperte
29、nsive 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,acute myocardial infarcti
30、on 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.losartan【Antihypertensive mechani
31、sm】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,short,Angiotensin receptor block
32、er,【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 oedema;But still can cause low blood pr
33、essure and high potassium.For patients with pregnancy.Promoting uric acid excretion,inhibiting renal tubule of uric acid absorption,short,抗高血压药_整理英文版课件,Pharmacological effects,Diastolic small artery smooth muscle,reduce the peripheral vascular resistance,lower blood pressureWith heart rate slows,dec
34、reased 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 lens,Pharmacological effects Diast,Pharmacological action and mechanism,Activate I1-im
35、idazoline 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 movement and the protection of gastric mucosa
36、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,Pharmacological action and mec,Clonidin
37、e,Process 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 excretion,ClonidineProcess in the body,Clinical application,First-line treatm
38、ent 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 glaucoma,Clinical applicationFirst-line,Adverse reactions,Dry mouth,sleepiness
39、,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.And long-term medication made the alpha 2 weeks the pre
40、synaptic 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)can alleviate.Withdrawal should be gradually reduced,Adverse
41、reactionsDry mouth,sl,The other central blood pressure medication,methyldopaA medium 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 sharemoxonidineF
42、or 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,dry mouth greatly reduce adverse reactions,The other central blood pres
43、su,Vasodilation medicine,Directly to relax vascular smooth muscle,decrease peripheral resistance and blood pressure to dropLong-term use antihypertensive vasodilators has the following disadvantagesCan theexcited sympathetic nerve,reflective increase cardiac output,heart rate speed upIncrease of ren
44、in 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 reactions,Vasodilation medicineDirectly,Sodium nitroprusside,Antihypertensive effects associated with an i
45、ncreased 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 treatment of hypertensive crisis.Also used in congestive heart failure,acute myocardi
46、al infarction and controlling hypertension during anesthesiaBecause of excessive step-down can cause nausea,vomiting,sweating,restlessness,palpitations and headache,Sodium nitroprussideAntihypert,Ganglion block medicinemecamylamine【Function characteristics】Antihypertensive effect strong,quickly;2.Ha
47、s inhibitory effect on both sympathetic and parasympathetic,adverse reactions,and the heavier,orthostatic hypotension;The parasympathetic ganglion block symptoms.3.Hypertensive crisis.,Ganglion block medicine,Prazosin,Process in the bodyAbsorption:good oral absorption,first eliminate the obvious,bio
48、availability of 60%Distribution:the combination of plasma protein rate was 97%Metabolism:liver metabolismDischarge:most bile excretion,by a small number of urine,PrazosinProcess in the body,Pharmacological effects and mechanism of action,Alpha 1 receptors on postsynaptic membrane of vascular smooth
49、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 receptor alpha,relieve dysuria prostate patients,Pharmacological effects and me,Clinical app
50、lication,Can be separately used treatment of mild and 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 effect,Clinical applicationCan be se