呼吸系统药理学医学课件

Antitussives,expectorants,andantiasmaticdrugsXimeiWuM.D.,Ph.D.Dept.ofpharmacology,ZJUMSDrugsactingonrespiratorysystemCough

antitussivedrugs

centrallyactingperipherallyactingSputum

expectorantdrugs

sputum-dilutingdrugsmucolyticdrugsAsthma

antiasthmaticdrugs

bronchialdilators

receptoragoniststheophyllinesmuscarinicantagonistsanti-inflammatorydrugs

glucocorticosteroidsmediatorreleaseinhibitorsCentrallyactingAddictivedrugs:

codeine可待因Non-addictivedrugs:

dextromethorphan右美沙芬pentoxyverine喷托维林(咳必清)Peripherallyactingbenzonatate苯佐那酯Codeine

可待因Dextromethorphan

右美沙芬1.PharmacologicaleffectssupressionofcoughmuscarinicandNMDAreceptorantagonism2.ClinicalusesUpperrespiratoryinfection,coughwithoutsputum3.AdverseeffectsAtropine-likesideeffectsContraindicatedinpatientswithglaucoma,pregnancy(<3m),psychoticdisorders,etc.

Pentoxyverine喷托维林(咳必清)

Benzonatate苯佐那酯PharmacologicaleffectsPeripherallyactingBlockingcoughreflexLocalanestheticeffectsCNSdepression2.Expectorants3.AntiasthmaticdrugsAsthmaAsthmaisphysiologicallycharacterizedbyincreasedresponsivenessofthetracheaandbronchitovariousstimuliandbywidespreadnarrowingoftheairwaysthatchangesinseverityeitherspontaneouslyorasaresultoftherapy.Itspathologicfeaturesarecontractionofairwaysmoothmuscle,mucosalthickeningfromedemaandcellularinfiltration,andinspissationintheairwaylumenofabnormallythick,viscidplugsofmucus.inflammationbronchoconstrictionAirwayhyperresponsivenessImmunologicalandnon-immunologicalstimuliWheezing(asthmaticsymptoms)glucocorticosteroidsdisodiumcromoglycate2receptoragonistsTheophyllinemuscerinicantagonists

ReceptoragonistsNon-selective：adrenaline,isoprotererol

2-selective:

moderate-acting:

salbutamol,terbutaline

long-acting:

salmeterol,formoterolTheophyllines:

aminophyllineMuscarinicantagonists:

ipratropine1.BronchialdilatorsBronchialdilators

2receptorselectiveagonistsSalbuterol沙丁胺醇Terbutaline特布他林1.Pharmacologicaleffects

Relaxingbronchialsmoothmuscles2.Clinicaluses

Controllingasthmaticsymptoms

Givenbyinhalation,oralorinjection3.Adverseeffects

SkeletalmuscletremorCardiacstimulation(largerdoses)Dysfunctionofmetabolism(hypokalemia,etc.)Salbuterol

沙丁胺醇Spacerusedforaerosolinhalation定量手控气雾器Spacerwillaidpatientsinhaletheaerosolizeddrugseasier2receptorselectiveagonistslong-actingSalmeterolFormoterolTheophyllines

AminophyllineBronchialdilators1.PharmacologicaleffectsBronchusdilation

Inhibitingphosphodiesterase;Blockingadenosinereceptors;Increasingcatecholaminerelease;Immunomodulation;Increasingrespiratorymusclecontractility;CNSstimulation,diuretic,gastricacidsecretion,etc.Theophyllines2.ClinicalusesBronchialasthma(p.o.,i.v.)Others:acutepulmonaryedema,etc.3.AdverseeffectsGIreactionsCNSstimulationAcutetoxication(i.v.injectiontoorapidly)

tachycarida,arrhythmia,seizure,coma,deathTheophyllines

MuscarinicantagonistsIpratropineBronchialdilatorsRelaxingbronchialsmoothmusclesNoeffectonsputumsecretionReplacedwithorcombinedwith2receptorselectiveagonists

Systemic(adverseeffect):

hydrocortisoneprednisone

dexamethasone

Inhalation:

beclomethasone

dipropionate

budesonide

triamcinolone

acetonide

fluticasonepropionate

flunisolideGlucocorticosteroidsBeclomethasonedipropionate

1.Pharmacologicaleffects(Antiinflammation)Inhibitinginflammatorycellactivities,Antibodyproduction,mediatorrelease,Inhibitincreasedresponsivenessofthetracheaandbronchi

2.ClinicalusesAsfirst-linedrugs,currentlyControllingchronicsymptomsIneffectiveforacutesymptoms

BeclomethasonedipropionateAdverseeffects

Local:

oropharyngealcandidiasis－usingspacer

Systemiceffectsa)Hypercorticism-likesyndrome:centralobesity(moonface,buffalohump,etc.);hypertension;glycosuria,hypokalemia;etc.b)Increasingsusceptibilitytoinfectionsc)Ingestivesystem:pepticulcers,etc.d)Cardiovascularsystem:hypertension,arteriosclerosise)Myopathyandosteoporosis:vertebralcompressionfractures,spontaneousfractures,especiallyinpostmenopausalwomenf)AdrenalsuppressionInhibitorsofmediatorreleaseDisodiumcromoglycate

(cromolyn)1.PharmacologicaleffectsInhibitingmediatorreleasefrommastorothercellsInhibitingsensoryneuropeptidereleaseandnon-specificalstimulusinducedbronchuscontraction2.Clinicaluses(onlyinhalation)

Preventionofallerg