呼吸系統(tǒng)教學(xué)課件：呼吸系統(tǒng)常用藥物 英文版

RespiratorySystemDrugsOverviewAirwaybasicsAntiastmaticdrugsantitussivesexpectorantsAirwayBasicsBronchialtreeTracheaBronchiBronchiolesAlveoliAirwayBasicsAutonomicnervoussystemControlsrateanddepththroughsmoothmusclecontraction/relaxationAcetylcholine(cholinergicreceptors)Norepinephrine(adrenergicreceptors)AirwayBasicsCholinergicreceptorsMedicinalblockersusedforallergies&coldsCausedecreasedsalivation,drymouth,andgastricactivityAdrenergicreceptorsAlpha(alpha-1&alpha-2):peripheralbloodvesselsBeta(beta-1&beta-2):cardiac/smoothmmandrespiratorytractrespectivelyAlpha-1&beta-1receptorstypicallyexcitatoryAlpha-2&beta-2receptorstypicallyinducerelaxationRespiratoryDrugs

AntiasthmaticdrugsBronchodilatorsUsedtocombatbronchoconstrictionAnti-inflammatoriesSteroidalNon-steroidalMedicinetypeOralMoreconsistent,butslowerMDIFasteracting,butoftenusedimproperlyAntiasthmaticdrugs

SympathomimeticAgentsDirectlyrelaxairwaysmoothmusclebystimulatingadenylcyclaseandincreasetheformationofcAMPintheairwaytissuesthatresultsinbronchodilatationInhibitreleaseofsomebronchoconstrictingsubstancesfromthemastcellsIncreasemucociliarytransport8Antiasthmaticdrugs

BronchodilatorsMechanismofaction1.RelaxbronchialASMbyincreasingcAMP;2.inhibittheallergicmediatorsbymastcells;Antiasthmaticdrugs

Betaagonists

AdrenalineBothαandβEphedrineIsoprenalineBothβ1andβ2β2agonistsshortacting;longacting

(forrelieve,usedprn)(forcontrol)Antiasthmaticdrugs

Bronchodilators-Betaagonists

ShortactingSalbutamol

β2>β1,30minafterPO,for4-6h;5minafterINH,for3-4hClenbuterolstrongselectorforβ2,10-20minafterPO,for4-6h;5-10minafterINH,for2-4hTerbutalineSimilartoSalbutamol,5-15minafterIH,for1.5-5hAntiasthmaticdrugs

Bronchodilators-Betaagonists

LongactingFormoterol2minafterINH,for12hProcaterolBambuterolSalmeterol15minafterINH,for>12hRelaxbronchialASM;inhibitinflammation,forlong-termcontrol.Antiasthmaticdrugs

TheophyllineMechanismofaction1.Inhibitphosphdiesterase(PDE),increasecAMP;2.Blockadenosinereceptors;3.interferewith[Ca2+]i;4.increaseclearance;5.anti-inflammation;Anti-inflammationbyTheophyllineAntiasthmaticdrugs

TheophyllineAntiasthmaticdrugs

Theophylline6-10mg/Kgforpills4-6mg/KgforIV0.8-1mg/KgforIVGSideeffect:gastrointestinalsymptoms(nausea,vomit)cardiovascularsymptoms(tachycardia,arrhythmia)Antiasthmaticdrugs

AnticholinergicsMechanismofactionBindstoAchreceptors,prevetingAchfrombindingAntiasthmaticdrugs

AnticholinergicsShortactingIpratropium25-75ug/time,2-3times/day5minafterINH,for4-6hLongactingTiotropium18ug/time,singledailyfor24hAntiasthmaticdrugs

CorticosteroidMechanismofactionAntiasthmaticdrugs

CorticosteroidImprovingallindicesofasthma:severityofsymptomsairwaycaliberbronchialreactivityfrequencyofexacerbationandqualityoflifeInhibitproductionofinflammatorycytokinesReducebronchialreactivityIncreaseairwaycaliberSideeffect:oralcandidiasisAntiasthmaticdrugs

CorticosteroidCorticosteroidInhalantsEitherpreventnarrowingorrelaxsmoothmuscleoflung;NOTusedforacuteasthmaUsedtopreventorreducefrequencyofchronicbronchialasthmaattacks(whennotcontrolledbybronchodilatorsornon-steroidmedications)Antiasthmaticdrugs

CorticosteroidCommonCorticosteroidInhalantsBeclomethasoneBudesonideFluticasoneSideEffects:Drymouth,hoarseness,wheezing,rashAntiasthmaticdrugs

CorticosteroidIntranasalSteroidsWorkbyshrinkingswollennasaltissueandreducinginflammationUsedforseasonalallergiesorhayfeverinvolvinginflammationofmucousmembranesofnasalpassagesAntiasthmaticdrugs

CorticosteroidCommonIntranasalSteroidsBeclomethasoneDiproprionate(Beconase,VancenaseRx)FluticasoneProprionate(FlonaseaerosolRx)Antiasthmaticdrugs

CorticosteroidCorticosteroidoraldoses:PrednisonPrednisolonelargedose,shortcourse,30-40mg/day,thentaperedto10mg/day.Antiasthmaticdrugs

CorticosteroidCorticosteroidintravenousdoses:HydrocortisoneSuccinateMethylprednisoloneforactueattackorexacerbationofasthmaorCOPDAntiasthmaticdrugs

CromolynSodium&Nedocromil

PreventmastcelldegranulationTakenprophylacticallyEffectivelyinhibitbothantigen-andexercise-inducedasthmaAlsousefulinreducingsymptomsofallergicrhinoconjunctivitisAntiasthmaticdrugs

CromolynSodium&Nedocromil

Sideeffect:throatirritation,cough,mouthdryness,chesttightnessandwheezing,reversibledermatitis,myositis,gastroenteritis,pulmonaryinfiltrationwitheosinophilsandanaphylaxisAntiasthmaticdrugs

LeukotrieneAntagonistsBlocktheactionofleukotrienesby:-inhibitionof5-lipoxygenase,therebypreventingleukotrienesynthesis -inhibitionofthebindingofleukotrieneD4toitsreceptorontargettissues,therebypreventingitsactionAntiasthmaticdrugs

LeukotrieneAntagonistsDrugcategories a.Zileuton–a5-lipoxygenaseinhibitor -600mgQID -maycausehepatotoxicity b.Zafirlukast–20mgBID Montelukast–10mgOD -areLTD4antagonistTakenorallyHavedemonstratedanimportantrolefroleukotrienesinaspirin-inducedasthmaTheireffectonsymptoms,airwaycaliber,bronchialreactivityandairwayinflammationarelessmarkedthaninhaledcorticosteroids,buttheyarealmostequallyeffectiveinreducingthefrequencyofexacerbationsAntiasthmaticdrugs

LeukotrieneAntagonistsAntiasthmaticdrugs

OtherDrugsAnti-IgEAntibodies drugsthatreducetheamountofIgEtomastcells inhibitssynthesisofIgEbyB-lymphocytes Omalizunab(anti-IgEMab)2.CalciumchannelBlockersinhibitairwaynarrowinginducedbyvarietyofstimuli3.NitricOxideDonorsrelaxationofsmoothmuscleandvasculatureverylipophilicdrug,canbeinhaledasagasmoreusefulinpulmonaryhypertensionAntiasthmaticdrugs

PossibleFutureTherapiesMonoclonalantibodiesdirectedagainstcytokinesAntagonistofcelladhesionmoleculesProteaseinhibitorsImmunomodulatorsAntitussives

ActionsandUses

SomeantitussivesdepresscoughcenterlocatedinmedullaandarecalledcentrallyactingdrugsSomeantitussivesareperipherallyactingdrugs,whichactbyanesthetizingstretchreceptorsintherespiratorypassages,therebydecreasingcoughAntitussivesareusedtorelievenonproductivecoughAntitussives

AdverseReactionsCentralnervoussystemreactions:Sedation;dizziness;lightheadednessGastrointestinalreactions:Nausea;vomiting;constipationNonprescriptioncoughmedicinescontainingtwoormoreingredientsproducefewadversereactionswhenusedasdirectedAntitussivesCodeineDextromethorphanPentoxyverineBenproperineMucolyticsandExpectorantsMucolyticsLiquefypulmonarysecretionsExpectorantsIncreasesecretions,reduceviscosity,andexpelsputumMucolyticsandExpectorantsAdequatefluidintakeSideeffectsContraindica