01罗红霉素盐酸氨溴索片英文说明书

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1、ROXISARAAMComposition:EachtabletofRoxisaraAMcontainsroxithromycin150mgandambroxolhydrochloride30mg.Description:Roxithromycinisasemisynthetic,long-acting,acid-stablemacrolideantibiotic.Ascomparedtoerythromycin,ithasaverysimilarantibacterialspectrumofaction,betterbioavailabilitybytheoralroute,betterti

2、ssuepenetration,andmuchlongerdurationofaction.ChemicallyitisdesignatedasErythromycin9-0-(2-methoxyethoxyl)methyloxime(C41H76N2O15=837.0).Ambroxolisanactivemetaboliteofbromhexineandhassimilarbutsomewhatlonger-lastingmucolyticaction.Chemicallyambroxol(ashydrochloridesalt)isdesignatedastrans-4-(2-Amino

3、-3,5dibromobenzylamino)cyclohexanolhydrochloride(C13H18Br2N2O1HCl=414.6).IthasbeenincorporatedintabletRoxisaraAMtofacilitatebetterpenetrationofroxithromycinintorespiratorytractfluidsforsuperiorantibacterialaction.PharmacologicalActionsandTheirMechanisms:RoxithromycinishighlyactiveagainstStreptococcu

4、spyogenesandS.pneumoniae,Staphylococcusaureus(methicillin-sensitive)*,Clostridia,Corynebacteriumdiphtheriae,Bacillusanthracis,Erysipelothrixrhusiopathy,Listeriamonocytogenes,Propionibacteriumacnes,andalsoagainstNeisseriagonorrhoeae,Moraxellacatarrhalis,Campylobacter,Gardnerellavaginalis,Legionellapn

5、eumophilia,andMycoplasmapneumoniae.OrganismsmoderatelysensitivetothedrugincludeS.viridans,N.meningitides,Haemophilusducrei,H.Influenzae,Helicobacterpylori,Bordetellapertussis,Campylobacterjejuni,Actinomyces,Chlamydiatrachomatis,Rickettsias,Treponemapallidum,Borreliaburgdorferi,andmycobacteriumscrofu

6、laceumandM.kansasi.(*Somestrainsmaydevelopresistanceduringthecourseoftherapywithroxithromycin).Roxithromycinbindstothe50Sribosomalsubunitofsusceptiblebacteriaandinhibitstheirgrowthandmultiplicationbydisruptingbacterialproteinsynthesis.Ambroxolliquefiestenaciousrespiratorytractsecretionsbydepolymeris

7、ingmucopolysaccharidefibresdirectlyaswellasbyliberatinglysosomalenzymes.Italsoincreasesthesecretionofthinbronchialfluids.Suchmucolyticandmucokineticactionsfacilitatepenetrationofantimicrobialagentsintotherespiratorytractfluidsandensureabetterandfasterclinicalresponse.ClinicalPharmacokineticsThereisn

8、osignificantpharmacokineticinteractionbetweenroxithromycinandambroxolpresentintabletRoxisaraAM.Therefore,thepharmacokineticsofthepreparationmayberegardedasequivalenttothatoftheindividualactivecomponentssummedup.About50%ofanoraldoseofroxithromycinisabsorbedfromthegastro-intestinaltract.Asingle150mgor

9、aldoseproducespeakplasmaconcentrationsofabout6to8mcg/mlafter2hours.Absorptionmaybereducedwhentakenafter,butnotbefore,ameal.Itiswidelydistributedintissuesandbodyfluids.Highconcentrationsareachievedinthelung,prostate,tonsils,skin,andepididymis.Itisalsoconcentratedinneutrophils,macrophages,andmonocytes

10、.Thedrugisabout86to91%serumproteinbound(mainlytoalpha1-acidglycoprotein).Itismetabolizedtoalimitedextentintheliver.About54%ofanadministereddoseisexcretedinthefeces,about10%intheurine,and10to20%intheexpiredair.Theeliminationplasmahalf-liferangesfrom8to13hours,butmaybelongerinpatientswithseverekidneyo

11、rliverfunctionimpairment,andchildren.Followingoraladministrationambroxolisrapidlyandcompletelyabsorbed.Afterintravenousadministration,theapparentvolumeofdistribution,theterminaleliminationhalf-lifeandthetotalplasmaclearanceweredeterminedtobe1.52L/kg,3.72h,and565ml/min,respectively.Thedrugismetaboliz

12、edextensivelytodibromoanthranilicacidandalmostcompletelyexcretedintheurine.Indications:TabletRoxisaraAMisindicatedforthetreatmentofthefollowingconditionscausedbysusceptiblemicroorganisms:Acutebronchitis(bacterial),acuteexacerbationsofchronicbronchitis,bronchopneumonia,pneumoniaduetoatypicalpathogens

13、,bacterialinfectionscomplicatingbronchialasthmaorbronchiectasis,sinusitisandotitismedia.Contraindications:TabletRoxisaraAMshouldnotbegiventopatientswithknownhypersensitivitytoeithermacrolideantibiotics,ambroxol,orbromhexine.Italsoshouldnotbegiventopatientsreceivingvasoconstrictiveergotalkaloids.Prec

14、autions:Inseverehepaticinsufficiency(e.g.hepaticcirrhosiswithjaundiceand/orascites)thedoseshouldbereducedbyhalf.Inpregnancythesafetyofroxithromycinandambroxoltothefoetushasnotbeenestablished.However,roxithromycinhasnotbeenfoundtobeteratogenicorfoetotoxicat40timesthehumantherapeuticdosesinseveralspec

15、iesoflaboratoryanimals.Thus,thepreparationshouldnotbeusedinpregnancyunlessclearlyindicated.Smallquantitiesofroxithromycinareexcretedinthebreastmilk.Breast-feedingbythemotherortreatmentofthemotherwithtabletRoxisaraAMshouldbediscontinuedifrequired.Sincemucolyticsmaydisruptthegastricmucosalbarriertable

16、tRoxisaraAMcontainingambroxolshouldbeusedwithcautioninpatientswithahistoryofpepticulceration.DrugInteractions:Concurrentadministrationofamacrolideantibioticandergotamineoritsderivativesmayprovokevasospasmandcauseseriousischaemia.Hence,tabletRoxisaraAMshouldnotbegivenalongwiththesedrugs.Noclinicallys

17、ignificantdruginteractionofroxithromycinoccurswithconcurrentadministeredantacids,carbamazepine,ciclosporine,oralcontraceptives,theophylline,triazolam,andwarlarin(prothrombintimeincreasedinpatientsreceivingvitaminKantagonists).Serumlevelsoffreedisopyramidecanbeincreasedduetodisplacementfromserumprote

18、inbindingsites.Likeothermacrolidesroxithromycinmayprolongthehalf-lifeofmidazolam.Macrolidesmayincreaseserumlevelsofterfenadinewhichmayresultinventriculararrhythmias.Thishasnotbeendocumentedwithroxithromycinbutcautioniswarrantedincaseofco-administration.Noclinicallysignificantdruginteractionhasbeende

19、scribedforambroxol.AdverseEffects:TabletRoxisaraAMisgenerallywelltoleratedbymostpatients.However,roxithromycinpresentinthepreparationmayoccasionallyproducegastro-intestinaldisturbancessuchasnausea,vomiting,epigastricpain,anddiarrhoea.Theseadverseeffectsarelessfrequent(4%oftreatedpatients)thanwithery

20、thromycin.Increasesinliverenzymevaluesandhepatitishavebeenreported.Rashes,urticaria,angioedema,andexceptionallybronchospasmandanaphylacticshockarehypersensitivityreactionsreported.Otheradverseeffectsreportedoccasionallyincludeheadache,dizziness,weakness,andchangesinbloodcellcount.Hypersensitivityrea

21、ctionsandmildgastro-intestinalside-effectsuchasconstipationanddrymouthmaybeoccasionallyproducedbyambroxol.DosageandAdministration:Adultswithnormalhepaticfunctionmildtomoderaterenalimpairment:Onetablettobetakentwiceaday(morningandevening)beforemealsforatleastupto2daysafterresolutionofthesymptoms.Theu

22、sualdurationoftherapyisbetween5and10days.Adultswithsevereliverdisease:Onetablettobetakenonceaday.Elderlypersons:Usualdosage.Children:Doseiscalculatedonthebasisofroxithromycincontent;2.5to4mgofroxithromycin/kgbody-weighttobegivenbeforemealstwicedailyforamaximumof10days.Storage:Storeinacool,dryanddarkplace.Presentation:Instripsof10s.