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1、DESCRIPTIONDOSTINEXTabletscontaincabergoline,adopaminereceptoragonist.Thechemicalnameforcabergolineis1-[(6-allylergolin-8ß-yl)-carbonyl]-1-[3-(dimethylamino)propyl]-3-ethylurea.ItsempiricalformulaisC26H37N5O2,anditsmolecularweightis451.62.Thestructuralformulaisasfollows:Cabergolineisawh
2、itepowdersolubleinethylalcohol,chloroform,andN,Ndimethylformamide(DMF);slightlysolublein0.1Nhydrochloricacid;veryslightlysolubleinn-hexane;andinsolubleinwater.DOSTINEXTablets,fororaladministration,contain0.5mgofcabergoline.Inactiveingredientsconsistofleucine,USP,andlactose,NF.CLINICALPH
3、ARMACOLOGYMechanismofAction:Thesecretionofprolactinbytheanteriorpituitaryismainlyunderhypothalamicinhibitorycontrol,likelyexertedthroughreleaseofdopaminebytuberoinfundibularneurons.Cabergolineisalong-actingdopaminereceptoragonistwithahighaffinityforD2receptors.Resultsofinvitrostudiesdem
4、onstratethatcabergolineexertsadirectinhibitoryeffectonthesecretionofprolactinbyratpituitarylactotrophs.Cabergolinedecreasedserumprolactinlevelsinreserpinizedrats.Receptor-bindingstudiesindicatethatcabergolinehaslowaffinityfordopamineD1,α1-andα2-adrenergic,and5-HT1-and5-HT2-serotoninrece
5、ptors.ReferenceID:2975239ClinicalStudies:Theprolactin-loweringefficacyofDOSTINEXwasdemonstratedinhyperprolactinemicwomenintworandomized,double-blind,comparativestudies,onewithplaceboandtheotherwithbromocriptine.Intheplacebo-controlledstudy(placebon=20;cabergolinen=168),DOSTINEXproduceda
6、dose-relateddecreaseinserumprolactinlevelswithprolactinnormalizedafter4weeksoftreatmentin29%,76%,74%and95%ofthepatientsreceiving0.125,0.5,0.75,and1.0mgtwiceweeklyrespectively.Inthe8-week,double-blindperiodofthecomparativetrialwithbromocriptine(cabergolinen=223;bromocriptinen=236intheint
7、ent-to-treatanalysis),prolactinwasnormalizedin77%ofthepatientstreatedwithDOSTINEXat0.5mgtwiceweeklycomparedwith59%ofthosetreatedwithbromocriptineat2.5mgtwicedaily.Restorationofmensesoccurredin77%ofthewomentreatedwithDOSTINEX,comparedwith70%ofthosetreatedwithbromocriptine.Amongp
