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CholestasisMedication
Updated:Aug21,2015
Author:HishamNazer,MB,BCh,FRCP,,DTM&HChiefEditor:CarmenCuffari,MDmore...

MEDICATION

Cholereticagents
ClassSummary
Ursodeoxycholicacidactstoincreasebileformationandantagonizestheeffectofhydrophobicbile
acidsonbiologicalmembranes.

Ursodeoxycholicacid(Actigall,Urso)
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Showntopromotebileflowincholestaticconditionsassociatedwithapatentextrahepaticbiliary
system.Decreasesthecholesterolcontentofbileandthereforereducesbilestoneandsludge
formation.

Barbiturates
ClassSummary
Theseagentsareusedtoinducehepaticenzymemetabolisminordertodecreaseserumbilirubin
levelsinsomepatientswithcholestasisinordertoimprovefunction.

Phenobarbital(Luminal)
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Mainlyusedasananticonvulsant,whichinterfereswithtransmissionofimpulsesfromthalamusto
cortexofbrain,resultinginimbalanceincentralinhibitoryandfacilitatorymechanisms.Usedin
cholestasistoinducetheCYP450systemintreatmentofneonatalhyperbilirubinemiaandloweringof
bilirubininchroniccholestasis.

Vitamins
ClassSummary
FatsolublevitaminsA,D,E,andKmustbeadministeredasindividualsupplementstoassureproper
absorption.

Phytonadione(AquaMEPHYTON)
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VitaminK.Fatsolublevitaminabsorbedbythegutandstoredintheliver.Necessaryforthefunction
ofclottingfactorsinthecoagulationcascade.Usedtoreplaceessentialvitaminsnotobtainedin
sufficientquantitiesinthedietortofurthersupplementlevels.

VitaminE(LiquiE)
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VitaminE.Preventionandtreatmentofhemolyticanemiasecondarytovitamindeficiencyorneedfor
dietarysupplementation.Protectspolyunsaturatedfattyacidsinmembranesfromattackbyfree
radicalsandprotectsRBCagainsthemolysis.

VitaminA(AquasolA)
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Neededforbonedevelopment,growth,visualadaptationtodarkness,testicularandovarianfunction,
andasacofactorinmanybiochemicalprocesses.

Ergocalciferol(Drisdol,Calciferol)
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VitaminD.Stimulatesabsorptionofcalciumandphosphatefromsmallintestineandpromotesrelease
ofcalciumfromboneintoblood.POsolutioncomesas8000U/mL(200mcg/mL,40U/mcg).

Opioidantagonists
ClassSummary
Theseagentsareusedtoalleviateprurituscausedbycholestasis.Theyblockopioidmediated
pathwaysofafferentnerves,whichmaybeproducingtheitchingsensation.

Naltrexone(ReVia)
Viewfulldruginformation
Cyclopropylderivativeofoxymorphonethatactsasacompetitiveantagonistatopioidreceptors.Do
notadministerthismedicationuntilthepatientisopioidfreefor710d.Availableas50mgtab.

Bilesaltresins
ClassSummary
Bileacidbindingresinsformanonabsorbablecomplexwithbileacidsintheintestine,whichinhibits
enterohepaticreuptakeofintestinalbilesaltsandtherebyincreasesthefecallossesofbilesaltbound
lowdensitylipoproteincholesterol.

Cholestyramine(Questran,Prevalite)
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Mayuseasadjunctinprimaryhypercholesterolemia.Formsanonabsorbablecomplexwithbileacids
intheintestine,which,inturn,inhibitsenterohepaticreuptakeofintestinalbilesalts.Dosebasedon
resincontent.

Antibiotics
ClassSummary
Antitubercularagentsinduceliverenzymesandamelioratepruritussecondarytocholestasis.

Rifampin(Rimactane,Rifadin)
Viewfulldruginformation
InhibitsRNAsynthesisinbacteriabybindingtobetasubunitofDNAdependentRNApolymerase,
which,inturn,blocksRNAtranscription.
Followup
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