Drug Drug Class Mechanism of Action Indications …...2017/12/02  · Drug Drug Class Mechanism of...

Drug DrugClass MechanismofAction Indications AdverseEffects Contraindications

AdrenocorticotropicHormone(AcTH)

NaturalPituitaryHormone

SynthesizedalongwithMelanocyteStimulatingHormone(MSH)fromPro-Opiomelanocortin.(CancauseHyperpigmentation).

StimulatesSecretionofCortisol,andAndrogens(DHEA)fromtheZonaFasciculataandZonaReticularis.

AldosteronesecretionfromtheZonaGlomerulosaismainlydependentonAngiotensinIIandElevatedPlasma

Potassium(Hyperkalemia)

DiagnosisofPrimaryvsSecondaryHypoadrenalism

Hyperpigmentation(FromExcessACTH)

PrednisoneTriamcinolone

Glucocorticoids(CortisolAgonist)

HydrocortisoneDexamethasoneFludrocortisonBetamethasone

Glucocorticoids(CortisolAgonist)

TreattheCompensatory↑inACTHNoNegativeFeedback-->AdrenalHypertrophy

---------------------------------------------------------------------Hydrocortisone/Dexamethasone:

ReplacementTherapy--SuppressesACTHFludrocortisone:

MineralocorticoidReplacementfortheSaltWastingDexamethasone:

UsedtotestforHighCortisolAssessment.IfDexamethasomeSUPPRESSESCortisol,patienthas

PituitaryAdenoma=CushingSyndromeIfDexamethasonedoesNOTsuppressCortisol,itisfrom

anEctopicOrigin(Tumor).

(CAH)21-HydroxylaseDeficiency↓Aldosterone↓Cortisol

↑Androgens----------------------------------------11-B-HydroxylaseDeficiency:↓Aldosterone↓Cortisol

↑Androgens(LessSevere)butpatientshaveHypertension,Hypokalemia,and

MetabolicAlkalosis--------------------------------------------

InflammationAutoimmuneDiseases

AllergiesCancer(Lymphomas)

OrganGraftRejectionReactionsPsoriasis+Hypercalcemia

Addison'sDisease(Hydrocortisone/Fludrocortisone)SecondaryAdrenalFailure(Drugs)

TherapeuticEffectsofGlucocorticoids

BetamethasoneDexamethasone

Glucocorticoids(CortisolAgonist)

SameasAboveSTIMULATIONOFTHEMATURATION

OFTHEFETUSLUNG

Drug DrugClass MechanismofAction Indications AdverseEffects Contraindications

Aminoglutethimide AdrenocorticalAntagonistsP450sccEnzymeInhibitor

BlocksConversionofCholesteroltoPregnenoloneDecreasedAdrenalProductionofALLAdrenalSteroids

↓Cortisol,↓Aldosterone,and↓DHEA

HyperadrenalismCauses:

AdrenalCarcinomaCAH

BreastCancer

IncreaseinACTH(Compensatory)CausesMSH-->Hyperpigmentation

OvercomethisbyCo-AdministrationofGlucocorticoidtoPreventACTHRelease

Drug DrugClass MechanismofAction Indications AdverseEffects Contraindications

Metyrapone AdrenocorticalAntagonist11-HydroxylaseEnzymeBlocker

SelectivelyBlocks11-HydroxylaseCausesDecreasedCortisolProduction

↓Cortisol,↑Aldosterone,and↑DHEA

UsedtoAddressAdrenalandPituitaryFunction

--------------------------------DiagnosisofPituitaryACTHReserveTreatment:Cushing'sSyndrome

SaltandWaterRetention(Aldosterone)Hirsutism(Androgens)

KetoconazoleAdrenocorticalAntagonist

17-a-HydroxylaseEnzymeBlocker20-LyaseEnzymeBlocker

Anti-FungalAgentAtHighDoses:InhibitsSeveralP450Enzymesinvolvedin

SteroidogenesisPrimarilyInhibits17-a-Hydroxylase

↓Cortisol,↑Aldosterone,and↓DHEAAndrogensDecreaseatLowDoses.

ALLHormonesDecreaseatHighDoses.

CushingSyndromeAcne

Hirsutism

Mitotane

AdrenocorticalAntagonistZonaFasciculata+

ZonaReticularisBlocker(Atrophy)

CausesSelectiveAtrophyofZonaFasciculataandZonaReticularis(ViaMitochondria)(Cortisol+AndrogenProduction)

CushingSyndrome(NotDrugofChoice)

AdrenocorticalCarcinoma

SevereGIDistressMentalConfusion

LethargyDermalToxicity

Drug DrugClass MechanismofAction Indications AdverseEffects Contraindications

Aldosterone NaturalAdrenalHormoneSynthesizedinZonaGlomerulosaofAdrenalCortex.

RegulatedbyAngiotensinIIControlsWaterandSaltRetention

Fludrocortisone AldosteroneAgonistSyntheticCorticosteroid.

MostCommonlyPrescribedSalt-RetainingHormone.

Spironolactone AldosteroneAntagonist

Potassium-SparingDiuretics.CompetewithAldosteroneforBindingSiteandDecreasesit'seffects.

----------------------------------------------------------------------AlsoActsasanAndrogenAntagonist

CongestiveHeartFailureTreatmentofPrimaryandSecondary

Hyperaldosteronism-------------------------------

HIRSUTISM

Eplerenone AldosteroneAntagonist

Potassium-SparingDiuretics.CompetewithAldosteroneforBindingSiteandDecreasesit'seffects.

----------------------------------------------------------------------MoreSpecificforMineralocorticoidReceptor

DoesNOTBlockAndrogenReceptors

CongestiveHeartFailureTreatmentofPrimaryandSecondary

Hyperaldosteronism-------------------------------