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Drug Drug Class Mechanism of Action Indications Adverse Effects Contraindications Adrenocorticotropic Hormone (AcTH) Natural Pituitary Hormone Synthesized along with Melanocyte Stimulating Hormone (MSH) from Pro-Opiomelanocortin. (Can cause Hyperpigmentation). Stimulates Secretion of Cortisol, and Androgens (DHEA) from the Zona Fasciculata and Zona Reticularis. Aldosterone secretion from the Zona Glomerulosa is mainly dependent on Angiotensin II and Elevated Plasma Potassium (Hyperkalemia) Diagnosis of Primary vs Secondary Hypoadrenalism Hyperpigmentation (From Excess ACTH) Prednisone Triamcinolone Glucocorticoids (Cortisol Agonist) Hydrocortisone Dexamethasone Fludrocortison Betamethasone Glucocorticoids (Cortisol Agonist) Treat the Compensatory ↑ in ACTH No Negative Feedback --> Adrenal Hypertrophy --------------------------------------------------------------------- Hydrocortisone/Dexamethasone: Replacement Therapy -- Suppresses ACTH Fludrocortisone: Mineralocorticoid Replacement for the Salt Wasting Dexamethasone: Used to test for High Cortisol Assessment. If Dexamethasome SUPPRESSES Cortisol, patient has Pituitary Adenoma = Cushing Syndrome If Dexamethasone does NOT suppress Cortisol, it is from an Ectopic Origin (Tumor). (CAH) 21-Hydroxylase Deficiency ↓ Aldosterone ↓ Cortisol ↑Androgens ---------------------------------------- 11-B-Hydroxylase Deficiency: ↓ Aldosterone ↓ Cortisol ↑Androgens (Less Severe) but patients have Hypertension, Hypokalemia, and Metabolic Alkalosis -------------------------------------------- Inflammation Autoimmune Diseases Allergies Cancer (Lymphomas) Organ Graft Rejection Reactions Psoriasis + Hypercalcemia Addison's Disease (Hydrocortisone/Fludrocortisone) Secondary Adrenal Failure (Drugs) Therapeutic Effects of Glucocorticoids Betamethasone Dexamethasone Glucocorticoids (Cortisol Agonist) Same as Above STIMULATION OF THE MATURATION OF THE FETUS LUNG Drug Drug Class Mechanism of Action Indications Adverse Effects Contraindications Aminoglutethimide Adrenocortical Antagonists P450scc Enzyme Inhibitor Blocks Conversion of Cholesterol to Pregnenolone Decreased Adrenal Production of ALL Adrenal Steroids ↓ Cortisol, ↓ Aldosterone, and ↓ DHEA Hyperadrenalism Causes: Adrenal Carcinoma CAH Breast Cancer Increase in ACTH (Compensatory) Causes MSH --> Hyperpigmentation Overcome this by Co-Administration of Glucocorticoid to Prevent ACTH Release Drug Drug Class Mechanism of Action Indications Adverse Effects Contraindications Metyrapone Adrenocortical Antagonist 11-Hydroxylase Enzyme Blocker Selectively Blocks 11-Hydroxylase Causes Decreased Cortisol Production ↓ Cortisol, ↑ Aldosterone, and ↑ DHEA Used to Address Adrenal and Pituitary Function -------------------------------- Diagnosis of Pituitary ACTH Reserve Treatment: Cushing's Syndrome Salt and Water Retention (Aldosterone) Hirsutism (Androgens) Ketoconazole Adrenocortical Antagonist 17-a-Hydroxylase Enzyme Blocker 20-Lyase Enzyme Blocker Anti-Fungal Agent At High Doses: Inhibits Several P450 Enzymes involved in Steroidogenesis Primarily Inhibits 17-a-Hydroxylase ↓ Cortisol, ↑ Aldosterone, and ↓ DHEA Androgens Decrease at Low Doses. ALL Hormones Decrease at High Doses. Cushing Syndrome Acne Hirsutism Mitotane Adrenocortical Antagonist Zona Fasciculata + Zona Reticularis Blocker (Atrophy) Causes Selective Atrophy of Zona Fasciculata and Zona Reticularis (Via Mitochondria) (Cortisol + Androgen Production) Cushing Syndrome (Not Drug of Choice) Adrenocortical Carcinoma Severe GI Distress Mental Confusion Lethargy Dermal Toxicity Drug Drug Class Mechanism of Action Indications Adverse Effects Contraindications Aldosterone Natural Adrenal Hormone Synthesized in Zona Glomerulosa of Adrenal Cortex. Regulated by Angiotensin II Controls Water and Salt Retention Fludrocortisone Aldosterone Agonist Synthetic Corticosteroid. Most Commonly Prescribed Salt-Retaining Hormone. Spironolactone Aldosterone Antagonist Potassium-Sparing Diuretics. Compete with Aldosterone for Binding Site and Decreases it's effects. ---------------------------------------------------------------------- Also Acts as an Androgen Antagonist Congestive Heart Failure Treatment of Primary and Secondary Hyperaldosteronism ------------------------------- HIRSUTISM Eplerenone Aldosterone Antagonist Potassium-Sparing Diuretics. Compete with Aldosterone for Binding Site and Decreases it's effects. ---------------------------------------------------------------------- More Specific for Mineralocorticoid Receptor Does NOT Block Androgen Receptors Congestive Heart Failure Treatment of Primary and Secondary Hyperaldosteronism -------------------------------

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Page 1: Drug Drug Class Mechanism of Action Indications …...2017/12/02  · Drug Drug Class Mechanism of Action Indications Adverse Effects Contraindications Metyrapone Adrenocortical Antagonist

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-------------------------------

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