Drug DrugClass MechanismofAction Indications AdverseEffects Contraindications

Estradiol NaturalGonadalHormones

AnEstrogen.PrincipalFemaleSexHormone

ProducedintheOvaryResponsibleforSecondaryFemaleSexCharacteristics------------------------------------------------------------------

Post-MenopausalEstrogen:Estrone(AdiposeTissue)----------------------------------------------------------------------------

Actions:StimulationDevelopmentofSexOrgansandSecondary

SexCharacteristics.PromoteSexualMaturationandGrowthinFemales

MaintenanceofMenstrualCycle.SensitizationofMyometriumtoOxytocinatTerm

FacilicationofLaborIncreaseSynthesisofClottingFactors

(II,VII,IX,X,Fibrinogen)DecreaseAnti-Thrombin

------------------------------------------------------------------------ContinuousExposure:

DecreasesLDL,IncreasedHDLDecreasedResorptionofBoneHyperplasiaofEndometrium

AnastrozoleLetrozole

ExemenstaneAromataseInhibtors

SelectiveAromataseInhibitorsDecreaseEstrogenSynthesis

PreventTestosterone-->Estradiol

&Androstenedione-->Estrone

Exemenstane:IrreverisibleNon-CompetitiveInhibitors

Post-MenopausalBreastCancerResistanttoTamoxifen

Drug DrugClass MechanismofAction Indications AdverseEffects ContraindicationsGanirelix GnRHAntagonist

UsedintheFollicularPhaseBlocksFSH/LHSecretions

FertilityTreatmentPolycysticOvarianSyndrome

Drug DrugClass MechanismofAction Indications AdverseEffects Contraindications

EndogenousEstrogen NaturalGonadalHormones

FemaleHypogonadismMenopausalHormoneTherapy

(PreandPost)OralContraception

(AlongwithProgesterone)PreventofOsteoporosisTurner'sSyndrome(XO)

GallStonesandPulmonaryEmbolismIncreasetheRiskofEndometrialandBreastCancer

Smokers(GallStones+PE)

EthinylEstradiolDiethylstilbetstrol

(DES)

NaturalEstrogens(Exogenous)

FemaleHypogonadismMenopausalHormoneTherapy

(PreandPost)OralContraception

(AlongwithProgesterone)PreventofOsteoporosisTurner'sSyndrome(XO)

GallStonesandPulmonaryEmbolismIncreasetheRiskofEndometrialandBreastCancer

-----------------------------------------------------------------------------DESDuringPregnancy

IncreaseVaginalAdenocarcinomainFemaleOffspring.

ClomipheneSelectiveEstrogenModulator

(SERM)HypothalamicAntagonist

BindsandInhibitstheEstrogenReceptor.InhibitstheActionofEstrogenbyReducingNegativeFeedbackontheHypothalamus/PituitaryGland.

IncreasesFSHandLHSecretion.

WidelyUsedforInductionofOvulation

UsedinAnovulation/PCOSPatients"FertilityPill"

MultiplePregnancy

TomoxifenSelectiveEstrogenReceptor

Modulator(SERM)

AntagonistonBreastPartialAgonistonEstrogenReceptor

AgonistonBlood,Bone,andLipidMetabolism

EstrogenReceptorPositiveBreastCancerinWomen

PartialAgonistonEndometrium-->EndometrialCancerIncreasedRiskofUterineMalignancyand

ThromboembolismorStroke

RaloxifeneSelectiveEstrogenReceptor

Modulator(SERM)

AntagonistonEndometriumandBreast.AgonistonBlood,Bone,LipidMetabolism

PreventionandTreatmentofPostmenopausalOsteoporosis.

CanbeusedforProphylaxisofBreastCancerinWomenwithRiskFactors.

DoesNOTcauseEndometrialCancerIncreasedRiskofThromboembolismandStroke

Drug DrugClass MechanismofAction Indications AdverseEffects Contraindications

ProgesteroneProgestin NaturalGonadalHormone

MostImportantProgestininHumansSynthesizedinOvary,Testis,andAdrenalCortexfrom

Cholesterol.LargeAmountsProducedandReleasedbythePlacenta

duringPregnancy.PrecursorforEstrogens,Androgens,andAdrenocortical

Steroids.-----------------------------------------------------------------

SelectivelyInhibitingPituitaryGonadotropinReleaseDecreasedMid-CycleLHSurge-->InhibitsOvulationThickensCervicalMucusandAltersEndometrium-->

ImpairImplantationoftheEggintheUterus

ContraceptivesforSmokers-ContraindicatedinEstrogen.

---------------------------------------------------AlsoUsedifPatienthasFamilyHistoryofBreastCancerorThromboembolic

Disease

IrregularandUnpredictableBleedingisCommon.FailureRatesareHigh.Medroxyprogesterone:

MayCauseSignificantBoneLoss(Osteoporosis)

MegestrolNorethindrone 1stGenerationProgestinAgonist ActslikeProgesterone(ShownAbove)

HormoneReplacementTherapyHormonalContraception(EndometrialCancerRisk)

Megestrol:IncreaseAppetiteinHIV/AID

DECREASEDRiskofEndometrialCancerHirsutismandAcne(Androgenic)AbnormalLipidandGlucoseLevels

Levonorgestrel 2ndGenerationProgestinAgonist ActslikeProgesterone(ShownAbove)HormoneReplacementTherapy

HormonalContraception(EndometrialCancerRisk)

HirsutismandAcne(Androgenic)AbnormalLipidandGlucoseLevels

Noregestimate 3rdGenerationProgestinAgonist ActslikeProgesterone(ShownAbove)HormoneReplacementTherapy

HormonalContraception(EndometrialCancerRisk)

HirsutismandAcne(Androgenic)AbnormalLipidandGlucoseLevels

Drospirenone 4thGenerationProgestinAgonist ActslikeProgesterone(ShownAbove)HormoneReplacementTherapy

HormonalContraception(EndometrialCancerRisk)

HirsutismandAcne(Androgenic)AbnormalLipidandGlucoseLevels

Mifepristone ProgesteroneAntagonist(PartialAgonist)

ProgesteroneAntagonist+GlucocorticoidAntagonistAbortifactant(+Misoprostol):

BlocksProgesteroneReceptorsinUterusCausingDetachmentofDevelopingFetus

MisoprostolcausesUterineContractions

Abortifactant----------------------------------------------

OneLargeDoseEffectivePost-CoitalEmergency

Contraception(Ifusedwith72hours)UsedtoTerminateEarlyPregnancy(Upto70Days)withMisoprostal

Nausea,Vomiting,VaginalBleeding,Sepsis

Drug DrugClass MechanismofAction Indications AdverseEffects Contraindications

LevonorgestrelPlanBOne-Step

Progestin-OnlyMorningAfterPill

SelectivelyInhibitingPituitaryGonadotropinReleaseDecreasedMid-CycleLHSurge-->InhibitsOvulationThickensCervicalMucusandAltersEndometrium-->

ImpairImplantationoftheEggintheUterus

EmergencyContraception1PillTakenAfterUnprotectedSexualIntercoursetoPreventPregnancy.MostEffectivewithinfirst24hours.

Nausea,Vomiting

LargeDoseEstrogen+

Progesterone

Estrogen+ProgesteroneMorningAfterPill

Estrogen+ProgesteroneEffectsEmergencyContraception:

Shouldbetakenwithin72hoursofunprotectedsexualintercourse.

UlipristalAcetateElla

SelectiveProgesteroneReceptorModulator(SPRM)

PreventsEndometrialImplantationofFertilizedEgg.InhibitsOvulationbyitsactionatHypothalamus,Pituitary

andOvary.Only60%Effective

EmergencyContraception:Usedwithin120hours(5days)afterunprotectedsexualintercourse.

Drug DrugClass MechanismofAction Indications AdverseEffects Contraindications

Progestin OralContraceptives

SelectivelyInhibitingPituitaryGonadotropinReleaseDecreasedMid-CycleLHSurge-->InhibitsOvulationThickensCervicalMucusandAltersEndometrium-->

ImpairImplantationoftheEggintheUterus

Smokers-ContraindicatedinEstrogenIrregularandUnpredictableBleedingiscommon.Failure

RatesareHigh.Medroxyprogesterone:?

Estrogen:EthinylEstradiol

+Progesterone:NorethindroneLevonorgestrelNoregestimateDromspirenon

CombinedOralContraceptives(COCs)

COCsAdministeredfor28-DayCycle(21DaysActiveDrug,7DaysPlacebo)

OralContraception:DecreasedRiskofOvarianCancer.

DecreasedRiskofEndometriosis/PIDDecreasedRiskofEctopicPregnancy

IncreasedBreastCancerRisk(EstrogenComponent)IncrreasedIndcienceofVenousThrombosisand

MyocardialInfarctionEdema

EstrogenComponent:SmokersFamilyHistoryofBreastCancer

orThrombembolicDisease

Drug DrugClass MechanismofAction Indications AdverseEffects Contraindications

Testosterone NaturalGonadalHormones

AnAndrogen.PrincipalMaleSexHormone

ProducedintheTestesResponsibleforSecondaryMaleSexCharacteristics

ProducedfromProgesterone

HypogonadismAnemia

Endometriosis

HirsutismAcne

DeepeningofVoice

Danazol WeakAndrogenDerivativeofTestosterone

WeakAndrogenDerivativeofTestosteronewithAnti-EstrogenicAcivity

PreventionofHereditaryAngioedema(C-1EsteraseInhibitor)

Endometriosis

FlutamideBicalutamide

AndrogenAntagonist(Competitive)

BlockAndrogenReceptors

ProstateCancerUsedwithGnRHAgonist

(fortheIntitial2-3Weeks)toCounteractFlareEffects

LiverToxicityGynecomastia

DecreasedLibido

FinasterideDutasteride 5-a-ReductaseInhibitors

OrallyActive5-a-ReductaseInhibitorsPreventsTestosterone-->DHT

CausesDecreasedDHTinProstateandSkin

BenignProstaticHypertrophy(BPH)MalePatternBaldness

ImpotenceGynecomastia(HighDoses)