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)