drug drug class mechanism of action indications adverse ... · 12/3/2017 · selective progesterone...

2
Drug Drug Class Mechanism of Action Indications Adverse Effects Contraindications Estradiol Natural Gonadal Hormones An Estrogen. Principal Female Sex Hormone Produced in the Ovary Responsible for Secondary Female Sex Characteristics ------------------------------------------------------------------ Post-Menopausal Estrogen: Estrone (Adipose Tissue) ---------------------------------------------------------------------------- Actions: Stimulation Development of Sex Organs and Secondary Sex Characteristics. Promote Sexual Maturation and Growth in Females Maintenance of Menstrual Cycle. Sensitization of Myometrium to Oxytocin at Term Facilication of Labor Increase Synthesis of Clotting Factors (II, VII, IX, X, Fibrinogen) Decrease Anti-Thrombin ------------------------------------------------------------------------ Continuous Exposure: Decreases LDL, Increased HDL Decreased Resorption of Bone Hyperplasia of Endometrium Anastrozole Letrozole Exemenstane Aromatase Inhibtors Selective Aromatase Inhibitors Decrease Estrogen Synthesis Prevent Testosterone --> Estradiol & Androstenedione --> Estrone Exemenstane: Irreverisible Non-Competitive Inhibitors Post-Menopausal Breast Cancer Resistant to Tamoxifen Drug Drug Class Mechanism of Action Indications Adverse Effects Contraindications Ganirelix GnRH Antagonist Used in the Follicular Phase Blocks FSH/LH Secretions Fertility Treatment Polycystic Ovarian Syndrome Drug Drug Class Mechanism of Action Indications Adverse Effects Contraindications Endogenous Estrogen Natural Gonadal Hormones Female Hypogonadism Menopausal Hormone Therapy (Pre and Post) Oral Contraception (Along with Progesterone) Prevent of Osteoporosis Turner's Syndrome (XO) Gall Stones and Pulmonary Embolism Increase the Risk of Endometrial and Breast Cancer Smokers (Gall Stones + PE) Ethinyl Estradiol Diethylstilbetstrol (DES) Natural Estrogens (Exogenous) Female Hypogonadism Menopausal Hormone Therapy (Pre and Post) Oral Contraception (Along with Progesterone) Prevent of Osteoporosis Turner's Syndrome (XO) Gall Stones and Pulmonary Embolism Increase the Risk of Endometrial and Breast Cancer ----------------------------------------------------------------------------- DES During Pregnancy Increase Vaginal Adenocarcinoma in Female Offspring. Clomiphene Selective Estrogen Modulator (SERM) Hypothalamic Antagonist Binds and Inhibits the Estrogen Receptor. Inhibits the Action of Estrogen by Reducing Negative Feedback on the Hypothalamus/Pituitary Gland. Increases FSH and LH Secretion. Widely Used for Induction of Ovulation Used in Anovulation/PCOS Patients "Fertility Pill" Multiple Pregnancy Tomoxifen Selective Estrogen Receptor Modulator (SERM) Antagonist on Breast Partial Agonist on Estrogen Receptor Agonist on Blood, Bone, and Lipid Metabolism Estrogen Receptor Positive Breast Cancer in Women Partial Agonist on Endometrium --> Endometrial Cancer Increased Risk of Uterine Malignancy and Thromboembolism or Stroke Raloxifene Selective Estrogen Receptor Modulator (SERM) Antagonist on Endometrium and Breast. Agonist on Blood, Bone, Lipid Metabolism Prevention and Treatment of Postmenopausal Osteoporosis. Can be used for Prophylaxis of Breast Cancer in Women with Risk Factors. Does NOT cause Endometrial Cancer Increased Risk of Thromboembolism and Stroke Drug Drug Class Mechanism of Action Indications Adverse Effects Contraindications Progesterone Progestin Natural Gonadal Hormone Most Important Progestin in Humans Synthesized in Ovary, Testis, and Adrenal Cortex from Cholesterol. Large Amounts Produced and Released by the Placenta during Pregnancy. Precursor for Estrogens, Androgens, and Adrenocortical Steroids. ----------------------------------------------------------------- Selectively Inhibiting Pituitary Gonadotropin Release Decreased Mid-Cycle LH Surge --> Inhibits Ovulation Thickens Cervical Mucus and Alters Endometrium --> Impair Implantation of the Egg in the Uterus Contraceptives for Smokers - Contraindicated in Estrogen. --------------------------------------------------- Also Used if Patient has Family History of Breast Cancer or Thromboembolic Disease Irregular and Unpredictable Bleeding is Common. Failure Rates are High. Medroxyprogesterone: May Cause Significant Bone Loss (Osteoporosis) Megestrol Norethindrone 1st Generation Progestin Agonist Acts like Progesterone (Shown Above) Hormone Replacement Therapy Hormonal Contraception (Endometrial Cancer Risk) Megestrol: Increase Appetite in HIV/AID DECREASED Risk of Endometrial Cancer Hirsutism and Acne (Androgenic) Abnormal Lipid and Glucose Levels Levonorgestrel 2nd Generation Progestin Agonist Acts like Progesterone (Shown Above) Hormone Replacement Therapy Hormonal Contraception (Endometrial Cancer Risk) Hirsutism and Acne (Androgenic) Abnormal Lipid and Glucose Levels Noregestimate 3rd Generation Progestin Agonist Acts like Progesterone (Shown Above) Hormone Replacement Therapy Hormonal Contraception (Endometrial Cancer Risk) Hirsutism and Acne (Androgenic) Abnormal Lipid and Glucose Levels

Upload: duongtuong

Post on 21-May-2018

216 views

Category:

Documents


3 download

TRANSCRIPT

Page 1: Drug Drug Class Mechanism of Action Indications Adverse ... · 12/3/2017 · Selective Progesterone Receptor Modulator (SPRM) Prevents Endometrial Implantation of Fertilized Egg

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

Page 2: Drug Drug Class Mechanism of Action Indications Adverse ... · 12/3/2017 · Selective Progesterone Receptor Modulator (SPRM) Prevents Endometrial Implantation of Fertilized Egg

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)