Gonadal Hormones Drugs Flashcards by TRISHA JOY BASILLE RODRIGUEZ

what are the 2 events of ovarian phase?

preovulatory phase = follicular phase
postovulatory phase = luteal phase

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what are the uterine endometrial phases?

Preovulatory phase = proliferative phase
postovulatory phase = secretory phase

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what are the different effects of Estrogen?

INC in size of uterus, fallopian tubes, vagina, & external genitalia

Thickening of vaginal epithelium (dyspareunia)

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what is the basis of fertility awareness method used for family planning or contraception?

Spninnbark estrogen in the Uterus

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Why are menopausal women more prone to osteoporosis and fractures?

Estrogen decreases bone resporption

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WHat are the other effects of estrogen in the body?

Favorable lipid profile EXCEPT for TAGS
INC CBG, TBG, SHBG, Transggerrin & renin substrate
INC 1972 factors
INC gallstone formation
SUppression of FSH

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WHat are the therapeutic uses of Estrogen?

Replacement —> Menopause, Primary Hypogonadism
Correct hormonal imablance —> Dysfunctional uterine bleeding
Reverse an abnormal/unwanted process —> Dysemnorrhea, Acne, hirsutism, male breast & prostate cancer
Contraception

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What are C/Is of Estrogen?

Estrogen-dependent neoplasms
Undiagnosed genital bleeding
Thromboembolic disorders
Liver disease
Heavy smokers
Pregnancy

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WHat are the goals of menopausal hormone therapy?

Relief of vasomotor symptoms
Tx of genitourinary symptoms
Tx of vulvovaginal symptoms
Prevention of bone fractures
CVS benefit if it starty early (<60yo, within 10 yrs of menopause)

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What do we call amenorrhea that is <1 yr?

Perimenopause

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What are the diff selective estrogen receptor modulator?

Tamoxifen
Raloxifene
Clomiphene

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What is the MOA of Tamoxifen, therapeutic use & important AEs?

MOA:
Breast —> binds to ER w/o activating them —> prevents Estrogen from binding

Uterus —> activates Estrogen receptors —> uterine cell proliferation

Use: Palliative tx in ER-positive breast cancer

AE: Deep vein thrombosis (lethal), INC risk of endometrial cancer hot flashes

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What is the use of Raloxifene?, & important AE?

Use: prevention & tx of postmenopausal osteoporosis, breast cancer prevention

AE: DVT, hot dlashes

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What is the MOA of Clomiphene, Therapeutic use, & AE?

MOA: Increases Gonadotropin secretion

Use: PCOS (Induction of ovulation)

AE: Ovarian enlargement (significant), multiple births, hot flshes, eye symptoms

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What are the 2 anti-estrogens?

Aromatase inhibitors
Estrogen receptor blocker

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What is the MOA of Aromatase inhibtors & drugs?

Inhibit the enzyme which converts androgen (testosterone) to androgen

AnasTROZOLE
Exemestane
LeTROZOLE

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What is the use of prescribing anti-estrogens?

breast cancers that are R to Tamoxifen

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What is the MOA of Estrogen recpetor blocker & drug unde rit?

Prevents dimerization

FUlvestrant

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What is the MOA of Progestins?

Similar to Estrogens & Steroids

INC in transcription of target genes in sensitive tissues

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What are co-repressors of Progestins?

Progesin recpetor modulator
Antagonist (Mifepristone)

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What are the effects of Progestin in the uterus?

DEC uterine motility
Cervical discharge
Endometrium —> secretory changes —> support embyro impant if pregnnacy occurs

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What is the effect of Progestin in the breast?

Acinar & lobular development

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What are the effects of Progestin to the brain?

DEC GnRH pulse in hypothalamus —> neg feedback
DEpressant or hypnotic effets —> taken at night to improve sleep
Thermogenic effect —> INC basal body temperature

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What type of chart is used by women to track their temperature upon waking up? WHy is this done?

Basal body temperature

Determine if woman ovulates & fertility awareness method of contraception

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What are the other effects of Progestin?

INC LDL w/ no change or slight DEC in HDL Mild catabolic effect Natriuretic effect

What is the use of synthetic Progesterone?

Menopausal hormone treatment

What are the 4 synthetic preparation of Progesterone?

21-Carbon progesterone analogs (Pregnanes) 19-Nortestosterone 13-Methyl derivatives (Estranes) 19-Nortestosterone 13-Ethyl derivatives (Gonanes) With Anti-andronergic. & Anti-Mineralocorticoid effect

WHat are the diff Pregnanes?

Dydrogesterone Medroxyprogesterone Megestrol

What synethic preparation of Progesterone has little or no adrogenic effect?

L-Norgesterol Desogesterol Etonegesterel

What are the AEs of Progestins?

INC in BP DEC HDL INC risk of breast carcinoma

WHat are the therapeutic uses of Progestin?

Contraception MHT/EPT Ovarian suppression Dysfunctional uterine bleeding Threatened miscarriage

WHat are the diff femal hormonal contraception?

1. COmbined Estrogen + Progestin 2. Progestin-only Contraceptives 3. Emergency/Post-coital contraceptives 4. Family planning methods

What are the MOA of Combined Estrogen + Progestin?

Inhibit ovulation —> DEC FSH, DEC LH ALters the endometrium —> x impalantation of embryo Alters cervical mucus —> x penetrated by sperm DEC fallopian tube secretion & motility

What are the diff forms of combined estrogen-Progestins/Oral contraceptives?

Oral contraceptive pills Vaginal ring Dermal patch

What are the 2 oral contraceptive pills?

Monophasic COCs Multiphasic COCs

Can you interchange use of tablets in multiphasic COCs?

No, all COCs must be taken at the same time for 21 days followed by a 7 day pill free period

What combination of Estorgen & Progesterone in Vaginal ring?

Etonogestrel (Progestin) & Ethinyl estradiol

WHat combined estrogen & progestin use used in dermal patches?

Norelgestromin & Ethinyl Estradiol => applied in skin every wk for 3 wks => another patch is applied a week after

What are AEs of Combined estrogen & Progestin?

Risk for CVS complciations Risk for cancers

What are C/Is of Combined estrogen + Progestin?

Hx of thrombophlebitis, thromboembolic disease, CVS disease, or coronary artery disease Markedly impaired liver function & liver tumors Congeintal hyperlipidemia Heavy smokers > 35 yo Migraine w/ focal aura DM w/ vascular involvement or >20yrs Uncontrolled HTN Breastfeeding <6wks postpartum Major surgery w/ prolonged immobilization

What are the MOA of Progestin-Only contraceptives?

Thicken cervival mucus Alter endometrium Inhibit ovulation

What are the indicatoins of Progestin-only contraceptives?

Hepatic disease HTN Psychosis Prior thromboembolism

What are C/I ofo Progesitn-only contraceptives?

Current preggos Breast cancer Acute liver disease Liver tumors Undiagnose abnormal genital bleeding

What are the diff forms of Progestin-only contraceptives?

Oral Parenteral Intrauterine system Progestin implants

What are “mini pills” or Progestin-only pills? What are it C/Is?

Lynestrenol (oral prep of Progestin-only) ABSOLUTE C/I: Preggos, breast cancer

What are AEs of Parenteral (DMPA) Progesterone-only contraceptives?

Breakthrough bleeding Delayed conception DEC HDL, INC LDL Weight gain Loss of bone mineral density

WHat are C/Is of DMPA?

Breast cancer & Preggos

What is the MOA of Levonorgestrel (intrauterine system of Progesterone-only contraceptive)?

Inhibit fertilization Inhibt implantation

What are AEs of Progestin-only contraceptives?

Irregular breakthrough bleeding —>Amenorrhea Does not impair breast milk production unlike Estrogens & Do not INC risk of thromboembolism

When should Emergency/Post-coital contaceptives be taken?

Taken w/in 72 hrs-120 hrs

What are the 3 examples of emergency contraceptives?

Progestin Combined Estrogen-Progestin Selective Progesterone-Receptor Modulator

What is the MOA of Androgens?

Converted by 5a-reductase to Dihdyrotestosterone —> binds to the androgen receptor in the cytoplsm

What are the side effects of Androgens?

Early fetal life Puberty Necessary for spermatogenesis Anabolic INC renaly EPO secretion & RBCs DEC HDL in high doses Inhibition of APG via neg feedback

What are the therapeutic uses of Androgens?

Androgen replacment therapy => Male hypogonadism, Andropause, male climcateric, ADAM GYN use => postpartumbreast engorgement & female breast carcinoma Improvement performance in sports

What are AEs of Androgens?

Diminished fertility (Most imprtant) Erythrocytosis with high doses DEC HDL, INC LDL w/ high doses Gynecomastia

What are C/I of Androgens?

Preggos Males w/ prostatic/breast cancer Infants & young children

What are the diff anti-androgens?

Competitive antagonists 5a-reductase inhibitors

What are the diff competitive antagonists & its MOA?

Cyproterone Acetate Flutamide Bicalutamide Spironolactone MOA: Blocks the action of testosterone on the internal genitalia, SM, erythropoiesis & bone

What are the uses & AEs of competitive antagonists?

Uses: Prostatic cancer, Hirsutism, Virilizing syndromes, male precocious puberty AE: Gynecomastia

What are the 2 5a-reductase inhibitors? MOA?

Finasteride Dutasteride MOA: Inhibits the eynzme that converts testosterone to DHT, preventing DHT effects on the external genitalia

What are hte uses of 5a-reductase inhibtors & AEs?

Uses: Benign prostatic hyperplaia Male baldness Female hirsutism AE: Importence & DEC libido

Gonadal Hormones Drugs Flashcards

(61 cards)