Gonadal Hormones Drugs Flashcards
what are the 2 events of ovarian phase?
preovulatory phase = follicular phase
postovulatory phase = luteal phase
what are the uterine endometrial phases?
Preovulatory phase = proliferative phase
postovulatory phase = secretory phase
what are the different effects of Estrogen?
INC in size of uterus, fallopian tubes, vagina, & external genitalia
Thickening of vaginal epithelium (dyspareunia)
what is the basis of fertility awareness method used for family planning or contraception?
Spninnbark estrogen in the Uterus
Why are menopausal women more prone to osteoporosis and fractures?
Estrogen decreases bone resporption
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
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
What are C/Is of Estrogen?
Estrogen-dependent neoplasms
Undiagnosed genital bleeding
Thromboembolic disorders
Liver disease
Heavy smokers
Pregnancy
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)
What do we call amenorrhea that is <1 yr?
Perimenopause
What are the diff selective estrogen receptor modulator?
Tamoxifen
Raloxifene
Clomiphene
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
What is the use of Raloxifene?, & important AE?
Use: prevention & tx of postmenopausal osteoporosis, breast cancer prevention
AE: DVT, hot dlashes
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
What are the 2 anti-estrogens?
Aromatase inhibitors
Estrogen receptor blocker
What is the MOA of Aromatase inhibtors & drugs?
Inhibit the enzyme which converts androgen (testosterone) to androgen
AnasTROZOLE
Exemestane
LeTROZOLE
What is the use of prescribing anti-estrogens?
breast cancers that are R to Tamoxifen
What is the MOA of Estrogen recpetor blocker & drug unde rit?
Prevents dimerization
FUlvestrant
What is the MOA of Progestins?
Similar to Estrogens & Steroids
INC in transcription of target genes in sensitive tissues
What are co-repressors of Progestins?
Progesin recpetor modulator
Antagonist (Mifepristone)
What are the effects of Progestin in the uterus?
DEC uterine motility
Cervical discharge
Endometrium —> secretory changes —> support embyro impant if pregnnacy occurs
What is the effect of Progestin in the breast?
Acinar & lobular development
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
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
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?
- COmbined Estrogen + Progestin
- Progestin-only Contraceptives
- Emergency/Post-coital contraceptives
- 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
