[PHARMA] CONTRACEPTION & FERTILITY Flashcards
ethinyl estradiol
diethyl stilbosterol side effects(4)
1-nausea, breast tenderness, weight gain
2-endometrial hyperplasia
↑endo & breast cancer risk
3-HTN & thromboembolism
4-male= feminization, impotence, decreased libido, gynecomastia
adv effects of ethinyl estradiol & diethyl stilbosterol in MALES (4)
1-impotence
2-decreased libido
3-feminization
4-gynecomastia
Synthetic estrogens
ethinyl estradiol
diethyl stilbosterol
synthetic estrogens uses (2)
1-OC
2-HRT in
(a) 1ry hypogonadism
(b) postmenopause
effects of synthetic estrogens during the postmenopausal period (3)
1- ↓osteoporosis
2-↓menopausal symptoms
3- Cardioprotective: ↓LDL ↑HDL
synthetic progestins(3)
1-norethindrone
2-norgestrel
3-medroxyprogesterone
synthetic progestins uses (3)
1-hormonal contraception
2-dysmenorrhea
3-endometriosis
synthetic progestins adv effects (5)
1-irregular bleeding followed by amenorrhea
2-edema, HTN, weight gain
3-depression
4-↓HDL
5-acne, hirustism
ovulation inducing agents (5)
1-clomiphene
2-bromocriptine
3-gonadorelin
4-hCG
5-human menopausal gonadotropins
ergot alkaloids (2)
1-methylergometrine
2-methylergonovine
methylergometrine & methylergonovine advantages (3)
1-potent
2-prolonged sustained uterine contractions
3-less toxic
methylergometrine & methylergonovine CI
delivery inducers= fetal distress & mortality
DOC in postpartum Hg
ergot alkaloids
ergot alkaloids mechanism of action
mixed partial agonists at α adrenoreceptors & 5HT receptors
ergot alkaloids route
-oral
-parenteral IM
-intramyometrial
why are ergots not given IV
cause severe VC
ergot alkaloids uses (3)
1-postpartum Hg
2-after C-section & instrumental surgery= prevent uterine atony
3-subinvolution of uterus
ergots CI (3)
1-pregnancy
2-HTN patients
3-coronary artery disease
ergots adv effects (6)
1-vasospasm
2-palpitations
3-↑ BP
4-seizures
5-abdominal pain, nausea, vomiting
6-↓milk production w/ prolonged usage
oral contraceptives mechanism of action
1-(-) FSH & LH= (-) ovulation
2- change cervical mucous= thick & viscid
3-↓ endometrial glycogen= inhibits implanatation
combined OCs
most effective estrog+progest
minipills
progestin only
less reliable but no risk of thromoboembolism
parenteral progestin preparations
1-implants norgesterel—> 5 years
2-depot injection: medroxyprogesterone–> every 3 months
OCs indication
contraception
irregular cycle
minor risks of OCs (3)
1-nausea, vomiting, headache
2-breast tenderness
3-edema
intermediate risks of OCs (3)
1-bleeding (low dose)
2-amenorrhea (high dose)
3-acne, hirstusim, skin pigmentation
major risks of OCS (4)
1-CVS= thromboembolism, pulmonary embolism, MI, stroke, HTN
2-carcinogenic= ↑ breast & endo cancer
3-depression
4-cholecystitis, jaundice, gall stones
drug interactions of OCs
enzyme inducers:
rifampcin ↓ efficacy of OC
increased risk of cervical & breast cancer caused by OCs can be ↓ by
adding progestins
clomiphene mechanism of action
partial agonist
(-) central estrogen receptors in hypothalamus
(-) feedback inhibition of FSHRH & LHRH
(+) ovulation & corpus luteum formation
clomiphene route
oral
clomiphene uses (2)
1-female infertility (ovulation disorders)
2-IVF w/ gonadotropins
IVF drugs (3)
1-clomiphene
2-GnRH
3-hCG
clomiphene adv effects (3)
1-hot flushes
2-multiple pregnancies
3-ovary overstimulation
tamoxifen uses
TTT of hormone-sensitive breast cancer
tamoxifen mechanism of action
selective estrogen receptor modulator (SERM) peripherally
ANTAGONIST–> Breast= (-) endogenous estrogen from activating receptors in estrogen sensitive cancer
AGONIST–> bone= increase density (-)osteoporosis in pt w/ breast cancer
uterus=↑ endo cancer risk
tamoxifen adv effects (3)
1-hot flushes
2-vaginal discharge
3-menstrual irregularity
raloxifen mechanism of action
SERM partial agonist
similar to estrogen on bone but NOT ON breast/uterus= no cancer risk
raloxifen uses
TTT of osteoporosis
drug causing ovary overstimulation
clomiphene
drugs reducing milk production
ergot alkaloids
acts centrally
clomiphene
acts peripherally
tamoxifen
treats osteoporosis
raloxifen
↑ risk of endometrial cancer
1-synthetic estrogens
2-tamoxifen
↑risk of cervical & breast cancer
combined OC
decrease risk of breast cancer
tamoxifen
used to induce abortion in case of intrauterine fetal death
mifepristone
raloxifene side effects
1-hot flushes, sweating
2-leg spasms
raloxifene CI
venous thromboembolism
combined OC CI
liver disease
contraindicated in coronary artery disease
ergots
contraindicated in venous thromboembolism
raloxifene
contraindicated in pregnancy & HTN patients
ergots
antiprogestin
mifepristone
mifepristone mechanism of action
competitive inhibitor of progesterone & glucocorticoids receptors
mifepristone use
therapeutic abortion
GnRH
1-gonadorelin
2-leuprolide
3-nafarelin
use of GnRH given in pulses
infertility= ↑gonadotropins= (+) ovulation
use of GnRH given continuously (3)
↓ gonadotropins:
1-cancer prostate
2-endometriosis
3-IVF
GnRH adv effects (3)
1-hot flushes, headache, depression
2-vaginal dryness, ovarian cyst, ↓libido
3-osteoporosis
GnRH anatogonist
ganirelix
ganirelix uses
1-controlled ovarian hyperstimulation ( inhibit LH surge)
2-advanced prostatic cancer
gonadotropins FSH, LH uses
1-(+) spermatogenesis + testosterone
2-(+) ovulation & ER/PR
drugs used in prostatic cancer
GnRH
ganirelix
hMG (3)
menotropins (FSH+LH)
urofollitropin (FSH) follitropin
r-FSH
hcG similar to
LH
hcG uses (3)
1-infertility–>IVF
2-undescended testis
3-1ry or 2ry amenorrhea dt ↓gonadotropins
gonadotropins adv effects (4)
1-hyperstimulation $
2-multiple births
3-spontaneous abortions
4-gynecomastia in males
pulsatile GnRH route
SC
hcG route
parenteral
