Lifecycle drugs Flashcards
Ethinyl estradiol MOA
Closely related drugs:
mestranol, estradiol valerate, conjugated equine or esterified estrogens, estradiol (oral, transdermal)
MOA:
agonist for estrogen receptors (ER) that act by: (1) binding to ERE elements in promoter to affect transcription (2) binding to other transcription factors to stimulate or inhibit transcription (3) binding to intracellular signaling molecules in the cytoplasm to regulate kinases and GPCR pathways
Clinical uses:
combined birth control methods, dysfunctional uterine bleeding, dysmenorrhea, menopausal symptoms, ovarian insufficiency, induces secondary sexual characteristics for delayed puberty
notes:
ethinyl estradiol and mestranol are resistant to first pass liver metabolism and are orally active.
Side effect:
“Thrombosis
Inc Breast Cancer Risk (?)”
Clomiphene
MOA: partial agonist/antagonist at ER
Use:
induces ovulation, male infertility
notes:
Clomiphene is a nonsteroidal compound with tissue-selective actions. It is used to induce ovulation in anovulatory women who wish to become pregnant. By selectively blocking estrogen receptors in the pituitary, clomiphene reduces negative feedback and increases FSH and LH output. The increase in gonadotropins stimulates ovulation.
ospemifene
MOA: partial agonist at ER on vaginal tissue
Use:
treat vaginal dryness, genito-vaginal pain due to vaginal atrophy
Notes:
selective estrogen receptor modulator (SERM) that acts as an estrogen agonist in the vagina and appears to have no clinically significant estrogenic effect on the endometrium or breast
Side effects:
hot flushes
tamoxifen
MOA:
SERM: acts as ER antagonist in breast CA but can be an agonist in other tissues (endometrium)
uses:
breast CA
Notes:
As an agonist of endometrial receptors, tamoxifen promotes endometrial hyperplasia and increases the risk of endometrial cancer
side effects:
hot flushes (an antagonist effect)
increases the risk of venous thrombosis (an agonist effect).
Tamoxifen has more agonist than antagonist action on bone and thus prevents osteoporosis in postmenopausal wome
raloxifene
MOA:
SERM: acts as ER antagonist or agonist depending on cell type
Use:
osteoporosis
Notes: "Raloxifene, approved for prevention and treatment of osteoporosis in postmenopausal women, has a partial agonist effect on bone. Like tamoxifen, raloxifene has antagonist effects in breast tissue and reduces the incidence of breast cancer in women who are at very high risk. Unlike tamoxifen, the drug h as no estrogenic effects on endometrial tissue"
Fulvestrant
MOA:
ER antagonist
Uses:
precocious puberty, breast cancer (resistant to tamoxifen)
Norethindrone acetate
MOA:
agonist for progesterone receptors (PR) that act by the same mechanisms listed for ER
Use:
combined or progestin only birth control, dysfunctional uterine bleeding, endometrial hyperplasia, menopausal symptoms
mifepristone
MOA:
competitive antagonist at PR
Uses:
Non-surgical abortion and miscarriage
emergecny contraception
Anastrazole
MOA:
inhibits aromatase enzyme and the conversion of androgens to estrogens in peripheral tissues
uses:
ovulation induction, estrogen dependent cancers (breast CA), treatment of fibroids
leuprolide
MOA:
GnRH receptor agonist that down-regulates receptor and suppresses gonadotropin (LH and FSH) secretion
uses:
delay pubertal maturation, precocious puberty, dysmenorrhea, endometrosis, fibroids, prostate CA
danazol
MOA:
partial agonist/antagonist at AR
Uses:
endometriosis
spironolactone
MOA:
aldosterone receptor antagonist with anti-androgen effect
Use:
treats hirsuitism associated with PCOS
testosterone
MOA: androgen receptor (AR) agonist that acts by the same mechanisms listed for ER
Uses: Androgen deficiency (increases bone density, libido, muscle mass). Induces secondary sex characteristics with delayed puberty, sexual dysfunction in women
flutamide
MOA:
AR antagonist
use:
prostate cancer
oxandrolone
MOA:
AR agonist
Uses:
anabolic effects, treatment of burns, osteoporosis
Finasteride
MOA:
inhibits the 5-a-reductase enzyme that metabolizes T to DHT
Uses:
BPH
Tamsulosin
MOA:
a1-adrenergic receptor antagonists
uses:
BPH
Abarelix
MOA:
GnRH receptor antagonists that suppress gonadotropin secretion
Uses:
Prostate Cancer
RhoD immunoglobulin
MOA:
IgG antibody prep used to prevent maternal immune reaction to fetal RhD positive erythrocytes
Uses
Used for vaginal bleeding and routine prophylaxis in RhD negative women
Bromocriptine
MOA:
dopamine D2 receptor agonist
uses:
used to treat hyperprolactinaemia and lactation suppression
Metoclopramide
MOA:
central and peripheral dopamine D2 receptor antagonist
Uses:
galactogogue, low milk supply
Domperidone
MOA:
dopamine D2 receptor antagonist (peripheral - does not cross blood brain barrier)
Uses:
galactogogue, low milk supply
Mifepristone
MOA:
antagonist at the progesterone receptor (PR)
Use:
pregnancy termination together with misoprostol
Misoprostol
MOA:
prostaglandin E1 analog
Uses:
induces uterine contractions, also used as a uterotonic for labor induction and treatment of postpartum hemorrhage
Methotrexate
MOA:
DHFR inhibitor
Use:
pregnancy termination together with misoprostol
Terbutaline
MOA:
b2 agonists that cause uterine relaxation
uses:
preterm labor
nifedipine
MOA:
calcium channel blocker which causes uterine relaxation
uses:
preterm labor
Magnesium sulfate
MOA:
likely works by inhibiting calcium channels, resulting in a reduction of intracellular calcium
Use:
preterm labor, fetal neuroprotection, treatment and prevention of eclampsia
Indomethacin
MOA:
inhibit calcium release from the sarcoplasmic reticulum and decreases production of prostaglandins that stimulate contractions and cervical change.
Use:
preterm labor
oxytocin
MOA:
acts on oxytocin GPCR (Gq-linked) to increase intracellular calcium and cause uterine contraction
use:
induce contractions during labor, postpartum hemorrhage, for abnormal milk-let down
cabroprost (hemabate)
MoA:
analogue of prostaglandin F2-alpha results in uterine contractions
uses:
used to treat postpartum hemorrhage
DONT USE WITH asthma
Methylergonovine (methergine)
MOA;
binds several GPCRs including 5-HT2A serotonin receptors leading to contraction of uterine smooth muscle
Use:
used to treat postpartum hemorrhage
don’t use with hypertensive patients
Misoprostol
MOA:
prostaglandin E1 analog
Use:
induces uterine contractions, also used as a uterotonic for labor induction and treatment of postpartum hemorrhage
Dinoprostone
MOA:
intravaginal prostaglandin insert
Uses:
induces uterine contractions and causes cervical ripening
Prostagladin E2
MOA:
intravaginal prostaglandin gel
USes:
induces uterine contractions and causes cervical ripening
