Pharmacology of Female Reproductive System Flashcards
What is Endometriosis?
Characterized by dysmenorrhea, dyspareunia, dysuria, pain during defecation and infertility
Goal of treatment is to decrease pain and induce regression/ control further growth of ectopic endometrial tissue
What drugs can be used for endometriosis?
- Combined oral contraceptives
- Progestin
- GnRH agonists
- Anastrozole
- Danazol
How do combined oral contraceptives help with endometriosis? MOA?
reduce pain by decreasing mestrual flow and regressing endometrial growth
What are the adverse effects of combined oral contraceptives?
Nausea, bloating, headache
C/I in women with history of thromboembolism
What is the MOA of Progestin?
Induce atrophy of endometrial tissue
What are the adverse effects of progestin?
Breakthrough bleeding, weight gain, fluid rentention and mood swings
Mechanism of action for Goserelin, leuprolide and nafarelin?
inhibit ovarian estrogen production-> estrogen deprivation diminishes endometrial implants
What are the adverse effects of goserelin, leuprolide, and nafarelin?
Bone loss -> prevented with Bisphosphonates
and vasomotor symptoms
What is the MOA of Anastrozole?
competitive inhibitor of aromatase activity
Adverse Effects of Anastozole?
arthralgia, diarrhea and osteoporosis
What is the MOA of Danazol?
synthetic derivative of 17 ethinyltestosterone
results in decrease FSH and LH
induces anovulation, amenorrhea and endometrial atrophy
What are the adverse effects of Danazol?
acne, hirsutism, occasional irreversible virilization,
menstrual irregularities, decreased breast size,
hepatotoxic and thromboembolism
What is Polycystic Ovarian Syndrome?
characterized by menstrual irregularities, amenorrhea or anovulation, hirsutism, acne and infertility
What medications can be used for Polycystic Ovarian Syndrome?
- Combined oral contraceptives
- Spironolactone
- Finasteride, flutamide
- GnRH agonist
- Clomiphene
- Metformin
How do combined oral contraceptives help polycystic ovarian syndrome? MOA?
decrease serum testosterone levels by decreasing ovarian androgen secretion and stimulating hepatic synthesis of sex hormone binding globulin SHGB
What is the MOA of spironolactone?
aldosterone receptor antagonist
weak inhibitor of testosterone synthesis also 5 alpha reductase
what is the MOA of finasteride and flutamide
anti androgen agents
also inhibts 5 alpha reductase and androgen R inhibitor
What is the MOA of GnRH agonists fo PCOS?
suppress ovarian androgen and estrogen synthesis
What is the MOA of Clomiphene citrate?
Ovulation inducer: blocks estrogen receptors in the hypothalamus and anterior pituitary inhibits estradiols negative feedback increase FSH and LH
What is the adverse effect of clomiphene citrate?
ovarian hyperstimulation increase incidence with multiple births ovarian cysts and hot flashes
What is the MOA of metformin?
corrects hyperinsulinemia in PCOS and may promote ovulation
What is menopause?
characterized by symptoms of estrogen deficiency (hot flashes, chills, sweating, headache, palpitations, vaginal and urethral atrophy, osteoporosis, cardiovascular changes)
What is the treatment for menopause ? and what is its MOA?
Post menopausal Hormonal Replacement Therapy
oral, transdermal and vaginal
lowest dose of estrogen for limited period of time
**can use bisphosphonates for bone loss
Hot flashes are the most common indication of short course of HRT
with intact uterus should take estrogen +progestin
what are the adverse effects of post menopausal hormonal replacement therapy
estogen only replacement can cause endometrial carcinoma
vasomotor symptoms can be relieved by clonidine
What are uterine leiomyomas?
fibroids, myomas
symptoms include: irregular excessive bleeding, pressure, pain during intercourse, pelvic pain, recurrent pregnancy loss, infertility, may be asymptomatic
surgery is the definitive treatment
reproductive years and regress after menopause
What are the medications for uterine leiomyomas?
- GnRH agonists
- Levonorgestrel
- Mifepristone
How does GnRH agonists help uterine leiomyomas?
significant reduction (35-60%) in uterine size within 3 months
What are the adverse effects of GnRH agonists?
hot flashes, sleep distrubances, vaginal dryness, myalgias, arthralgias, bone loss, impairment of mood cognition
What are the MOA of Levonorgestrel?
reduction in uterine volume and bleeding and increase in hematocrit
What is the MOA of mifepristone?
anti progesterone
