Reproduction Drugs Flashcards
(24 cards)
Name 4 estradiol esters (steroidal)
Estradiol (valerate and cypionate)
Estrone Sulfate
Equilin Sulfate
quinestrol
What is the mechanism and applications of estradiol esters and alkyl estrogens
Absorbed though skin, mucous membranes, GI tract; body wide distribution via sex hormone binding globulin.
Contraception, primary hypogonadism, postemenopausal hormone therapy
Name 2 alkyl estrogens
Ethinyl estradiol
Mestranol
Name a non-steroidal synthetic estrogen
Diethylstilbestrol (DES)
Name a non-steroidal anti estrogen; SERM
Tamoxifen citrate (Nolvadex)
name a non-steroidal anti estrogen
Clomiphene citrate (Clomid)
How does tamoxifen work and what is it used for?
Blocks estrogen from binding to ER and causing growth in ER+ breast cancers.
What are the side effects of tamoxifen?
Pre-estrogenic effect on uterine epithelium increases the risk of endometrial cancers.
How does clomiphene citrate work and what is it used for?
Blockes estrogen binding to hypothalamic receptors (no estradiol negative feedback on gonadotropins) –> increased secretion of gonadotropins and LH –> ovulation.
It is used to stimulate ovulation in patients who want to get preggers
What are the side effects of clomiphene citrate
Hot flashes, multiple pregnancy
Name two natural progesterone products
Micronized progesterone and transvaginal progesterone
What is the mechanism and side effects of transvaginal progesteron
Binds to PR; vaginal gel (uterine effects without first pass metabolism and minimal systemic side effects
Fatigue and Drowsiness
Name 4 synthetic progesterones
Medroxyprogesterone
norethindrone
norgestrel
Megestrol
What are the side effects of synthetic progesterones?
Important: edema, abdominal bloating; less commonly strong androgenic effects (hirsutism, acne)
Others: Anxiety, irritability, depression, muscular pain; increased risk of thrombus and PE
What are the applications of all progesterone products?
Contraception and hormone replacement therapy
What are the 3 types of combination contraception pills? What are their mechanisms and what are their side effects
Monophasic, Biphasic, and triphasic orthonovum.
COnstant level of estrogen suppresses FSH and LH surge; progesterone suppresses LH surge, thickens cervical mucus and leads to endometrial atrophy.
Side effects are as with synthetic estrogens and progesterones
What is the mini-pill? what are its indications and side effects?
It is progestin only.
It is less effective than combo pill but is use in patient with estrogen containdications, good in lactating women (estrogen reduces milk production)
It is more likely to produce irregular menstrual cycle
What type of drug is levonogestrel (Plan B) how does it work?
synthetic progestogen.
Prevents implantation
What is mifepristone ( RU-486, korlym) how does it work? what are its side effects
Anti-progestin; glucocorticoid receptor antagonist.
Competitively binds to progesterone receptor(leading to detachment of fetus)
Abortion, cushings syndrome
What are 3 PDE-5 inhibitors?
Sidenafil citrate (Viagra t0.5 4hrs) Vardenafil HCl (Levitra t0.5 4hrs) Tadalafil (Cialis t0.5 17.5hrs)
What are the side effects of PDE-5 inhibitors?
Headache, dizziness, change in vision
When are PDE-5 inhibitors contarindicated
in patients on nitrates or alpha blockers.
What is the mechanism of micronized progesterone and its side effects?
binds to PR; decreades first pass metabolism and enhances dissolution to micronization.
Fatigue and Drowsiness
What are the side effects of etrogen products?
Weight gain, HTN; less commonly, may cause breast cancer, DVT, cervical and endometrial cancer.
Nausea breast tension/pain, vaginal bleeding, headache.
