Hormones and Contraceptives Flashcards
MOA of Ethinyl estradiol
synthetic estrogen. Has ethinyl groups (triple bonds) which greatly decrease hepatic metabolism.
In conjunction with progestins, drop FSH and LH levels to prevent ovulation and pregnancy.
MOA of levonorgestrel
synthetic progestin. Thickens cervical mucus to stop sperm. Blocks ovulation 70% of the time.
Progesterone = Pro-pregnancy
breast development, pregnancy maintenance, inhibits uterine contraction, alters carb metab, stimulates fat uptake and bad lipid profile.
MOA of norgestrel
synthetic progestin. Thickens cervical mucus to stop sperm. Blocks ovulation 70% of the time.
Progesterone = Pro-pregnancy
breast development, pregnancy maintenance, inhibits uterine contraction, alters carb metab, stimulates fat uptake and bad lipid profile.
MOA of mestranol
synthetic estrogen.
In conjunction with progestins, drop FSH and LH levels to prevent ovulation and pregnancy.
MOA of mifepristone
antiprogestin. Blocks binding of progesterone to its receptors. Stimulates uterine contractions. Used to terminate pregnancy or as delivery inducer. (must be less than 49 days into pregnancy to abort)
MOA of fluoxymesterone
testosterone derivative. Oral delivery, short acting. Alkylation of 17-a psoition allows oral admin becuase it decreses hepatic metabolism.
MOA of testosterone transdermal patches
better than oral or injection.
MOA of danazol
androgen. Used to treat endometriosis and PMS. Weakly androgenic. IM injection. Long acting.
ADE of testosterone supplementation?
Makes ladies into dudes and dudes into ladies.
virilizing females.
Feminizing males because testot converted to estradiol.
Suppression of LH and FSH decereases testis, spermatogen.
Decreases HDL and increases LDL increasing CHD risk.
MOA of cyproterone acetate
Competes with DHT for androgen repceptor to prevent translocation to nucleus.
IM injection, long acting. Used to treat acne, baldness, hirsutism.
ADE of cyproterone acetate
inhibits libido
MOA of flutamide
androgen receptor antagonist. Treats prostate cancer.
ADE of flutamide
Hepatic toxicity and must be taken 3x daily
MOA of onapristone
antiprogestin. a more pure antagonist.. Used to terminate pregnancy. (must be less than 49 days into pregnancy)
MOA of anastrozole
aromatase inhibitor. non-steroidal. used after tamoxifen failure. Decreases estrogen to extremely low levels by inhibiting conversion of adrenal androgens to estrogens.
MOA of letrozole
aromatase inhibitor. non-steroidal. used after tamoxifen failure. Decreases estrogen to extremely low levels by inhibiting conversion of adrenal androgens to estrogens.
MOA of testosterone cypionate derative
testosterone derivative.
MOA of copper IUD
one of the most effective contraceptives. Copper is spermacidal. Effective for 15-20 years.
ADE of copper IUDs
copper can cause cramping and progestin-irrugular bleeding. High initial cost, low overall. Must be inserted by physician.
MOA of vaginal contraceptive rings
one of the most effective contraceptives. Inserted by patient.
ADE of vaginal contraceptive rings
discomfort, headaches, vaginal discharge. Not effective for 7 days.
Which hormone would make myometrium smooth muscle hyperpolarized: estrogen or progesterone? What effect does this have?
Progesterone is elevated in pregnancy. It hyperpolarizes uterine smooth muscle membranes making them non-excitable and preventing release of arachidonic acid, preventing prostaglandins from being made.
What effect does estrogen have on myometrium gap junctions?
estrogen increases the number of gap junctions that couple the myometrial muscle cels. This also increases the receptors for contractile agonists, making contraction more likely
What do tocolytics do?
prevent contraction –> prevent premature parturition and delay delivery for brief periods
What do oxytocics do?
induce contractions. –>labor. control postpartum uterine hemorrhage. Therapeutic abortion
What are the 3 natural estrogens?
estradiol (most potent and principal ovarian steroid)
estrone
estriol (least potent, placental steroid and made from estradiol and estrone in liver and adipose)
What are the differences between selective estrogen receptor modulators and antiestrogens?
SERM = selective estrogen receptor modulator. Produce estrogen effects only where beneficial (bone, brain, liver) and avoid breast and endometrium. Ex. tamoxifen.
Antiestrogens (clomiphene) antagonize all tissues and are used as ovulation inducing agents.
How are the majority of estrogens and androgens transported in blood?
bound to sex hormone binding globulin (SHBG)
How would administration of estrogen affect SHBG and free androgen levels?
estrogen will increase SHBG, decreasing free angrogen levels
How is progesterone primarily transported in blood?
bound to transcortin
What effect do estrogens have on lipid profile?
increase HDL, decrease LDL and lower incidence of CHD in pre-menopausal women. Estrogens do increase risk of stroke+DVT though because of increased clotting factors.
What effect do estrogens have on bone resorption? How?
decrease bone resorption and oppose osteoporosis by decreasing activity and number of osteoclasts
What effect do estrogens have on hepatic proteins and clotting factors?
increases TBG, transcortin, SHBG and clotting factors.
Usually giving estrogen is a bad idea for cancer. It can stimulate progression of endometrial and breast tumors. When is it helpful?
prostate cancer.
What effect does progesterone have on carb metab?
increases basal insulin levels and promotes glycogen storage.
What effect does progesterone have on lipid profile?
Opposite of estrogen. Decreases HDL and increases LDL. Also stimulates LPL (fat transfer from lipoproteins to tissue) Increase risk of CHD.
Which hormone is responsible for the spike in body temperature at ovulation?
progesterone
What is the minipill?
progestin only pill.
A patient asks what the most effective forms of contraception are
Sterilization, IUDs, progestin implants, —> least effective = barriers like condoms and diaphragms
In addition to antibiotics, what other drugs can cause oral contraceptives to fail?
rafampin, anti-HIV agents, anticonvulsants, and St. John’s wort.
Compare DHT to tesetosterone.
DHT is made by 5a-reductase. It is more potent and binds 10x tighter than testosterone
ADEs of progesterone?
GI, menstrual disorders, bad lipid profiles, depression, acne, weight gain
ADE of letrozole
non-steroidal AIs can cause cataracts.
Hot flashes, Nausea, Hair thinning (no effect on adrenal steroids/thyroid function). arthralgia/diarrhea but less gyn Sx then tamoxifen.
ADE of anastrozole
non-steroidal AIs can cause cataracts.
Hot flashes, Nausea, Hair thinning (no effect on adrenal steroids/thyroid function). arthralgia/diarrhea but less gyn Sx then tamoxifen.
