pharm of reproduction Flashcards
1
Q
natural estrogens
A
- estradiol (E2), estrone (E1) and estriol (E3)
- ovary is primary source of E2 in premenopasual women
- aromatase converts testosterone to estradiol and androstenedione to estrone
- aromatase present in ovaries, placenta, adrenal gland, adipose tissue, testicles and brain
- E2 has extensive 1st pass effect –> metabolized in liver to E1 so its not used orally (micronization increases t1/2)
2
Q
physiologic effects of estrogen
A
- (-) and (+) feedacback on gonadotropin release
- increases HDL and lowers LDL (good- one thing I have going for me..)
- decreases bone resorption
- increase body fat, salt and fluid retention
3
Q
tx uses of estrogen
A
- contraception: negative feedback on gonadotropins
- primary hypogonadism: used as replacement tx in PTs with E deficiency
- postmenopausal hormone tx: reduce hot flashes, atrophic vaginitis and prevent osteoporosis
4
Q
common adverse effects of estrogens
A
- nausea
- breast tenderness
- vaginal bleeding
- HA
- weight gain
- HTN
5
Q
less common adverse effects of E
A
- breast cancer (controversial)
- DVT and PE (stimulates liver to make clotting factors at high concentrations)
- HA and stroke
- gallbladder diseasee
- cervical and endometrial cancers (E is proliferative)
6
Q
contraindications of E
A
- PTs with breast of endometrial cancers, endometriosis and undiagnosed vaginal bleeding
- generally contraindicated in PTs with thromboembolic disease, HTN, hepatic disease of FHx of breast/uterine cancer
7
Q
Tamoxifen
A
- SERM (non steroidal)
- antiestrogenic effect on mammary epi
- pro-estrogenic effect on endometrium and bone
- tx: ER (+) breast cancers but must be used at much higher concentration than E to compete effectively
- prolonged use –> endometrial carcinoma
8
Q
Clomiphene citrate
A
- fertility pill
- E antagonist - blocks E binding to its receptor in hypothalamus –> inhibit E (-) feedback –> increased secretion of LH and FSH –> ovulation
- 50-100 mg for 5 days
9
Q
adverse effects of Clompihene
A
- symptoms of menopause (hot flashes) – because it’s antiestrogenic
- stomach pain
- HA
- upset stomach
- vomiting
- multiple pregnancy
10
Q
physiologic effects of progesterone
A
- secreted by CL or by placenta during pregnancy
- stimulates endo to develop secretory glands and support fertilized egg implantation
- growth suppressing effect on endometrium
- negative feedback on hypothalamus to stop releasing gonadotropins
11
Q
synthetic progestins
A
- medroxyprogesterone, Norethindrone, Norgestrel, Megestrol
- more SE than natural progestins
- strong androgenic activity –> hirsutism, acne
12
Q
contraindications of progestins
A
- thromboembolic disorders
- liver disease (metabolized in liver)
- undiagnosed vaginal bleeding
- pregnancy –> atrophic effect on endometrium
**note: only the Estrogens can cause cancer
13
Q
combined oral contraceptives/the pill/BC
A
- most effective form (99.9%) –> failure rates due to poor compliance
- estrogenic agent: suppress FSH secretion –> prevent follicle maturation; prevent LH surge
- progestin agent: prevent LH surge; thicken cervical mucosa to make impenetrable to sperm and reduces risk of endometrial cancer
14
Q
progestin-only oral contraceptives
A
- less effective than COCs
- useful when estrogens are contraindicated (ie: FHx of endometrial cancer)
- lactating women (E in COC reduces milk production)
- more likely to produce irregular menstrual cycles (E provides endometrial stability) –> break through bleeding!
15
Q
postcoital contraceptive (morning after pill)
A
- interferes with implantation and/or delays ovulation
- higher does of levonorgestrel (progestrin)
- no RX needed
