Womens Health * Flashcards
Estrogens *
Drug- estradiol- multiple forms, PO-estrace/topical-dirigel, estrogel/ transdermal-alora, climara, vivelle/cream-estrace/insert-vagifem/ring-estring, femring-conjugated estrogens (premarin), esterfied estrogens (menest), estropipate, ethyl estradiol
MOA- activated steroid receptor complex interacts with nuclear chromatin to initiate hormone specific RNA synthesis
Uses:
-post menopausal HRT for vasomotor instability, vaginal atrophy, if the women had a uterus progestogen must be used as well to reduce risk of endometrial cancer, if no uterus unopposed estrogen is used and progestins can cause HLD, ADE are less in those using for contraception, can use patch or gel, increase risk of CV event and breast cancer, women with GU symptoms best to use vaginal estrogens
-contraception- combination of estrogen and progestogen is best, oral, transdermal, vaginal
-replacement in premenopausal women who are deficient- for primary hypogonadism estrogen minims natural cycle and progestogen stimulate development of secondary sexual characteristics, may be continued until after growth has completed, for premature menopause-estrogen and progestogen replacement is used
AE-nausea, breast tenderness, elevated BP, elevation of TG, peripheral edema; increased risk of VTE, increase risk of breast and endometrial cancer
Selective estrogen receptor modulators *
Drugs-tamoxifen, toremifene (fareston), raloxifene (evista), clomiphene (clomid), ospemifene (osphena)
MOA-compete with estrogen for binding in breast tissue, does not have appreciable estrogen receptors agonist activity in endometrium unlike others, no risk of endometrial CA, clomiphene acts as a partial estrogen agonist and interferes with negative feedback of estrogen on the hypothalamus, increase secretion of gonadotropin releasing hormone and gonadotropins, stimulating ovulation
Uses
-tamoxifen-metastatic breast CA, after mastectomy or XRT for breast CA, prevent of breast CA
-raloxifene-prevention of breast CA, prevention and tx of osteoporosis in post menopausal women
-clomiphene-used for infertility from anovulatory cycles
-ospemifene-tx for dyspareunia from menopause
Pharm-rapid absorb via PO, tamoxifen-
ADE- tamoxifene and toremifene-hot flashes, nausea, endometrial hyperplasia, malignancies
-raloxifene-hot flashes, leg cramps, VTE, avoid use of questrans as this increases risk
-clomiphene-HA, nausea, vasomotor flushes, visual disturbances, ovarian enlargement, increased risk of multiple births dose related
D-D- many as it’s CYP450 isoenxyme
Progestogens *
Drugs-many-desogestrel, dienogest, drospirenone, etonogestrel, levonorgestrel, medroxyprogesterone, norelgestromin, norethindrone, progesterone
MOA- promotes development of secretory endometrium that accommodates implantation of newly forming embryo, if conception occurs progesterone continues to be products to marination the endometrium and reduce contractions, if conception does not occur release of progesterone from corpus luteum stops this declines cause menstruation to occur
Uses-contraception-combined with estrogen, hormone deficiency, DUB, dysmenorrhea, endometriosis, infertility
AE-HA, depression, and weight gain, changes in libido, progestins derived from 19-nortesterone posses some androgenic activity and can cause acne and hirsutism, norgestimate and drospirenone are preferred in women with acne but can raise K
Progesterone antagonist *
Drug-mifepristone (mifeprex)
MOA- Progesterone antagonist with partial agonist activity,
Uses- abortion , Often combined with prostaglandin analog misoprostol to induce contractions
ADE- abdominal pain, uterine bleeding, incomplete termination of pregnancy
Contraceptives *
Interferes with ovulation. Most common pharmacological intervention for preventing pregnancy
Major classes-combined oral contraceptive, patch, rings, progestins-ring or injection, LARCs-inolant or IUD, emergency
MOA- estrogens provide negative feedback on the release of LH and FSH by the pituitary preventing ovulation, progestin thickens cervixal mucus
ADE estrogen- breast fullness, fluid retention, HA, nausea, elevated BP, VTE, thrombophlebitis
ADE progestins-depression, changes in libido, hirsutism, acne
Cervical CA risk may be increase, but associated with decrease risk of endometrial and ovarian CA
Should not be used those greater than 35 and smoke
Combined oral contraceptives *
Drug- Combination of estrogen and progestin
Monophasic combination pills contain a constant dose of estrogen and progestin over 21-24 days
Triphasuc attempt to mimic natural female cycle-most contain a constant dose of estrogen with increase doses of progestin given over 3 successive 7 day periods-acid pills are taken 21-24 days followed by 4-7 days placebo, for 28 total days, withdrawal bleeding occurs during hormone free period
Extended cycle contraception 84 pills followed by 7 days placebo results in less withdrawal bleeding
Most common estrogen-ethinyl estradiol
Most common progestins-norethinadrone, norethindrone acetate, levonorgestrel, desogestrel, norgestimate, drosperidone
First choice for starting should be a monophasic product with a 2nd generation progestin
Other uses- regulating cycle, reduce heavy bleeding, management of acne, dysmenorrhea, PMS, reduce risk of ovarian, endometrial and colon CA, prevent bone loss reduce risk of osteoporosis
Products with drospirenone less likely to have HTN more likely to improve mood and lessen weight gain with PMS
Contraceptive patch *
Drug- ethyl estrogen with a progestin
Applied once a week for 3 weeks
Each patch worn for one week and withdrawal bleed on fourth week
Similar efficacy for PO contraceptives but less effective in those greater than 90 kg
May give more estrogen than oral more risk for VTE and higher body mass
Emergency contraception *
Reduces chance of pregnancy after an episode of unprotected sex or ineffective protection
Reduces chance of pregnancy to 0.2-3%
High doses of levonorgestrel or high doses of ethinyl estradiol and levonorgestrel
Should be taken ASAP after intercourse preferable within 72 hours
Progestins only EC better tolerated than estrogen/progestin combination
Alternatives-progesterone agonist/angagonist-ulipristal (Ella) can be used as EC within 5 days of unprotected sex
Plan B, one step, next choice, one dose, my way, cooper IUD up to 5 post unprotected sex can also be used
Androgens *
Drugs- many- testosterone based
MOA- exogenous testosterone binds to androgen receptor sites, needs DHT to synthesize
Uses- primary hypogonadism, testosterone replacement with low levels not related to aging, gender change, chronic wasting, off label use for performance enhancing
ADE- non males- masculine changes like acne growth, facial hair, deep voice, male pattern baldness, changes in menstrual cycle-do not use in pregnancy-in males- priapism, impotence, gynecomastia, masculine changes-in children-abnormal sexual maturation
Increased risk for CV even
Antiandrogens *
Drugs- Finasteride (proscar) and dutasteride (avodart) are use for BPH
Flutamide (eulexin), bicalutamide (casodex), enzalutiamide (xtandi), nilutamide (nilandron) acts as a competitive inhibitors of androgens at the target cell for tx of prostate CA
MOA- Counter make hormonal action interfering with synthesis of androgens
Non hormonal contraceptives *
Vaginal spermicides
Male and female condoms
Diaphragm-rx requires, left in place for 6 hours
Cervical cap-tx required can be left in place 48 hours
Sponge-left in place 6 hiurs
Para guard copper IUD rx required
Drugs to manage menopause *
Systemic hormones like estrogen alone or in combination with progestin for vasomotor symptoms for 5 years or less
Also SSRI, SNRIs (paroxetine) clonidine , gabapentin (both not FDA approved for hot flashes)
No recommendations for phytoesteogens, herbals, or bio identical regiments for s/s
Oral and transdermal regiments reduced hot flashes by 75%
Contraindications-undiagnosed vaginal bleeding, estrogen dependent malignancy, DVT hx, migraines, endometriosis, liver disease, strong FH of breast CA
ALL ESTROGEN PRODUCTS HAVE A BLACK BOX WARNING FOR INCREASED RISK OF DEMENTIAL IN POSTMENOPAUSAL WOMEN GREATER THAN 65 YEARS
Bazedoxifene/conjugated estrogen
Used for menopause for vasomotor symptoms
Bazedoxifene acts as a antagonist for estrogen receptors in uterine tissue, also for osteoporosis in women with a uterus
SE- muscle spasms, diarrhea, nausea, indigestion, upper abd pain
Vaginal rings *
Drug- Ethyl estrogen and etonogesterol
Inserted and left 3 weeks, fourth week remove for withdrawal bleed
Most common reason for DC is irritation or device expulsion
Progestin only pill*
“Mini pill”
Usually norethindrone
Daily low continuous dose
Less effective than COC
irregular cycle can occur
For those who are breastfeeding or intolerant to estrogen containing products
