Women's Health- Quiz 2 Flashcards
Estrogens
Examples
Strength
Examples: Estradiol, Estrone, Estriol, ethinyl estradiol
Strength: Estradiol most potent from ovary (premenopausal), Estrone 1/3 potency of Estradiol.
Estrogens
Most prevalent in pre/postmenopause
Estrogen made by the placenta
Metabolism
Most prevalent in premenopause: Estradiol
Most prevalent in postmenopause: Estrone
Estrogen made by the placenta: Estriol
Metabolism: PO high first pass, transported by albumin and sex hormone binding globulin. Glucoronide and sulfate conjugation
Estrogens
MOA
Uses
ADE
MOA: activated steroid-receptor complex interacts with nuclear chromatin to initiate hormone specific RNA synthesis
Uses: post menopausal hormone therapy, contraception, replacement in the premenopausal patients ie, hypogonadism, premature menopause, surgical menopause
ADE: Nausea, breast tenderness, VTE, MI, breast and endometrial CA
—Estrogen can cause cholestasis which presents as itching, dark urine, and pale BMs
Estrogen
Elimination
Excreted in the urine
SERMS
Examples
Selective estrogen receptor modulators
-ifen or -ifene
Examples: tamoxifen, raloxifene, clomiphene, ospemifene
SERMS
MOA
Uses
-Tamoxifen & raloxifene: compete with estrogen on estrogen receptors in the breast.
-Raloxifene does NOT stimulate endometrial growth
-Clomiphene: partial estrogen agonist, increasing GrH, causing ovulation
Uses:
—-Tamoxifen: metastatic breast CA, prophylactic risk reduction in breast ca
—-Raloxifene: prophylactic risk reduction in breast ca, osteoporosis tx post menopausal
—–Clomiphene: infertility
SERMS
ADE
ADE: tamoxifen: hot flashes and nausea, endometrial hyperplasia and malignancies. Lots of drug interactions
Raloxifene: hot flashes and leg cramps, DVT, PE.
Clomiphene: multiple gestation (twins)
Ospemifene: stimulate endometrial growth
Progestogens
Examples
MOA
Uses
Examples: desogestrel, dienogest, drospirenone, levonorgestrel, norethindrone, medroxyprogesterone
MOA: in women, promotes the endometrium. Continues to increase if conception occurs decreasing uterine contractions and further supporting the endometrium. IF no conception occurs progesterone stops causing menstruation
Uses: Contraception, tx hormone deficiency, dysmenorrhea, endometriosis management, and infertility
Progesterone Antagonist
Name
Use
ADE
Mifepristone (RU-486)
–Pregnancy termination due to interference with progesterone needed to maintain pregnancy.
–Often combined with prostaglandin analog MISOPROSTOL to cause uterine contractions.
ADE: abdominal pain, uterine bleeding and possibility of incomplete termination of pregnancy.
What are the 8 types of contraception
- Combination oral contraceptives (Estrogen & progestin)
- Transdermal patch
- Vaginal ring
- Progestin only pills
- Injectable progestin
- Progestin implant
- Progestin IUD
- Non-hormonal IUD
Combination oral contraceptives
usually ethinyl estradiol and progestin
–Monophasic (constant dose of estrogen and progestin) one week of placebo for withdrawal bleeding
–Triphasic (constant dose of estrogen with increasing doses of progestin) one week of placebo for withdrawal bleeding. Triphasic is the closest to the natural cycle
-If taken properly highly effective
-associated with a DECREASED risk of endometrial and ovarian ca
Transdermal patch contraceptive
Combination Ethinyl estradiol with progestin (either norelgestromin or levonorgestrel)
–Applied for 3 weeks then off for a week for withdrawal bleeding
–Can be applied to abdomen, upper torso, or buttock
–LESS EFFECTIVE IN WOMEN >90KG! Contraindicated in women with BMI>30 as the risk of VTE is much higher
–Similar efficacy to oral contraceptives
Vaginal Ring
ethinyl estradiol and etonogestrel
-Inserted in vagina x 3 weeks then removed for withdrawal bleeding.
-most common reason for discontinuation is device related ( vaginal irritation or device expulsion
–Similar efficacy to oral contraceptives
Progestin-only pills
Called the “mini-pill”
usually norethindrone at continuous dose
–LESS effective than the combination pills
Injectable progestin
Medorxyprogesterone acetate
IM or SQ every 3 months
–Return to fertility can be delayed several months after discontinuation
–Weight gain is common
–CONTRIBUTES TO BONE LOSS therefore should not be sued for more than 2 years if possible.
Progestin implant
Etonogestrel
Subdermal in upper arm
–lasts up to 3 yrs, reverses when removed
–progestin implants and IUDs are the MOST effective contraceptives, as they are not reliant on patient adherence.
–has not been studied in women >130% IBW as it may be less effective
Progestin intrauterine device
levonorgestrel
–lasts 3-7 yrs (depends on brand)
–Contraindicated in women with pelvic inflammatory disease, or history of ectopic pregnancy.
–Highly effective for the treatment of heavy menstrual bleeding
–progestin implants and IUDs are the MOST effective contraceptives, as they are not reliant on patient adherence
–Good for those that have contraindications to estrogen
Nonhormonal intrauterine device
Copper
Lasts up to 10 years
–can increase menstrual bleeding
Hormonal contraceptive ADE
Breast fullness, fluid retention, HA, nausea, HTN
Progestins: depression changes in libido, hirsutism, acne
Estrogens: rarely but possible VTE, thrombophlebitis, MI and stroke
—-these are usually in women >35yo who smoke therefore estrogen should be avoided in this population
—All hormonal contraceptives have small risk for cervical Ca. May not be related to meds but lifestyle as women are less likely to use barrier methods as well increasing potential exposure to HPV that we know causes cervical cancer
–Efficacy decreased with Abx use, also rifampin, carbamazepine and phenytoin
Progestogens
Pharmacokinetics
ADE
Pharmacokinetics: micronized progesterone is rapidly absorbed after oral ingestion. Metabolized by liver, excreted by kidney.
—–Progestins that are derived from 19-nortestosterone have androgenic activity, therefore will cause acne and hirsutism. In women use norgestimate and drospiernone as they cause less acne (but can increase K)
ADE: HA, depression, weight gain and libido changes
What contraceptive is safe during breast feeding?
Progestin only pills “mini-pill”
Hormonal contraceptives
MOA
Estrogens negative feedback inhibiting release of LH and FSH by pituitary preventing ovulation
Progestins: thicken cervical mucous interfering with the transport of sperm. Withdrawal of progestin stimulates menstrual bleeding. Progestins can inhibit LH and FSH as well
Postcoital/Emergency contraceptives
Most common is high dose levonorgestrel or ethinyl estradiol with levonorgestrel
—these are available OTC for those >17 (they are still)
—should be taken ASAP or at least within 72hrs
Progestin only (levonorgestrel only) is better tolerated
Progesterone agonist/antagonist Ulipristal (Ella) can be used up to 5 days after unprotected sex but requires a prescription
Insertion of copper IUD within 5 days is also considered emergency contraception that becomes long term contraception
Androgens
Examples
MOA
Example: testosterone, 5 alpha dihydrotestosterone (DHT), androstenedione, dehydroepiandrosterone (DHEA), danzol
testosterone: made in testes and adrenal gland in men, made in small amounts by thecal cells in ovaries and adrenal glands in women
MOA: anabolic and or masculinizing effects in both men and women
