Estrogens and Androgens

Question 1

Estrogen

Answer 1

steroid hormone that diffuses across membrane to bind to nuclear receptor (coronary arteries + HT cells) to stimulate transcription

Tx: contraception, cancer, osteoporosis, premature menopause, infertility, relieve menopausal symptoms, stimulate development in hypogonadism

AE: uterine bleeding, endometrial cancer, MI, HTN, Thromboembolism, HA, Nausea

Question 2

Estradiol

Answer 2

most potent produced by ovary and main one in premenopausal women

Question 3

Estrone

Answer 3

produced by ovary and main one in post-menopausal women

Question 4

Estriol

Answer 4

produced by placenta and main one during pregnancy

Question 5

GnRH Analogs (3) name them

Answer 5

pulse dose causes increase in FSH/LH
continuous dose causes decrease FSH/LH

Leuprolide, Gonadorelin, and Nafarelin

Question 6

Raloxifene

Answer 6

Selective Estrogen Receptor Modulators

Antagonist at breast tissue (tx breast cancer) and decreases bone reabsorption and little effect in endometrium

AE: increase thrombus

Question 7

Tamoxifene

Answer 7

Antagonist at breast tissue ( treat breast cancer)

Agonist in uterus (increases uterine cancer risk)

AE: crystalline retinopathy, macular edema, corneal opacities, cataracts, optic neuritis

Selective Estrogen Receptor Modulators

Question 8

Clomiphene

Answer 8

Antagonist at all types of receptors and mainly blocks estrogen mediated -FB so it increases LH/FSH to treat infertility and induce ovulation/spermatogenesis

Selective Estrogen Receptor Modulators

Question 9

Progestogens

Used for?

Names? (7)

AE?

Answer 9

treats hormonal deficiency, contraception, controls dysfunctional uterine bleeding

Drospirenone
Levonorgestrel
Medroxyprogesterone: synthetic are more stable to FPM
Megestrol
Norelgestromin
Norethindrone
Progesterone: produced in response to LH in H/F in adrenal cortex

AE: Weight gain, HA, Depression, Acne

Question 10

Mifepristone

Answer 10

progesterone antagonist

early in pregnancy can lead to abortion ~ contraceptive

Question 11

Testosterone

Answer 11

anabolic agent (bone growth and absorption, internal genitalia, and increase muscle mass)

Tx: osteoporosis, chronic wasting, and recovery from sx

Question 12

Flutamide

Answer 12

androgen receptor antagonist

blocks testosterone at target organs (tx prostatic carcinoma)

Question 13

Nilutamide and Bicalutamide

Answer 13

androgen receptor antagonist

usually with GnRH to decrease LH/testosterone

Question 14

Contraceptive

Answer 14

prevent ovulation by impairing gametogenesis and interfering with gestation

combo of progestin and estrogen

AE: Fluid retention, HA, Nausea, Vomit, CV, Cervical Cancer, Abnormal Glucose tolerance, Weight gain

Question 15

Monophasic

Answer 15

constant dose of both hormones over 21 days

last 7 days is placebo

Question 16

Triphasic

Answer 16

mimics natural cycle with constant estrogen and elevating progestin in 3 weeks

last week is placebo

Question 17

Transdermal Patch

Answer 17

contains ethinyl estradiol and norelgestromin

comparable efficacy but less effective if more than 198 lbs (more AE)

Question 18

Progestin-only Pills

Answer 18

only norethindrone and take daily on continuous schedule

for breastfeeding women, intolerant to estrogen and smokers

Question 19

Injectable

Answer 19

Medroxyprogesterone acetate

admin every 3 mos and weight gain is common but not for more than 2 years bc infertility and bone loss

Question 20

Progestin Implant

Answer 20

subdermal implant of etonogestrel (lasts 3 years) and less effective with heavier women

Question 21

Emergency Contraception

Answer 21

High dose of Progestin (0.75mg levonorgestrel)

High Dose Estrogen + Progestin (100 ng ethinyl estradiol and 0.5mg levonorgestrel)

either must be administered within 72 hours

take 2nd dose 12 hrs after 1st dose

progestin only formulations are usually tolerated better