Reproductive

Question 1

Leuprolide

Answer 1

MOA: GnRH analog with agonist properties when used in pulsatile fashion
Antagonistic when continuous (downregulates GnRH receptor)

Clinical: Infertililty (pulsatile)
Continuous: Prostate cancer (with flutamide), uterin fibroids, precroscious puberty

Toxicity: antiandrogen, nausea, vomiting

Question 2

Tamoxifen

Answer 2

Selective estrogen receptor modulator
MOA: antagonist on breast tissue, agonist at uterus and bone (Increases bone mineral density), decreases LDL

Clinical: treat and prevent recurrence of estrogen responding breast cancer

Toxicity: endometrial cancer (endometrial polyps, hyperplasia)

Question 3

Tamsulosin and terazosin

Answer 3

MOA: a1 antagonist

Clinical: prevents smooth muscle contraction in BPH, treats symptoms

SE: orthastatic hypotension, dizziness

Question 4

Hormone replacement therapy

Answer 4

Used for relief or prevention of meonopausal symptoms (hot flashes, vaginal atrophy) and osteoporosis (increased estrogen, decreased osteoclast activity)

Toxicity: unopposed estrogen replacement therapy increases the risk of endometrial cancer so progesterone is added
Possible increased cardiovascular risk

Question 5

Anastrozole/exemestane, letrozole

Answer 5

MOA: aromatase inhibitors

Clinical: breast cancer in postmenopausal women

Question 6

Progestins

Answer 6

MOA: bind progestereon receptors, decreasing growth and increases vascularization of endometrium

Clinical: oral contraceptives and treatment of endometrial cancer and abnormal uterine bleeding

Question 7

Menotropin

Answer 7

Acts like FSH leading to formation of dominant follicle

Question 8

Raloxifene

Answer 8

Selective estrogen receptor modulator
MOA: agonist on bone, antagonist at uterus

Clinical: osteoporosis (decreases resorption of bone)

Toxicity: increase risk of thormoembolic events

Question 9

Mifepristone (RU-486)

Answer 9

MOA: competitive inhibitor of progestins at progesterone receptors

Clinical: termination of pregnancy. Admistered with misoprostol

Toxicity: heavy bleeding, GI effects (nausea, vomiting, anorexia), abdominal pain

Question 10

Synthetic progestins, estrogen

Answer 10

Oral contraception
Estrogen and progestins inhibit LH/FSH preventing estrogen surge (no ovulation)

Progestins: thickening of cervical mucus limiting access of sperm to uterus
Inhibit endometrial proliferation making endometrium less suitable for implantation

CI: smokers>35 y.o. (increased risk of CV events-DVT, pulmonary embolism, ischemic stroke), patients with thromobemolism and stoke, estrogen dependent tumor, hypertryglyceridemia, decompensated or active liver disease, pregnancy

SE: breakthrough menstrual bleeding, breast tenderness, weight gain

Question 11

Estrogens

Answer 11

Ethinyl estradiol, DES, mestranol
MOA: bind estrogen receptors

Clinical: Hypogonadism or ovarian failure, menstrual abnormalities, HRT in postmenopausal women, men with androgen dependent prostate cancer

Toxicity: increase risk of endometrial cancer, bleeding in postmenopausal women, clear cell adenocarcinoma of vagina in females exposed to DES in utero, increased risk of thrombi

CI: Estrogen respoding breast cancer, history of DVTs

Question 12

Terbutaline

Answer 12

B2 agonist that relaxes the uterus

Decreases contraction frequency in labor

Question 13

Danazol

Answer 13

MOA: synthetic androgen that acts as partial agonist at androgen receptors

Clinical: endometriosis and hereditary angioedema

Toxicity: weight gain, edema, acne, hirsutism, masculization, decresaed HDL levels, hepatoxicity

Question 14

Testosterone/methyltestosterone

Answer 14

MOA: agonist at androgen receptors

Clinical: treats hypogonadism and promotes development of secondary sex characteristics, stimulation of anabolism to promote recovery from burn or injury

Toxicity: masculinization in females, decreased intratesticular testosterone inhibiting release of LH leading to gonadal atrophy
Premature closure of epiphyseal plates
increase LDL, decrease HDL

Question 15

Finasteride, dutasteride

Answer 15

MOA: 5a reductase inhibitor (decrease conversion of testosterone to DHT)

Clinical: BPH, hair growth

SE: decrease libido, erectile dysfunction, takes 6-12 months

Question 16

Spironolactone

Answer 16

MOA: inhibits steroid binding (17a hydroxylase and 17, 20 desmolase)

Clinical: used with ketoconazole to prevent hirstuism in PCOD

SE: gynecomastia and amenorrhea

Question 17

Clomiphene

Answer 17

Selective estrogen receptor modulator
Antagonist at hypothalamus receptors

Prevents normal feedback inhibition and increase release of LH and FSH from pituitary stimulating ovulation

Clinical: infertility due anovulation (PCOS)

Toxicity: hot flashes, ovarian enlargement, multiple simultaneous pregnancies, and visual disturbances

Question 17

Ketoconazole

Answer 17

MOA: inhibits steroid synthesis (17, 20 desmolase)

Clinical: used with spironolactone to prevent hirstuism in PCOD

SE: gynecomastia and amenorrhea

Question 18

Sildenafil, vardenafil

Answer 18

MOA: phosphodiesterase inhibitor leading to incresae cGMP
Smooth muscle relaxation in corpus cavernousm increasing blood flow and penile erection

Clinical: treatment of ED

Toxicity: headache, flushing, dyspepsia, impaired blue-green color vision
Life threating hypotension in patients taking nitrates

Question 19

Flutamide

Answer 19

MOA: nonsteroidal competitive inhibitor of androgens at the testosterone receptor
Decreasing stimulatory effect of androgens on primary tumor or mestatases leading to decreased size

Clinical: prostate carcinoma

Use with leuprolide to decrease rise in testosterone

SE: hot flashes, gynecomastia, and impotence

Question 20

Magnesium Sulfate

Answer 20

IV used for eclampsia