Fa Pharm Reproductive

Front 1

leuprolide

Back 1

GnRH analog with agonist properties when used in pulsatile fashion; antagonist properties when used in continuous fashion.

use: infertility (pulsatile), prostate cancer (continuous - use with flutamide), uterine fibroids.

toxicity: antiandrogen, n/v

Front 2

testosterone (methyltestosterone)

Back 2

agonist at androgen receptors

use: treats hypogonadism and promote development of secondary sex characteristics, stimulateion of anabolism to promote recovery after burn or injury; treat ER -positive breast cancer (exemestane).

toxicity: causes masculinization in females; reduces intratesticular testosterone in males by inhibiting releaese of LH (via negative feedback), leading to gonadal atrophy. premature closure of epiphyseal plates. increased LDL, dercreased HDL.

Front 3

antiandrogens

finasteride (propecia)

Back 3

a 5a-reductase inhibitor (reduces conversion of testosterone to dihydrotestosterone [DHT]). useful in BPH. also promotes hair growth-used to treat male pattern baldness

Front 4

antiandrogens

flutamide

Back 4

a nonsteroidal competitive inhibitor of androgens at the testosterone receptor. used in prostate carcinoma.

Front 5

antiandrogens

ketoconazole

Back 5

inhibits steroid synthesis by inhibiting desmolase.

use: treatment of polycystic ovarian syndrome to prevent hirsutism

ae: gynecomastia and amenorrhea

Front 6

antiandrogens

spironolactone

Back 6

inhibits steroid binding

use: treatment of polycystic ovarian syndrome to prevent hirsutism

ae: gynecomastia and amenorrhea

Front 7

estrogens
ethinyl estradiol, DES, mestranol

Back 7

binds estrogen receptors
use: hypogonadism or ovarian failure, menstrual abnormalities, HRT in postmenopausal women; use in men with androgen-dependent prostate cancer.
toxicity: increased 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: ER positive breast cancer, history of DVTs.

Front 8

estrogen partial agonist
(selective estrogen receptor modulators - SERMs)

clomiphene

Back 8

partial agonist at estrogen receptors in hypothalamus. prevents normal feedback inhibition and increase releaes of LH and FSH from pituitary, which stimulates ovulation.

use: treat infertility and PCOS. may cuase hot flahes, ovarian enlargment, multiple simultaneous pregnancies, and visual disturbances.

Front 9

estrogen partial agonist
(selective estrogen receptor modulators - SERMs)

tamoxifen

Back 9

antagonist on breast tissue.

use: treat and prevent recurrence of ER positive breast cancer.

Front 10

estrogen partial agonist
(selective estrogen receptor modulators - SERMs)

raloxifene

Back 10

agonist on bone; reduces resorption of bone; used to treat osteoporsis.

Front 11

hormone replacement therapy (HRT)

Back 11

used for relief or prevention of menopausal symptoms (hot flashes, vaginal atrophy), and osteoporosis (increased estrogen, decreased osteoclastic activity by inhibition of IL1)

unopposed estrogen replacement thearpy (ERT) increasese the risk of endometrial cancer, so progesterone is added. possible increased CV risk

Front 12

anastrozole/exemestane

Back 12

aromatase inhibitors used in postmenopausal women with breast cancer.

Front 13

progestins

Back 13

bind progesterone reeptors, reduce growth, and increase vascularizaiton of endometrium.

use: used in oral contraceptives and in the treatment of endometrial cancer and abnormal uterine bleeding.

Front 14

mifepristone (RU-486)

Back 14

competitive inhibitor of progestins at progesterone receptors.

ues: termination of pregnancy. adminstered with misoprostol (PGE1).

toxicity: heavy bleeding, GI effects (n/v, anorexia), abdominal pain.

Front 15

dinoprostone

Back 15

PGE2 analog causing cervical dilation and uterine contraction, inducing labor.

Front 16

ritodrine/terbutaline

Back 16

b2 agonist that relax the uterus; reduces premature uterine contraction.

Ritodrine allows teh fetus to 'return to dreams" by preventing early delivery.

Front 17

tamsulosin

Back 17

a1 antagonist used to treat BPH by inhibiting SM contarction. selective for a1A,D receptors (found on prostate) vs. vascular a1B receptors.

Front 18

sildenafil, vardenafil

Back 18

inhibit cGMP phosphodisterase, causing increaesd cGMP, SM relaxation in the corpus cavernosum, increased blood flow, and penile erection.

use: treatment of erectile dysfunction.

toxicity: ha, flushing, dyspepsia, impaired blue-green color vision. risk of life threatening hypotension in patients taking ntirates.

sildenafil and vardenafil fill the penis.

"Hot and seaty," but then ha, heartburn, hypotension.