Reproductive Pharmacology

Front 1

Leuprolide

Back 1

GnRH analog with agonist properties when used in pulsatile fashion.

Used for infertility, prostate cancer, uterine fibroids.

Toxicity: antiandrogen, N/V.

Front 2

Testosterone

Back 2

Synthetic androgens that act as androgen receptor agonist.

Used as androgen replacement therapy in men, hypogonadism, burns/injuries.

Toxicity: causes masculinization in females, gonadal atrophy, increased LDL and decreased HDL.

Front 3

Ethinyl estradiol, DES, Mestranol

Back 3

Synthetic estrogen that stimulates the estrogen receptor.

Used for replacement therapy in post-menopausal women, oral contraception.

Toxicity: risk of endometrial cancer, uterine bleeding, thrombosis, CI in breast cancer patients or h/o DVT.

Front 4

SERM (Selective Estrogen Receptor Modulators)

Back 4

1. Clomiphene
2. Tamoxifen
3. Raloxifene

Front 5

Clomiphene

Back 5

Partial estrogen receptor agonist in hypothalamus; prevents feedback inhibition and increased release of LH and FSH from pituitary.

Used for infertility, stimulates ovulation.

Toxicity: hot flashes, ovarian enlargement, multiple simultaneous pregnancies.

Front 6

Tamoxifen

Back 6

Estrogen antagonist on breast tissue.

Used for treatment and prevention of ER+ breast cancer.

Front 7

Raloxifene

Back 7

Estrogen agonist on bone, reduces resorption of bone.

Used for treatment of osteoporosis.

Front 8

Hormone Replacement Therapy (HRT)

Back 8

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

Unopposed ERT increases the risk of endometrial cancer, so progesterone is added. Possible increased in CV risk.

Front 9

Progestins

Back 9

Bind progesterone receptors, reduce growth and increase vascularization of endometrium.

Used in oral contraceptives, endometrial cancer, and abdominal uterine bleeding.

Front 10

Oral Contraceptives

Back 10

Synthetic progestins, estrogen.

Inhibit LH/FSH and thus prevent estrogen surge, no LH surge, no ovulation.

Progestins cause thickening of cervical mucus, limiting access of sperm to uterus; also inhibit endometrial proliferation, making uterus less suitable for implantation of embryo.

CI: smokers > 35, h/o thromboembolism or stroke, h/o estrogen-dependent tumor.

Front 11

Mifepristone

Back 11

Competitive inhibitor of progestins and progesterone receptors.

Used for as abortive method, administered with Misoprostol.

Causes heavy bleeding, GI effects, and abdominal pain.

Front 12

Anastrozole

Back 12

Aromatase inhibitors used in postmenopausal women with breast cancer.

Front 13

Ritodrine/Terbutaline

Back 13

Beta-2 agonist that relaxes the uterus; reduces premature uterine contractions.

Ritodrine allows the fetus to "Return to Dreams" by preventing early delivery.

Front 14

Antiandrogens

Back 14

1. Finasteride
2. Flutamide
3. Ketoconazole
4. Spirinolactone

Front 15

Finasteride

Back 15

5-alpha-reductase inhibitor that decreases conversion of testosterone to dihydrotestosterone.

Used in BPH, male-pattern baldness.

Front 16

Flutamide

Back 16

Nonsteroidal competitive inhibitor of androgens at the testosterone receptor.

Used in prostate cancer.

Front 17

Ketoconazole

Back 17

Inhibits steroid synthesis (desmolase).

Used in prostate cancer and prevent hirsutism.

Toxicity: amenorrhea and gynecomastia.

Front 18

Spirinolactone

Back 18

Competitive inhibitor of aldosterone.

Used for hirsutism.

Front 19

Danazol

Back 19

Synthetic androgen that acts as a partial agonist at androgen receptors.

Used in endometriosis and hereditary angioedema.

Toxicity: weight gain, edema, acne, hirsutism, masculinization, decreased HDL levels.

Front 20

Tamsulosin

Back 20

Alpha-1 agonist used to treat BPH by inhibiting smooth muscle contraction.

Selective for alpha-1 receptors found in prostate.

Front 21

Sildenafil/Vardenafil

Back 21

Fill the penis... inhibit cGMP PDE, causing increased cGMP, smooth muscle relaxation in the corpus cavernosum, increased blood flow, and penile erection.

Used for ED.

Toxicity: "Hot and sweaty but then headache, heartburn, and hypotension"; headache, flushing, dyspepsia, impaired color vision, hypotension esp. if on nitrates.