Reproductive Pharmacology

Front 1

Leuprolide

Back 1

Mechanism- GnRH analog; agonist if used in a pulsatile fashion, antagonist if used continuously.
Use- Infertility (pulsatile), prostate cancer, uterine fibroids (continuous)
Toxicity- Antiandrogen, N/V

Front 2

Testosterone

Back 2

Mechanism- Agonist at androgen receptors.
Use- Hypogonadism, promote development of secondary sex characteristics, stimulation of anabolism to promote recovery after burn/injury; ER-positive breast cancer (exemestane)
Toxicity- Masculinization in females, inhibits LH to reduce intratesticular testosterone in males (gonadal atrophy), premature closure of epiphyseal plates, increase LDL, decrease HDL

Front 3

Finasteride

Back 3

Mechanism- 5a-reductase inhibitor
Use- BPH, promote hair growth to treat male-pattern baldness

Front 4

Flutamide

Back 4

Mechanism- Nonsteroidal competitive inhibitor of androgens at the testosterone receptor.
Use- Prostate carcinoma

Front 5

Ketoconazole

Back 5

Mechanism- Inhibits desmolase (inhibits steroid synthesis)
Use- PCOS to prevent hirsutism
Toxicity- Gynecomastia, amenorrhea

Front 6

Spironolactone

Back 6

Mechanism- Inhibits steroid binding
Use- PCOS to prevent hirsutism
Toxicity- Gynecomastia, amenorrhea

Front 7

Ethinyl estradiol, DES, mestranol

Back 7

Mechanism- Bind estrogen receptors
Use- Hypogonadism, ovarian failure, menstrual abnormalities, HRT in PM women, men with androgen-dependent prostate cancer.
Toxicity- Increase risk of endometrial cancer, bleeding in PM women, DES causes clear cell adenocarcinoma of vagina in females exposed to DES in utero, increased risk of thrombi. CX in ER-positive breast cancer and history of DVTs

Front 8

Clomiphene

Back 8

Mechanism- Partial agonist at estrogen receptors in the hypothalamus. Prevents normal feedback inhibition and increases release of LH and FSH.
Use- Stimulate ovulation for PCOS or infertility
Toxicity- Hot flashes, ovarian enlargement, multiple pregnancies, visual disturbances

Front 9

Tamoxifen

Back 9

Mechanism- Antagonist on breast tissue
Use- Prevention of recurrence of ER-positive breast cancer (but also agonist on endometrial tissue so increases risk of endometrial cancer)

Front 10

Raloxifene

Back 10

Mechanism- Agonist at the estrogen receptor on bone to reduce resorption.
Use- Osteoporosis

Front 11

HRT

Back 11

Use- Prevention of menopausal symptoms (hot flashes, vaginal atrophy, osteoporosis). Progesterone and estrogen
Toxicity- Possible CV disease

Front 12

Anastrozole/exemestane

Back 12

Mechanism- Aromatase inhibitors
Use- PM women with breast cancer

Front 13

Progestins

Back 13

Mechanism- Bind progesterone receptors, reduce growth, and increase vascularization of endometrium
Use- Oral contraceptives, treatment of endometrial cancer and abnormal uterine bleeding

Front 14

Mifepristone (RU-486)

Back 14

Mechanism- Competitive inhibitor of progestins at progesterone receptors.
Use- Termination of pregnancy; administered with misoprostol (PGE1)
Toxicity- Heavy bleeding, GI effects (N/V/anorexia), abdominal pain

Front 15

Dinoprostone

Back 15

Mechanism- PGE2 analog causing cervical dilation and uterine contraction to induce labor.

Front 16

Tamsulosin

Back 16

Mechanism- a1 antagonist used to treat BPH by inhibiting smooth muscle contraction. Specific for a1A,D receptors (found on prostate) versus a1B receptors found on vasculature (does not decrease bp)

Front 17

Sildenafil, vardenafil

Back 17

Mechanism- Inhibit cGMP phosphodiesterase, causing increased cGMP, smooth muscle relaxation in the corpus cavernosum, increased blood flow, and penile erection.
Use- Treat ED
Toxicity- Headache, flushing, dyspnea, impaired blue-green color vision, risk of life-threatening hypotension in patients taking nitrates.