DA2 EX2 DRUGLIST: REPRODUCTIVE SYSTEM

GnRH agonists

1. Leuprolide

2. -relins

goserelin, nafarelin, buserelin, triptorelin

GnRH antagonists

-relix

cetorelix, ganirelix, degarelix

GnRH agonist indication

prostate cancer, some cases breast cancer

5a-reductase inhibitors

Dutasteride (Avodart)

Finasteride (Proscar, Propecia)

Finasteride indication

prostatic hyperplasia (propecia for male pattern baldness)

Adverse effects of 5a-reductase inhibitors

Decreased libido, ED

Aromatase inhibitors

-stane

Exemestane, formestane

-ozole

Anastrozole, letrozole

Steroidal aromatase inhibitors

-stane

Exemestane, formestane

Nonsteroidal aromatase inhibitors

-ozole

Anastrozole, letrozole

MOA steroidal aromatase inhibitors

suicide inhibitors; irreversible inactivation

MOA of nonsteroidal aromatase inhibitors

competitive inhibition of aromatase; interaction with P450 heme groups

Adverse effects of aromatase inhibitors

Osteoporosis, hot flashes

SERMs

Tamoxifen, raloxifene, bazedoxifene

Tamoxifen activity in

Breast?

Endometrium?

Bone?

Breast: antagonist

Endometrium: partial agonist

Bone: partial agonist

MOA of tamoxifen?

Inhibition of estrogen-dependent growth of breast cancer (can stimulate endometrial growth)

T/F: Tamoxifen has antihyperlipidemic effects.

True

Adverse effects of tamoxifen?

DVT, hot flashes, endometrial cancer

Raloxifene activity in

Breast?

Bone?

Endometrium?

Breast: no effect

Bone: agonist

Endometrium: no effect

T/F: Raloxifene is an agonist in liver, benefits cholesterol balance.

True

Adverse effects of raloxifene?

DVT, stroke

Clomiphene MOA

Antagonize estrogen receptor in hypothalamus and anterior pituitary; partial agonist in ovaries

Effect of clomiphene

Induce LH surge and ovulation

Indication of clomiphene

Infertility

Side effect of clomiphene

Works too well; twins, triplets

Androgen receptor antagonists

-amide

Flutamide, bicalutamide, nilutamide, enzalutamide

Indication of androgen receptor antagonists

Metastatic prostate cancer

T/F: Flutamide can be used to treat benign prostatic hyperplasia.

True

T/F: Androgen receptor antagonists can be used to treat hirsutism.

True

Progesterone receptor antagonists

Mifepristone, misoprostol, asoprisnil

Mifepristone MOA

Competitive inhibition of P action

Misoprostol MOA

Prostaglandin analogue, stimulates uterine contraction

Misoprostol indication

Termination of first trimester pregnancy

Asoprisnil MOA

Inhibition of tissue growth derived from endometrium

Indication for asoprisnil

Endometriosis, uterine leiomyomata (fibroids)

Hormonal contraceptives

Estrogen-progestin

Progestin-only

Synthetic estrogens

Ethinyl estradiol, mestranol, estradiol cypionate

Action of estrogen in the

Pituitary

Ovary

Uterus

Vagina

Cervix

Pituitary: Regulate the release of LH and FSH

Ovary: Stimulate follicular growth

Uterus: Stimulate growth and proliferation of non-secretory endometrium

Vagina: Change in skin tone

Cervix: Increase thin mucus favoring sperm

Action of estrogen in bones

Decrease resorption, maintain Ca2+ content

Action of estrogen in liver

Improve cholesterol profile

Action of estrogen in blood

Increase coagulability

Serious side effects of estrogen

VTE (blood clot)

HTN

Gall bladder disease

Endometrial, ovary, breast cancer

Progestin-only contraceptives

Norethindrone, desogestrel

MOA of progestin-only contraceptives

Alter GnRH pulsing frequency, decrease anterior pituitary responsiveness to GnRH

Block ovulation, endometrial proliferation

Synthetic progestins

Megestrol

Hydroxyprogesterone caproate

Medroxyprogesterone acetate

Progesterone only pills are referred to as ____-pills

mini pills (once daily)

Injections for progesterone only BC last how long

12 WEEKS

Emergency contraceptives

Mifepristone, levonorgestrel