Gonadal Hormones and Inhibitors

ethinyl estradiol subclass

estrogen

mechanism of action of ethinyl estradiol

activation of estrogen receptors that lead to changes in the rates of transcription of estrogen-regulated genes

prodrug that is converted to ethinyl estradiol

mestranol

long-acting estrogens administered IM

estrogen esters

clinical application of estrogen esters

hypogonadism

norgestrel subclass

progestin

mechanism of action for norgestrel

activation of progesterone receptors that lead to changes in the rates of transcription of progesterone-related genes

progesterone derivatives

medroxyprogesterone acetate and megestrol acetate

subclass of norethindrone and ethynodiol

older 19-nortesosterone derivatives

what are some newer 19-nortestosterone derivatives

desogestrel, norelgestromin, norgestimate, and etonogestrel

what is a spironolactone derivative

drospirenone

older and newer 19-nortestosterone derivatives and spironolactone derivatives fall under what subclass of drugs

progestins

tamoxifen and toremifene subclass

SERMs

mechanism of action for tamoxifen and toremifene

estrogen antagonist actions in breast tissue and CNS and estrogen AGONIST effects in liver and bone

clinical application of tamoxifen

prevention and adjuvant treatment of hormone-responsive breast cancer

raloxifene subclass

SERMs

clinical application of raloxifene

approved for osteoporosis and prevention of breast cancer in selected patients (antagonist effects in breast, CNS, and endometrium and AGONIST effects int he liver)

bazedoxifene clinical applications

approved for treatment of menopausal symptoms and prophylaxis of postmenopausal osteoporosis in combo with conjugated estrogens

clomiphene mechanism of action

partial agonist at estrogen receptor

clinical applications of clomiphene

used for ovulation induction and antagonist effect in pituitary increases gonadotropin secretion

fulvestrant subclass

estrogen receptor antagonist

mechanism of action of fulvestrant

estrogen receptor antagonist in ALL tissues

clinical application of fulvestrant

adjacent treatment of hormone-responsive breast cancer that is resistant to first-line anti estrogen therapy

anastrozole subclass

aromatase inhibitor

mechanism of action for anastrozole

reduces estrogen synthesis by inhibiting aromatase enzyme

clinical application of anastrozole

adjacent treatment of hormone-responsive breast cancer

drug similar to anastrozole

letrozole

an irreversible aromatase inhibitor is what

exemestrane

name a GnRH agonist

leuprolide

name a GnRH receptor antagonist

Ganirelix and cetrorelix

mechanism of action for danazol

weak CYP450 inhibitor and partial agonist of progestin and androgen receptors

clinical application of danazol

endometriosis and fibrocystic breast disease

mifepristone subclass

antiprogestin

mifepristone mechanism of action

progestin and glucocorticoid receptor antagonist

clinical application of mifepristone

used in combination with a prostaglandin (like misoprostol) for medical abortion

testosterone subclass

androgen

mechanism of action for testosterone

androgen receptor agonist

clinical application of testosterone

male hypogonadism and weight gain in patients with wasting syndromes

what are some oral androgens

fluoxymesterone and methyltestosterone

what is a long-acting androgen for parenteral administration

testosterone esters

drug that is an increased ratio of anabolic-to-androgenic activity in laboratory animals

anabolic steroids

ADR for anabolic steroids?

cholestatic jaundice and liver toxicity

finasteride subclass

5 alpha reductase inhibitor (antiandrogen)

mechanism of action for finasteride

inhibition of 5a-reductase enzyme that converts to testosterone to dihydrotestosterone

clinical applications of finasteride

BPH and male pattern hair loss

other 5 alpha reductase inhibitor that’s not finasteride

dutasteride

flutamide subclass

androgen receptor antagonist

mechanism of action of flutamide

competitive inhibition of androgen receptor

clinical application of flutamide

advanced prostate cancer

drugs similar to flutamide but with a lower risk of hepatotoxicity

bicalutamide and nilutamide

mineralocorticoid receptor antagonist that has androgen receptor antagonist activity

spironolactonec

clinical application of spironolactone

hirsutism

ketoconazole subclass

androgen synthesis inhibitor

mechanism of action for ketoconazole

inhibition of CYP450 enzymes involved in androgen synthesis

clinical applications of ketoconazole

advanced prostate cancer that is resistant to first-line anti androgen drugs