194-195- pharm

Question 1

action of GnRH on receptor

Answer 1

pulsatile (physiologic) secretion stimulates. Continuous secretion desensitizes receptors as do long-acting superagonsits

Question 2

Gonadorelin: what is it? diagnostic use? therapeutic use?

Answer 2

synthetic GnRH. Used diagnostically to distinguish whether pituitary unresponsiveness is due to hypothal or pit failure (eg. hypogonadotropic hypogonadism) by injecting then measuring LH. Also used to treat hypothalamic hypogonadotropic hypgonad. used in women for tx of INFERTILITY

Question 3

leuprolide: what is it? therapeutic uses in males? Side affects?

Answer 3

GnRH superagonist. Desensitizes pituitary GnRHR (decreased FSH/LH and decreased androgen). Used to suppress precious puberty in males (continuous). Also used for prostate CA (continuous). Side effects: ED, initial “flare” resulting in bone pain. HA, pituitary dysfxn
Used in women to tx infertility (pulsatile), uterine fibroids (continuous)

Question 4

cetrorelix

Answer 4

true GnRH receptor antagonist (decreases FSH/LH and androgens). Used for prostate CA

Question 5

IN males, what inhibits LH? FSH?

Answer 5

androgen,

Inhibin

Question 6

What cells do FSH and LH act on in males

Answer 6

FSH= sertoli (sperm, androgen binding protein)
LH= Leydig (cleaves cholesterol which is RLS in T synthesis)

Question 7

Diagnostic use of gonadotropins like hCG. Therapeutic use?

Answer 7

determine if delayed puberty is primary gonadal or at hypothal/pituitary. Inject hCG and see if testosterone increases

induce spermatogenesis in hypogonadotrophic hypogonad. Give FSH/LH injection

Used sequentially to induce ovulation in female

Question 8

two enzymes that convert testosterone in men peripherally? where is each important?

Answer 8

5a-reductase- all over

aromatse- brain, bone, liver, adipose

Question 9

oral testosterone is called___

Answer 9

methyltestosterone or stanozolol

Question 10

androgen antagonists and their uses

Answer 10

flutamide (hirsutism, prostate CA), spironolactone.

Question 11

finasteride, dutasteride

Answer 11

5 a reductase inhibitors. treat BPH

Question 12

gossypol

Answer 12

damages seminiferous tubules. Male conraceptive

Question 13

estrogen agents

Answer 13

ethinyl estradiol, diethylstilbestrol (DES), mestranol

Question 14

norethindrone, levonorgestrel

Answer 14

progestins (levonorgestrel is Plan B)

Question 15

what can be used to induce ovulation

Answer 15

GnRH, gonadotropins, clomiphene

Question 16

tamoxifen

Answer 16

SERM. anti-estrogen on mammary gland. used to treat ER-positive breast CA

Question 17

fulvestrant

Answer 17

SERM. used for breast CA

Question 18

anastrozole/exemestane

Answer 18

aromatase inhibitors used in post menopausal women with breast CA

Question 19

endometriosis tx

Answer 19

danazole (weak androgen that binds to progestin receptors).

Leuprolide

Question 20

which gonadotropin is inhibited by estrogen? by progesterone?

Answer 20

FSH
LH
Both inhibit GnRH