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Flashcards in Repro Deck (24)
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1

Leuprolide
MOA

GnRH analog
Pulsatile - agonist
Continuous - antagonist

2

Leuprolide
Clinical use

Infertility (pulsatile)
Prostate cancer, uterine fibroids (continuous)
Precocious puberty (continuous)

3

Estrogens (Ethinyl estradiol, DES, mestranol)
Clinical use

Binds estrogen receptors.
For hypogonadism, ovarial failure, menses abnormalities, HRT.

4

Estrogens
Toxicity

Inc. risk Endometrial cancer.
Bleeding in postmenopause.
CI in ER-positive breast cancer, hx of DVT.

5

Clomiphene
[MOA, clinical use]

SERM -- Estrogen receptor antagonist at hypothalamus.
Prevents feedback inhibition -- inc. LH/FSH -- ovulation.
For infertility (anovulation).

6

Tamoxifen
[MOA, clinical use, toxicity]

SERM: Antagonist at breast; agonist at bone, uterus.
Treat and prevent recurrence of ER/PR-positive breast cancer.
Tox: inc. risk of thromboembolism, endometrial cancer.

7

Raloxifene
[MOA, clinical use]

SERM: Antagonist at breast, uterus; agonist at bone.
Treat osteoporosis.
Inc. risk of thromboembolism.

8

Hormone replacement therapy.
For what?
Estrogen? Progesterone?

For menopausal sx, osteoporosis.
Unopposed estrogen inc. risk of endometrial cancer -- add progesterone (estrogen + progesterone).

9

Progestins
[MOA, clinical use]

Bind progesterone receptors. Used in OCPs.
Dec. growth and inc. endometrial vascularization.
For endometrial cancer, abnormal uterine bleeding.

10

Oral contraception
MOA

Estrogen + progestin.
Inhibit LH/FSH -- no estrogen surge -- no LH surge -- no ovulation.
> Progestins: thick cervical mucus, limits sperm access to uterus; inhibit endometrial proliferation, so harder to implant.

11

Oral contraception
Contraindications

Smokers > 35 y.o
Hx of thromboembolism, stoke
Hx. of estrogen-dependent tumor

12

Terbutaline, Ritodrine
Clinical use

B2-agonists
Relax the uterus.
To dec. contraction frequency in labor.

13

Testosterone
Clinical use

Androgen receptor agonist.
For hypogonadism; to develop secondary sex chars.

14

Testosterone
Toxicity

Masculinization in females.
Gonadal atrophy in males (inhibits LH release) -- dec. intratesticular testosterone.
Premature closure of epiphyseal plates.

15

Finasteride
[MOA, use]

Antiandrogen; 5a-reductase inhibitor (testosterone --> DHT).
For BPH, male-pattern baldness.

16

Flutamide
[MOA, use]

Antiandrogen; Nonsteroidal competitive androgen receptor inhibitor.
For prostate CA.

17

Ketoconazole
[MOA, use, SE]

Antiandrogen.
Inhibits 17,20-desmolase (cholesterol -- androgen) -- Inhibits steroid synthesis.
For polycystic ovarian syndrome -- reduce androgenic sx.
SE: gynecomastia, amenorrhea

18

Spironolactone
[MOA, use, SE]

Antiandrogen.
Inhibits steroid binding, 17a-hydroxylase, 17,20-desmolase.
For polycystic ovarian syndrome.
SE: gynecomastia, amenorrhea

19

Tamsulosin
[MOA, use]

a1-antagonist (alpha1A,D receptors in prostate).
Inhibit smooth muscle contraction, for BPH.
Treat BPH

20

Sildenafil, Vardenafil, Tadalafil
[MOA, clinical use]

Inhibit PDE-5 -- inc. cGMP -- smooth muscle relaxation in corpus cavernosum, inc. blood flow -- penile erection.
For erectile dysfunction.

21

Sildenafil, Vardenafil, Tadalafil
Toxicity

Life-threatening Hypotension in pts taking nitrates.
Headache, heartburn

22

Anastrozole/Exemestane
[MOA, use]

Aromatase inhibitors.
Used in postmenopausal women w/ ER-positive breast cancer.
*Source of estrogen after menopause becomes peripheral conversion of androgens.

23

Danazol
[MOA, use]

>Partial agonist at androgen receptors -- induces a state of pseudomenopause by suppressing ovarian fxn and inhibits FSH/LH secretion, causing endometrial atrophy.
>For endometriosis, hereditary angioedema.

24

Mifepristone (RU-486)
[MOA, use]

Competitive inhibitor of pregestins at progesterone receptor.
Termination of pregnancy.
*Administer w/ misoprostol (PGE1)