Repro Pharm Flashcards

1
Q

Leuprolide mech

A

GnRH analog
Agonist if pulsatile
antagonist if continuous (downregulates GnRH receptor in pituitary -> decreased FSH/LH -> low T/E in M/F

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2
Q

Leuprolide clinical use

A

Pulsatile - Infertility

Continuous - prostate cancer (+ flutamide), uterine fibroids, precocious puberty

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3
Q

Leuprolide tox

A

Antiandrogen, n/v

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4
Q

Methyltestosterone/testosterone mech.

A

Agonist at androgen receptors

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5
Q

Methyltestosterone use

A

Treats hypogonadism, promotes secondary sex characteristics, stimulation of anabolism to promote recovery after burn or injury

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6
Q

Methyltestosterone tox

A

masculinization in females, reduces intratesticular T in males by inhibiting release of LH (via negative feedback), gonadal atrophy, premature closure of epiphyseal plates, Increased LH, decreased HDL

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7
Q

Antiandrogens

A

Finasteride, Flutamide, Ketoconazole, Spironolactone

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8
Q

Finasteride

A

5a reductase inhibitor (decreased conversion of T to DHT). Useful in BPH. Also promotes hair growth (treats male pattern baldness (to treat use something that encourages female breast growth)). Side Effects: impotence, decreased sexual function, gynecomastia.

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9
Q

Flutamide

A

A nonsteroidal competitive inhibitor of androgens at the T receptor. Use - prostate cancer

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10
Q

Ketoconazole

A

Inhibits steroid synthesis (inhibits 17,20-desmolase)

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11
Q

Spironolactone

A

Inhibits steroid binding

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12
Q

Ketoconazole, Spironolactone

A

treat PCOS to prevent hirsutism. Side effects = gynecomastia & amenorrhea

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13
Q

Estrogens

A

ethinyl estradiol, DES, mestranol

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14
Q

Estrogen mech

A

Bind E receptors

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15
Q

Estrogens Use

A

Hypogonadism or ovarian failure, menstrual abnormalities, HRT in postmenopausal women; use in men with androgen dependent prostrate cancer.

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16
Q

Estrogen Tox

A

increased risk of endometrial cancer, bleeding in postmenopausal women, clear cell adenocarcinoma of vagina in females exposed to DES in utero, increased risk of thrombi

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17
Q

Estrogen contraindications

A

ER (+) breast cancer, hx of DVTs

18
Q

SERMs

A

Clomiphene, Tamoxifen, Raloxifene

19
Q

Clomiphene mech

A

SERM; partial E receptor agonist in hypothalamus. Prevents normal feedback inhibition & increased release of LH & FSH from pituitary, which stimulates ovulation.

20
Q

Clomiphene use

A

Used to treat infertility & PCOS.

21
Q

Clomiphene tox

A

May cause hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances

22
Q

Tamoxifen mech & use

A

antag on breast tissue, agonist for endometrium (cancer risk) & bone (prevents loss). TX - prevent recurrence of ER(+) breast cancer.

23
Q

Raloxifene mech & tx

A

Agonist on bone, Antag endometrium. reduces bone resorption of bone. TX - osteoporosis

24
Q

Hormone Replacement Therapy

A

used for relief of menopause sx & osteoporosis (increased estrogen, decreased osteoclast activity). Unopposed estrogen replacement therapy increases the risk of endometrial cancer, so progesterone is added. Poss increased CV risk.

25
Q

Anastrozole/exemestane

A

Aromatase inhibitors used in postmenopausal women with breast cancer.

26
Q

Progestins mech

A

bind progesterone receptors, reduce growth, increase vascularization of endometrium

27
Q

Progestin use

A

oral contraceptives, endometrial cancer, abnorm uterine bleeding.

28
Q

Mifepristone (RU-486) mech

A

competitive inhibitor of progestins at progesterone receptors

29
Q

Mifepristone (RU-486) use

A

termination of pregnancy, admin w/misoprostol (PGE1)

30
Q

Mifepristone (RU-486) tox

A

heavy bleeding, GI, abdominal pain

31
Q

Oral contraception

A

Estrogen & progestin inhibit LH/FSH -> prevent E surge -> no LH surge -> no ovulation. Progestins thicken surgical mucous, limiting sperm access. Progestins also inhibit endometrial proliferation, thus making it less suitable for the implantation of embryo.

32
Q

OCP contraindications

A

smoker>35 due to increased risk of cardiovascular events, hx of thromboembolism, stroke, E-dependent tumor

33
Q

Tertbutaline

A

Beta2 agonist

relaxes uterus, reduces premature uterine contractions, (also bronchodilates)

34
Q

Tamsulosin

A

alpha1 antagonist
Tx- BPH by inhibiting smooth mm contraction. Selective fro alpha 1A,D receptors in prostate
(alpha 1b = vascular)

35
Q

Sildenafil, vardenafil mech

A

Inhibit phosphodiesterase 5, prevents breakdown of cGMP, causes smooth mm relaxation in the corpus cavernosum, increases blood flow & penile erection. (NO & ANP also activate cGMP 2nd msgr to increase cGMP)

36
Q

Sildenafil, vardenafil use

A

erectile dysfunction

37
Q

Sildenafil, vardenafil tox

A

headache, flushing, dyspepsia, impaired blue/green color vision. risk of life-threatening hypoTN in pts taking nitrates.

38
Q

Danazol mech

A

synthetic androgen; partial agonist at receptors

39
Q

Danazol use

A

endometriosis & hereditary angioedema

40
Q

Danazol tox

A

weight gain, edema, acne, hirsutism, masculinization, decreased HDL, hepatotox