Drugs 0514FA Flashcards by ashley bui

leuprolide MOA

GnRH analog.

agonist properties when used in PULSATILE fashion.

antagonist properties when used in CONTINUOUS fashion (down regulate GnRH receptor in pituitary to decrease LH, FSH).

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leuprolide USE

infertility (pulsatile).
uterine fibroids (continuous).
prostate cancer (continuous) - use with flutamide.

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leuprolide TOX

antiandrogen.
nausea.
vomiting.

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testosterone (methyltestosterone) MOA

agonist at androgen receptors

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testosterone (methyltestosterone) USE

treat hypogonadism, promote secondary sex characteristics.

stimulate anabolism to promote recovery after burn or injury.

treat ER-pos breast cancer (EXEMESTANE).

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testosterone (methyltestosterone) TOX in females

masculinization.
premature closure of epiphyseal plates.
increase LDL, decrease HDL.

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testosterone (methyltestosterone) TOX in males

reduce intratesticular testosterone by inhibiting LH release (neg fb) - GONADAL ATROPHY.
premature closure of epiphyseal plates.
increase LDL, decrease HDL.

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finasteride

antiandrogen.

5 alpha reductase inhibitor - decrease conversion of testosterone to DHT.

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finasteride USE

BPH.

male pattern baldness (promotes hair growth).

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flutamide

antiandrogen.

nonsteroidal competitive inhibitor of androgens at testosterone receptor.

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flutamide USE

prostate carcinoma

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ketoconazole

antiandrogen.

inhibits steroid synthesis via DESMOLASE.

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ketoconazole USE

polycystic ovarian syndrome - prevent hirsutism.

SE: gynecomastia, amenorrhea.

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spironolactone

antiandrogen.

inhibit steroid binding.

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spironolactone USE

polycystic ovarian syndrome - prevent hirsutism.

SE: gynecomastia, amenorrhea.

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estrogens

ethinyl estradiol.
DES.
mestranol.

MOA: bind estrogen receptors.

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estrogens USE

hypogonadism.
ovarian failure.
menstrual abn.
HRT postmenopause.
androgen-dependent prostate cancer.

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estrogens TOX

increase risk of endometrial cancer.
bleeding in postmenopause.
increase risk of thrombi.
clear cell adenocarcinoma of vagina (in females exposed to DES in utero).

estrogens contraindications

ER-pos breast cancer.

h/o of DVT.

clomiphene

SERM.
partial agonist at estrogen receptors in hypothalamus.
prevents normal feedback inhibition and increases LH, FSH release from pituitary to stimulate ovulation.

clomiphene USE

treat infertility.

PCOS.

clomiphene TOX

hot flashes.
ovarian enlargement.
multiple simultaneous pregnancies.
visual disturbances.

tamoxifen

SERM. antagonist on breast tissue - used to treat and prevent recurrence of ER-pos breast cancer

raloxifene

SERM. agonist on bone - reduces resorption of bone. used to treat osteoporosis

HRT

for relief or prevention of menopausal sx (hot flashes, vag atrophy) and osteoporosis (increase estrogen, decrease osteoclast activity)

ERT

unopposed estrogen increases risk of endometrial cancer so PROGESTERONE is added. possible increased CV risk.

anastrozole, exemestane

aromatase inhibitors for postmenopausal women with breast cancer (prevents androgen to estrogen conversion)

progestins

bind progesterone receptors to reduce growth and increase vascularization of endometrium

progestin USE

part of OCP. | treat endometrial cancer and abn uterine bleeding.

mifepristone (RU-486)

competitive inhibitor of progestins at progesterone receptors

mifepristone USE

termination of preg - admin with MISOPROSTOL (PGE1) to increase uterine contractions to expel contents

mifepristone TOX

``` heavy bleeding. GI effects (nausea, vom, pain, anorexia) ```

OCP

synthetic progestins + estrogen. both inhibit LH, FSH and thus prevent estrogen surge. no estrogen surge = no LH surge = no ovulation.

add'l functions of progestins in OCP

thicken cervical mucus to limit access of sperm to uterus. inhibit endometrial proliferation to make it less suitable for embryo implantation. counteract risk of endometrial cancer due to unopposed estrogen.

SE of OCP use

weight gain. breast tenderness. breakthrough menstrual bleeding. CV events: DVT, PE, ischemic stroke, MI.

contraindications for OCP

``` smokers > 35 yo. h/o of thromboembolism, stroke. h/o of estrogen-dependent tumor. hypertriglyceridemia. liver disease. pregnancy. ```

ritodrine, terbutaline

beta 2 agonists that relax uterus to reduce premature uterine contractions.

tamsulosin

alpha 1 antagonist used to treat BPH by inhibiting smooth muscle contraction. selective for alpha 1A, D receptors in prostate (vs. vascular alpha 1B)

sildenafil, vardenafil, tadalafil MOA

inhibit cGMP phosphodiesterase - increased cGMP, smooth muscle relaxation in corpus cavernosum, increased blood flow, and penile erection

sildenafil, vardenafil, tadalafil USE

erectile dysfunction

sildenafil, vardenafil, tadalafil TOX

headache. flushing. dyspepsia. impaired blue-green color vision.

drug interactions with | sildenafil, vardenafil, tadalafil

risk of life threatening hypotension in pts taking nitrates (nitroglycerin)

danazol

synthetic androgen that acts as partial agonist at androgen receptors. used for endometriosis and hereditary angioedema.

danazol TOX

``` weight gain. edema. acne. hirsutism. masculinization. decreased HDL. ```