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47 Cards in this Set
- Front
- Back
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What is clomiphene and what does it do?
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SERM: inhibits action of estrogen on hypothalamus and pituitary and increases the release of GnRH, FSH, and LH
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What does ketoconazole do to the ovary?
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Inhibits P-450 of ovarian steroidgenic pathway and inhibits formation of testosterone and androstenedione
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What does anastrozole do to the ovary
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Inhibits aromatase to decrease the synthesis of estrogen
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What is the mechanism of finasteride
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Antiandrogen; a 5a-reductase inhibitor (Decreasese conversion of testosterone to DHT)
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What is finasteride used for
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BPH; promote hair growth - used to treat male pattern baldness
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What is the mechanism of flutamide
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A nonsteroidal competitive inhibitor of androgens at testosterone receptor
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What is flutamide used for
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Prostate carcinoma
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What is the mechanism of ketoconazole as an antiandrogen?
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Inhbiits steroid synthesis
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What is the mechanism of spironolactone as an antiandrogen
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Inhibits steroid binding and steroid synthesis
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What is the mechanism of leuprolide
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GnRH analog with agonist properties when used in a pulsatile fashion; antagonist properties when used in continuous fashion
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What are the clinical uses of leuprolide?
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Infertility (pulsatile), prostate cancer (continuous - use with flutamide), uterine fibroids
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Toxicities of leuprolide
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Antiandrogen, nausea, vomiting
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What is the mechanism of sildenafil
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Inhibit cGMP phosphodiesterase, causing increased cGMP, smooth muscle relaxation in corpus cavernosum, increasing blood flow and penile erection
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What is the mechanism of vardenafil
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Inhibit cGMP phosphodiesterase, causing increased cGMP, smooth muscle relaxation in corpus cavernosum, increasing blood flow and penile erection
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What are the toxicities of sildenafil and vardenafil
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Headache, flushing, dyspepsia, impaired blue-green color vision. ORisk of life threatening hypotension in patients taking nitrates
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What is the mechanism of Mifepristone
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Competitive inhibitor of progestins at progesterone receptors
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What is the other name for Mifepristone
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RU-486
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What is Mifepristone used for
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Termination of pregnancy. Administered with misoprostol (PGE1)
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What is misoprostol and why is it sued in addition with mifepristone
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PGE1; for labor induction
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What are the toxicities fo mifepristone
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Heavy bleeding, GI effects (nausea, vomiting, anorexia), abdominal pain
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Inhibit cGMP phosphodiesterase, causing increased cGMP, smooth muscle relaxation in corpus cavernosum, increasing blood flow and penile erection
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Sidenafil, vardenafil
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GnRH analog with agonist properties when used in a pulsatile fashion; antagonist properties when used in continuous fashion
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Leuprolide
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How do oral contraceptives work?
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Baseline estrogen levels prevent midcycle estrogen surge. Progestins arrest proliferative phase and cause gland atrophy. Progestins also inhibit LH and prevent LH surge.
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True or false, oral contraceptives reduce the risk of endometrial and ovarian cancer
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TRUE
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true or false: oral contraceptives increase the incidence of ectopic pregnancy
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FALSE
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True or false: oral contraceptives reduce pelvic infections
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TRUE
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What are some disadvantages of oral contraceptives
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Increased triglycerides, deperession, weight gain, nausea, hypertension, hypercoagulable state
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What is added to estrogen replacement therapy to decrease the risk of endometrial cancer
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progesterone
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What is dinoprostone used for?
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PGE2 analog causing cervical dilation and uterine contraction, inducing labor
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What is ritodrine used for?
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B2 agonists that relax the uterus; reduce premature uterine contractions
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Terbutaline used for?
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B2 agonists that relax the uterus; reduce premature uterine contractions
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What is anastrazole used for?
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Aromatase inhbitors used in postmenopausal women with breast cancer
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What is exemestane
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Aromatase inhbitor used in postmenopausal women with breast cancer
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Aromatase inhbitor used in postmenopausal women with breast cancer
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Anastrazole and exemestane
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B2 agonists that relax the uterus; reduce premature uterine contractions
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Terbutaline and ritodrine
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What is testosterone as a drug used for? Whatis another name for it
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Methylteestosterone. Tx: hypogonadism and promote development of secondary sex characteristics; stimulation of anabolism to promote recovery after burn or injury; treat ER-positive breast cancer
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What are some names of estrogens used pharamceutically
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Ethinyl estradiol, DES, mestranol
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What are some of the clnical uses of estrogen analogs
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Hypogonadism or ovarian failure, menstrual abnormalitiese, HRT in postmenopausal women; use in men with androgen-dependent prostate cancer
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Diethylstillbestrol is a synthetic analog of
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Estrogen
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What are the toxicities of estrogen analogs
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Increased risk of endometrial cancer, bleeding in postmenopausal women, clear celll adenocarcinoma of vagina in females exposed to DEES in utero, increased risk of thrombi.
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What is the clinical use of progestins?
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Oral contraceptives, tx of endometrial cancer, abnormal uterine bleeding
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What are 3 common SERMs used
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Clomiphene, tamoxifen, raloxifene
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Where does clomiphene act and what does it do?
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Partial agonist of estrogen receptors in pituitary gland. Prevents normal feedback inhibition and increases release of LH and FSH from pituitary, which stimulates ovulation
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What are the uses for clomiphene?
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Infertility and PCOS
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Toxicities of clomiphene
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Hot flashes, ovarian enlargement, multiple simulaneous pregnancies, and visual disturbances
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What does tamoxifen do?
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Antagonist on breast tissue; used to treat and prevent recurrence of ER-positive breast cancer
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What does raloxifene do?
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Agonist on bone; reduces resorption of bone; used to treat osteoporosis
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