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30 Cards in this Set
- Front
- Back
What are the clinical uses of finasteride (propecia)?
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Benign prostate hyperplasia and male-pattern baldness
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What is the mechanism of finasteride?
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5alpha reductase inhibitor --> decreases conversion of testosterone to dihydotestosterone
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What is the clinical use of flutamide?
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Prostate carcinoma
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What is the mechanism of flutamide?
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Non-steroidal competitive inhibitor of androgens at the testosterone receptor
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Ketoconazole and spironolactone can be used to treat polycystic ovarian syndrome and hirsutism. What are some potential side effects?
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Gynecomastia and amenorrhea
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How does ketoconazole act?
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Inhibit steroid synthesis
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How does spironolactone act?
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Inhibit steroid binding
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What is the clinical use of leuprolide?
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Infertility (pulsatile), prostate cancer (continuous - use with flutamide), uterine fibroids
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What is the mechanism of leuprolide?
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GnRH analog - agonist when pulsatile; antagonist when continuous
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What is the toxicty of leuprolide?
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Antiandrogen, nausea, vomiting
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What are the clinical uses of sildenafil and vardenafil?
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Erectile dysfunciton
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What is the mechanism of sildenafil and vardenafil?
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Inhibit cGMP phosphodiesterase --> increase cGMP smooth muscle relaxation in corpus cavernosum, increased blood flow and penile erection
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What is the toxicity of sildenafil and vardenafil?
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Headache, flushing, dyspepsia, impaired blue-green color vision; do not take nitrates! Risk of life-threatening hypotension
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What is the clinical use of mifepristone (RU-486)?
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Termination of pregancy (admin with misoprostol)
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What is the mechanism of mifepristone?
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Competitive inhibitor of progestins at progesterone receptor
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What is the toxicity of mifepristone?
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Heavy bleeding, GI effects: nausea, vomiting, anorexia, abdominal pain
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What is the effect of oral contraceptives on endometrial and ovarian cancer?
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Decrease risk of both
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What is dinoprostone?
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PGE2 analog that causes cervical dilation and uterine contraction --> induces labor
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What is ritodrine/terbutaline?
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Beta2 agonists that relax the uterus
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What is anastrozole?
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Aromotase inhibitor used in postmenopausal women with breast cancer
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What is the clinical use of methyltestosterone?
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Treat hypogonadism and promote development of secondary sex characteristics; stimulation of anabolism to promote recovery after burn or injury; treat ER-positive breast cancer (exemestane)
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What is the toxicity of methyltestosterone?
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Masculinization in females, decreases intratesticular testosterone in mlaes by inhibiting Leydig cells, leading to gonadal atrophy; premature closure of epiphyseal plates; increase LDL, decrease HDL
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What is the clinical use of ethinyl estradiol, DES, mestranol?
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Hypogonadism or ovarian failure, menstrual abnormalities, HRT in postmenopausal women; androgen-dependent cancer in men
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What is the toxicity of ethinyl estradiol, DES, mestranol?
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Increase risk of endometrial cancer, bleeding in postmenopausal women, clear cell adenocarcinoma of vagina in females exposed to DES in utero, increased risk of thrombi; contraindicated in ER-positive breast cancer
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What is the clinical use of progestins?
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Oral contraceptives + treatment of endometrial cancer and abnormal uterine bleeding
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What the clinical use of clomiphene?
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Infertility and PCOS
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What is the mechanism of clomiphene?
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Partial agonist at estrogen receptors in hypothalamus --> prevent normal feedback inhibition and increase release of LH and FSH from pituitary --> stimulate ovulation
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What is the toxicity of clomiphene?
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Hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances
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What is the clinical use and mechanism of tamoxifen?
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Estrogen antagonist on breast tissue; treat and prevent recurrence of ER-positive breast cancer
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What is the clinical use and mechanism of raloxifene?
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Estrogen agonist on bone; reduces reabsorption --> treat osteoporosis
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