Pharm Quiz Summer 1

What are the causes of primary hypoandrogenism?
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What are the causes of primary hypoandrogenism?
target organ insensitivity, varicocele, cryptorchidism, deficient steroidogenesis, 5-alpha-reductase deficiency, testicular trauma (orchidectomy, bilateral torsion, irradiation, orchitis, testicular infection, infiltrative disorders (sarcoidosis, hemochromatosis)), cytotoxic agents (cyclophosphamide, chlorambucil, cisplatin, opioids)
What are the causes of secondary hypogonadism?
GnRH deficiency, hypothalamic-pituitary tumors (craniopharyngioma, adenoma, meningioma) or trauma (pituitary apoplexy, radiation, panhypopituitarism), hyperprolactinemia, chronic systemic illness (cirrhosis, renal failure, HIV)
What are the most prevalent causes of hypoandrogenism?
obesity, alcoholism, aging
What are the oral testosterone formulations?
17-alpha-alkylated androgens, methyltestosteron and fluoxymesterone
Which exogenous androgens are more likely to cause hepatotoxicity and hepatic tumors?
17-alpha-alkylated androgens, methyltestosterone and fluoxymesterone
What are the typical esterified androgen intramuscular testosterone formulations?
testosterone undecanoate, testosterone cypionate, testosterone enanthate
What is the duration of action of esterified androgen intramuscular testosterone formulations?
2-4 weeks
What are the indications of Oxandrolone?
adjunct in corticosteroids therapy to help relieve bone pain associated with osteoporosis
What are the adverse effects of androgens in females?
virilization effects such as hirsutism, clitoromegaly, and a lower voice pitch limit the use of androgens in females, amenorrhea/ oligomenorrhea in premenopausal women, alopecia, breast and uterine atrophy
What are the adverse effects of androgens in males?
gynecomastia and breast tenderness, priapism, oligospermia, testicular atrophy, BPH, unmasking or exacerbation of prostate cancer, alopecia, premature closure of epiphyses
What are the adverse effects of androgens in all patients?acne, changes in libido, changes in glucose tolerance, increases the incidence of cardiovascular diseaseWhat are the adverse contraindications of androgens?BPH and symptoms of lower urinary tract obstruction, prostate cancer, breast cancer, pregnancy or breast feeding mothers, severe heart failure, polycythemiaWhich drugs have actions potentiated by the treatment with androgens?Warfarin (anticoagulant activity), Epoetin alfa (hematopoietic activity), cyclosporine (plasma concentration)What is the effect of androgen treatment on glucose metabolism?exogenous androgens decreases blood glucose, a lower dose of anti diabetic medication will be required to avoid the risk of hypoglycemia in type II diabetic patientsWhat are the indications for treatment with anti-androgens?precocious puberty, congenital adrenal hyperplasia, androgen-secreting tumors, androgen-dependent prostate cancerWhat GnRD superagonists are indicated for treatment of prostate cancer and precocious puberty in males?Leuprolide, GoserelinWhat GnRH antagonists are indicated for the treatment of prostate cancer?DegarelixWhat drug is a weak antagonist at the androgen receptor and aldosterone receptor used for the treatment of ascites, pulmonary edema, hypertension, hyperaldosteronism, and hypokalemia?spironolactoneoff-label uses for spironolactonehirsutism, PMS, PCOSWhat drug is a non steroidal androgen receptor antagonist used to treat androgen sensitive prostate cancer. Available as an oral formulation taken 3 times a day?FlutamideWhich drugs are non steroidal androgen receptor antagonists used to treat androgen sensitive prostate cancer. Available as an oral drug taken once per day?Bicalutamide, nilutamide, enzalutamideWhat are the adverse effects of androgen receptor antagonists?hypoandrogenic symptoms (decreased libido, impotence, hot flashes, edema, anemia, gynecomastia, mastalgia), may be hepatotoxicWhat drug is an androgen receptor antagonist used for the treatment of metastatic castration-resistant prostate cancer, in patients previously treated with docetaxel?EnzalutamideWhat drug is an androgen synthesis inhibitor used to treat metastatic castration-resistant prostate cancer?AbirateroneWhat is the mechanism of action of Abiraterone?Inhibits the action of CYP17 (17-alpha-hydroxylase + 17,20-desmolase), blocking the synthesis of androgens and cortisolWhat additional drug do patients taking Abiraterone need to be prescribed to reduce symptoms of adrenal insufficiency?prednisoneWhat is the mechanism of action of finasteride and dutasteride?Inhibit the actions of 5-alpha-reductase, blocking the conversion of testosterone to the more active androgen 5-alpha-DHTWhich isoform does finasteride inhibit?type II isoform of 5-alpha-reductaseWhich isoform does dutasteride inhibit?type I and II isoforms of 5-alpha-reductaseWhat are the adverse effects of dutasteride and finasteride?inhibition of 5-alpha-reductase disrupts normal development of the male fetus (teratogenic)Why are dutasteride and finasteride contraindicated in pregnant women?inhibition of 5-alpha-reductase disrupts normal development of the male fetusWhat is the mechanism of action of finasteride?Inhibits the actions of 5-alpha-reductase thereby disruption the process of balding or receding hairline in malesWhat drug is a PDE5 inhibitor used in the treatment of BPH?TadalafilWhat drugs are used to relieve the symptoms of BPH by relaxing the smoothie muscle to ease the occlusion of the urinary tract?Alpha-1 blockers (doxazosin, terazosin, tamsulosin, alfuzosin)What GnRH antagonist is used to induce chemical castration in the treatment of hormone-sensitive prostate cancer?DegarelixWhich drug formulation is a buccal tablet?NatestoWhat are the contraindications of Oxandrolene?carcinoma, kidney failure, hypercalcemia, pregnancyShould spironolactone be used in pregnancy?It crosses the placenta and enters breast milkWhat is the mechanism of action of PDE5 inhibitor?Selective inhibitors of cGMP prolonging effect of NOWhich PDE5 inhibitor has the longest duration of action (36 hours)?TadalafilContraindications of PDE5 inhibitors?nitrate therapy, cardiovascular disease or hepatic disease, penile structural abnormality or predisposition to priapism, pregnancy. Do not administer with alpha blockers, antihypertensives, or alcohol as they cause hypotensionWhat are the natural estrogens?17-B-Estradiol, Estriol, Estrone, CEEWhat natural estrogen is the most potent in the premenopausal stage, once it has been modified?17-B-estradiolWhich estrogen is the metabolite of estradiol produced by the placenta?EstriolWhich natural estrogen is the predominant form in menopause?EstroneWhat are the synthetic estrogens?Conjugated synthetic estrogens A, ethynyl estradiol, ethinyl validate, mestranol, diesthylstilbesterolWhat is micronization?Reduction in size of the average diameter of 17-B-estradiol particle to nanometer scale to improve its bioavailabilityWhat are the micronized estrogens?Micronized estrogen (Estrace) Esterified estrogens (Menest) Estropipate (Ogen)Which estrogen is a man made mixture of estrogens, sodium estrone sulfate and sodium equaling sulfate?MenestWhich estrogen is a natural estrogen prepared from purified crystalline estrone, solubilized as the sulfate and stabilized with piperazine?OgenWhich estrogen is a natural estrogen, less potent than estradiol, at higher concentrations in blood during pregnancy and after menopause?EstroneWhich estrogen is less potent than estradiol, undetectable in non-pregnant women; however during pregnancy, it's synthesized in very high quantities by the placenta?EstriolWhich synthetic estrogens are used for contraception?Ethinyl estradiol, mestranol, estradiol valerateDrawbacks of synthetic estrogens compared to natural estrogensmore undesirable effects on liver enzymes, clotting factors, and blood pressureWhich natural estrogen is isolated from pregnant equine urine used for menopausal hormone therapy?PremarinWhich estrogen is derived from plants and contains 9 of the 10 estrogens known to be found in natural conjugated equine estrogens?Conjugated Synthetic Estrogens, AWhich estrogen is a synthetic oral, non steroidal estrogen whose use was discontinued but remains of interest because daughters exposed to it in utero have an increased risk of developing abnormal cells in the cervix and vagina?DiethylstilbestrolIndications for HRT (estrogen)?primary hypogonadism due to premature ovarian developmental failure (Turner syndrome), ovariectomy in premenopausal womenWhich drug should be used in menopausal women with osteoporosis and vasomotor symptoms, is added to their treatment with estrogen in order to reduce the risks of uterine cancer?ProgesteronePhysiological effects of estrogensproliferation of uterine endometrium, myometrium, cervix, vagina, changes the consistency of vaginal mucus (thin, copious, and stringy). increased protein synthesis in liver and increased blood HDL and triglyceride levelsAdverse effects of estrogensbreast tenderness, uterine bleeding, cardiovascular thromboembolic disease, endometrial cancers, and gallbladder diseaseWhat mutation along with smoking increases the risks of blood clots and CVT during estrogen treatment?factor V leidenWhat is the term for a scenario where a woman with healthy cardiovascular system at low hormonal replacement concentrations is protective, however at high hormonal concentrations or in the presence of pre-existing cardiovascular disease has adverse cardiovascular effects?Paradoxical effect of estrogen on the cardiovascular systemWhat are the consequences of oral compared to transdermal administration of estrogens?transdermal route avoids first pass effect but you don't get the elevated HDLWhat is part of the natural life cycle that occurs when the ovarian supply of responsive follicles is exhausted, the absence of follicles resulting in the loss of estradiol and progesterone secretions?menopauseWhich estrogen is a natural estrogen synthesized by action of aromatase, which converts androstenedione to estrone in peripheral tissues (skin and fat) during menopause?EstroneWhat are the symptoms of hypoestrogenism?vaginal and urethral atrophy (vulvovaginal atrophy, dryness, burning, sometimes bleeding, dyspareunia, infections, prolapse, dysuria, urinary urgency), loss of elasticity and skin wrinkling, osteoporosis, increased cardiovascular disease and disruption of REM sleep with consequent fatigueWhat are the vasomotor symptoms of menopause?symptoms during menopause, characterized by mood swings, emotional complaints, restlessness, loss of rEM sleep, hot flashes, with sensation of warmth and heat followed by profuse sweating. usually resolve in 3-5 yearsHow do you treat the symptoms of menopause?Estrogen replacementWhat estrogen formulations are suitable for the treatment of vasomotor effects of menopause?oral (CEE, micronized estradiol, esterified estrogens estropipate), transdermal (climate, vivelle Dot), vaginal rings (Femring)What are the topical estrogen formulations used to treat vaginal atrophy in menopause?vaginal gel (EstroGel), vaginal cream (Premarin vaginal), vaginal tablets (Vagifem)What are the topical estrogen formulations likely to cause systemic effects and secondary exposure?emulsion (Estrasorb) and sprays (Evamist)What estrogen levels are used to treat the symptoms of menopause relative to those for contraception?20% of the contraceptive potencyWhich SSRI is used to treat moderate to severe vasomotor symptoms of menopause at lower doses as compared to its use for psychiatric conditions?ParoxetineWhat is the intravaginal formulation approved for the treatment of moderate to severe dyspareunia caused by vulvovaginal atrophy?Prasterone (contained DHEA)mechanism of action of estrogensbind intracellular nuclear receptors and the hormone or drug-receptor complex then acts as a ligand-activated transcription factor to regulate gene transcriptionWhich contraceptive is an orally active natural progesterone modified by micronization. Like all progesterones it is metabolized by first pass effect in the liver?PrometriumWhat molecules are used in female contraceptives but are derived from either testosterone or 17-alpha-hydroxyl-progesterone? The testosterone derived forms may retain androgenic activity, which tends to account for the side effectssynthetic progestinsWhat are the synthetic progestins derived from testosterone?levonorgestrel, norgestrel, desogestrel, etonogestrel, norgestimate, norelgestrominWhat is the metabolite of desogesterol?etonogestrelWhat is the metabolite of norgestimate?norelgestrominWhich progestins are derived from 17-alpha-hydroxyl-progesterone?hydroxyprogesterone, hydroxyprogesterone caproate, medroxyprogesterone acetate, megestrol acetateWhat is a synthetic progestin, related to spironolactone, has anti-androgenic and anti-aldosterone effects used as a contraceptive and for menopausal hormone replacement?drospirenoneWhat are the indications for progestins?dysfunctional uterine bleeding, amenorrhea, endometriosis, endometrial and renal cell carcinoma, luteal phase defect and the prevention of recurrent premature birthWhat are the adverse reactions to progestins?headache, depression, weight gain, loss of libido, increased LDL levelsMechanism of action of progestinsbinds to intracellular nuclear receptor and the drug-receptor complex acts as a ligand-activated transcription factor to regulate gene transcriptionmetabolism of progestinshydroxylation via cytochrome P450 3A4, conjugation by sulfonation and glucuronidationindications of ulipristal acetateprevents ovulation, emergency contraception, pre-operative treatment of uterine fibroidsWhat is special about SPRMs?Progesterone agonists in some and antagonists in othersside effects of ulipristal acetateheadache, nausea, fatigue, abdominal pain. Do not use in patients with liver disease, pregnant, or lactatingWhat drugs are likely to interact with ulipristal acetate?progesterone and glucocorticoid receptor agonists, substrates of CYP3A4 (rifampin, phenytoin, St. Johns wort, carbamazepine, ritonovir)mechanism of action of mifepristoneblocks the activity of progesterone by binding to its endogenous native receptorindications of mifepristoneabortifacient up to 70 days (stimulates smooth muscle contractions in uterus), hyperglycemia in Cushing's syndromeways mifepristone acts to prevent pregnancy from occurringdelays ovulation, interrupting the chances of sperm and egg meeting by decreasing their linear progression through the female reproductive tract, prevents implantation of a fertilized zygoteWhat is the role of progesterone?after conception, in anticipation for pregnancy, it induces the thickening of the uterine lining creating an ideal supportive environment in the uterus for the implantation of the zygotechanges in cervical mucus as a means of contraceptionthin, slick, watery, and copious (high estrogen and estradiol)