Term
| Mixed agonists with estrogenic effects are called... |
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Definition
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Term
| What does 5a-reducatase do? Which drug inhibits it? |
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Definition
| convert testosterone to DHT, finasteride |
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Term
| What is finasteride used to treat? |
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Definition
| BPH and male-pattern hair loss |
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Term
| Estrogen _____ triglyceride levels and ______ LDL cholesterol. |
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Definition
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Term
| Estrogen use by post-menopausal women is associated with a small increase in the risk of... |
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Definition
| breast cancer and CV events |
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Term
| Dose dependent toxicity of estrogen includes... |
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Definition
| nausea, breast tenderness, increased risk of migraines, thromboembolic events, GB disease, hypertriglyceridemia, hypertension |
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Term
| DES is associated with... |
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Definition
| infertility, ectopic pregnancy and vaginal adenocarcinoma in the daughters of women who took it |
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Term
| older drugs like L-norgestrel and norethindrone are more _____ than the newer drugs (norgestimate, desogestrel) |
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Definition
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Term
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Definition
| a full estrogen receptor antagonist |
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Term
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Definition
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Term
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Definition
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Term
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Definition
|
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Term
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Definition
| an androgen receptor antagonist |
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Term
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Definition
| an androgen synthesis inhibitor |
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Term
| Ketoconazole and danazole have inhibitory effects on... |
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Definition
|
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Term
| What effect do progestins have on metabolism? |
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Definition
| they affect carbohydrate metabolism and stimulate deposition of fat |
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Term
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Definition
| may increase BP, decrease HDLs, reversible decrease in bone density, delayed resumption of ovulation after termination of therapy |
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Term
| What do hormonal contraceptives contain? |
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Definition
| either a progestin or a progestin plus an estrogen |
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Term
| What's in postcoital contraceptives? Which variety causes fewer side-effects? |
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Definition
| progestin alone, estrogen alone, or a combo - progestin-only has fewer side-effects |
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Term
| Progestin-only contraceptives do not always... |
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Definition
| inhibit ovulation, instead working through effects on cervical mucus glands, uterine tubes and endometrium |
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Term
| Users of combo hormonal contraceptives have decreased risks of... |
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Definition
| ovarian cysts, ovarian cancer, endometrial cancer, benign breast disease, PID, ectopic pregnancy, iron-deficiency anemia, rheumatoid arthritis |
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Term
| The major toxic effects of combined hormonal contraceptives relates to the action of the estrogenic component on... |
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Definition
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Term
| Is the life-time risk of breast cancer different for users of hormonal contraceptives? |
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Definition
| no, but there may be an earlier onset |
|
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Term
| what are the toxicities of hormonal contraceptives? |
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Definition
| breakthrough bleeding, nausea, breast tenderness, headache, skin pigmentation, depression. Older, more androgenic progestins can cause weight gain, acne, hirsutism |
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Term
| A high dose of estrogen is post-coital contraceptives is associated with... |
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Definition
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Term
| Tamoxifen is effective in the treatment of what? What is its action at that site? |
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Definition
| hormone-responsive breast cancer, antagonist |
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Term
| What is the action of Tamoxifen at endometrial receptors? What is the effect of this? |
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Definition
| agonist, promotes endometrial hyperplasia and increases the risk of endometrial cancer |
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Term
| What are some side effects of Tamoxifen? |
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Definition
| hot flashes (antagonist effect), increases the risk of venous thrombosis (agonist effect), prevents osteoporosis (due to more agonist than antagonist effect) |
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Term
| Which drug is structurally related to Tamoxifen and has similar properties? |
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Definition
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Term
| How is raloxifene like tamoxifen? How is it different? |
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Definition
| partial agonist effect on bone, antagonist effects in breast tissue and reduces the incidence of breast cancer for high-risk women. Adverse effects - hot flashes and DVT. Unlike - no estrogenic effects on endometrial tissue. |
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Term
| What is clomiphene? What does it do? |
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Definition
| a nonsteroidal compound with tissue-selective actions, induces ovulation in anovulatory women who want to get preg, selectively blocks estrogen receptors in pituitary and reduces negative feedback thereby increasing FSH and LH |
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Term
| What is used for treatment of breast cancer that has developed resistance to tamoxifen? |
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Definition
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Term
| Anastrozole and related compounds (letrozole) are... |
|
Definition
| nonsteroidal competitive inhibitors of aromatase |
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Term
| Which drug is an irreversible aromatase inhibitor? |
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Definition
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Term
| Anastrozole, letrozole, and exemestane are used in the treatment of... |
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Definition
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Term
| Which drug inhibits several p450 enzymes involved in gonadal steroid synthesis, and is a weak partial agonist of progestin, androgen and glucocortcoid receptors? What is it used for? |
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Definition
| Danazol, sometimes used for endometriosis and fibrocystic disease of the breast |
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Term
| Continuous administration of _______ suppresses gonadotropin secretion and thereby inhibits ovarian production of estrogens and progesterone |
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Definition
| GnRH agonists - i.e. leuprolide |
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Term
| GnRH agonists are used in combo with other agents in which clinical situations? What can happen if they are used in premenopausal women for more than 6 mo? |
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Definition
| controlled ovarian hyperstimulation, precocious puberty, short term treatment of endometriosis and uterine fibroids. Decreased bone density |
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Term
| What is RU486? It is often combined with which other drug? What does that drug do? |
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Definition
| Mifepristone (RU486) is an orally active steroid antagonist of progesterone and glucocorticoids, used as abortifacient in early preg. Combo with misoprostol, a PGE analogue |
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Term
| Side effects of mifeprostone + misoprostol are primary due to _____ and include... |
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Definition
| misoprostol, N/V/D, vaginal cramping, bleeding |
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|
Term
| Testosterone is synthesized from... |
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Definition
|
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Term
| Testosterone is converted in several organs to ____, which is the active hormone in those tissues |
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Definition
|
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Term
| What are two drugs that have an increased ratio of anabolic to androgenic action in laboratory tests? |
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Definition
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|
Term
| All of the anabolic steroids have full ______ effects when used in humans |
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Definition
|
|
Term
| In both sexes, high doses of anabolic steroids can cause... |
|
Definition
| cholestatic jaundice, elevation of LFTs, possibly hepatocellular carcinoma |
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|
Term
| Flutamide and related drugs are... |
|
Definition
| nonsteroidal competitive antagonists of androgen recepts |
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|
Term
| Spironolactone inhibits _____ receptors and is used in the treatment of _____ in women. |
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Definition
|
|
Term
| Which class of drugs is less likely than other antiandrogens to cause impotence, infertility and loss of libido? |
|
Definition
| 5a-reductase inhibitors like finasteride |
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|
Term
| During the first week of therapy with leuprolide, an androgen receptor antagonist (like _____) is used to prevent the _____ that can result from the surge in testosterone synthesis caused by the initial agonist action. |
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Definition
|
|
Term
| How do combined hormonal contraceptives help women with hirsutism? |
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Definition
| the estrogen acts on the liver to increase production of SHBG, which reduces the concentration of free androgen in the blood |
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Term
| Which drug is an antifungal that also inhibits gonadal and adrenal steroid synthesis? |
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Definition
|
|
Term
| ethynl estradiol, estrone, estriol and mestranol are all... |
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Definition
|
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Term
| norgestrel, medroxyprogesterone, progesterone, norgestimate and norethindrone are all... |
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Definition
|
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Term
| Tamoxifen, raloxifene and clomiphene are... |
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Definition
|
|
Term
| Anastrozole and letrozole are... |
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Definition
|
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Term
|
Definition
|
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Term
|
Definition
|
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Term
|
Definition
|
|
Term
| Oxandrolone and stanozolol are... |
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Definition
|
|
Term
| methyltestosterone and fluoxymesterone are... |
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Definition
|
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Term
|
Definition
| androgen receptor antagonist |
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