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Gonadal Hormones and Inhibitors
Pharmacology of gonadal hormones
61
Pharmacology
Professional
11/20/2011

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Term
Mixed agonists with estrogenic effects are called...
Definition
SERMs
Term
What does 5a-reducatase do? Which drug inhibits it?
Definition
convert testosterone to DHT, finasteride
Term
What is finasteride used to treat?
Definition
BPH and male-pattern hair loss
Term
Estrogen _____ triglyceride levels and ______ LDL cholesterol.
Definition
increases, decreases
Term
Estrogen use by post-menopausal women is associated with a small increase in the risk of...
Definition
breast cancer and CV events
Term
Dose dependent toxicity of estrogen includes...
Definition
nausea, breast tenderness, increased risk of migraines, thromboembolic events, GB disease, hypertriglyceridemia, hypertension
Term
DES is associated with...
Definition
infertility, ectopic pregnancy and vaginal adenocarcinoma in the daughters of women who took it
Term
older drugs like L-norgestrel and norethindrone are more _____ than the newer drugs (norgestimate, desogestrel)
Definition
androgenic
Term
What is fulvestrant?
Definition
a full estrogen receptor antagonist
Term
What is tamoxifen?
Definition
a SERM (mixed agonist)
Term
what is anastrozole?
Definition
an aromatase inhibitor
Term
What is mifepristone?
Definition
anti-progestin
Term
What is flutamide?
Definition
an androgen receptor antagonist
Term
What is ketoconazole?
Definition
an androgen synthesis inhibitor
Term
Ketoconazole and danazole have inhibitory effects on...
Definition
p450c17
Term
What effect do progestins have on metabolism?
Definition
they affect carbohydrate metabolism and stimulate deposition of fat
Term
Toxicity of progestins?
Definition
may increase BP, decrease HDLs, reversible decrease in bone density, delayed resumption of ovulation after termination of therapy
Term
What do hormonal contraceptives contain?
Definition
either a progestin or a progestin plus an estrogen
Term
What's in postcoital contraceptives? Which variety causes fewer side-effects?
Definition
progestin alone, estrogen alone, or a combo - progestin-only has fewer side-effects
Term
Progestin-only contraceptives do not always...
Definition
inhibit ovulation, instead working through effects on cervical mucus glands, uterine tubes and endometrium
Term
Users of combo hormonal contraceptives have decreased risks of...
Definition
ovarian cysts, ovarian cancer, endometrial cancer, benign breast disease, PID, ectopic pregnancy, iron-deficiency anemia, rheumatoid arthritis
Term
The major toxic effects of combined hormonal contraceptives relates to the action of the estrogenic component on...
Definition
blood coagulation
Term
Is the life-time risk of breast cancer different for users of hormonal contraceptives?
Definition
no, but there may be an earlier onset
Term
what are the toxicities of hormonal contraceptives?
Definition
breakthrough bleeding, nausea, breast tenderness, headache, skin pigmentation, depression. Older, more androgenic progestins can cause weight gain, acne, hirsutism
Term
A high dose of estrogen is post-coital contraceptives is associated with...
Definition
significant nausea
Term
Tamoxifen is effective in the treatment of what? What is its action at that site?
Definition
hormone-responsive breast cancer, antagonist
Term
What is the action of Tamoxifen at endometrial receptors? What is the effect of this?
Definition
agonist, promotes endometrial hyperplasia and increases the risk of endometrial cancer
Term
What are some side effects of Tamoxifen?
Definition
hot flashes (antagonist effect), increases the risk of venous thrombosis (agonist effect), prevents osteoporosis (due to more agonist than antagonist effect)
Term
Which drug is structurally related to Tamoxifen and has similar properties?
Definition
Toremifene
Term
How is raloxifene like tamoxifen? How is it different?
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.
Term
What is clomiphene? What does it do?
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
Term
What is used for treatment of breast cancer that has developed resistance to tamoxifen?
Definition
fulvestrant
Term
Anastrozole and related compounds (letrozole) are...
Definition
nonsteroidal competitive inhibitors of aromatase
Term
Which drug is an irreversible aromatase inhibitor?
Definition
exemestane
Term
Anastrozole, letrozole, and exemestane are used in the treatment of...
Definition
breast cancer
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?
Definition
Danazol, sometimes used for endometriosis and fibrocystic disease of the breast
Term
Continuous administration of _______ suppresses gonadotropin secretion and thereby inhibits ovarian production of estrogens and progesterone
Definition
GnRH agonists - i.e. leuprolide
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?
Definition
controlled ovarian hyperstimulation, precocious puberty, short term treatment of endometriosis and uterine fibroids. Decreased bone density
Term
What is RU486? It is often combined with which other drug? What does that drug do?
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
Term
Side effects of mifeprostone + misoprostol are primary due to _____ and include...
Definition
misoprostol, N/V/D, vaginal cramping, bleeding
Term
Testosterone is synthesized from...
Definition
progesterone and DHEA
Term
Testosterone is converted in several organs to ____, which is the active hormone in those tissues
Definition
DHT
Term
What are two drugs that have an increased ratio of anabolic to androgenic action in laboratory tests?
Definition
oxandrolone, stanozolol
Term
All of the anabolic steroids have full ______ effects when used in humans
Definition
androgenic agonist
Term
In both sexes, high doses of anabolic steroids can cause...
Definition
cholestatic jaundice, elevation of LFTs, possibly hepatocellular carcinoma
Term
Flutamide and related drugs are...
Definition
nonsteroidal competitive antagonists of androgen recepts
Term
Spironolactone inhibits _____ receptors and is used in the treatment of _____ in women.
Definition
androgen, hirsutism
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
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.
Definition
flutamide, tumor flare
Term
How do combined hormonal contraceptives help women with hirsutism?
Definition
the estrogen acts on the liver to increase production of SHBG, which reduces the concentration of free androgen in the blood
Term
Which drug is an antifungal that also inhibits gonadal and adrenal steroid synthesis?
Definition
ketoconazole
Term
ethynl estradiol, estrone, estriol and mestranol are all...
Definition
estrogens
Term
norgestrel, medroxyprogesterone, progesterone, norgestimate and norethindrone are all...
Definition
progestins
Term
Tamoxifen, raloxifene and clomiphene are...
Definition
SERMs
Term
Anastrozole and letrozole are...
Definition
aromatase inhibitors
Term
Danazol is...
Definition
a synthesis inhibitor
Term
Mifepristone is an...
Definition
antiprogestin
Term
Leuprolide is an...
Definition
GnRH agonist
Term
Oxandrolone and stanozolol are...
Definition
anabolic steroids
Term
methyltestosterone and fluoxymesterone are...
Definition
androgens
Term
Bicalutamide as a...
Definition
androgen receptor antagonist
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