Term
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Definition
Non-steroidal compounds from plants w estrogen-like structures and estrogenic or anti- activity
Usually weak activity
Risk/benefit not yet clear |
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Term
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Definition
Competitive estrogen rec antagonist that dec estrogen stim of tumor cells
Rx of choice to rx breast cancer in POST-MENOPAUSAL women and select pre-menopausal
Rx for long-term prevention of recurrent cancer
Acts on:
Bone density, uterus, HDL/LDL, clotting |
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Term
| Tamoxifen adverse effects |
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Definition
N/V
hot flashes
inc endometrial cancer |
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Term
| Selective Estrogen Receptor Modulators (3) |
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Definition
Tamoxifen
Toremifene
Raloxifene |
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Term
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Definition
Enter nuc binding ER, but the resulting complex is only PARTIALLY convervted to active form
May act as agonist in one tissue, but antagonist in another |
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Term
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Definition
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Term
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Definition
SERM
Acts on:
Bone density, blood clotting |
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Term
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Definition
Exemestane
Anastrozole
Letrozole
Inhibit final step in estrogen synth
Used in addition to tamoxifen to reduce estrogen stim |
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Term
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Definition
NON-STEROIDAL aromatase inh
Cx hot flashes |
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Term
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Definition
| NON-STEROIDAL aromatase inh |
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Term
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Definition
1. Maintain pregnancy
2. Development of secretory endometrium
3. Prolif of acini in mammary glands
4. Blunting of estrogenic effects
5. Crossover effects at androgen rec |
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Term
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Definition
| Progestin w anti-androgenic and anti-mineralocorticoid activity |
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Term
| Pharmacokinetcs of progestins |
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Definition
Highly lipophilic
Extensively bound to plasma proteins
Hepatic metabolism
Progesterone- not orally active
"19-Nor" compounds- orally effective |
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Term
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Definition
Slow release progesterone
Injected parenterally, slowly absorbed, transformed over months to progesterone, which quickly is cleared.
Single injection can last months |
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Term
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Definition
"abortion pill" - Used in 1st trimester
Competitive antagonist at progesterone and glucocorticoid receptors
Terminates pregnancy
Disrupts normal ovulation
Blocks progesterone mediated stim
Inc plasma levels of ACTH and adrenal steroids |
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Term
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Definition
"19-Nor" progestin
Oral contraceptive
Has undesirable androgenic activity |
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Term
| Norgestrel (Levonorgestrel) |
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Definition
"19-Nor" compound used as oral contraceptive
Least androgenic activity |
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Term
| Combination oral contraceptives |
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Definition
Inh ovulation by:
suppressing LS/FSH levels
eliminating LH surge
inh sperm penetration |
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Term
| Combined OC adverse effects (6) |
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Definition
1. Hirsuitism
2. Inc BP
3. Inc BrCa risk
4. Inc thromboembolic events
5. GB dz
6. Benign hepatoma |
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Term
| Combined OC contraindications (6) |
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Definition
1. CV disorders
2. hormone-dep neoplasia
3. Liver tumors or dysfx
4. Pregnancy
5. Smoking
6. Age |
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Term
| Oral Contraceptive rx interactions resulting in dec efficacy |
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Definition
Induction of hepatic enzymes (barbituates, rifampin, phenytoin)
Interferance w enterohepatic cycling (ampicillin, tetracycline) |
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Term
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Definition
1. hypodgonadism
2. Breast cancer
3. Stimulate erythropoiesis
4. Rx Hereditary angioneurotic edema
5. Rx AIDS-related m. wasting |
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Term
| Oxandrolone adverse effects (3) |
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Definition
1. Liver toxicity
2. Inc LDL/dec HDL
3. May dec fertility in men |
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Term
| Flutamide adverse effects (3) |
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Definition
1. Gynecomastia and impotence if used alone, so used w GnRH analogs
2. Hepatotoxcicity |
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Term
| Finasteride contraindications (2) |
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Definition
1. Women who are or may become pregnant
2. Liver impairment |
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Term
| Cyproterone adverse effects |
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Definition
| May inh spermatogenesis and libido |
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Term
| Dihydrotestosterone effects (4) |
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Definition
1. Inc body and facial hair
2. Acne
3. Scalp hair recession
4. Prostate enlargement |
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Term
|
Definition
1. Penile and scrotal enlargement
2. SPermatogenesis
3. Vocal cord enlargement
4. Muscle mass increase
5. Male libido and sexual performance
6. Erythropoiesis |
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