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1.11
Hormone Replacement Therapy
| Term | Definition |
|---|---|
| Menopause symptoms | 1. hot flashes 2. vaginal dryness, urogenital atrophy 3. arthralgia and myalgia 4. sleep pattern disturbances 5. osteoporosis 6. significant rise in CV disease |
| HRT formulations-clinical uses | 1.primary ovarian failure 2. menopause symptoms (hot flashes, vaginal dryness, osteoporosis) |
| Recommendations for HRT | 1. in women with intact uterus 2. women who have undergone hysterectomy |
| Selective Estrogen Receptor Modulators (SERMs): background | increased pharmacodynamic complexity of estrogen receptor activation/blockade -variable co-activator/co-repressor activities at estrogen receptor depending on ligand -variable effects depending on cell type and activated promoter |
| Selective Estrogen Receptor Modulators (SERMs): background-goal | to produce tissue-specific activation/inhibition of estrogenic effects |
| SERM DRUGS (3) | Clomiphene (CLOMID) Tamoxifen (NOLVADEX) Raloxifene (EVISTA) |
| SERM DRUG: Tamoxifen (NOLVADEX) | breast cancer treatment |
| SERM DRUG: Raloxifene (EVISTA)- therapeutic use | treatment and prevention of osteoporosis and breast cancer in post menopausal women |
| SERM DRUG: Raloxifene (EVISTA)- Adverse Effects | 3-fold increase in deep vein thrombosis and pulmonary embolism |
| SERM DRUG: Clomiphene (CLOMID)-"antiestrogen" | shown to induce ovulation in anovulatory women |
| SERM DRUG: Clomiphene (CLOMID)- stimulates release of: | LH and FSH --> maturation of ovarian follicle and ovulation -may block estrogen receptors in hypothalamus and pituitary -no feedback inhibition on gonadotropin release |
| SERM DRUG: Clomiphene (CLOMID)- induces: | pregnancy |
| SERM DRUG: Clomiphene (CLOMID)-most common side effect | vasomotor symptoms (hot flashes) ovarian enlargement |
| Aromatase inhibitors: type 1 | substrate analogs that act as suicide inhibitors |
| Aromatase inhibitors: type 2 | interact reversibly with the heme groups of CYPs |
| Aromatase inhibitors: type 2 DRUGS | Anastrozole Letrozole |
| Aromatase inhibitors: MOA | 1. inhibit the conversion of estrogen from androgens by aromatase 2. considered the standard care of ER+ adjuvant therapy |
| Aromatase inhibitors: therapeutic uses | Breast cancer |
Created by:
megangodfrey97
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