Reproduction pharm Flashcards
Alternative oestrogen receptors?
PM receptors?
GPCR? (GPR30)
SERMs
Selective oestrogen receptor modulators
Oestradiol - agonist
Tamoxifen, Faloxifene - partial agaonist
Fulvestrant - antagonist
Tamxifen
SERM
Partial agonist
Palliative treatement of metastatic breast cancer after lumpectomy
Aromatase inhibitors
Increase free survival after tamoxifen resistance
Decreases contralateral breast cancer, decrease some oestrogen blockade side-effcts (thromboemolic events, endometrial cancer)
Cyproterone
Androgen receptor antagonist (steroidal)
Prostate cancer
Androgenisation in females
Flutamide
Androgen receptor antagonist (non-steroidal)
May have selective action at prostate
Metastatic prostate cancer
Finasteride
5areductase inhibitor
Decrease DHT in prostate, seminal vesicles, epididymis
Hair loss
Combined preparations OCP
mixture of oestrogen and progesteron in fixed ratio fo doses
Sequential preparations OCP
Ratio of doses varies to correspond approximately with changes in endogenous oestrogen and progesterone
Not commonly used
Progesteone only preparations (min-pill)
Less effective but used when OCP contraindicated eg during lactation
Estradiol
Natural oestrogen absorbed but synthetics preferred
Ethynyloestradiol
Mestranol
Progesterone
Natural progesterone not orally active, must use synthetics
Earlier - Levonorgestrel, norethisterone (some have androgenic activity)
Newer - desogestrel, gestodene
New - cyproterone, drospirenone (anti-androgenic)
Spironolactone - anti-androgenic activity
Other contraceptives
Vaginal ring - etonogestrel and ethinyloestradiol
Progesteron only - medroxyprogesterone (IM injection), etonorgesterel (subdermal implant), levonorgestrel (IUD)
Emeregency contraceptives - morning after pill
