pharmacology Flashcards
uses of oestrogen replacement therapy
hypogonadism in children
primary amenorrhoea (+progestin)
contraceptive (+progestin)
menopause (+progestin)
what are the benefits of postmenopausal hormone therapy
- improved bone density
- relief from hot flushes, fatigue and vaginal dryness
- reverses atrophy of vulva, vagina and urethra
- improved sleep
- reduced incidence of colorectal cancers
- reduced incidence of CVD?
- reduced incidence of AD?
what are the risks of postmenopausal oestrogen hormone therapy
- breast tenderness
- nausea
- fluid retention
- increased risk of breast/uterine cancer
- increased risk of thromboembolism/stroke
what are the 4 ways oestrogen causes cellular effects
- crosses to cytoplasmic receptors –> homodimer –> SRE –> gene transcription
- crosses to cytoplasmic receptors –> heterodimer –> SRE –> gene transcription
- can bind to receptor on the cytoplasmic membrane
- bind to GPCR
(last two account for rapid effects)
what are the effects of oestrogen and progesterone in the breast
oestrogen –> growth
progesterone –> differentiation
increased risk of breast cancer is associated with what receptors
oestrogen and progesterone positive in the breast
what are the two partial agonists of oestrogen (SERM)
tamoxifen
raloxifene
what are the effects of tamoxifen
stimulates uterus and CVS and bone but antagonist to breast and CNS
what are the effects of raloxifene
stimulates bone and CVS, but antagonist to breast, uterus and CNS
what is fulvestrant
antagonist to oestrogen receptors throughout the body
when is tamoxifen used
palliative treatment of metastatic breast cancer and adjuvant after lumpectomy
adverse effects of tamoxifen
- endometrial hyperplasia, polyps and cancer
- thromboembolic events
- thrombocytopaenia
- ocular toxicity
- menopausal symptoms
why are aromatase drugs useful for treating breast cancer
because its activity is high in breast adipose mesenchymal tissue
what are the effects of aromatase inhibitors
- improved disease free survival after tamoxifen
- reduced incidence of contralateral breast cancer
- number of thromboembolic events
- incidence of endometrial cancer
what are the adverse effects of aromatase inhibitors
- increased bone loss and fracture risk
- increased arthralgia
- potential poorer lipid profile, hepatic steatosis and metabolic syndrome with long-term use
- menopausal signs
where are the major places that DHT act in males
prostate
seminal vesicles
epididymus
skin
which enzyme converts testosterone to DHT
5-alpha-reductase
what are the main actions of DHT
prostate development
external virilisation
sexual maturation
how does testosterone travel in the blood
bound to steroid hormone binding globulin
action of testosterone in the cell
can bind to androgen receptor in the cytoplasm or can bind directly on receptors in the nucleus
what are the medical uses of androgens
- hypogonadism in children
- senile osteoporosis
- speed recovery from surgery and chronic debilitating diseases
- promotes skeletal growth in pituitary dwarfism
- endometriosis