gender affirming pharmacotherapies Flashcards
what are the most commonly used puberty blockers
gonadotropin-releasing hormone (GnRH) agonists
what do gonadotropin-releasing hormone agonists do
inhibit release of sex hormones e.g. testosterone and oestrogen
prevent actions of luteinizing hormone (LH) and
follicle stimulating hormone (FSH)
where is gonadotropin-releasing hormone (GnRH) produced
cells in hypothalamus
gonadotropin-releasing hormone (GnRH) is a decapeptide. what is this
ten amino acids in size
when gonadotropin-releasing hormone (GnRH) is produced, where does it go
released into small blood vessels, carried to pituitary gland
how do gonadotropin-releasing hormone (GnRH) change throughout childhood
low in childhood
inc as puberty begins
what occurs when gonadotropin-releasing hormone (GnRH) reaches the pituitary gland
gonadotropin-releasing hormone (GnRH) activates its receptor, gonadotropin-releasing hormone receptor (GnRHR)
what is the gonadotropin-releasing hormone (GnRH) receptor called
gonadotropin-releasing hormone receptor (GnRHR)
what is the gonadotropin-releasing hormone receptor (GnRHR)
seven transmembrane GPCR
what does gonadotropin-releasing hormone receptor (GnRHR) activation lead to
release of:
luteinizing hormone (LH)
follicle stimulating hormone (FSH)
what function does luteinizing hormone (LH) and follicle stimulating hormone (FSH) have in males
signal for testes to produce testosterone and produce sperm
what does testosterone stimulate
secondary sex characteristics e.g. penis, scrotum, facial hair growth
what function does luteinizing hormone (LH) and follicle stimulating hormone (FSH) have in females
signal ovaries to produce oestrogen hormones e.g. oestradiol and regulate menstrual cycle
stimulate development of secondary sexual characteristics e.g. breast development/ hips broadening
what is an example of an oestrogen hormone
oestradiol
what are other examples of puberty blockers (4)
goserelin
histrelin
leuprolide
triptorelin
what are puberty blockers traditionally used in
treatment of breast or prostate cancers
how do gonadotropin-releasing hormone (GnRH) agonists work
diretly stimulating the gonadotropin-releasing hormone receptor (GnRHR) in the pituitary gland
do not quickly dissociate
what is the initial impact of the gonadotropin-releasing hormone (GnRH) agonist binding to the gonadotropin-releasing hormone receptor (GnRHR)
flare effect
up to 10 fold increase in luteinising hormone
up to 2 gold increase in follicle stimulating hormone
what is the impact of the gonadotropin-releasing hormone (GnRH) agonist binding to the gonadotropin-releasing hormone receptor (GnRHR) after continuous administration
decrease in luteinising hormone and follicle secreting hormone
via receptor downregulation by internalisation of receptors
gonadotropin-releasing hormone receptors (GnRHR) removed from cell surface in pituitary gland, cannot interact with agonist anymore