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342 > gender affirming pharmacotherapies > Flashcards

gender affirming pharmacotherapies Flashcards

1
Q

what are the most commonly used puberty blockers

A

gonadotropin-releasing hormone (GnRH) agonists

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2
Q

what do gonadotropin-releasing hormone agonists do

A

inhibit release of sex hormones e.g. testosterone and oestrogen

prevent actions of luteinizing hormone (LH) and
follicle stimulating hormone (FSH)

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3
Q

where is gonadotropin-releasing hormone (GnRH) produced

A

cells in hypothalamus

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4
Q

gonadotropin-releasing hormone (GnRH) is a decapeptide. what is this

A

ten amino acids in size

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5
Q

when gonadotropin-releasing hormone (GnRH) is produced, where does it go

A

released into small blood vessels, carried to pituitary gland

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6
Q

how do gonadotropin-releasing hormone (GnRH) change throughout childhood

A

low in childhood
inc as puberty begins

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7
Q

what occurs when gonadotropin-releasing hormone (GnRH) reaches the pituitary gland

A

gonadotropin-releasing hormone (GnRH) activates its receptor, gonadotropin-releasing hormone receptor (GnRHR)

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8
Q

what is the gonadotropin-releasing hormone (GnRH) receptor called

A

gonadotropin-releasing hormone receptor (GnRHR)

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9
Q

what is the gonadotropin-releasing hormone receptor (GnRHR)

A

seven transmembrane GPCR

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10
Q

what does gonadotropin-releasing hormone receptor (GnRHR) activation lead to

A

release of:

luteinizing hormone (LH)
follicle stimulating hormone (FSH)

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11
Q

what function does luteinizing hormone (LH) and follicle stimulating hormone (FSH) have in males

A

signal for testes to produce testosterone and produce sperm

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12
Q

what does testosterone stimulate

A

secondary sex characteristics e.g. penis, scrotum, facial hair growth

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13
Q

what function does luteinizing hormone (LH) and follicle stimulating hormone (FSH) have in females

A

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

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14
Q

what is an example of an oestrogen hormone

A

oestradiol

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15
Q

what are other examples of puberty blockers (4)

A

goserelin
histrelin
leuprolide
triptorelin

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16
Q

what are puberty blockers traditionally used in

A

treatment of breast or prostate cancers

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17
Q

how do gonadotropin-releasing hormone (GnRH) agonists work

A

diretly stimulating the gonadotropin-releasing hormone receptor (GnRHR) in the pituitary gland

do not quickly dissociate

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18
Q

what is the initial impact of the gonadotropin-releasing hormone (GnRH) agonist binding to the gonadotropin-releasing hormone receptor (GnRHR)

A

flare effect

up to 10 fold increase in luteinising hormone
up to 2 fold increase in follicle stimulating hormone

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19
Q

what is the impact of the gonadotropin-releasing hormone (GnRH) agonist binding to the gonadotropin-releasing hormone receptor (GnRHR) after continuous administration

A

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

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20
Q

result of The Cass Review

A

NHS england - puberty blockers not routine treatment for children with gender dysphoria

BMA - disagreed, calling for ban to be lifted

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21
Q

other than as a puberty blocker, what other role does gonadotropin-releasing hormone (GnRH) have

A

supressing endogenous sex hormone production

switch off body’s sex hormone production, cross sex hormones can be administered

22
Q

in MTF, which gonadotropin-releasing hormone (GnRH) are injected to reduce testosterone production 2

A

goserelin
leuprorelin

23
Q

why does administration of oestrogen lower testosterone

A

negative feedback in hypothalamic pituitary gonadal axis

24
Q

why do MTF require anti androgen medication after oestrogen admin

A

testosterone levels are decreased to be low for a male but above normal range for a female after oestrogen admin alone

further inhibits testosterone

25
Q

examples of anti-androgen medication aka MTF (3)

A

spironolactone
finasteride
cyproterone

26
Q

what is spironolactone

A

mild antiandrogen

androgen receptor (AR) competitive antagonist

competes with androgen

27
Q

what is the androgen receptor a target for (2)

A

testosterone

more potent androgen dihydrotestosterone (DHT) - produced from testosterone

28
Q

what other function does spironolactone have

A

reduce effects of androgens produced by adrenal glands as well as testes

29
Q

what can a high dose of spironolactone induce

A

breast development, feminization, lack of spontaneous erections

30
Q

what is cyproterone

A

anti androgen

acts as an androgen receptor antagonist

helps counteract flare effect of gonadotropin-releasing hormone (GnRH) agonists, reduces testosterone surge

31
Q

what is finasteride

A

inhibitor of enzyme 5α-reductase

32
Q

what is the enzyme 5α-reductase responsible for

A

converstion of testosterone into DHT (more potent androgen)

33
Q

what gonadotropin-releasing hormone (GnRH) agonists are injected for FTM (2)

A

goserelin
leuprorelin

34
Q

examples of oestrogen blockers for FTM (2)

A

tamoxifen (oestrogen receptor antagonists)

anastrozole (aromatase inhibitors)

35
Q

what does endogenous oestrogen bind to

A

oestrogen receptor (ER)

36
Q

what occurs once the ER-oestrogen receptor complex is formed

A

translocates to nucleus

activates gene transcription and translation of oestrogen-regulated genes

37
Q

how does tamoxifen function

A

oestrogen receptor ER antagonist, prevents oestrogen binding/ activating

reduces oestrogen effects

38
Q

what is anastrozole FTM

A

aromatase enzyme inhibitor

aromatase coverts androgens to oestrogens

thus reduces oestradiol and inc testosterone levels

39
Q

what GnRH agonists are used MTF

A

goserelin
leuprorelin

40
Q

what GnRH agonists are used FTM

A

goserelin
leuprorelin

41
Q

what cross sex hormones are used MTF

A

oestrogens

42
Q

what cross sex hormones are used FTM

A

testosterone

43
Q

what hormone receptor antagonists are used MTF

A

spironolactone
cyproterone

44
Q

what hormone receptor antagonists are used FTM

A

tamoxifen

45
Q

what hormone production inhibitors are used MTF

A

finasteride

46
Q

what hormone production inhibitors are used FTM

A

anastrozole

47
Q

risks/ side effects of testosterone therapy

A

polycythaemia - inc rbc in blood

48
Q

risks/ side effects of oestrogen therapy

A

venous thromboembolisms (VTE)

49
Q

risks/ side effects of both oestrogen and testosterone therapy

A

inc cvd risk

inc development of type 2 diabetes

impaired fertility

50
Q

what is aromatase

A

enzyme

converting androgens (male sex hormones) into estrogens (female sex hormones)

51
Q

MTF effects

A

redistrubution of body fat

dec muscle mass

softer less oily skin

testicular atrophy

breast development

52
Q

FTM effects

A

vaginal atrophy

cessation of menses

clitoral enlargement

increased muscle mass

deepening of voice

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