Pharmacology: Hormonal treatment in non malignancy gynaecological conditions

Question 1

What is the danger of unopposed oestrogen?

Answer 1

proliferation of uterine endometrium

premenopausal: irregular bleeding
postmenopause: endometrial hyperplasia when used alone as HRT

Question 2

Which situation can you used oestrogen alone?

Answer 2

HRT when the woman has undergone hysterectomy

Question 3

In reproductive years what is the most potent endogenous estrogen?

Answer 3

17-beta-estradiol E2
estrone E1
Both made from ovaries
Estriol E3 is least protent and made from metabolism of E1

Question 4

After menopause what it the premodinant oestrogen?

Answer 4

E1 as oestrogen secretion stops
Peripheral aromatisation of androstenedione in adipose tissue.
Overweight women have 2 x more E1/E2

Question 5

In orally administered oestrogen what does the addition of ethinyl group E2 do? (Ethinyl estradiol)

Answer 5

Prevents inactivation and enables efficient gut absorption

Question 6

What type of drug is clomiphene citrate?

Answer 6

Selective oestrogen receptor modulator

Acts centrally blocking negative feedback of oestrogen to induce FSH

Question 7

What type of drugs is tamoxifen? What are its effects in different parts of the body?

Answer 7

Selective oestrogen receptor modulator
Oestrogen antagonist in breast
Agonist in skeleton + CV system
Causes endometrial hyperplasia/adenocarcionoma

Question 8

Where is progesterone chiefly produced?

Answer 8

Corpus luteum, small amount from adrenal cortex
1mg/day pre-ovulation
20-30mg luteal phase
pregnancy the placenta

Question 9

effects of progesterone?

Answer 9

increases viscoivty of cervical mucus
promotes glandular development of breast
increases body temp
induction of decidual developement

Question 10

Where is progesterone metabolism?

Answer 10

Liver, excreted in bile, little enterohepatic circulation

Question 11

Which progesterones are made from 21-carbons?

Answer 11

Medroxyprogesterone acetate (Depot)
Dydrogesterone

Question 12

Potential benefits of 21-carbon progesterones?

Answer 12

Less androgenic

Question 13

Which drugs are made from 19 carbon derived for noreithisterone?

Answer 13

Noreithisterone

Levonrgestrel

Question 14

Properities of 19 carbon progesterones

Answer 14

Androgenic properties

Question 15

What drugs is drospirenone?

Answer 15

C17 chemically related to spironolactone

Antimineral coticoid and antiandrogenic

Question 16

Why is continuous or cyclic progesterone important in HRT

Answer 16

Protect the endometrium,

Question 17

Common SE of progesterones

Answer 17

Weight gain
Acne 
Fluid retention 
Headache 
breast tenderness 

C19: more androgen acne & hirsutism

Question 18

What limits the use of danazol?

Answer 18

Androgen effects: hirsutism, voice change, oedema

Question 19

How do GnRH antagonist work?

Answer 19

Block GnRH binding to pituitary gland → noFSH/LH

Question 20

How do GnRH agonist work?

Answer 20

Non-pulsaltive administration leads to down regulation of GnRH receptors

Question 21

What happens when first administrating GnRH agonist?

Answer 21

Surge - 2 weeks patients symptoms will worsen

Question 22

SE GnRH agonist

Answer 22

Menopause like symptoms flushes night sweater insomnia decreased labido headache mood swing vaginal dryness change in breast size acne muscle pain poor mood
fall in bone density
to prevent give oestrogen add back therapy

Question 23

Which oral medication POP COCP or danazol works best for mennorhagia

Answer 23

Danazol but limited use due to SE profile

Question 24

Oral medications vs IUS for mennorhaiga

Answer 24

LNG-IUS appears more efficient

fewer SE

Question 25

Are COCP effective for dysmenorrhoea

Answer 25

Evidence is week

Question 26

How is COCP used in endometriosis?

Answer 26

Long term cycle use 3 monthly

Question 27

What other medical Tx can be used for endometrisis

Answer 27

IUD
Danazol - limited use
GnRH analogues with add back therapy

Question 28

In HRT what is the recommend duration of progesterone to protect the endometrium

Answer 28

12-14 days

Question 29

What route can you give oestrogen

Answer 29

Oral
Transdermal 
Vaginal cream
Pesseries/rings
subcut impact

Question 30

SE HRT

Answer 30

VTE
gall bladder disease
stroke
BC

Question 31

What symptom of the menopause can progesterone alone treat?

Answer 31

hot flushes

Question 32

What is tibolone?

Answer 32

Synthetic steroid that has oestrogen and progesterone and androgenic effects. Can be used as an alternative HRT.