Repro/ Post-repro Drugs

Question 1

Describe the effect oestrogen and progesterone have on the other’s receptors.

Give some roles of testosterone.

Answer 1

Oestradiol - stimulates progesterone receptor production
Progesterone inhibits oestrogen receptor production.

Hairy body
Deep voice
Anabolism
Aggression

Question 2

Give some side effects of oestrogen.

Answer 2

Breast tenderness 
Water retention leading to oedema
Thromboembolism 
Impaired glucose tolerance 
Endometrial, ovarian and breast cancer risk. 
Nausea and vomiting.

Question 3

Give some side effects of progesterone.

Answer 3

Weight gain 
Fluid retention 
Acne 
N/V 
Depression, irritability, PMS 
Lack of concentration

Question 4

Give some side effects of testosterone.

What is it bound to?

Answer 4

Anabolic
Acne
Voice changes
Increases aggression
Inhibition of spermatogenesis - therefore infertility
Atherosclerosis risk - decreased HDL increased LDLs

Sex hormone binding globulin.

Question 5

Give three risks of anabolic steroid usage.

Medical use?

Answer 5

Increased liver cancer risk
Cholestatic jaundice risk
Increased CHD risk

Aplastic anaemia

Question 6

Oestrogen PK.

Absorption?

Excretion ?

Answer 6

natural and synthetic oestrogens are well absorbed from GI and mucous membranes and skin

Liver - natural - rapid
Synthetic - less rapid

Urine as glucoronides and sulfates/

Question 7

Progesterone PK.

Progesterone binding?

Metabolised?

Excretion?

Answer 7

Mainly albumin with some stored in adipose - NOT SEX HORMONE BINDING GLOBULIN

Liver - pregnenalone and prenanediol.

Urine - conjugated to glucoronic acid.

Question 8

Give some things that increase the risk of VTE of the combined contraceptive pill.

Answer 8

Smoking
Long-term use in women over 35
Obesity and hypertension

Question 9

Affect of soya protein products on COCP?

Answer 9

Enhance oestrogen absorption and reduce its storage in adipose and muscle and therefore cause half life to reduce from 15 to 7 hours.

Question 10

What symptoms does HRT improve?

Answer 10

Flushing
Sweats
Dyspareunia
Osteoporosis

NOT HEART DISEASE

Question 11

In which cases should unopposed oestrogen cause increased risk of endometrial and ovarian cancer?

What does opposed estrogen increase risk of developing?

What are oral HRT preparations associated with risk off?

Affect on lipid profile?

Answer 11

Women without hysterectomy

Breast cancer

Stroke

increased HDL, decreased oxoLDL, decreased TAG, decreased lipoprotein(a)

Question 12

Mifepristone (RU486) use?

MOA

Answer 12

Termination of pregnancy.

Progesterone and glucocorticoid receptor antagonist blocking action of progesterone causing increased prostaglandins and causing uterine contractions as a result.

Also increases sensitivity of PGs to the myometrium inducing menstruation.

Question 13

Name three SERMs.

Answer 13

Tamoxifen
Raloxifene
Clomiphene

Question 14

What can be used in anovulation Tx?

MOA

Answer 14

Clomiphene

Binds to ER in the anterior pituitary blocking them preventing negative feedback from oestrogen meaning more GnRH is released caused increased stimulation of the ovaries.

Question 15

Two uses of Ulipristal acetate.

Answer 15

SPRM

Emergency contraception
Uterine fibroid treatment

Question 16

Uses of raloxifene?

Answer 16

Prevention of post-menopausal osteoporosis

Treatment of oestrogen positive breast cancers (fewer side effects than tamoxifen)