16. Reproductive Pharmacology

Question 1

What receptors does oestrogen act on?

Answer 1

ERa and ERb

Question 2

What are natural forms of therapeutic oestrogen?

Answer 2

Oestradiol

Oestriol

Question 3

What are synthetic forms of oestrogen?

Answer 3

Mestranol
Stilbestrol
Ethinylestradiol

Question 4

What are the clinical uses of oestrogen?

Answer 4

Contraception
Treat primary ovarian failure (eg. Turner’s syndrome)
Treat secondary ovarian failure (menopause)

Question 5

What are the side effects of oestrogen?

Answer 5

Nausea, vomiting
Retention of salt and water, causing oedema and increased BP
Increased risk thromboembolism
Increased risk or uterine, ovarian and breast cancer

Question 6

What are the contraindications of oestrogen?

Answer 6

Oestrogen dependent tumours
Undiagnosed genital bleeding
Liver disease
History of thromboembolism
Heavy smokers

Question 7

What is Tamoxifen used for?

Answer 7

Oestrogen antagonist

Treat oestrogen positive breast cancer

Question 8

What is Clomifene used for?

Answer 8

Oestrogen antagonist
Induces ovulation (used as fertility treatment)
Inhibits oestrogen binding in AP preventing normal negative feedback
Causes increased FSH and LH which stimulates ovaries

Question 9

What are the actions of progesterone?

Answer 9

Maturation of endometrium
Supports gestation and embryogenesis
Increases insulin and insulin response
Increases body temperature
Depressant

Question 10

Why are testosterone derivatives given instead of natural or derivatives of progesterone?

Answer 10

Naturally occurring are inactive orally

Derivatives must be delivered IM

Question 11

Name 2 testosterone derivates

Answer 11

Norgestrel

Desogestrel

Question 12

What are the clinical uses of progesteogens?

Answer 12

Contraception
HRT
Endometriosis
Endometrial cancer

Question 13

What are the side effects of progestogens?

Answer 13

Weak androgenic action
Fluid retention
Weight changes
Libido changes
Depression
PMS, irregular menstrual cycles
Increased risk of thromboembolism

Question 14

Name an anti-progestegen

Answer 14

Mifepristone

Question 15

How does Mifepristone work?

Answer 15

Acts as a competitive receptor antagonist at the progesterone receptor

Question 16

Name 2 drugs that could be part of a combined pill

Answer 16

Ethinylestradiol and norethisterone

Question 17

What is the dosing of a combined pill?

Answer 17

Taken for 21 consecutive days and 7 hormone free days

Question 18

What is the mechanism of action of a combined pill?

Answer 18

Oestrogen inhibits FSH release and development of the ovarian follicle
Progestogen inhibits LH release and prevents ovulation, makes cervical fluid inhospitable for sperm

Question 19

What are the side effects of a combined pill?

Answer 19

Weight gain, nausea, mood changes, skin pigementation

Hypertension, breast cancer, thromboembolism

Question 20

What is the mechanism of action of a progestogen-only pill?

Answer 20

Makes cervical mucous inhospitable to sperm
Inhibits LH release
Prevents ovulation

Question 21

What medications can interfere with oral mediactions?

Answer 21

CYP-enzyme inducing antibiotics
Causes vomiting or diarrhoea
Seizure medication
St John’s wort

Question 22

Name a progestogen-only injectable

Answer 22

Medroxyprogesterone

Question 23

How often are progestogen only injectables administered?

Answer 23

Every 3 months

Not suitable for use for more than 2 years

Question 24

Name a progestogen-only subdermal implant

Answer 24

Etonogestrel

Question 25

How long does a subdermal progestogen-only implant last?

Answer 25

3 years

Question 26

What are the mechanisms of action of emergency contraception?

Answer 26

Prevents ovulation or delays movement of egg in fallopian tube and thickens cervical mucous

Question 27

Name 2 emergency contraceptives

Answer 27

Levonorgestrel
Ulipristal acetate (ellaOne)

Question 28

How long does Levonorgestrel last?

Answer 28

Must be taken within 72 hours

Question 29

How long does ellaOne last?

Answer 29

Up to 120 hours