Sex Hormones And HRT

Question 1

What is the most potent form of oestrogen?

Answer 1

Oestradiol

Question 2

What hormone is inv. in androstenedione to oestrone conversion?
Also in testosterone to oestradiol?

Answer 2

Aromatase

Question 3

2 clinical uses of HRT

Answer 3

Primary ovarian failure (eg turners)

Menopause symptom control (flushes)

Question 4

Oestrogen metabolic actions

Answer 4

Mild anabolic
Na+ retention (water retention)
Increased HDLs,     Impair glucose tolerance 
Increased blood coagulability
Decreased bone resorption

Question 5

Side effects of giving oestrogens

Answer 5

N&V
Water retention
Increased thromboembolic risk
Endometrial hyperplasia risk

Question 6

Actions of progesterone

Answer 6

Secretory endometrium,    Thicken/acidify cervical mucus
Anabolic
Increased basal temp
Increased fluid retention
(Mood changes)

Question 7

Side effects of progesterone

Answer 7

Weight gain, fluid retention
Acne, PMS, depression
Reduced libido
Reduced concentration
Breakthrough bleeding

Question 8

Clinical uses of progesterone

Answer 8

W oestrogen in COCP
As POP or implant
In HRT (to prevent endometrial hyperplasia)
Endometriosis
HIGH dose - in levonorgestrel (emergency contraception)

Question 9

What are the sex steroids derived from? Where do they act?

Answer 9

Cholesterol. Nuclear receptors

Question 10

COCP important pharmacokinetics

Answer 10

CYP450 metabolism

Question 11

Common COCP ADRs

Answer 11

Weight gain, acne, irritability, headaches

Question 12

Serious ADRs of COCP

Answer 12

VTE, stroke, MI, hypertension

Question 13

Disadvantages of POP compared to COCP

Answer 13

No anti ovulatory (less effective) and poor cycle control

So irregular bleeding common

Question 14

Emergency contraception: up to 72 hours

Answer 14

Levonorgestrel

A high dose of progesterone

Question 15

Emergency contraception: up to 120 hours (5 days)

Answer 15

Ullipristal acetate (prog. Receptor modulator)

Question 16

Risks of HRT

Answer 16

High risk endometrial/ovarian cancer w unopposed oestrogen

Increases lipids and thrombosis risk increased (MI, stroke, IHD)

Question 17

What can anti oestrogens can be used for clinically? Give an eg drug

Answer 17

Fertility treatment (eg clomiphene)
Blocks oestrogen receptors so less negative feedback (as compete w body's own oestrogen) makes the body think it need to produce lots of oestrogen so high GnRH and ovary stimulation etc. ovulation induction

Question 18

Tamoxifen. Indication, MoA and ADR

Answer 18

Oestrogen receptor positive breast cancer
Competes w oestrogen for nuclear receptor then blocks transcription of oestrogen responsive genes
Hot flushes (as less oestrogen effects make you feel menopausey)

Question 19

Anti progesterones can be used in what clinical scenario

Give the example drug

Answer 19

Induces labour, can be used in Medical termination of pregnancy
Mife pristone

Question 20

Give an eg Anti androgen

Answer 20

Cyproterone

Question 21

Anti androgens block testosterone/progesterone

Give 3 clinical uses

Answer 21

Precocious puberty in males
Hirsuitism in females
Adjuvant therapy in prostate cancer

Question 22

Name a SERM

Answer 22

Raloxifene

Question 23

What can you use SERMs for?

Answer 23

Allow you to increase oestrogen effects in protective scenarios eg on bone in osteoporosis treatment, without inducing unwanted effects eg proliferator of endometrium leading to cancer risk