Pharmacology of female sex hormones

Question 1

What are the four superfamilies of receptors?

Answer 1

• Ligand-gated ion channels
• G-protein coupled receptors
• Kinase-linked receptors
• Nuclear receptors
  (1 - fastest 2 -slowest)

Question 2

How does superfamily 4 work?

Answer 2

• Agonist (hormone) binds to an intracellular receptor
• Zinc finger domain opens up and allows binding to hormone responsive element located upstream from gene promotor region of DNA

Question 3

What genetic changes can superfamily 4 result in?

Answer 3

Inc or Dec:

1) activity of RNA polymerase
2) which will affect gene transcription
3) which will affect translation of mRNA
4) which will alter synthesis of new protein altered cell response

• Which will either enhance or suppress gene expression

Question 4

Can oestrogen and progesterone be taken in pill form?

Answer 4

• no very large 1st pass effect orally

Question 5

In what form are oestrogen and progesterone given?

Answer 5

ethinyloestradiol (oestrogen)

Levonorgestrol or norethisterone (progesterone)

Question 6

What occurs to oral contraceptives (pill) when be metabolised?

Answer 6

• Undergo extensive first pass
• levels of active hormone low and can be influenced by conditions affecting gut and liver
• dietary changes and use of antibiotics can affect active concentrations
• issues are avoided by parenteral administration (patch or implant)

Question 7

How are female contraceptives often classified?

Answer 7

• Most contraceptives are hormonal

- either progesterone only or progesterone and oestrogen

Question 8

What are the routes of admission?

Answer 8

• Oral
• Injected
• Implant
• Intrauterine

Question 9

What is usually first line contraceptive?

Answer 9

Combined oral contraceptive pill (the pill)

Question 10

What hormones will the COCP affect?

Answer 10

Oestrogen and progesterone

Question 11

When should the COCP be taken?

Answer 11

21 days on 7 days off

Question 12

When is the COCP contraindicated?

Answer 12

• Migraine with aura
• Heavy smoker and above 35
• Breastfeeding
• Uncontrolled hypertension
• Personal history of VTE/cardio/CV disease or current breast cancer

Question 13

What is the most common brand name for POP?

Answer 13

Cerelle

Question 14

What are the forms of progesterone only contraceptive?

Answer 14

• Progesterone only pill (POP)
• Injectable form (Depo Provera)
• ## LARC (long acting reversible contraception)

Question 15

What are the most common side effects of progesterone only?

Answer 15

• Irregular bleeding/spotting

Question 16

What is the brand name for LARCs?

Answer 16

implants nexplanon or mirena coil (contains hormones unlike copper coil)

Question 17

What contraceptives have the highest failure rate?

Answer 17

non-hormonal methods

Question 18

What are the brand names for the morning after pill and how long after can the pill be taken?

Answer 18

• Levonelle or EllaOne

- Can be taken 0-120 hours after

Question 19

What are the forms of emergency contraception?

Answer 19

• Morning after pill

- Copper coil

Question 20

What factors will play into the choice of contraceptive?

Answer 20

• PMH
• Organ function
• Allergies
• Cost
• Risk: Benefit

Question 21

What should patients look out for when taking COCP

Answer 21

swollen calf

Question 22

In what condition is hormone replacement therapy used?

Answer 22

Menopause

Question 23

What are the symptoms of menopause?

Answer 23

• poor sleep
• Mood changes
• Dry skin and hair

Question 24

When in HRT necessary?

Answer 24

• Early menopause to ensure bone health

- Can also be used in menopause