Immunosuppressants

Question 1

What do they do?

Answer 1

Suppress or prevent the immune response.
Used in transplant rejection and inflammatory diseases (e.g. RA, severe eczema, IBD)

Question 2

Antiproliferative immunosuppressants

Answer 2

• Azathioprine
• Mercaptopurine
• Mycophenolate mofetil

Question 3

Other immunosuppressants

Answer 3

• Ciclosporin
• Tacrolimus
• Corticosteroids

Question 4

What is the risk associated with immunosuppressants?

Answer 4

High risk of infections
AVOID live vaccines

Question 5

Azathioprine/Mercaptopurine

Answer 5

Mercaptopurine inhibits purine metabolism = inhibits DNA, RNA and protein synthesis.
Azathioprine is metabolised to mercaptopurine

Question 6

Azathioprine/Mercaptopurine - Side effects

Answer 6

Hannah Buys Ama The Longest Human Dick
- Hypersensitivity reactions
- Bone marrow suppression
- Anaemia
- Leucopoenia
- Thrombocytopenia
- Decreased appetite
- Hepatotoxicity (at high doses)

Question 7

Azathioprine/Mercaptopurine - hypersensitivity reactions

Answer 7

STOP immediately
- Rash
- Fever
- Myalgia
- Arthralgia
- Malaise
- N + V
- Diarrhoea

Question 8

Azathioprine/Mercaptopurine - bone marrow suppression

Answer 8

Pre-treatment screening for Thiopurine Methyl Transferase
- The enzyme thiopurine methyltransferase (TPMT) metabolises thiopurine drugs.
- Risk of myelosuppression is increased in patients with reduced enzyme activity.

Question 9

Mycophenolate mofetil

Answer 9

Metabolised to mycophenolic acid.
More selective mode of action than purine synthesis inhibitors e.g. Azathioprine

Question 10

Mycophenolate mofetil - side effects

Answer 10

• Hypogammaglobinaemia
• Bronchiectasis
• Bone marrow suppression

Question 11

Mycophenolate mofetil - hypogammaglobinaemia

Answer 11

Immune system does not produce enough immunoglobulin
Recurrent infections = measure serum immunoglobulin

Question 12

Mycophenolate mofetil - bronchiectasis

Answer 12

Airways of the lungs remain permanently damaged and widened due to persistent infection.
Respiratory symptoms e.g. cough, dyspnoea

Question 13

Mycophenolate mofetil - Pregnancy

Answer 13

Genotoxic + teratogenic
- Women = 2 methods of effective contraception up to 6 weeks after discontinuing.
- Men = use condoms OR female partners use effective contraception up to 90 days after stopping

Question 14

Tacrolimus - MoA

Answer 14

Calcineurin inhibitor

Question 15

Tacrolimus - side effects

Answer 15

• Heart
• Kidney
• Liver
• Bone marrow
• Blood
• Neurotoxicity
• Eye disorders
• Skin

Question 16

Tacrolimus - Heart

Answer 16

Cardiomyopathy e.g. arrhythmias

Question 17

Tacrolimus - Bone marrow

Answer 17

Blood dyscrasias

Question 18

Tacrolimus - Blood

Answer 18

Hypertension
Hyperglycaemia
Hyperkalaemia
Hyperuricaemia

Question 19

Tacrolimus - Neurotoxicity

Answer 19

Headaches + tremors

Question 20

Tacrolimus - Eye

Answer 20

Blurred vision
Photophobia

Question 21

Tacrolimus - Skin

Answer 21

Rashes
Toxic epidermal necrolysis

Question 22

Patient counselling

Answer 22

• Avoid exposure to sunlight/UV - use SPF
• Avoid grapefruit juice + foods high in potassium (high tacrolimus level)
• Driving may be impaired

Question 23

Tacrolimus

Answer 23

MHRA = oral tacrolimus is brand specific. Reports of toxicity + transplant rejection on switching between products

Question 24

Ciclosporin - MoA

Answer 24

Lowers activity of T cells and their immune response

Question 25

Ciclosporin - side effects

Answer 25

• Kidneys
• Liver
• Bone marrow
• Blood
• Visual disturbances
• Gingival hyperplasia
• Neurotoxicity

Question 26

Ciclosporin - Bone marrow

Answer 26

Blood dyscrasias

Question 27

Ciclosporin - Blood

Answer 27

Hyperlipidaemia
Hypertension
Hyperkalaemia
Hypomagnesaemia

Question 28

Ciclosporin - patient counselling

Answer 28

• Avoid exposure to sunlight/UV - use SPF
• Avoid grapefruit juice + foods high in potassium (high ciclosporin level)