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PRE-REG-Thuri > CANCER + IMMUNE SYSTEM: IMMUNOSUPPRESSANTS > Flashcards

CANCER + IMMUNE SYSTEM: IMMUNOSUPPRESSANTS Flashcards

1
Q

List 2 calcineurin inhibitors?

A

Ciclosporin

Tacrolimus

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2
Q

What are 3 antiproliferative agents?

A

Azathioprine
Mercaptopurine
Mycophenolate

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3
Q

What should be avoided in patients on immunosuppressants?

A

live vaccines- high risk of infection

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4
Q

List 5 other immunosuppressants?

A

Belatacept

corticosteroid

sirolimus

MABs- e.g. belimumab, basiliximab, canakinumab

Anti-thymocyte immunoglobulin

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5
Q

What are the 2 indications of ciclosporin?

A

Prevention of graft rejection following bone marrow, kidney, liver, pancreas, heart, lung, + heart-lung transplantation,

Prophylaxis and treatment of graft-versus-host disease.

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6
Q

Which of the 2 calcineurin inhibitors has a higher incidence of neurotoxicity?

A

tacrolimus

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7
Q

What is sirolimus licensed for?

A

renal transplantation.

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8
Q

What is the indication of basiliximab?

A

prophylaxis of acute rejection in allogeneic renal transplantation.

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9
Q

What 2 drugs is basiliximab usually given with?

A

ciclosporin

corticosteroid

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10
Q

What is belatacept used for?

A

Licensed for prophylaxis of graft rejection in adults undergoing renal transplantation who are seropositive for the Epstein-Barr virus.

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11
Q

What class is belatacept?

A

Belatacept is a fusion protein and co-stimulation blocker that prevents T-cell activation.

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12
Q

What 3 drugs are usually used with Belatacept?

A

It is used with interleukin-2 receptor antagonist induction, in combination with corticosteroids and a mycophenolic acid.

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13
Q

What 2 indications are anti-thymocyte immunoglobulin licensed for?

A

prophylaxis of organ rejection in renal + heart allograft recipients

Treatment of corticosteroid-resistant allograft rejection in renal transplantation.

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14
Q

How can tolerability of anti-thymocyte immunoglobulin be increased?

A

Pre-treatment with an IV corticosteroid +antihistamine;

+ paracetamol may also be beneficial.

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15
Q

What is the MOA of azathioprine?

A

Blocks purine synthesis - prevent DNA, RNA + protein synthesis

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16
Q

What are 4 SEs of azathioprine? (BAN-PH)

A

Blood disorders

Nausea

Pancreatitis

Hypersensitivity

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17
Q

What screening is done for azathioprine + why?

A

TMPT- check thiopurine methyltransferase levels before drug.

Checked due to risk of myelosuppression

25-65 u/ml

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18
Q

What 3 drugs are TMPT levels checked for?

A

azathioprine, mercaptopurine, tioguanine

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19
Q

What are the monitoring requirements for azathioprine?

A

Toxicity

Monitor FBC weekly (more often with higher doses or if severe RI) for first 4 weeks.

Then monitor every 3 months.

Blood tests + monitoring for signs of myelosuppression are essential in long-term treatment.

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20
Q

What drug does azathioprine interact with and needs a dose reduction?

A

Allopurinol

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21
Q

What are 2 patient counselling points for azathioprine?

A

Take after food + report signs of infection or blood disorders. (e.g. fever, sore throat or mouth ulcers, bruising or bleeding).

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22
Q

What is a contraindication of azathioprine?

A

Patients who are hypersensitive to mercaptopurine

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23
Q

What is azathioprine converted into?

A

Mercaptoprine

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24
Q

What is the dose reduction for patients on azathioprine and allopurinol?

A

Manufacturer advises reduce dose to 1/4 of the usual dose with concurrent use of allopurinol.

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25
Q

What are the 4 SEs of mycophenolate mofetil? (BPH-G)

A

Blood disorders, Bronchiectasis

Pulmonary fibrosis

Hypogammaglobinaemia- low

GI effects

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26
Q

What 2 conditions are azathioprine unlicensed in?

A

Severe refractory eczema

Suppression of transplant rejection

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27
Q

What is MOA of mycophenolate mofetil?

A

Blocks guanosine synthesis

-Prevents DNA, RNA + protein synthesis

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28
Q

How is mycophenolate mofetil prescribed?

A

By brand

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29
Q

What is monitored for mycophenolate mofetil?

A

FBC

WEEKLY for 4 weeks then 2 times a month for 2 months then every month in the first year

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30
Q

What are 3 cautions of using mycophenolate mofetil?

A

Persistent respiratory symptoms- cough

Serious GI disease - UC

Repeat infection - serum IG

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31
Q

How many pregnancy tests need to be done before starting Mycophenolate mofetil?

A

2 pregnancy tests 8–10 days apart are recommended

32
Q

What is 2 counselling points for mycophenolate mofetil?

A

Report signs of infection, blood disorder
e.g. sore throat, fever, mouth ulcers, bruising or bleeding.

Discuss PPP + effects on pregnancy for males.

33
Q

What is contraception regimen for women on Mycophenolate mofetil?

A

At least 1 method of effective contraception before + during treatment.

Take it 6 weeks AFTER stopping drug - use 2 methods of effective contraception are preferred

34
Q

What is MHRA warning for Mycophenolate mofetil?

A

Mycophenolate mofetil + mycophenolic acid are genotoxic - risk cannot be fully excluded.

Updated contraception advice for male patients (2018).

35
Q

How many methods of contraception is preferred after discontinuing mycophenolate mofetil?

A

2

36
Q

How many days should male patients and female partner use contraception when on mycophenolate mofetil?

A

Male patients or their female partner should use effective contraception during treatment + for 90 days after discontinuation.

37
Q

What is MOA of tacrolimus?

A

Blocks calcineurin which activates T- cells.

38
Q

How is tacrolimus prescribed?

A

By brand

39
Q

What are the 5 SEs of tacrolimus? (BaNCS)

A

Blood disorders- hypErkalaemia

Nephrotoxicity

Cardiac myopathy

Sunlight

40
Q

What electrolyte imbalance can tacrolimus cause?

A

hyperkalaemia

increased glucose + urea

41
Q

What are the 5 monitoring parameters done for tacrolimus?

A

BP and ECG - for hypertrophic changes

Fasting blood glucose

Renal and hepatic function - electrolytes, plasma protein

42
Q

What syndrome to monitor in tacrolimus?

A

posterior reversible encephalopathy syndrome (PRES)

43
Q

What is a MHRA warning related to tacrolimus?

A

prescribe by brand name only, to reduce the risk of inadvertent switching

can cause toxicity + graft rejection.

44
Q

How is therapeutic drug monitoring done for tacrolimus?

A

After initial dosing, +for maintenance treatment, tacrolimus doses should be adjusted based on tacrolimus trough concentration.

45
Q

Can tacrolimus be used in pregnancy?

A

avoid unless benefit outweighs potential risk

46
Q

Why is tacrolimus avoided in pregnancy?

A

crosses the placenta +risk of premature delivery, intra-uterine growth restriction, hyperkalaemia +renal toxicity.

47
Q

What are the 4 maternal risk of using tacrolimus during pregnancy?

A

Maternal risk of hyperglycaemia,
hypertension
pre-eclampsia
renal impairment

48
Q

What is 2 key patient counselling pointS for tacrolimus?

A

Avoid excess UV sun light - wear SPF sunscreen.

Report symptoms of eye problems.

49
Q

What is the 2 tacrolimus brands that are MR capsules which are taken OM?

A

Advagraf and Dailiport

50
Q

What type of drugs can interact with tacrolimus to increase toxicity?

A

Enzyme inhibitors - Amiodarone, azoles, macrolides, rate limiting CCBs.

51
Q

What 3 drinks should a patient avoid when taking tacrolimus as it increases toxicity?

A

Pomelo, pomegranate + grapefruit juice

52
Q

What 4 drugs reduce tacrolimus concentration? (CP2R)

A

Carbamazepine

Phenobarbital

phenytoin

rifampicin

53
Q

What 6 drugs can interact with tacrolimus to increase nephrotoxicity?

A

Aminoglycosides, cephalosporin, ciclosporin, glycopeptides, methotrexate, NSAIDs

54
Q

What 6 drugs can interact with tacrolimus and cause hyperkalaemia?

A

ACEi/ARB

Aldosterone antagonist

K sparing diuretic

NSAID

Trimethoprim

Heparin

55
Q

What is ciclosporin MOA?

A

Blocks calcineurin which activates T cells.

56
Q

What are 4 SEs of ciclosporin?

A

Blood disorders

HypErkalaemia - increased glucose, urea, lipids, BP (reduced Mg).

Gingival hyperplasia

Nephrotoxicity

57
Q

What are 3 of the electrolyte balances that are caused by ciclosporin?

A

hypErkalaemia

Higher glucose, urea, BP, lipids

Low Mg

58
Q

What 5 Monitoring parameters for ciclosporin?

A

Electrolytes- K, BP, lipids + RFT, LFT

59
Q

What is an MHRA warning linked to ciclosporin?

A

for oral ciclosporin - prescribe + dispense by brand.

60
Q

What drug class would patient be hypersensitive to if they were contra-indicated to tacrolimus?

A

Macrolides

Tacrolimus- also a macrolide abx.

61
Q

What 4 drugs/classes can interact with tacrolimus + increase toxicity?

A

Amiodarone, Azoles, Macrolides, Rate limiting CCBs.

62
Q

What 4 drugs reduce ciclosporin levels?

A

Carbamazepine, phenobarbital, phenytoin, rifampicin

63
Q

What is 2 key counselling points for ciclosporin?

A

Avoid pomelo, grapefruit juice + purple grape juice.

Avoid excessive exposure to UV light,
In psoriasis + atopic dermatitis, avoid use of UVB or PUVA.

64
Q

What 3 fruits to avoid when taking ciclosporin?

A

Pomelo

grapefruit juice

purple grape juice

65
Q

What 6 drugs can interact with ciclosporin to cause nephrotoxicity?

A

Aminoglycoside

Cephalosporin

Ciclosporin

Glycopeptides

Methotrexate

NSAIDS

66
Q

What 6 drugs/classes can interact with ciclosporin and cause hypErkalaemia?

A

ACEi/ARB, aldosterone antagonist, K-sparing diuretics, NSAIDs, Trimethoprim, Heparin

67
Q

What 2 juices increase ciclosporin levels?

A

Pomelo

Grapefruit juice

68
Q

What juice decreases ciclosporin levels?

A

Purple grape juice

69
Q

can you drive if you take ciclosporin?

A

Yes - can increase risk of blurred vision when using via eye.

70
Q

What are some monitoring parameters for ciclosporin?

A

whole blood ciclosporin concentration- trough level dependent on indication.

71
Q

In long term management of nephrotic syndrome, what is monitored?

A

Regular eye examinations if using for >12 months.

72
Q

What point to tell patient taking ciclosporin via eye?

A

Keep eyes closed for 2 minutes after using eye drops to increase local drug action + reduce systemic absorption.

73
Q

How to take ciclosporin orally?

A

Mix solution with orange or apple juice, or other soft drink (to improve taste) immediately before taking (and rinse with more to ensure total dose).

Do NOT mix with grapefruit juice.

Total daily dose should be taken in 2 divided doses.

74
Q

What to do to ciclosporin dose if patient also taking octreotide?

A

increase dose by 50% or switch to IV administration with concurrent use of octreotide.

75
Q

What 3 condition is ciclosporin unlicensed in?

A

Children under 3 months

Children under 16 years for atopic eczema or psoriasis

Ulcerative colitis

PRE-REG-Thuri (44 decks)

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