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CPT > Immunosuppressants > Flashcards

Immunosuppressants Flashcards

1
Q

What are some examples of immunosuppressants?

A 
Corticosteroids 
Methotrexate 
Azathioprine 
Ciclosporin
Tacrolimus 
Cyclophosphamide
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2
Q

What is the method of action for corticosteroids?

A

Prevent IL-1 and IL-6 production by macrophages
Inhibit all stages of T cell activation

Not targeted, so produce many side effects

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3
Q

What is azathioprine used for?

A

SLE and vasculitis maintenance therapy

IBD

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4
Q

Describe the pharmacodynamics of azathioprine

A

6-MP is metabolised by TPMT
TPMT gene is highly polymorphic

Low/absent TPMT => risk of myelosupression

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5
Q

What is the mechanism of action of azathioprine?

A

Cleaved to 6-MP which decreases DNA and RNA synthesis

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6
Q

What are some adverse effects of azathioprine?

A

Bone marrow suppression - need to monitor FBC
Inc risk of malignancy - esp in transplant pts
Inc risk of infection
Hepatitis - monitor LFTs

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7
Q

What are some examples of calcineurin inhibitors?

A

Ciclosporin

Tacrolimus

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8
Q

What are calcineurin inhibitors used for?

A

Transplantation
Atopic dermatitis
Psoriasis

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9
Q

What are some adverse effects of calcineurin inhibitors?

A

Renal toxicity - check BP and eGFR

Inhibits cytochrome P-450

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10
Q

What is the mechanism of action of calcineurin inhibitors?

A

Active against helper T cells => prevent IL-2 production
Drug-protein complexes bind to calcineurin

Ciclosporin - binds to cyclophilin protein
Tacrolimus - binds to tacrolimus binding protein

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11
Q

What is mycophenolate mofetil used for in practice?

A

Primarily in transplantation

Also good for induction and maintenance therapy in lupus nephritis/vasculitis

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12
Q

What is the mechanism of action of mycophenolate mofetil?

A

Inhibits inosine monophosphate dehydrogenase => reduced guanosine synthesis

Impairs B and T cell proliferation
Spares other rapidly dividing cells

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13
Q

What are some adverse effects of mycophenolate mofetil?

A

Nausea, vomiting and diarrhoea

Myelosuppression

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14
Q

What is the method of action of cyclophosphamide?

A

Alkylating agent - cross links DNA
Unable to replicate

Suppress T and B cell activity

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15
Q

What are some indications for cyclophosphamide?

A

Lymphoma, leukaemia
Lupus nephritis
Wegener’s granulomatosis; ANCA-vasculitis

Lower dose used for non-cancer

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16
Q

Describe pharmacodynamics of cyclophosphamide

A

Converted in liver - CYP P450

17
Q

Describe pharmacokinetics of cyclophosphamide

A

Excretion - kidney

Produces a metabolite which is toxic to the bladder => haemorrhagic cystitis

18
Q

What are some important considerations for cyclophosphamide?

A

Significant toxicity =>
Inc risk of bladder cancer, lymphoma and leukaemia
Risk of infertility
Adjust dose with renal impairment

19
Q

What are some indications for methotrexate use?

A

Good standard treatment for RA

Malignancy
Psoriasis
Crohn’s disease

20
Q

What is the mechanism of action of methotrexate?

A

Reversible competitive inhibition of dihydrofolate reductase
Therefore inhibits purine and thymidine synthesis
Inhibition of DNA, RNA and protein synthesis

21
Q

What is the mechanism of action of methotrexate for non-malignant disease?

A

Not really clear

Not through anti-folate action

Possibly:
Inhibits accumulation of adenosine
Inhibits T cell activation
Suppresses expression of intracellular adhesion molecules

22
Q

Describe pharmacokinetics of methotrexate

A

Oral bioavailability 33%

Long half life therefore weekly dosing

Renal excretion

23
Q

How is methotrexate used in practice?

A

Well tolerated
Improved QoL
Retardation of joint damage

24
Q

What are some adverse effects of methotrexate?

A 
Mucositis 
Marrow suppression 
Hepatitis and cirrhosis 
Pneumonitis 
Inc risk of infection

Highly teratogenic, can cause abortion

25
Q

What is the mechanism of action go sulphasalazine?

A

Relieves pain and stiffness

Fight infection

26
Q

What are the immunological effects of sulphasalazine?

A

T cells:
Inhibit proliferation
Apoptosis
Inhibit IL-2 production

Neutrophils:
Reduced chemotaxis
Reduced degranulation

27
Q

What are some adverse effects of sulphasalazine?

A

Myelosuppression
Hepatitis
Rash

Nausea and vomiting
Abdo pain

28
Q

How is sulphasalazine used in practice?

A

Effective
V few drug interactions
No carcinogenic potential
Safe in pregnancy

29
Q

How are immunosuppressant “biologicals” produced?

A

Extracted from living systems eg whole blood, blood components, stem cell therapy

Recombinant DNA technology produces substances that are nearly identical to key signalling proteins eg growth hormone, EPO

Monoclonal antibodies block substances in the body or target a specific cell type

30
Q

What are the effects of blocking TNF-α?

A

Decreased inflammation
Decreased angiogenesis
Decreased joint destruction

31
Q

What are some risks of blocking TNF-α activity?

A

TB reactivation

TNF-α released by macrophages in response to TB infection
Essential for development and maintenance of a granuloma

Therefore need to screen for latent TB before anti-TNF treatment

32
Q

What is the mechanism of action of rituximab?

A

Immunosuppressant

Binds to specific cell-surface markers on B cells
Causes B cell apoptosis

V effective in RA

CPT (21 decks)

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