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Pharmacology > Immunosuppressants > Flashcards

Immunosuppressants Flashcards

1
Q

How do Corticosteroids work?

A

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

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2
Q

What side effects are associated with corticosteroids?

A

Cataracts, thrush, hair loss, muscle weakness, think skin, cushings

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3
Q

What is the mechanism of action for Azathioprine?

A

An anti-metabolite

It decreases DNA and RNA synthesis

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4
Q

What adverse effects are associated with Azathioprine?

A

Bone marrow suppression
Increased risk of malignancy
Increased risk of infection

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5
Q

What enzyme metabolises 6 mercaptopurine?

A

TPMT

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6
Q

Name the Calcineurin inhibitors you have studied

A

Ciclosporin

Tacrolimus

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7
Q

What is the mechanism of action for calcineurin inhibitors?

A

They are active against helper T cells, preventing production of IL-2 via calcineurin inhibitors

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8
Q

What is the role of calcineurin regarding T cells?

A

Calcineurin exerts phosphatase activity of activated T cells then nuclear factor migration starts IL-2 transcription

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9
Q

What does ciclosporin bind to?

A

Cyclophilin protein

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10
Q

What side effects are associated with calcineurin inhibitors?

A

Gum hypertrophy
Renal toxicity
BP and EGFR checks required regularly

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11
Q

What is the mechanism of action of Mycophenolate Mofetil?

A

A pro drug that inhibits monophosphate dehydrogenase which is required for guanosine synthesis
Thus impairing B and T cells proliferation

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12
Q

Mycophenolate mofetil inhibits what enzyme?

A

Inosine monophasphate dehydrogenase

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13
Q

Mycophenolate mofetil impairs the production of what cells?

A

B and T cells

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14
Q

What are the most common side effects of Mycophenolate mofetil?

A 
Nausea 
Vomiting
Diarrhoea
Myelosuppression
Mouth ulcers
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15
Q

What is the mechanism of action for cyclophosphamide?

A

Cytotoxic agent
Alkylating
Cross links DNA so it cant replicate
Suppresses B and T cell activity

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16
Q

What is the main active metabolite of cyclophosphamide?

A

4-hydroxycyclophosphamide

17
Q

How is cyclophosphamide excreted?

A

By the kidney

18
Q

What metabolite of cyclophosphamide is toxic to the bladder epithelium and can lead to haemorrhagic cystitis?

A

Acrolein

19
Q

What is the antidote for Acrolein?

A

Mesna

And use aggressive hydration

20
Q

What drug is the gold standard for RA?

A

Methotrexate

21
Q

What enzyme does Methotrexate inhibit?

A

Dihydrofolate reductase

22
Q

Methotrexate works best during what phase of the cell cycle?

A

S phase

23
Q

Which immunosuppressive can be used as an abortifactant?

A

Methotrexate

24
Q

What is the key carrier of 1 carbon subunits in purine and thymidine synthesis?

A

Tetrahydrofolate

25
Q

What are the side effects of methotrexate that respond to folic acid supplementation?

A

Mucositis

Marrow suppression

26
Q

Describe the dosing of methotrexate

A

Weekly

27
Q

What drugs displace methotrexate when it is protein bound?

A

NSAIDs

28
Q

What is the effect of Sulfasalazine on T cells?

A

Inhibition of proliferation
Possible T cell apoptosis
Inhibition of IL-2

29
Q

What is he effect of sulfasalazine on neutrophils?

A

Reduced chemotaxis

Reduced degranulation

30
Q

Where do biopharmaceuticals come from?

A

From living systems:
Whole blood
Blood components
Stem cell therapy

31
Q

What are the effects of blocking TNF-a using biologicals?

A

Decreased inflammation
Decreased angiogenesis
Decreased joint destruction

32
Q

What is a major risk of Anti-TNF-a therapy?

A

TB reactivation
This is because TNF-a is released by macrophages in response to M.Tb.
TNF-a is essential for development and maintenance of granulomata.

33
Q

What does Rituximab bind to?

A

CD20 on B cells

Causes B cell apoptosis

Pharmacology (11 decks)

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