Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Orthopaedics > Immunosuppressants and Biologics > Flashcards

Immunosuppressants and Biologics Flashcards

1
Q

What are the indications for immunosuppressant use?

A 
After/before transplant to reduce risk of rejection
Autoimmune diseases
- RA
- psoriasis/psoriatic arthritis
- lupus
- autoimmune haemolytic anaemia
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Name some classes of immunosuppressants.

A

Glucocorticoids (steroids)
Anti-metabolic agents
Calcineurin inhibitors
Biologic therapy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is azathioprine?

A

An antimetabolite (purine synthesis inhibitor and purine analgoue)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What is azathioprine mostly used in?

A

Transplant

Vasculitis - inflammation of blood vessels (can kill you - irreversible in the lungs and kidneys)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Describe the mechanism of action of azathioprine.

A 
Purine synthesis inhibitor blocks an important enzyme in purine production
Purine analogue (TGTP)  is incorporated into the DNA
- causes chain termination and cytotoxicity
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What are the side affects and risks of Azathioprine?

A

Side effects
Lecucopenia - not therapeutic like some drugs (this indicates the dose is too high and they are at risk of infection)
A lot of the drugs are hepatotoxic
Risks
Allopurinol - inhibits XO which forces active azathioprine down an over productive pathway (dangerously low WCC)
Sun exposure - transplant patients have higher risks of melanoma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is mycophenolate mofetil?

A

Inhibits purine biosynthesis - inosine monophasphate dehydrogenase
Less nephrotoxic and bone marrow toxic than azathioprine (more commonly used)
Can cause GI toxicity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

When is mycophenolate mofetil used?

A

For transplant and vasculitis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Describe the mechanism of action of mycophenolate mofetil.

A

In lymphocytes, the de novo synthesis of purines is less active
The drug is an inhibitor of inosine monophosphate dehydrogenase
B and T cells therefore can’t proliferate as they can’t acquire the appropriate DNA within the lympocyte

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What is the mechanism of action of Methotrexate?

A

Inhibits the action of the enzyme dihydrofolate reducatase (DHFR)
- can’t make or use folic acid, which is needed for synthesis of thymidine, meaning that DNA synthesis is impaired
- also inhibits GART and AlCARTF
- targets T-cell activation by an accumulation of adenosine
Methotrexate is brought into a cell by transporters, where it is polygutamated (attaching a large insoluble molecule to the soluble methotrexate to keep it in the cell)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What is methotrexate?

A

An anti-metabolite of the antifolate type

  • inhibits synthesis of DNA
  • inhibition of T cell activation and suppression of intracellular adhesion molecule expression produced by T cells
  • selective down regulation of B cells
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What are the side effects of methotrexate?

A 
GI - nausea and vomiting 
Leucopenia 
Thrombocytopenia 
Liver (enzyme and cirrhosis)
Pulmonary fibrosis - RA carries risk of interstitial lung disease anyway 
Pneumonitis
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What is ciclosporin used for?

A

Transplants
Psoriasis
RA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Describe the mechanism of action of ciclosporin.

A

Binds to ciclophillin and forms a complex that inhibits calcineurin

  • calcineurin then dephosphorylates nuclear factor of activation of T cells (NFATC)
  • this goes into the cell nucleus and increases IL-2 expression (a regulator of T-cell proliferation)
  • leads to T-cell cytokine expression
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What are the complications of using ciclosporin?

A

Drug interactions (increases or decrease ciclosporin levels within the body)
Hypertension
Tremor
Hisutism
Preparation brand - each brand is slightly different and giving a patient a different one can affect bioavailability of the drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Which drugs interact with ciclosporin?

A 
Increase blood ciclosporin levels
- calcium channel blockers
- grapefruit juice
- antibiotics 
- anti-fungal agents
Decrease blood ciclosporin levels
- anticonvulsants
- ant-TB agents
- St John's wart
17
Q

What biologic therapies are there?

A 
Cytokine targeting (anti-TNF)
Anti-cellular (rituximab) 
Receptor targeting (herceptin)
Endogenous product (interferon alpha)
18
Q

What is the mechanism of action of an anti-TNF agent?

A

Blocks TNF-alpha and beta interactions with TNF cell receptors

  • stops cell entry into inflammatory environment
  • prevents signalling to continue the inflammatory response
19
Q

What are the side effects and risks of anti-TNF agents?

A 
Cancer
Chronic infection
Severe heart failure
TB - reactivation 
- granuloma formation relies on the ability of the body to produce TNF alpha. These drugs could breakdown the structure of the granuloma, and reactive the infection 
Live vaccines 
Demyelination
20
Q

What are the recommended screening for biologic therapies?

A

TNF inhibition - congestive heart failure, TB, viral hepatitis and any neurodegenerative conditions.
Anakinra (IL-1 receptor antagonist) - FBC and lung disease
Abatacept (modified antibody) - TB
Rituximab (monoclonal antibody) - Ig levels and viral hepatitis
Toclizumab (monoclonal antibody) - FBC, diverticulitis, LFTs, TB, viral hepatitis and any neurodegenerative conditions

21
Q

Name some anti-TNF agents.

A

Infliximab
Etanercept
Adalimumab

22
Q

What is the mechanism of action of Rituximab?

A

Anti-B cell therapy

  • targets CD20 found on B cells and pre-B cells (but not plasma cells)
  • induces B-cell apoptosis
23
Q

What are the side effects and risks of Rituximab?

A

Infusion reaction - chimaeric
Possible viral reactivation
Progressive multifocal leukoencephalopathy
- inflammation of white matter of the brain following reaction of the JC virus
- can be seen in immunocompromised people or AIDS

24
Q

What is the most important signalling molecule in RA and giant cell arthritis?

A

IL6 - blockade of this is the most effective treatment (toclizumab and sarilumab)

25
Q

In psoriasis and psoriatic arthritis, what is the most important signalling molecule?

A

IL- 12/23 and IL-17 - treated with ustekinumab and briakinumab.

26
Q

Which drugs blockade IL-1 (JIA and gout treatment)?

A

Anakinra
Canakinumab
Rilonacept

27
Q

Name some kinase inhibitors.

A

Sorafenib
Dasatinib
Eroltinib
Tofactinib

Orthopaedics (13 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions