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Flashcards in Drugs Deck (13)
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1
Q

What is the mechanism of action of methotrexate?

A

Inhibits dihydrofolate reductase enzyme which usually converts dihyrdofolate to tetrahydrofolate therefore continuously replenishing the cells supply of folates

2
Q

Metabolism of methotrexate?

A

90% excreted unchanged by the kidneys

small and insignficant amount recycled in the bile

3
Q

Main ADRs of MTX?

A

GI - nausea, vomiting, mouth ulcers
macrocytosis, bone marrow suppression dose limiting effect
hypersensitivity pneumonitis
hepatotoxicity - raised inflammatory markers
fever
fatigue, headache
alopecia, rash

4
Q

Mechanism of action of leflunomide?

A

inhibits pyrimidine synthesis

prevents active cells from moving from G1 to S phase

5
Q

ADRs of leflunomide?

A

Most similar to MTX
*most significant is diarrhoea
in combination with MTX leads to increased pneumonitis, peripheral neuropathy, immune suppression and increased rates of liver impairment

6
Q

Treatment for leflunomide toxicity?

A

Cholestyramine washout

7
Q

Mechanism of hydroxychloroquine?

A

blocks TLR pathways of innate immune system preventing innate immune activation

8
Q

Side effects of hydroxychloroquine?

A

ocular toxicity - corneal depositis and retinopathy, require monitoring
skin changes
GI upset

9
Q

Hydroxychloroquine in pregnancy?

A

limited data but does reduce amount of congenital heart block in those with Ro/La antibodies
If stopped before conception - high rates of disease flares

10
Q

Examples of TNF inhibitors?

A

Entanercept - receptor fusion protein
Infliximab - chimeric monoclonal antibody against TNF
Adalimumab - humainsed monoclonal
Golimumab
Certolizumab - fab fragment of humanised monoclonal antibody

11
Q

Examples of IL-1 drugs?

A

Anakinra

12
Q

Example of IL-6 drugs?

A

Tocilizumab

13
Q

CTLA-4 fusion protein?

A

Abatacept