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Medicine > Locomotor RA drugs > Flashcards

Locomotor RA drugs Flashcards

1
Q

Methotrexate MoA

A

DMARD
Folate Acid Antagonist
• Enters cell -> polyglutamated.
• Prevents proliferation during cell mitosis by inhibiting dihydrofolate reductase (purine metabolism) and prevents DNA/RNA metabolism by inhibiting thymidylate synthase.
• Stops production of pro-inflammatory cytokines and of any additional fibroblasts.
• Prevents binding of IL1b to surface of cells.

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2
Q

Methotrexate Side Effects

A

Due to indiscriminate to dividing cells:
• Can cause liver problems
• Can affect blood count.

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3
Q

Methotrexate Administration

A
  1. Oral
  2. Subcutaneous/intramuscular

Loading dose: 50mg a week
Maintenance dose: 2.5mg tablet.

(!) 3-12 weeks before benefit seen.

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4
Q

Sulfasalazine MoA

A 
DMARD
Old sulfur antibiotic
•	Moa not well understood.
•	Not well absorbed across gut. 
	~ 15% of parent drug. 
	Converted to 5-ASA
•	5-ASA: treats UC and relieves arthritis symptoms (believes to have some sort of role in the gut).

Normally cells in the gut produce IL-6, IL-17 and TNFa, that get can into the blood stream and lead to inflammation
• Modulating immune system in gut: modulates distant sites of cytokine travel.

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5
Q

Sulfasalazine Administration

A

Start 500mg daily, then gradually increase over 4 weeks to 1g twice a day.

(!) 12 weeks before benefit seen.

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6
Q

Hydrochloroquine MoA

A

Anti-Malarial
• MoA not well understood.
• Accumulates in lysosomes: increases pH, which decreases protein modification.
o Cytokines often secreted with precursors that need to be modified.
• Block TLR9: recognises DNA containing immune complexes  decreases activation of dendritic cells.

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7
Q

Hydrochloroquine Side Effects

A

Can get a rash from taking it.

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8
Q

Hydrochloroquine Administration

A

Start 400mg daily

Reduced to 2-3 times a week.

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9
Q

Leflunomide MoA

A

DMARD
• Moa not well understood
• Inhibits DNA and RNA synthesis though a different pathways vs methotrexate.
• Inhibits pyrimidine synthesis.

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10
Q

Leflunomide Administration

A

10-20mg a day (1st 3 days higher dose than 100mg a day).

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11
Q

Gold Salts MoA

A

DMARD
• Moa not well understood
People experience very different effects.

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12
Q

Gold Salts Administration

A

Intramuscular injections

10-20mg a day.

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13
Q

Etanercept MoA

A

TNF Alpha Blocker
Fusion protein between TNF receptor 2 and FC human IgG1
• Extracellular receptor stuck to human FC.
• Finds free TNFa alpha in the system.

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14
Q

Etanercept Administration

A

Subcutaneous injection
50mg once per week.

(!) 1-4 week for effect.
Progressive improvement over 3-6m.

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15
Q

Infliximab MoA

A

TNF Alpha Blocker
Monoclonal antibody vs TNF alpha.
• Design against mouse binding site of TNFa. .
• Remains 75% human IgG.

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16
Q

Adalimumab MoA

A

TNF Alpha Blocker
Human TNF alpha monoclonal antibody
• Binds to TNFa both soluble and bound.

17
Q

Adalimumab Administration

A

Subcutaneous injection
100mg once a week

(!) 2-4 weeks for effect.

18
Q

Anankinra MoA

A

IL-1 Blocker
Human recombinant IL-1 receptor antagonist.
• Different from normal IL-1 by addition of methionine to the N-terminal.

19
Q

Canakinumab MoA

A

IL-1 Blocker
Human monoclonal antibody IL-1 beta.
• Approved for some rare autoimmune syndromes
• Trials for COPD and gout

20
Q

Rinalocept MoA

A

IL-1 Blocker
Dimeric fusion protein extracellular domain of IL1R1 and Fc human IgG
• Used more for acute gout.

21
Q

Rituximab MoA

A

B-Cell Blocker
(For patients who fail to respond to one or more anti-TNF alpha agents).
• Chimeric monoclonal antibody against CD20 primarily found on surface of B-cells.
Destroys both normal and malignant B-cells
• In combination with methotrexate

22
Q

Rituximab Administration

A

• Single course of 2 infusions of 1000mg given 2 weeks apart  Depletes B-cells for up to 6 months and possibly 1 year
(!) Effects seen around 3 months after infusions

23
Q

Abatacept MoA

A

T-Cell Blocker
Fusion protein IgG fused to extracellular domain of CTLA-4.
• Activating negative switch of signal (CTLA-4)  stops T-cell.

 similar reports of clinical symptom improvement compared to TNF alpha but radiological results are not as good.

Advantage: slower onset for TNF alpha inhibits
Disadvantage: fewer adverse events.

24
Q

> Abatacept Administration

A
  • i.v. infusion over 30mins to 1hr once a month
  • Dosage dependent on body weight.

(!) Response around 3 months

25
Q

Betalacept MoA

A

T-Cell Blocker

anti-C2D28, modulate T-cell signalling

26
Q

Tocilizumab MoA

A

IL-6

Humanized monoclonal antibody against IL-6 receptor

27
Q

Tocilizumab Administration

A

i.v. infusion (8mg/kg monthly)

In combination with methotrexate.

Medicine (6 decks)

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