Rheumatoid arthritis drugs Flashcards

1
Q

What are NSAIDS used for in RA

A

The NSAIDS provide symptomatic relief of pain and stiffness, but do not alter disease progression

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2
Q

What is the mechanism of action of NSAIDs

A

block eicosanoid synthesis by inhibiting COX-1 and COX-2

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3
Q

What do DMARDs do in RA

A

They reduce the rate of disease progression by preventing erosive damage

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4
Q

What is the general mechanism of the DMARDs

A

The mechanism of action is unclear, although long-term depression of the inflammatory response must be implicated, although they appear to have little direct anti-inflammatory activity

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5
Q

What is the mechanism of action of the DMARD Sulphasalazine

A
  • It is hydrolyzed by gut bacteria to sulphapyridine and 5-aminosalicylic acid
  • Sulphapyridine reduces the absorption of antigens from the colon that may promote joint inflammation
  • 5-aminosalicylic acid reduces the synthesis of inflammatory mediators e.g. ecosanoids and cytokines
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6
Q

What is the onset of action time for Sulphasalazine

A

1-3 months

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7
Q

What are the side effects of Sulphasalazine

A
  • Myelosupression
  • GI upset
  • Revesible decrease in sperm count
  • Reduction in WBC count
  • Anaphylaxis
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8
Q

What is the mechanism of action of the DMARD Gold

A
  • Inhibit lymphocyte proliferation
  • Inhibit release and activity of lysosomal enzymes released which decreases the amount of joint damage
  • Decrease production of toxic O2 metabolites from phagocytes
  • Inhibit chemotaxis of neutrophils
  • Inhibit induction of IL-1 and TNF-alpha
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9
Q

What is the onset of action time for Gold

A

3-6 months

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10
Q

What are the side effects of Gold

A
  • Myelosupression
  • Proteinuria
  • Agranuloctosis
  • Aplastic anaemia
  • Skin rashes
  • Diarrhoea
  • Glomerulonephritis
  • Serious toxic effect in 10% of patients
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11
Q

What is the mechanism of action of the DMARD Methotrexate

A
  • Inhibition of enzymes involved in purine metabolism so:
  • Inhibit accumulation of adenosine
  • Inhibition of T-cell activation
  • Suppression of adhesion molecule expression by T-cells
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12
Q

What is the onset of action time for Methotrexate

A

1-2 months

most rapid

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13
Q

What are the side effects of Methotrexate

A
  • Myelosupression
  • Hepatic fibrosis
  • Cirrhosis
  • Pulmonary infiltrates
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14
Q

What is the onset of action time for Hydroxychloquine

A

2-6 months

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15
Q

What are the side effects of Hydroxychloquine

A

Macular damage

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16
Q

What is the onset of action time for Lefunomide

A

1-3 months

17
Q

What are the side effects of Lefunomide

A
  • Diarrhoea
  • Alopecia
  • Rash
  • Headache
  • Risk of immunosupression infection
18
Q

What is the onset of action time for Cyclosporine

A

1-2 months

19
Q

What are the side effects of Cyclosporine

A
  • Renal insufficiency
  • Anaemia
  • Hypertension
20
Q

What is the onset of action time for Azathioprine

A

2-3 months

21
Q

What are the side effects of Azathioprine

A
  • Myelosupression
  • Hepatotoxicity
  • Lymphoproliferative disorders
22
Q

What is the onset of action time for Minocycline

A

1-3 months

23
Q

What are the side effects of Minocycline

A
  • Hyperpigmentation
  • Dizziness
  • Vaginal yeast infections
24
Q

How are corticosteroids used in RA and how are they given

A
  • Used in combo with NSAIDs and DMARDs

* Inta-articular injections of individual joints e.g knee

25
Q

what is the mechanism of action of corticosteroids

A
  • Immunosuppressant, acts on cell-mediated (B-cell, T-cell and macrophage) immune responses
  • Decrease transcription of pro-inflammatory genes e.g. IL-2, TNF-alpha, Interferon-gamma, chemokines
  • Suppresses phospholipase A2 and thus block eicosanoid production
  • Glucocorticoid induced granulocytosis/ neutrophilia
26
Q

When are biologics used to treat RA

A

they are very expensive so:

•when patients have failed 2 standard DMARDs one of which will have been Methotrexate for at least 6 months

27
Q

What are the side effects of the biologics

A
  • Nausea
  • Low grade fever
  • Anorexia
28
Q

What are the Contraindications for biologics

A
  • Pregnancy or breastfeeding
  • Chronic leg ulcers
  • Previous TB
  • Septic arthritis
  • Sepsis of joint prosthetic
  • Persistent chest infections
  • Indwelling urinary catheter
  • MS
  • Malignancy
29
Q

What exactly are biologics?

A

monoclonal antibodies that mainly target TNF-alpha

30
Q

Give some examples of biologics

A
Etanercept
Infliximab 
Adalimumab
Anakinra 
Abatacept 
Rituximab
31
Q

What is the target of Etanercept

A

TNF-alpha

32
Q

What is the target of Infliximab

A

TNF-alpha

33
Q

What is the target of Adalimumab

A

TNF-alpha

34
Q

What is the target of Anakinra

A

Type 1 IL-1R

35
Q

What is the target of Abatacept

A

CD80/86

36
Q

What is the target of Rituximab

A

CD20