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MSK > OA/RA Drugs > Flashcards

OA/RA Drugs Flashcards

This deck tests your knowledge of osteoarthritis / rheumatoid arthritis drugs.

1
Q

What anti-inflammatory drugs can be used to treat OA/RA?

A
  1. NSAIDs (diclofenac, eterocoxib, paracetamol)
  2. Corticosteroids (hydrocortisone)
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2
Q

What do anti-inflammatory drugs do for OA/RA?

A

They provide symptomatic relief of inflammatory symptoms

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3
Q

What is polysaccharide SYSADOA?

A

Systematic, slow-acting drugs for OA
(intra-articular hyaluronic acid)

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4
Q

What is intra-articular hyaluronic acid?

A
  • GAG, naturally found in the synovial fluid
  • Plays a role in cartilage health and protection, shock absorption / energy dissipation, and lubrication
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5
Q

How does intra-articular hyaluronic acid work?

A
  1. Anti-inflammatory
  2. Replenishes HA
  3. Reduces chondrocyte cell death and damage
  4. Raw material for biosynthesis of cartilage
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6
Q

What are the major adverse effects of intra-articular hyaluronic acid?

A

Only minor allergic reactions

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7
Q

What are DMARDs?

A
  • Disease-modifying anti-rheumatic drugs
  • Classified as cs (conventional synthetic), ts (targeted synthetic), and b (biologic)
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8
Q

What are the csDMARDs?

A

MS LeeCH
Methotrexate, Sulfasalazine, Leflunomide, Chloroquine, Hydroxychloroquine

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9
Q

What is the only tsDMARD?

A

Tofacitinib

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10
Q

What are the bDMARDs?

A

AATARi
Anti-TNF mABs, Anakinra, Tocilizumab, Abatacept, Rituximab

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11
Q

What is methotrexate?

A

Folic acid analog; firstline DMARD

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12
Q

What three things does methotrexate inhibit?

A
  1. Inhibits AICAR transformylase
  2. Inhibits dihydrofolate reductase (DHFR)
  3. Inhibits thymidylate synthesis
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13
Q

How does methotrexate inhibiting AICAR transformylase work?

A
  • Inhibiting AICAR transformylase leads to adenosine accumulation
  • Adenosine binds to adenosine receptors, which exert anti-inflammatory effects like (a) inhibiting inflammatory cytokine production (IL-1, IL-6, TNF), (b) inhibiting activation and function of immune cells, (c) inhibiting cell apoptosis and chemotaxis
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14
Q

How does methotrexate inhibiting DHFR work?

A
  • DHFR produces tetrahydrofolate, which is necessary for the production of purines and thymidylate
  • Without these, DNA replication and repair in rapidly-dividing immune cells is inhibited
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15
Q

How does methotrexate inhibiting thymidylate synthesis work?

A
  • Thymidylate is needed for pyrimidine synthesis
  • Without this, DNA replication and repair in rapidly-dividing immune cells is inhibited
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16
Q

How can you increase the efficacy of methotrexate?

A

Polyglutamate it, so it is retained for longer in immune / liver cells

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17
Q

How is methotrexate cleared?

A

Hepatic metabolism > Renal excretion

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18
Q

What are the six adverse effects of methotrexate?

A
  1. nausea / vomiting
  2. oral / GI ulcers
  3. immunosuppression
  4. bone marrow suppression
  5. hepatorenal toxicity
  6. pneumonitis (HS)
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19
Q

How do you prevent methotrexate toxicity?

A
  • Concomitant folic acid OR folinic acid 12-24h later
  • Folinic acid is more effective as it does not rely on DHFR function
  • Folic acid is cheaper
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20
Q

What is sulfasalazine?

A

It is a prodrug, which is converted by gut microflora into sulfapyridine and 5-aminosalicylic acid

21
Q

What do sulfapyridine and 5-ASA do?

A
  • Sulfapyridine inhibits production of inflammatory cytokines (e.g. IL-6, TNF)
  • 5-ASA inhibits production and function of inflammatory mediators (e.g. leukotrienes, prostaglandins)
22
Q

What are the five adverse effects of sulfasalazine?

A
  1. Nausea / Vomiting
  2. Headache
  3. Sulfa allergy skin rash
  4. Haemolytic anaemia and neutropenia
  5. Reversible male infertility (sulfapyridine)
23
Q

What is leflunomide?

A

Prodrug, converted to active metabolite teriflunomide

24
Q

What does teriflunomide do?

A
  1. Inhibits DHODH, which synthesises pyrimidines
  2. Inhibits NF-kB pathway, which helps lymphocytes activate/survive + produces inflammatory cytokines
25
Q

What are the five adverse effects of leflunomide?

A
  1. Diarrhoea
  2. Elevated liver enzymes
  3. Weight gain
  4. Teratogen (perform colestyramine washout before pregnancy)
  5. Alopecia
26
Q

What is unique about leflunomide’s half-life?

A

Very long

27
Q

How is leflunomide cleared?

A

Hepatic metabolism + biliary excretion

28
Q

What is chloroquine/hydroxychloroquine?

A

Anti-malarial agent, which is also anti-inflammatory

29
Q

What does chloroquine/hydroxychloroquine do?

A
  1. Antioxidant activity
  2. Inhibits production of inflammatory cytokines
  3. Increases lysosome pH, thus decreasing antigen presentation
30
Q

Is chloroquine/hydroxychloroquine a good DMARD?

A

No, least potent

31
Q

What are the five adverse effects of chloroquine/hydroxychloroquine?

A
  1. Nausea/Vomiting
  2. Stomach pain
  3. Dizziness
  4. Ocular toxicity with chronic use
  5. Alopecia
32
Q

What is tofacitinib?

A

A Jakinib, which is a non-selective Janus kinase inhibitor

33
Q

Is tofacitinib effective?

A

Yes, best used with methotrexate / other csDMARDs, but not bMARDS

34
Q

What does tofacitinib do?

A
  • Inhibits JAK-STAT cell signalling pathway (by inhibiting JAKs, especially 1/3)
  • Disrupts almost all immune cell processes, esp. lymphocyte differentiation and function
35
Q

What are the five adverse effects of tofacitinib?

A
  1. Immunosuppression (can cause opportunistic herpes zoster infection in Asians)
  2. Anaemia (erythropoietin and thrombopoietin rely on JAKs)
  3. Cytopenia
  4. Risk of malignancies (anti-cancer effects of JAK inhibited, e.g. NK activation)
  5. Hyperlipidemia (due to lack of chronic inflammation)
36
Q

What are the four anti-TNF mAbs?

A

I AGE
Infliximab, adalimumab, golimumab, Etanercept

37
Q

What do the anti-TNF mAbs do?

A
  1. “-mAbs” bind to and inhibit TNF-a
  2. Etanercept is a recombinant fusion protein, which binds to and inhibits TNF-a and LT-a
38
Q

What are the five adverse effects of anti-TNF mAbs?

A
  1. Immunosuppression
  2. Aplastic anaemia
  3. Malignancies, esp. lymphoma
  4. Optic neuritis
  5. Exacerbated multiple sclerosis (TNF-a has protective effects on myelin; without it, further demyelination occurs)
39
Q

What are the two contraindications of anti-TNF mAbs, due to immunosuppression?

A
  1. Live vaccine patients
  2. Hep B patients
40
Q

What is anakinra?

A

It is a modified IL-1R antagonist protein

41
Q

What does anakinra do?

A

It competitively inhibits with IL-1 to bind to its receptor

42
Q

What are the three adverse effects of anakinra?

A
  1. Immunosuppression
  2. Malignancies
  3. Injection site reaction
43
Q

What is tocilizumab?

A

Anti-IL-6R mAb, prevents Il-6 from binding to its receptor by binding to receptor first

44
Q

What are the adverse effects of tocilizumab?

A
  1. Immunosuppression
  2. Neutropenia
  3. Hyperlipidemia
  4. Increased liver enzymes
  5. CYP enzyme interaction (IL-6 normally downregulates these enzymes)
  6. Skin eruptions (autoimmune)
45
Q

What is abatacept?

A

Recombinant fusion protein which binds to CD80 / 86, and prevents CD28 activation = blocks T-cell activation and proliferation

46
Q

What are the two adverse effects of abatacept?

A
  1. Respiratory reaction, esp. in COPD patients
  2. Malignancies
47
Q

What is rituximab?

A

Chimeric mAb which binds to CD20 = blocks B-cell activation and proliferation

48
Q

What are the two adverse effects of rituximab?

A
  1. Respiratory reaction, esp. in COPD patients
  2. Rash with first dose

MSK (6 decks)

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