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 Auto immune disease
 Joint inflammation, synovial proliferation and
destruction of articular cartilage
 IgM activates ...
Non biologics
Immunosupressants – methotrexate
Sulfasalazine
Chloroquine
Leflunomide
Biologics
TNF inhibitors – infli...
NSAIDs
Afford symptomatic relief
 Reduce inflammation, pain, swelling
and
morning stiffness
 Improve joint function
 D...
Methotrexate:
DMARD of 1st
choice
 Folate antagonist
 Potent immunosuppressant and anti-inflammatory
action
 Inhibits: ...
 AE: oral ulceration and g.i upset, dose dependent
progressive liver damage
 Contraindications: pregnancy, breastfeeding...
 Sulfapyridine + 5ASA – antiinflammatory
 Suppress superoxide radicals and cytokine
production
 Limited effect – main e...
 Remission in RA – 3-6 months
 Low toxicity – efficacy is also low
 Reduce monocyte IL1, antigen processing,
lysosomal ...
 TNF 𝞪 inhibitors
 Suppress macrophage and T cell function
 Quick response – depress joint erosion
 Effective monother...
 Immunosuppressant and anti-inflammatory
 Decreases the production of inflammatory
cytokines viz. TNF-α, IFN-γ, IL-1
 R...
 Used on a short-term basis – immediate
relief /acute exacerbations/ to control systemic
manifestations
 Intrarticular i...
 Metabolic disorder – recurrent episodes of
acute and chronic arthritis
 Abnormal amounts of urates in the body
 Deposi...
Acute gout:
 Sudden onset following rapid fluctuations in
plasma uric acid level
 Metatarsophalangeal joint of the great...
1. NSAIDs
2. Colchicine
3. Corticosteroids
1. NSAIDs
 Indomethacin, piroxicam, diclofenac,
etoricoxib
 High and repeated doses
 Inhibit
urate crystal phagocytosis...
2. Colchicine:
MOA: depolymerization of microtubules in
granulocytes
granulocyte migration and phagocytosis
Inhibits the r...
 Relieves acute attacks of gout
 Used for the prophylaxis of recurrent
episodes of gouty arthritis
A/E:
 Diarrhea, nausea, vomiting
 Hepatic necrosis
 Rarely, bone marrow suppression
 Overdoses: bloody diarrhoea, hema...
Corticosteroids
 Intraarticular injection
 Refractory cases not responding to NSAIDs/
colchicine
Chronic gout:
Chronic hyperuricaemia  development of
tophi in the synovia  joint deformities
 Pain and stiffness in the...
A. Uricosuric drugs: probenecid, sulfinpyrazone
B. Uric acid synthesis inhibitors : allopurinol
Probenecid
 Inhibits the active renal tubular reabsorption of
uric acid promotes its excretion
 Prevents formation of ne...
 Probenecid x penicillins :
Inhibits urinary excretion of penicillins
prolonged action of penicillins.
 Sulfinpyrazone
Prevents reabsorption of uric acid
 Gastric irritation
 C/I: peptic ulcer
URIC ACID SYNTHESIS INHIBITOR...
Allopurinol
Xanthine
oxidase
Xanthine
oxidase
Uses:
 Chronic tophaceous gout
 Recurrent renal urate stones
 Secondary hyperuricemia - cancer chemotherapy/
thiazides
...
A/E:
 Hypersensitivity reactions
 GIT upset
 CNS: headache, dizziness, peripheral neuritis
May precipitate acute attack...
Thank youThank you
Drugs used in rheumatoid arthritis and gout
Drugs used in rheumatoid arthritis and gout
Drugs used in rheumatoid arthritis and gout
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Drugs used in rheumatoid arthritis and gout

Drugs used in rheumatoid arthritis and gout

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Drugs used in rheumatoid arthritis and gout

  1. 1.  Auto immune disease  Joint inflammation, synovial proliferation and destruction of articular cartilage  IgM activates compliment and release cytokines  Attracts neutrophils – lysosomal destruction
  2. 2. Non biologics Immunosupressants – methotrexate Sulfasalazine Chloroquine Leflunomide Biologics TNF inhibitors – infliximab, adalimumab IL-1 antagonist – Anakinra Others – prednisolone, gold salts
  3. 3. NSAIDs Afford symptomatic relief  Reduce inflammation, pain, swelling and morning stiffness  Improve joint function  Do not halt the disease progression
  4. 4. Methotrexate: DMARD of 1st choice  Folate antagonist  Potent immunosuppressant and anti-inflammatory action  Inhibits: proliferation of activated T-cells cytokine production chemotaxis of neutrophils  Stimulates apoptosis in immune-inflammatory cells
  5. 5.  AE: oral ulceration and g.i upset, dose dependent progressive liver damage  Contraindications: pregnancy, breastfeeding, liver disease
  6. 6.  Sulfapyridine + 5ASA – antiinflammatory  Suppress superoxide radicals and cytokine production  Limited effect – main effect in IBD  AE: neutropenia, thrombocytopenia and hepatitis
  7. 7.  Remission in RA – 3-6 months  Low toxicity – efficacy is also low  Reduce monocyte IL1, antigen processing, lysosomal stabilization  Used when few joints involved  Corneal opacity and retinal damage
  8. 8.  TNF 𝞪 inhibitors  Suppress macrophage and T cell function  Quick response – depress joint erosion  Effective monotherapy  Usually combined to MTX  Gold salts:  Depresses CMI  Aurothiomalate (i.v.)and auranofin (oral)  More AE – no longer used
  9. 9.  Immunosuppressant and anti-inflammatory  Decreases the production of inflammatory cytokines viz. TNF-α, IFN-γ, IL-1  Rapid symptomatic relief; slows the rate of joint destruction  Relieves the severe systemic manifestations of RA – pericarditis, vasculitis, scleral nodules
  10. 10.  Used on a short-term basis – immediate relief /acute exacerbations/ to control systemic manifestations  Intrarticular injection – triamcinolone, hydrocortisone, prednisolone involvement of 1 or 2 major joints  Oral prednisolone  Low doses and gradual withdrawal of steroids - recommended
  11. 11.  Metabolic disorder – recurrent episodes of acute and chronic arthritis  Abnormal amounts of urates in the body  Deposition of monosodium urate crystals in joints and cartilages  Hyperuricemia
  12. 12. Acute gout:  Sudden onset following rapid fluctuations in plasma uric acid level  Metatarsophalangeal joint of the great toe  Tarsal joints, ankles, and knees
  13. 13. 1. NSAIDs 2. Colchicine 3. Corticosteroids
  14. 14. 1. NSAIDs  Indomethacin, piroxicam, diclofenac, etoricoxib  High and repeated doses  Inhibit urate crystal phagocytosis Chemotactic migration of leukocytes into the inflammed joints
  15. 15. 2. Colchicine: MOA: depolymerization of microtubules in granulocytes granulocyte migration and phagocytosis Inhibits the release of glycoprotein  reduces inflammation and joint destruction Antimitotic drug
  16. 16.  Relieves acute attacks of gout  Used for the prophylaxis of recurrent episodes of gouty arthritis
  17. 17. A/E:  Diarrhea, nausea, vomiting  Hepatic necrosis  Rarely, bone marrow suppression  Overdoses: bloody diarrhoea, hematuria, shock, CNS depression and respiratory failure
  18. 18. Corticosteroids  Intraarticular injection  Refractory cases not responding to NSAIDs/ colchicine
  19. 19. Chronic gout: Chronic hyperuricaemia  development of tophi in the synovia  joint deformities  Pain and stiffness in the joints
  20. 20. A. Uricosuric drugs: probenecid, sulfinpyrazone B. Uric acid synthesis inhibitors : allopurinol
  21. 21. Probenecid  Inhibits the active renal tubular reabsorption of uric acid promotes its excretion  Prevents formation of new tophi  Plenty of fluid intake – to prevent formation of renal urate calculi  A/E: gastric irritation, dyspepsia, allergic dermatitis Toxicity: convulsions, nephrotic syndrome
  22. 22.  Probenecid x penicillins : Inhibits urinary excretion of penicillins prolonged action of penicillins.
  23. 23.  Sulfinpyrazone Prevents reabsorption of uric acid  Gastric irritation  C/I: peptic ulcer URIC ACID SYNTHESIS INHIBITORS Allopurinol: Reduces uric acid synthesis by competitively inhibiting xanthine oxidase Allopurinol Alloxanthine  noncompetitive inhibitor of xanthine oxidase
  24. 24. Allopurinol Xanthine oxidase Xanthine oxidase
  25. 25. Uses:  Chronic tophaceous gout  Recurrent renal urate stones  Secondary hyperuricemia - cancer chemotherapy/ thiazides  During treatment of blood dyscrasias  As antiprotozoal agent – kala-azar
  26. 26. A/E:  Hypersensitivity reactions  GIT upset  CNS: headache, dizziness, peripheral neuritis May precipitate acute attack of gout Prevented  colchicine, indomethacin C/I: pregnancy and lactation hypersensitive patients
  27. 27. Thank youThank you

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