Drugs for Rheumatoid arthritis & gout, DMARDS, NSAIDS, methotrexate, TNF alpha inhibitors, glucocorticoids, colchicine

1. Dr. Resu Neha Reddy
Junior Resident
Osmania Medical College

2.  Auto immune disease
 Joint inflammation, synovial proliferation
and destruction of articular cartilage
 IgM activates compliment and release
cytokines
 Attracts neutrophils – lysosomal
destruction
 Local PGs synthesis  Inflammation &
pain

4.  NSAIDs
◦ Afford symptomatic relief
◦ Reduce inflammation, pain, swelling
and morning stiffness
◦ Improve joint function
◦ Do not halt the disease progression

5. Non biologics Biologics Others
Immunosupressants –
Methotrexate,
Cyclophosphamide,
Azathioprine,
Cyclosporine,
Chloroquine,
Hydroxychloroquine
Leflunomide
TNF inhibitors –
A – Adalimumab,
C - certolizumab,
E - Etanercept,
Inhibitors - Infliximab,
Goli – Golimumab
T cell activation # -
Abatacept
IL-1 # - Anakinra
IL – 6 # - Tocilizumab
Gold salts
Penicillamine
Sulphasalizine

6.  DMARD of 1st choice
 Folate antagonist
 Potent immunosuppressant & anti inflammatory
 Inhibits:
◦ proliferation of activated T-cells
◦ cytokine production
◦ chemotaxis of neutrophils
 Stimulates apoptosis in immune-inflammatory cells
 AE: oral ulceration and g.i upset, dose dependent
progressive liver damage
 Contraindications: pregnancy, breastfeeding, liver disease

7.  MOA
◦ Traps free radicals
◦ Suppresses T-lymphocyte response to mitogens
◦ Stabilizes lysosomal enzymes
◦ Decreases leukocyte chemotaxis
 USES
◦ Mild erosive RA
◦ Dose 200mg BD
 ADVERSE EFFECTS
◦ corneal deposits, opacity, neuropathy, myopathy

8.  Remission in RA – 3-6 months
 Low toxicity – efficacy is also low
 Hydroxychloroquine is preferred
 Reduce monocyte IL1, antigen processing,
lysosomal stabilization
 Used when few joints involved
 Corneal opacity and retinal damage

9.  Produced from fungus Beauveria nivea
 PK
◦ Peak plasma concentration 1.5 to 2 hrs
◦ Extensively metabolized in liver by
CYP3A4
 Uses
◦ RA not responding to Methotrexate
 Toxicity
◦ Nephrotoxicity

12.  Suppress macrophage and T cell function
 Quick response – depress joint erosion
 Effective monotherapy
 Usually combined to MTX

17.  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

18.  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

20.  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

22.  Sudden onset following rapid fluctuations in
plasma uric acid level
 Metatarsophalangeal joint of the great toe
 Tarsal joints, ankles, and knees

23.  NSAIDs
 Colchicine
 Corticosteroids

26.  Uses
◦ Relieves acute attack of gout
◦ Used for prophylaxis of recurrent episodes of gouty
arthritis
 A/E:
◦ Diarrhea, nausea. Vomiting
◦ Hepatic necrosis
◦ Rarely, bone marrow suppression
 Overdose:
◦ Bloody diarrhea, hematuria, shock, CNS depression
& resp. Failure

27.  Intra-articular injection
 Refractory cases not responding
◦ NSAIDs
◦ Colchicine

28.  Chronic hyperuricaemia
development of tophi in the synovia
joint deformities
Pain and stiffness in the joints

29.  Uric acid synthesis inhibitors :
◦ Allopurinol
◦ Febuxostat
◦ Rasburicase
 Uricosuric drugs:
◦ Probenecid
◦ sulfinpyrazone
◦ Benzbromarone
◦ Lesinurad

33.  Probenecid
 Inhibits the active renal tubular reabsorption
ofmuric 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