What type of drug is Methotrexate?
Conventional DMARD
Methotrexate is commonly used to treat rheumatoid arthritis.
What is the mechanism of action (MOA) of Methotrexate?
↑ Adenosine → ↓ inflammation; ↓ cytokines (TNF-α, IL-1, IL-6); suppresses T- & B-cell proliferation; inhibits AICAR transformylase
What are the indications for Methotrexate?
Rheumatoid arthritis
What are the common side effects (S/E) of Methotrexate?
Mouth ulcers, mucosal bleeding
What are the contraindications (CI) for Methotrexate?
Blood dyscrasias, renal/hepatic disease, infections (herpes/varicella), pregnancy, elderly
What are the adverse drug reactions (ADRs) associated with Methotrexate?
Hepatotoxicity, nephropathy, additive antifolate effects with TMP-SMX, mucosal ulceration
What type of drug is Chloroquine?
Antimalarial/DMARD
What is the mechanism of action (MOA) of Chloroquine?
Unknown; immune modulator
What are the indications for Chloroquine?
Rheumatoid arthritis, lupus
What are the common side effects (S/E) of Chloroquine?
Ocular toxicity (retinopathy), QT prolongation
What are the contraindications (CI) for Chloroquine?
Caution in QT prolongation, requires ocular monitoring
What are the adverse drug reactions (ADRs) associated with Chloroquine?
Risk of irreversible ocular damage, requires monitoring of FBC, liver and renal function
What type of drug is Leflunomide?
Conventional DMARD
What is the mechanism of action (MOA) of Leflunomide?
Inhibits dihydroorotate dehydrogenase → ↓ pyrimidine synthesis → ↓ DNA/RNA synthesis in immune cells
What are the indications for Leflunomide?
Rheumatoid arthritis (not juvenile RA)
What are the common side effects (S/E) of Leflunomide?
GI upset, stomatitis, ↑ liver enzymes, hypertension
What are the contraindications (CI) for Leflunomide?
Pregnancy (male & female – 2-year washout), hypersensitivity, not for juvenile RA
What are the adverse drug reactions (ADRs) associated with Leflunomide?
Hepatotoxicity (rare), SJS, agranulocytosis, anaphylaxis
What type of drug is Sulfasalazine?
Conventional DMARD
What is the mechanism of action (MOA) of Sulfasalazine?
↓ RF, ↓ T-cell and B-cell activity, ↓ IL-1, IL-6, IL-12, TNF-α
What are the indications for Sulfasalazine?
Rheumatoid arthritis, often in combination with MTX
What are the common side effects (S/E) of Sulfasalazine?
Nausea, hypersensitivity
What are the contraindications (CI) for Sulfasalazine?
Sulfa allergy (implied), requires blood and organ function monitoring
What are the adverse drug reactions (ADRs) associated with Sulfasalazine?
Hepatotoxicity, myelotoxicity, megaloblastic anaemia