Immunosuppressants

M E C H A N I S M O F A C T I O N

• Gold salts accumulate in bone marrow, liver & spleen. • Impairs macrophage function and cytokine activity which supresses phagocytosis and lysosomal enzyme activity. • Inhibits PG synthesis and complement activation. • Potentially acts by suppressing IgM antibody responses and formation of immune complexes as well as IL-1 generation.

C L I N I C A L N O TE

• Absorption decreased by food. Metabolised in the liver, excreted in urine and faeces

I M M U N O S U PPR E S SA N T S

M E T H O T R E X A T E

M E C H A N I S M O F A C T I O N • Folic acid antagonist that decreases inflammatory cells in the synovium • Reversibly inhibits dihydrofolate reductase • Leading to reduced intracellular levels of THF and therefore preventing the synthesis of purines and thymidine

I N D I C A TI O N S • Reducing joint erosions in established and early rheumatoid arthritis

C O N T R A I N D I C A TI O N S • Renal dysfunction • Liver disease • Active infectious disease • Excessive alcohol consumption.

L E F L U NO M I D E

M E C H A N I S M O F A C T I O N • Pyrimidine synthesis inhibitor that works by inhibiting dihydroorotate dehydrogenase. • It undergoes biotransformation to active metabolite to inhibit the dihydroorotate dehydrogenase. • Prevents pyrimidine synthesis by specifically targeting lymphocyte proliferation. • Also inhibits osteoclast production and therefore slows progression.

I N D I C A TI O N S • Active rheumatoid arthritis as a disease-modifying antirheumatic drug (DMARD). • Active psoriatic arthritis.