Pharmacology and pharmacokinetics of methotrexate in rheumatic disease. Practical issues in treatment and design

Rheum Dis Clin North Am. 1997 Nov;23(4):757-78. doi: 10.1016/s0889-857x(05)70359-8.


Methotrexate (MTX) is among the most effective drugs for treatment of rheumatoid arthritis and has been proven valuable in the treatment of multiple other disorders of immune regulation. MTX has been administered at a wide range of doses and dose intervals, in conjunction with multiple other drugs, and in patients with a broad range of concomitant disorders. To design a safe and effective MTX treatment plan for an individual patient, the provider must have knowledge of the pharmacology and drug interactions of this effective but potentially dangerous medication. The first section of the article reviews MTX structure, pharmacology pharmacokinetics, and mechanisms of action in rheumatic disease. The second section examines factors that can be used to increase MTX efficacy and decrease toxicity.

Publication types

  • Review

MeSH terms

  • Antirheumatic Agents / chemistry
  • Antirheumatic Agents / pharmacokinetics*
  • Antirheumatic Agents / pharmacology*
  • Humans
  • Methotrexate / chemistry
  • Methotrexate / pharmacokinetics*
  • Methotrexate / pharmacology*
  • Rheumatic Diseases / drug therapy*
  • Rheumatic Diseases / metabolism
  • Treatment Outcome


  • Antirheumatic Agents
  • Methotrexate