Colchicine disposition in human leukocytes after single and multiple oral administration

Clin Pharmacol Ther. 1993 Oct;54(4):360-7. doi: 10.1038/clpt.1993.161.


Inasmuch as leukocytes were reported to be an active pharmacologic compartment, colchicine disposition was determined in plasma, granulocytes, and mononuclear cells in healthy volunteers after 1 mg oral single and multiple doses. After the single dose, maximal colchicine concentration was observed at 1 hour in plasma and 47 hours later in leukocytes. This delay was confirmed by the slow accumulation of colchicine by lymphocytes in culture. In the multiple-dose study, mean granulocyte colchicine concentration (20 to 53 ng/10(9) cells) were twofold higher than in mononuclear cells (9 to 24 ng/10(9) cells). Mean predicted colchicine multiple-dose granulocyte and mononuclear cell concentrations were 2.5-fold and ninefold higher, respectively, than those measured. After the last dose, colchicine decreased, with half-life values between 41 and 46 hours for leukocytes and 49 hours for plasma. This study validates leukocytes as a microcompartment whose kinetics correlates with colchicine biologic effects.

MeSH terms

  • Administration, Oral
  • Adult
  • Cells, Cultured
  • Colchicine / administration & dosage
  • Colchicine / blood*
  • Granulocytes / metabolism
  • Half-Life
  • Humans
  • Leukocytes / metabolism*
  • Leukocytes, Mononuclear / metabolism
  • Lymphocytes / metabolism
  • Male
  • Middle Aged


  • Colchicine