Colchicine is an antiinflammatory agent effective against gout flares and familial Mediterranean fever [14] via interference with migration of neutrophils to sites of inflammation that have been induced by deposits of monosodium urate crystals in synovial fluid. In addition, colchicine blocks the inflammasome complex in neutrophils and monocytes, which mediate interleukin-1beta activation.
藥動學
Absorption:
1. Tmax: (young subjects) 1.3 hours; (elderly) 1.25 hours; (hepatic impairment) 2.16 hours
2. Bioavailability: Approximately 45% Distribution:
1. Vd: 5 to 8 L/kg
2. Protein binding, Albumin: 39% Metabolism:
Hepatic: Partial via CYP3A4 and glucuronidation Excretion:
1. Fecal: Extensive; Renal: 40% to 65% unchanged
2. Dialyzable: No, less than 5%
禁忌症
Concomitant use of p-glycoprotein or CYP3A4 inhibitors, including all protease inhibitors except fosamprenavir, in patients with hepatic or renal impairment.
懷孕分類
C
哺乳分類
Probably safe; in animal tests colchicine can decrease breast milk production and change the composition of the milk but no harmful effects have been reported
副作用
Diarrhea, Nausea, Vomiting
劑量和給藥方法
Prophylactic dose:
0.6mg QD-BID (maximum: 1.2 mg/day). In patients with GI intolerance, some experts give 0.6 mg every other day Acute attack of gout: Day 1:Oral: 1.2 mg at the first sign of flare, followed by 0.6 mg after 1 hour (maximum total dose: 1.8 mg/day on day 1). Initiate as soon as possible, ideally within 12 to 24 hours of flare onset; consider alternative agents if >36 hours since flare onset.
In patients who were already receiving prophylactic colchicine at the time of their flare, some experts give the higher 1.8 mg/day dosing regimen on day 1 of the flare, in place of the usual prophylactic dose. Day 2 and thereafter: Oral: 0.6 mg once or twice daily until flare resolves. Some experts continue for 2 to 3 days after flare resolves.
In patients who were already receiving prophylaxis at the time of their flare, some experts give 0.6 mg twice daily (total dose: 1.2 mg/day) from day 2 until ~48 hours after flare resolution, and then resume the previous prophylactic dose.