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*used by ancient Greeks, so along with the opiates, is probably the earliest recorded medication still in current use

  • 6th C AD, Alexander of Tralles proposed use of colchicine for joint pain
  • 1763, specifically described in the Dx & Rx of gout
  • 1820: 1st isolated
  • recent uses include: familial Mediterranean fever, primary biliary cirrhosis & Behcet's syndrome
  • the large-scale COLCOT (Colchicine Cardiovascular Outcomes Trial) and LoDoCo2 (Low Dose Colchicine Trial 2) showed a 32% reduction in major adverse cardiovascular events or need for urgent revascularization making it likely it will be added to the secondary prevention guidelines for heart disease


  • alkaloid f. Colchicum autumnale (autumn crocus or meadow saffron) used for arthritis since 6thC. isol.1820;
  • A unique anti-inflammatory effective only in gout ? acting mainly as an anti-mitotic agent & thus also used in research on cell division & function;
  • binds to the intracellular protein tubulin, preventing its alpha & beta forms polymerising to form microtubules, thereby disrupting the microtubular network causing:
    • impaired protein assembly in the Golgi apparatus
    • decreased endocytosis & exocytosis
    • altered cell shape
    • depressed cellular motility
    • arrest of mitosis - usually in metaphase
  • reduces CRP levels


  • lipid soluble alkaloid
  • well absorbed orally
  • extensive 1st pass metabolism ⇒ oral bioavailability 40%
  • peak plasma levels 30-120min
  • short plasma half-life of 20-90min due to intracellular tissue binding (Vd = 2.1L/kg)
  • elimination:
    • renal 30-40%
    • hepatic with eneterohepatic recycling

Clinical use:

Acute Rx gout:

  • While colchicine is effective for treating acute gout it has a slow onset of action, with limited effectiveness if treatment is delayed and a narrow therapeutic index 1)
  • Colchicine should not be used unless non-steroidal anti-inflammatories are contraindicated, or have been used and found to lack analgesic efficacy or to have unacceptable side effects in the individual
  • The elderly may be more susceptible to cumulative toxicity with colchicine, and due to age-related renal function impairment, other treatments such as corticosteroids should be considered.
  • If colchicine is used in the elderly lower doses should be given and a maximum cumulative dose of 3mg over four days should be observed
  • Reduce dose in those with moderate renal impairment - do NOT use in those with severe renal impairment.
  • Maximum dose in healthy adults in the first 24 hours is 2.5mg and the total dose given in an acute attack should not exceed 6mg over four days.
  • regime 1 for otherwise healthy adults over 50kg:
    • 1mg initially, then 0.5mg every six hours until pain relief is obtained.
  • regime 2 for otherwise healthy adults over 50kg:
    • 0.5mg bd for 3 days.
  • NB. used to be given until no pain or GIT effects (4-10mg) BUT 7-8mg may be lethal !

Prophylactic Rx of gout:

  • 0.5mg 2-4x/wk → 1.8mg/d depending on frequency attacks;

Common Adverse Effects:

  • In moderate doses well tolerated;
  • Most common are GIT effects due to effect on rapidly prolif. epith. cells, esp. in jejunum → N/V/D/abdo. pain which are the earliest effects of OD;
  • Thus, give 1-2hrly doses & stop if GIT effects, but these may worsen as lag effect of several hrs b/n dose & GIT effect!

Chronic use:

  • risk of :
    • agranulocytosis;
    • aplastic anaemia
    • myopathy
    • alopecia
    • azospermia
    • in the COLCOT study, 0.9% risk of pneumonia vs 0.4% in placebo group


  • severe renal impairment
  • severe hepatic impairment
  • hypersensivity reaction
  • pregnancy

Specific Precautions:

  • elderly, cardiac/hepatic/renal/GIT disease; PH poor tolerance to it;
  • potentially fatal colchicine toxicity from hepatic/renal disease or drug interactions with CYP3A4 inhibitors such as:
    • clarithromycin (eg. used as part of triple therapy for Helicobacter eradication in peptic ulcer Mx)
colchicine.txt · Last modified: 2022/07/12 08:10 by gary1

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