Source: Health Products Regulatory Authority (IE) Revision Year: 2022 Publisher: Tiofarma B.V., Benjamin Franklinstraat 5-10, 3261 LW Oud-Beijerland, Netherlands
Pharmacotherapeutic group: drugs for gout, with no effect on uric acid metabolism
ATC code: M04AC01
The mechanism of action of colchicine in the treatment of gout is not completely known. Urate crystals are phagocytosed by leukocytes. Hereby inflammatory factors are released. Colchicine inhibits these processes. Other properties of colchicine, such as interaction with microtubules, could also contribute to its action. Onset of actions is approximately 12 hours after oral administration and is maximal after 1 to 2 days.
Colchicine is rapidly and almost completely absorbed after oral administration. Maximum plasma concentrations are met usually after 30 to 120 minutes.
Plasma protein binding of colchicine is approximately 30%. It accumulates in leucocytes.
Colchicine is partially metabolized in the liver and then then in part via the bile. It is largely excreted (80%) in unchanged form and as metabolites in the faeces. 10-20% is excreted in urine. The plasma half-life is 30-60 minutes and approximately 60 hours in leukocytes.
No pharmacokinetics data are available in children.
Colchicine causes DNA damage in vitro and chromosomal aberrations were observed in vivo. No toxicity data are available from own preclinical research.
Studies in animals have shown that colchicine-induced disruption op microtubule formation has an effect on meiosis and mitosis. After colchicine exposure a reduced sperm count and sperm cells with abnormal morphology have been demonstrated in male animals. The doses used in these studies were substantially higher than the dose prescribed for use in patients. High doses of colchicine can cause teratogenicity and embryo toxicity in mice, rats and rabbits.
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