Colchicine
From Ganfyd
rINN: Colchicine
Pharmacological Information
Pharmacology Images
Colchicine in the:
BNF-registration required
BNF for children-registration required
Metabolism & Interactions
Inhibitors of CYP3A4 increase colchicine toxicity
Mechanism of Action
Anti-mitotic agent
Other Issues for Colchicine
Impairs the absorption of vitamin B12
Relevant Clinical Literature
Systematic reviews from Pubmed
Other Literature
Please read pharmacological data limitations
Contents |
Introduction
Valuable to treat acute gout in those with heart failure, renal problems or other contra-indications to NSAIDs. It is an alkaloid found in Autumn crocus with a low therapeutic index.
 | Colchicine is used to create fertile bigger nicer plants...whats nasty in animals is a wonderful way to create vigorous hybrids in plants |
Clinical Use
- It decreases urate crystal phagocytosis and neutrophil migration, possibly by several mechanisms
- Cytogenetics
- Colchicine binds to tubulin, the major protein component of the microtubules that help to separate the 2 sets of chromosomes in mitotic cell division. Treatment of cells with colchicine causes the cells to arrest at metaphase, allowing analysis of the chromosomes.
Indications
Administration
Oral.
- Gout Low dose (1.2mg stat , 0.6 mg after at least 1 hour) to a total of 1.8 mg has now been shown to have equal effectiveness to and much better side effect profile than older high dose regimes of frequent dosing until the flare resolves or until gastrointestinal toxicity occur.[1]
Clinical Issues
- Use only in patient situations where toxic symptoms will be recognised as such and the drug stopped. It is very effective if you get the dose right and in patients who are willing to suffer nausea and diarrhoea to cure those little devils in the big toe. The elderly or frail may get an adequate acute response to only say 500 micrograms every 8 hours, and will thank you for not inducing acute toxicity in your attempts to control their gout. Do not give more than 6mg total dose (for typical 3 day course) to a healthy adult at 3 hourly dosing. Dosage during allopurinol induction for 2 weeks can be 500 micrograms daily.
Contra-indications
- Severe renal failure (GFR < 10 ml/min)
Cautions and Interactions
- Absorption limited by the multidrug resistance efflux transporter P-glycoprotein (P-gp)
- Metabolised by CYP3A4
- Myopathy when used with ciclosporin.
- Erythromycin, clarithromycin and tolbutamide have caused colchicine toxicity. Same is likely to apply to all the classic inhibitors of CYP3A4.
Side effects
- Nausea
- Diarrhoea
- Agranulocytosis (dose dependent)
Special advice
Chronic treatment in renal failure (creatinine >170 µmol/L) should be monitored and one recommendation is a blood count and creatine kinase every 6 months of continued use[2].
Pharmacology
References
- ↑ Information for Healthcare Professionals: New Safety Information for Colchicine FDA Accessed 4 Aug 2009
- ↑ Mikuls TR, MacLean CH, Olivieri J, Patino F, Allison JJ, Farrar JT, Bilker WB, Saag KG. Quality of care indicators for gout management. Arthritis and rheumatism. 2004 Mar; 50(3):937-43.(Link to article – subscription may be required.)
