Chemical formula: C₂₂H₂₅NO₆ Molecular mass: 399.443 g/mol PubChem compound: 2833
Colchicine interacts in the following cases:
Colchicine may increase sensitivity to CNS depressants and enhance the response to sympathomimetic agents.
Grapefruit juice may increase plasma levels of colchicine. Grapefruit juice should therefore not be taken together with colchicine.
Co-administration with P-gp inhibitors and/or moderate or strong CYP3A4 inhibitors will increase the exposure to colchicine, which may lead to colchicine-induced toxicity including fatalities. If treatment with a P-gp inhibitor or a moderate or strong CYP3A4 inhibitor is required in patients with normal renal and hepatic function, a reduction in colchicine dosage or interruption of colchicine treatment is recommended.
Colchicine is a substrate for both CYP3A4 and the transport protein P-gp. In the presence of CYP3A4 or P-gp inhibitors, the concentrations of colchicine in the blood increase. Toxicity, including fatal cases, have been reported during concurrent use of CYP3A4 or P-gp inhibitors such as macrolides (clarithromycin and erythromycin), ciclosporin, ketoconazole, itraconazole, voriconazole, HIV protease inhibitors, calcium channel blockers (verapamil and diltiazem) and disulfiram.
A reduction in colchicine dosage or an interruption of colchicine treatment is recommended in patients with normal renal or hepatic function if treatment with a P-gp inhibitor or moderate or strong CYP3A4 inhibitor is required. A 4-fold reduction in colchicine dosage is recommended when co-administered with a P-gp inhibitor and/or a strong CYP3A4 inhibitor. A 2-fold reduction in colchicine dosage is recommended when co-administered with a moderate CYP3A4 inhibitor.
The risk of myopathy and rhabdomyolysis is increased by a combination of colchicine with statins, fibrates, ciclosporin or digoxin.
Colchicine administration in animals induces significant reductions in fertility.
Concomitant administration of azithromycin and P-gp substrates such as colchicine has been reported to result in increased serum levels of P-gp substrate. Therefore, if colchicine and azithromycin are administered concomitantly, the possibility of elevated serum colchicine concentrations should be considered.
Colchicine may react with cyclosporin leading to an increased risk of nephrotoxicity and increased plasma-cyclosporin concentration.
Substances such as cimetidine and tolbutamide reduce metabolism of colchicine and thus plasma levels of colchicine increase.
Concomitant use with clarithromycin may lead to colchicine toxicity. Colchicine is a substrate for both CYP3A and the efflux transporter, P-glycoprotein (Pgp). Clarithromycin and other macrolides are known to inhibit CYP3A and Pgp. When clarithromycin and colchicine are administered together, inhibition of Pgp and/or CYP3A by clarithromycin may lead to increased exposure to colchicine. Patients should be monitored for clinical symptoms of colchicine toxicity.
Reversible malabsorption of cyanocobalamin (vitamin B12) may be induced by an altered function of the intestinal mucosa in coadministration with colchicine.
Colchicine should not be used in patients undergoing haemodialysis since it cannot be removed by dialysis or exchange transfusion.
Colchicine may cause severe bone marrow depression (agranulocytosis, aplastic anaemia, thrombocytopenia). The change in blood counts may be gradual or very sudden. Aplastic anaemia in particular has a high mortality rate. Periodic checks of the blood picture are essential.
If patients develop signs or symptoms that could indicate a blood cell dyscrasia, such as fever, stomatitis, sore throat, prolonged bleeding, bruising or skin disorders, treatment with colchicine should be immediately discontinued and a full haematological investigation should be conducted straight away.
Colchicine may cause severe bone marrow depression (agranulocytosis, aplastic anaemia, thrombocytopenia). The change in blood counts may be gradual or very sudden. Aplastic anaemia in particular has a high mortality rate. Periodic checks of the blood picture are essential.
If patients develop signs or symptoms that could indicate a blood cell dyscrasia, such as fever, stomatitis, sore throat, prolonged bleeding, bruising or skin disorders, treatment with colchicine should be immediately discontinued and a full haematological investigation should be conducted straight away.
Colchicine is genotoxic in vitro and in vivo, and is teratogenic in animal studies. Colchicine is therefore contraindicated in pregnancy.
Women of childbearing potential have to use effective contraception during treatment.
Colchicine is excreted in breast milk. Therefore, use of colchicine is contraindicated in women who are breastfeeding.
Colchicine administration in animals induces significant reductions in fertility.
No details are available regarding the influence of colchicine on the ability to drive and use machines. However, the possibility of drowsiness and dizziness should be taken into account.
The following adverse reactions have been observed.
The frequencies are listed under one of the following classifications:
Very common >1/10
Common >1/100 and <1/10
Uncommon >1/1000 and <1/100
Rare >1/10 000 and <1/1000
Very rare <1/10 000
Not known (cannot be estimated from the available data)
Not known: bone marrow depression with agranulocytosis, aplastic anemia and thrombocytopenia.
Not known: peripheral neuritis, neuropathy.
Common: abdominal pain, nausea, vomiting and diarrhoea.
Not known: gastrointestinal haemorrhage.
Not known: hepatotoxicity.
Not known: alopecia, rash.
Not known: myopathy and rhabdomyolysis.
Not known: renal damage.
Not known: amenorrhoea, dysmenorrhoea, oligospermia, azoospermia.
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