What is Colchicine?
Colchicine is an active ingredient used for the treatment of gout and periodic illness or family Mediterranean fever.
The brand names of Colchicine in the United States are: Colcrys, Mitigare, Gloperba.
Colchicine Mechanism of Action (MOA)
It reduces the inflammatory response following the deposition of urate crystals in the joints, as it decreases the leukocyte flow, inhibits the phagocytosis of the urate microcrystals, thus reducing the production of lactic acid avoiding an acid pH, and thus the precipitation of the urate crystals.
Therapeutic Indications and Colchicine Dosage
Oral.
Adults:
– Acute gout attack: 1 mg/at the first sign of gout attack. If pain cannot be relieved, administer 1 mg/1 or 2 hours after the first intake. Maximum: 2 mg/day, dosage guideline max. 4 consecutive days, without exceeding a total accumulated dose of 6 mg during the 4 days.
– Preventive treatment of gout attacks during initial therapy with allopurinol or uricosurics: 1 mg/day.
– Periodic illness or familial Mediterranean fever: 1-2 mg/day (in 2 daily doses or in 1 single dose).
– Treatment of chronic gout: 1 mg/day.
Children and adolescents under 18 years of age:
– Acute attack of gout, prevention of attacks of gout and chronic gout: There are not enough data to establish recommendations in this age group.
– Periodic illness or familial Mediterranean fever:
Children > 12 years: 1 mg-2 mg/day. It can be divided into two daily doses or a single dose.
Children from 4 to 6 years old: 0.3 mg-1.8 mg/day.
Children from 6 to 12 years old: 0.9 mg-1.8 mg a day.
These doses can be administered in a single dose or in two.
Moderate renal insufficiency: reduce doses by half and/or increase dose intervals.
Contraindications of Colchicine
- Colchicine hypersensitivity.
- Pregnancy.
- Severe renal failure and hemodialysis patients.
- Grave liver failure.
- Severe gastrointestinal disorders.
- Stomach ulcer.
- Cardiac disorders.
- Hematological alterations (blood dyscrasias).
- During the 14 days following the use of CYP3A4 and/or P glycoprotein inhibitors.
Warnings and Precautions with Colchicine
- Kidney failure and/or liver failure (dose adjustment).
- Elderly (cumulative dose in 4 days should not exceed 3 mg), children, weakened or alcohol abusers (risk of cumulative toxicity).
- Suppress or reduce doses if diarrhoea occurs.
- Risk of: leukopenia, granulocytopenia, thrombocytopenia, pancytopenia, aplastic anaemia and myelosuppression (periodic blood tests).
- Neuromuscular toxicity and rhabdomyolysis (increased in the elderly and patients with renal insufficiency).
- Avoid grapefruit juice.
- Narrow therapeutic margin and in case of very toxic overdose, do not exceed the dose, as it can be fatal.
- With hepatobiliary and renal insufficiency it may be necessary to adjust the dosage.
- During the treatment of acute gout attack, the patient must be continuously monitored for renal or hepatobiliary insufficiency.
- Concomitant of atorvastatin, simvastatin, pravastatin, fluvastatin, gemfibrozil, fenofibrate, fenofibric acid or bezafibrate (themselves associated with myotoxicity), digoxin or cyclosporine with colchicine, can potentiate the appearance of myopathies.
Liver failure
Colchicine is contraindicated in severe liver failure.
Caution in hepatic insufficiency (close monitoring and dose reduction).
Kidney failure
Colchicine is contraindicated in severe renal failure.
Caution in moderate renal insufficiency (reduce dose by half and/or increase dose intervals).
Interactions with Colchicine
- Precautions should be increased when colchicine is associated with active ingredients that are metabolized or interact with the cytochrome P450 system, particularly with the isoenzyme CYP3A4, or with glycoprotein P.
- Potential appearance of myopathies with concomitant use of: atorvastatin, simvastatin, pravastatin, fluvastatin, gemfibrozil, fenofibrate, fenofibric acid or bezafibrate, digoxin or cyclosporine.
- Increased toxicity with: clarithromycin, erythromycin or telithromycin, CYP3A4 substrates and inhibitors, itraconazole, ketoconazole, indinavir, nelfinavir, ritonavir, saquinavir, grapefruit juice.
- Increased serum concentrations with: azithromycin.
- Decreases absorption of: vitamin B12.
Pregnancy and Colchicine
Contraindicated.
Breastfeeding
Colchicine is excreted through breast milk.
Do not administer during lactation.
Effects on driving ability
Colchicine has not been described as having any effect on the ability to drive vehicles or use machines.
Adverse reactions and side effects of Colchicine
Diarrhea, nausea, vomiting, abdominal pain.
Another adverse reaction identified after evaluation of pharmacovigilance data is hepatic toxicity.
⭐⭐⭐⭐⭐ VIDEO OF COLCHICINE/COLCRYS (DRUG).
Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).
In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.
Resources:
UNII: SML2Y3J35T
ChemIDplus
DrugPortal
PubChem CID: 6167
NCI Thesaurus: C385