White, round, biconvex, uncoated tablets with break line on one side and plain on other side.
Each tablet contains: Colchicine 500 mcg.
Antigout.
Pharmacology: Pharmacodynamics: Mechanism of Action: Colchicine reduces neutrophil-mediated inflammatory response by disrupting cytoskeletal functions thereby blocking the β-tubulin polymerisation into microtubules, and preventing the activation, degranulation, and migration of neutrophils into the inflamed area. In familial Mediterranean fever, it may interfere with intracellular assembly of the inflammasome complex present in neutrophils and monocytes which mediates interleukin-1β activation.
Onset: Pain relief: Approximately 18-24 hours.
Pharmacokinetics: Peak plasma concentrations of Colchicine are reached within 2 hours of oral administration. Colchicine is partially deacetylated in the liver and the unchanged drug and its metabolites are excreted in the bile and undergo intestinal reabsorption. Colchicine is found in high concentrations in leucocytes, kidneys, the liver, and spleen. Most of the drug is excreted in the faeces but 10 to 20% is excreted in the urine and this proportion rises in patients with liver disorders.
Colchicine is used for the relief of acute gout and for the prophylaxis of acute attacks, particularly during the first few months of treatment with allopurinol or uricosurics. Colchicine has also been used in several other conditions including amyloidosis, Behcet's syndrome, familial Mediterranean fever, idiopathic thrombocytopenic purpura, pericarditis, primary biliary cirrhosis and pyoderma gangrenosum.
If Colchicine is used for acute attacks of gout, then treatment should be started as soon as possible and an effect may be expected within 12 hours. The recommended oral dose is 1 mg initially then 0.5 mg every 2 to 3 hours until pain relief is obtained or gastrointestinal adverse effects occur; the total dose should not exceed 10 mg. At least 3 days should elapse before another course is given. The dose by mouth is 0.5 to 1.2 mg initially, then 0.5 or 0.6 mg every 1 to 2 hours or 1 to 1.2 mg every 2 hours until pain is relieved or gastrointestinal adverse effects occur; the maximum total dose is 6 mg. Colchicine has sometimes been given intravenously in a dose of 1 or 2 mg over 2 to 5 minutes with additional doses of 0.5 or 1 mg every 6 to 24 hours as required to a total dose of not more than 4 mg in one course; once this amount of Colchicine has been given, further doses should not be given by any route for at least 7 days.
When used for the short-term prophylaxis of gout, doses by mouth are 0.5 or 0.6 mg once to three times daily.
Consideration should be given to using reduced dosages in patients with mild to moderate renal impairment.
Or as prescribed by the physician.
Symptoms: 1st stage: Nausea, vomiting, abdominal pain, haemorrhagic gastroenteritis, electrolyte imbalance, volume depletion, leukocytosis, hypotension in severe cases.
2nd stage: Multisystem organ dysfunction, acute renal failure, confusion, coma, ascending peripheral motor and sensory neuropathy, myocardial depression, pancytopenia, dysrhythmias, respiratory failure, and consumption coagulopathy.
Management: Symptomatic and supportive treatment. Perform gastric lavage within 1 hour of ingestion. Consider activated charcoal administration within 1 hour of presentation in adults who ingested doses >0.1 mg/kg and any amount in children.
Blood dyscrasias. Severe renal (including haemodialysis patients), and hepatic impairment (except in familial Mediterranean fever). Concomitant use with P-glycoprotein (P-gp) inhibitors or strong CYP3A4 inhibitors in patients with renal or hepatic impairment.
Colchicine should be given with great care to old and debilitated patients who may be particularly susceptible to cumulative toxicity. It should also be used with caution in patients with cardiac, hepatic, renal or gastrointestinal disease. Care should also be exercised if treating pregnant patients since Colchicine is known to be teratogenic in animals and there have also been some suggestions of a risk of fetal chromosome damage in humans.
Colchicine should not be administered by subcutaneous or intramuscular injection as it causes severe local irritation.
Contraindicated during pregnancy and breastfeeding.
The most frequent adverse effects of oral Colchicine are those involving the gastrointestinal tract and may be associated with its antimitotic action. Diarrhea, nausea, vomiting, and abdominal pain are often the first signs of toxicity and are usually an indication that Colchicine therapy should be stopped or the dose reduced. Bone marrow depression with agranulocytosis, thrombocytopenia, and aplastic anaemia have occurred on prolonged treatment and local reactions such as thrombophlebitis and neuritis. Extravasation may cause tissue necrosis.
Adverse effects after intravenous administration include cardiac arrhythmias and local reactions such as thrombophlebitis and neuritis.
Seek medical attention immediately at the first sign of any adverse drug reaction.
Increased risk of myopathy and rhabdomyolysis with statins, fibrates, digoxin, ciclosporin. Increased plasma concentration with cimetidine and tolbutamide. May cause reversible malabsorption of vitamin B12. Concomitant use with phenylbutazone may increase risk of leucopenia, thrombocytopenia or bone marrow depression. NSAIDs may increase risk of gastrointestinal ulceration or haemorrhage. Reduced efficacy of prophylactic gout therapy with cytolytic antineoplastic agents.
Potentially Fatal: Increased risk of toxicity with CYP3A4 or P-gp inhibitors such as macrolides (e.g., clarithromycin, erythromycin), HIV protease inhibitors (e.g., ritonavir, atazanavir), Ca2+ channel blockers (e.g., verapamil, diltiazem), ketoconazole, itraconazole, voriconazole, ciclosporin, disulfiram.
Food Interaction: Increased plasma concentrations with grapefruit juice. Increased blood uric acid levels and risk of gastrointestinal toxicity with alcohol.
Laboratory Interference: May cause false-positive results in urine tests for erythrocytes or hemoglobin levels. May interfere with urinary determination of 17-hydroxycorticosteroids using the Reddy, Jenkins and Thorn procedures.
Store at temperatures not exceeding 30°C.
M04AC01 - colchicine ; Belongs to the class of preparations with no effect on uric acid metabolism. Used in the treatment of gout.
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