Adult: For the treatment of acute gout flares: Initially, 1 mg followed by 0.5 mg after 1 hour, given within 12 hours of flare onset. Treatment may resume after 12 hours, if necessary, with a Max dose of 0.5 mg 8 hourly. Treatment course ends when symptoms are relieved or when a total of 6 mg has been given. Another course may be repeated after at least 3 days. Alternatively, give 1.2 mg at the 1st sign of the flare followed by 0.6 mg after 1 hour; Max of 1.8 mg over a 1-hour period. Treatment and dosage recommendations may vary among countries or individual products (refer to specific product guidelines).
Oral Familial Mediterranean fever
Adult: 1.2-2.4 mg daily given as a single dose or in 2 divided doses, may be increased or decreased as necessary in increments of 0.3 mg daily. Treatment recommendations may vary among countries or individual products (refer to specific product guidelines). Child: 4-6 years 0.3-1.8 mg daily; >6-12 years 0.9-1.8 mg daily; >12 years Same as adult dose. All doses may be given as a single dose or in 2 divided doses.
Oral Prophylaxis of acute gout
Adult: During initiation of urate-lowering therapy: 0.5 mg bid. Alternatively, 0.6 mg once daily or bid; Max of 1.2 mg daily. Treatment duration is based on flare frequency, gout duration, and the presence and size of tophi. Treatment and dosage recommendations may vary among countries or individual products (refer to specific product guidelines).
Nhóm bệnh nhân đặc biệt
Patients taking P-gp inhibitors and moderate or strong CYP3A4 inhibitors (with normal renal and hepatic function): Dose reduction or interruption is recommended.
Suy thận
Familial Mediterranean fever:
Patients on haemodialysis: Initially, 0.3 mg daily, increase if necessary, according to individual safety and tolerability.
CrCl (mL/min)
Dosage
<30
Initially, 0.3 mg daily, increase if necessary, according to individual safety and tolerability.
30-80
Dose reduction may be required.
Dosage recommendations may vary among countries or individual products (refer to specific product guidelines).
Acute gout; Prophylaxis of acute gout:
Moderate: Reduce dose or increase dosing interval. Severe or patients on haemodialysis: Contraindicated. Dosage recommendations may vary among countries or individual products (refer to specific product guidelines).
Suy gan
Familial Mediterranean fever:
Severe: Dose reduction may be required.
Acute gout; Prophylaxis of acute gout:
Severe: Contraindicated.
Cách dùng
May be taken with or without food.
Chống chỉ định
Blood dyscrasias. Severe renal (including haemodialysis patients), and hepatic impairment (when used for acute gout). Pregnancy and lactation. Concomitant use with P-glycoprotein (P-gp) inhibitors or strong CYP3A4 inhibitors in patients with renal or hepatic impairment. Contraindications may vary among individual products (refer to specific product labelling for detailed information).
Thận trọng
Patient with CV disease, gastrointestinal disorders, abnormalities in blood counts. Debilitated patients. Not indicated as an analgesic to treat pain from other causes. Concomitant use with P-gp inhibitors and moderate or strong CYP3A4 inhibitors (with normal renal and hepatic function). Mild to moderate renal and hepatic impairment (when used for acute gout); renal and hepatic impairment (when used for familial Mediterranean fever). Children (when used for familial Mediterranean fever) and elderly.
Tác dụng không mong muốn
Significant: Neuromuscular toxicity, rhabdomyolysis (chronic treatment); gastrointestinal effects (e.g. abdominal pain, diarrhoea, nausea, vomiting). Eye disorders: Delayed corneal wound healing. Gastrointestinal disorders: Rarely, gastrointestinal haemorrhage. General disorders and administration site conditions: Fatigue. Investigations: Increased ALT or AST, elevated creatine phosphokinase. Musculoskeletal and connective tissue disorders: Myotonia, muscle weakness, myopathy. Nervous system disorders: Headache, neuropathy, peripheral neuritis. Reproductive system and breast disorders: Amenorrhoea, dysmenorrhoea, oligospermia, azoospermia. Respiratory, thoracic and mediastinal disorders: Pharyngolaryngeal pain. Skin and subcutaneous tissue disorders: Rash, alopecia. Potentially Fatal: Severe bone marrow depression (e.g. aplastic anaemia, pancytopenia; agranulocytosis, thrombocytopenia, leucopenia); respiratory distress syndrome.
Monitor CBC, serum uric acid, renal function, LFTs. Assess for gastrointestinal symptoms and neuromuscular toxicity.
Quá liều
Symptoms: 1st stage (occurs within 24 hours of ingestion): Nausea, vomiting, abdominal pain, haemorrhagic gastroenteritis, electrolyte imbalance, volume depletion, leucocytosis, hypotension in severe cases. 2nd stage (occurs within 24-72 hours of ingestion): Life-threatening complications, including 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 have ingested doses >0.1 mg/kg and any amount in children.
Tương tác
Increased risk of myopathy and rhabdomyolysis with HMG-CoA reductase inhibitors (e.g. atorvastatin, simvastatin), fibrates, digoxin. May cause reversible malabsorption of vitamin B12. Decreased therapeutic effect with acidifying agents (e.g. ammonium chloride, ascorbic acid, acid phosphates). Enhanced therapeutic effect with alkalinising agents (e.g. Na bicarbonate, K citrate). May enhance the sensitivity to CNS depressants (e.g. opiates, sedative hypnotics, benzodiazepines). Concomitant use with phenylbutazone may increase risk of leucopenia, thrombocytopenia or bone marrow depression. May increase the risk of gastrointestinal ulceration or haemorrhage with other NSAIDs. Reduced efficacy of prophylactic gout therapy with cytolytic antineoplastic agents. Tolbutamide and cimetidine increase the plasma levels of colchicine. 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), Ca channel blockers (e.g. verapamil, diltiazem), ketoconazole, itraconazole, voriconazole, ciclosporin, disulfiram.
Tương tác với thức ăn
Increased plasma concentrations with grapefruit juice; avoid concomitant use. Increased blood uric acid levels and risk of gastrointestinal toxicity with alcohol.
Ảnh hưởng đến kết quả xét nghiệm
May cause false-positive results in urine tests for erythrocytes or Hb levels. May interfere with urinary determination of 17-hydroxycorticosteroids using the Reddy, Jenkins and Thorn procedure.
Tác dụng
Description: Mechanism of Action: Colchicine acts by inhibiting the neutrophil-mediated inflammatory responses induced by monosodium urate crystals in synovial fluid. It disrupts cytoskeletal functions through the inhibition of β-tubulin polymerisation into microtubules, thereby 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: Approx 18-24 hours. Pharmacokinetics: Absorption: Rapidly and almost completely absorbed. Bioavailability: Approx 45%. Time to peak plasma concentration: 0.5-3 hours. Distribution: Concentrated in leucocytes, kidney, spleen, and liver (except the heart, skeletal muscle, and brain). Crosses the placenta and enters breast milk. Volume of distribution: Approx 5-8 L/kg. Plasma protein binding: Approx 39%, primarily to albumin. Metabolism: Metabolised in the liver via demethylation by the CYP3A4 isoenzyme into 2 primary metabolites (2-O-demethylcolchicine and 3-O-demethylcolchicine), and 1 minor metabolite (10-O-demethylcolchicine or known as colchiceine). Undergoes enterohepatic recycling. Excretion: Mainly via faeces (80%, as unchanged drug and metabolites); urine (10-20%). Elimination half-life: 27-31 hours.
Đặc tính
Colchicine Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 6167, Colchicine. https://pubchem.ncbi.nlm.nih.gov/compound/Colchicine. Accessed June 27, 2022.
Bảo quản
Store between 20-25°C. Protect from light and moisture. Follow applicable procedures for receiving, handling, administration, and disposal.
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