Colchicine
- Atc Codes:M04AC01
- CAS Codes:64-86-8
- PHARMGKB ID:64-86-8
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Colchicin; Belgium: Colchicine; Bulgaria: Colchicum; Cyprus: Colchicine; Czech Republic: Colchicum Dispert; France: Colchicine; Germany: Colchicum-Dispert; Greece: Colchicine; Hungary: Colchicum-Dispert; Italy: Colchicina; Luxembourg: Colchicine; Malta: Colchicine; Netherlands: Colchicine; Poland: Colchicum-Dispert; Romania: Colchicine; Slovakia: Colchicum-Dispert; Spain: Colchicine; UK: Colchicine.
North America
Canada: Colchicine; USA: Colcrys.
Latin America
Argentina: Colchicina, Xuric; Brazil: Cixin, Colchin, Colchis, Colcitrat; Mexico: Colchiquim, Sixol, Ticolcin.
Asia
Japan: Colchicine.
Drug combinations
Colchicine and Allopurinol
Colchicine and Probenecid
Chemistry
Colchicine: C~22~H~25~NO~6~. Mw: 399.44. (1) Acetamide, N-(5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo[a]heptalen-7-yl)-, (S)-; (2) Colchicine. CAS-64-86-8.
Pharmacologic Category
Antigout Agents. Colchicine Alkaloid. (ATC-Code: M04AC01).
Mechanism of action
Mechanism of principal (antigout) effect is not completely known; apparently reduces inflammatory response to deposition of monosodium urate crystals in joint tissues, possibly by inhibiting polymorphonuclear leukocyte (PMN) metabolism, mobility, chemotaxis, and/or other leukocyte functions. Also interferes with sodium urate deposition by directly decreasing lactic acid production by PMN and indirectly reducing acid production by decreasing phagocytosis. Has weak anti-inflammatory activity, but no analgesic activity. Possible common mechanism of action for anti-inflammatory and antimitotic effects may be related to the dissolution of PMN microtubules. In vitro, inhibits secretion of serum amyloid A protein. Administered orally, may alter functional capacity of ileal mucosa and induce a reversible malabsorption syndrome. Decreases lactic dehydrogenase and increases lysosomal enzyme activity in intestinal mucosa.
Therapeutic use
Acute gouty arthritis attacks (treatment and prevention of recurrences).
Pregnancy and lactiation implications
Teratogenic in mice and hamsters. Chromosomal aberrations reported in prolonged colchicine therapy. It has been suggested that patients on prolonged colchicine therapy may have a greater risk of producing trisomic offspring if conception occurs during therapy with the drug. Distributed into milk. No adverse effects reported in breast-fed infants of women receiving colchicine therapy who were observed over periods of up to 10 months.
Unlabeled use
Primary biliary cirrhosis. Familial Mediterranean fever. Pericarditis.
Contraindications
Hypersensitivity to colchicine or any component of the formulation. Severe renal, gastrointestinal, hepatic, or cardiac disorders. Blood dyscrasias. Pregnancy (parenteral).
Warnings and precautions
Dosage reduction is recommended in patients who develop gastrointestinal symptoms (anorexia, diarrhea, nausea, vomiting) or weakness related to drug therapy. Severe local irritation can occur following SubQ or I.M. administration. Use with caution in mild-to-moderate cardiac disease. Use with caution in mild-to-moderate hepatic (do not administer I.V. in hepatobiliary obstruction) or renal (I.V. form should not be administered) impairment. Use with caution in the elderly. Use I.V. administration only with extreme caution (potential for serious, life-threatening complications; should not be administered in renal insufficiency, hepatobiliary obstruction, patients >70 years of age, or recent oral colchicine use). May cause false-positive results in urine tests for erythrocytes or hemoglobin. Patients who become pregnant while receiving colchicine therapy may be at greater risk of producing trisomic offspring.