An oral administered, potent anti-inflammatory drug.
Oral tablets with a half-life of 9.3 – 10.6 hours
Prescribed for gout, and for its cathartic and emetic effects.
Use is just as effective in the treatment of pseudogout.
Used to treat familial Mediterranean fever, pericarditis, and Behçet’s disease.
Pain-relieving and anti-inflammatory effects for gout were linked to its ability to bind with tubulin.
Inhibits vesicle transport, cytokine secretion, phagocytosis, and in neutrophils inhibits chemotaxis and enzyme release during phagocytosis.
Colchicine has effects on the chemotaxis of inflammatory cells such as neutrophils and monocytes and on the intracellular transportation of vesicles such as endosomes and exosomes.
Colchicine inhibits the expression of E-selectin, an adhesion molecule important for binding leukocytes to endothelial cells, and the recruitment of monocytes and neutrophils to inflamed tissue.
Inhibits tubulin polymerization and microtubule generation and, possibly effects on cellular adhesion molecules, inflammatory chemokines and the inflammasome.
It reduces neutrophil production of free radicals like superoxide.
Adding colchicine to a culture during mitosis is part of the standard procedure for doing karyotype studies.
Inhibits neutrophil motility and activity, leading to an anti-inflammatory effect.
Recommended as a first time drug for prophylaxis In gout.
Used for oral aphthosis, genital aphthosis, and joint manifestations of Behcet disease.
Used for constipation-predominant irritable bowel syndrome in women, and for treatment of severe or persistent aphthous ulcers.
It is commonly indicated for the treatment of gout, familial Mediterranean fever, and pericarditis.
Long-term treatment contraindicated in patients with advanced renal failure.
Ten to 20% of a colchicine dose is excreted unchanged by the kidneys, and is not removed by hemodialysis.
Cumulative toxicity occurs with renal impairment and severe neuromyopathy may result, with proximal weakness, elevated creatine kinase, and sensorimotor polyneuropathy.
Toxicity can be potentiated by the concomitant use of statins and fibrates.
May be associated with a risk of myopathy.
Colchicine has also been associated with disrupting inflammasome activation, thereby suppressing caspase-1 activation and the subsequent release of IL-1β and IL-18.
This neuromuscular condition may be irreversible, and result in hypercapnic respiratory failure and death.
Side-effects include gastrointestinal symptoms, neutropenia. anemia and hair loss.
Following a toxic exposure symptoms start 2 to 5 hours after ingestion and include burning in the mouth and throat, fever, vomiting, diarrhea, abdominal pain, and kidney failure.
With toxic exposure multiple-system organ failure may occur within 24 to 72 hours., with shock, renal failure, bone marrow failure, respiratory insufficiency and death.
Grapefruit exposure increases the risk of toxicity.
No specific antidote exists.
Colchicine usual adult dose for acute gout
Oral: Initial: Gout Flare: 1.2 mg orally at the first sign of the flare followed by 0.6 mg one hour later.
Maximum: Gout Flare: 1.8 mg orally over a one hour period
Usual Adult Dose for Familial Mediterranean Fever
1.2 mg to 2.4 mg orally daily, administered in 1 or 2 divided doses
The dose should be increased as needed to control disease and as tolerated in increments of 0.3 mg/day to a maximum recommended daily dose.
Usual Adult Dose for Gout – Prophylaxis
Oral: 0.5 to 0.6 mg orally once a day for 3 to 4 days a week (less than 1 attack/year).
0.5 to 0.6 mg orally once a day (greater than 1 attack/year).
Severe cases may require 1 to 1.8 mg/day.
Usual Adult Dose for Biliary Cirrhosis
0.6 mg orally twice a day.
Usual Adult dose for Sarcoidosis
0.6 mg orally twice a day.
Usual Adult dose for Pseudogout – Prophylaxis
0.6 mg orally twice a day.
Usual Adult Dose for Fibromatosis
Initial: 0.6 to 1.2 mg orally once a day each day for the first 1 to 2 weeks.
Maintenance: 0.6 to 1.2 mg orally once a day 1 to 2 times per week is often used to prevent recurrence of fibromatosis.
Usual Adult Dose for Aphthous Stomatitis – Recurrent
0.5 to 0.6 mg orally daily.
Usual Adult Dose for Behcet’s Disease
0.5 to 1.5 mg orally once a day.
Usual Adult Dose for Constipation – Chronic
0.6 mg orally three times daily for 4 weeks
Usual Adult Dose for Sweet’s Syndrome
0.6 mg orally twice daily.
Usual Pediatric Dose for Familial Mediterranean Fever
Oral:
4 to 6 years: 0.3 to 1.8 mg daily, administered in 1 or 2 divided doses.
6 to 12 years: 0.9 to 1.8 mg daily, administered in 1 or 2 divided doses.
Over 12 years: 1.2 to 2.4 mg daily, administered in 1 or 2 divided doses.
Liver dose adjustments generally not required, unless severe impairment is present.
Should not be coadministered with protease inhibitors.
Doses higher than 1.8 mg over a 1 hour period for gout flare are not proven more effective and are not recommended.
Should not be given in patients with renal or liver impairment in conjunction with P-gp or strong CYP450 3A4 inhibitors, as life-threatening and fatal colchicine toxicity may occur.
Safety not been established in pediatric patients less than 4 years of age.
The recommended dose for patients undergoing dialysis should be reduced to a single dose of 0.6 mg, and should not be repeated more than once every 2 weeks.
Colchicine may be given without regard to meals.
Prophylaxis is utilized when instituting urate lowering therapy with allopurinol or
Prophylaxis regimens should be .6 mg once or twice daily for duration of six months.
For pseudogout acute attacks should be dosed 0.5 mg three times per day and 0.5 mg daily for prophylaxis.
The addition of colchicine to aspirin or steroid therapy improves recurrent pericarditis at 72 hours, and after 15 months of use results in a 51% reduction in the rate of recurrent pericarditis compared to 24% in a group without colchicine.
Superior to either aspirin or prednisone in recurrent pericarditis.
Preliminary evidence suggests it may decrease C-reactive protein levels, myocardial infarctions, and mortality in patients with coronary artery disease.
Evidence suggests it may prevent stent stenosis in patients with diabetes and coronary disease.
Preoperative administration for open-heart surgery reduced postoperative atrial fibrillation by 45%.
Use in Bechet’s disease decreases mucocutaneous lesions and joint symptoms significantly.
Colchicine Cardiovascular Outcomes Trial (COLCOT) utilized at a dose of 0.5 mg daily in patients with recent myocardial infarction lead to a significantly lower risk of ischemic cardiovascular events than placebo: supporting the role of inflammation in atherosclerosis and its complications (Nidorf SM).
Colchicine is commonly used to treat different inflammatory diseases such as gout, as well as some autoinflammatory diseases, and cardiac conditions including viral pericardial syndromes.
There is a positive effect of colchicine in respiratory syncytial virus replication and suppression of secondary airway inflammation given the promoted expression of IFN-α and IFN-β1 of colchicine and regulation of anti-oxidative factor production.
There is a wide range of clinical literature on the effect of colchicine inhibiting viral disease like adenoviral and adeno-associated viral, herpes simplex virus type 1, Epstein-Barr virus,and hepatitis virus.