Colchicine
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Colchicine
Colcrys, Mitigare, Gloperba, Lodoco (low-dose cardiovascular)
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Summary
Common uses
Acute gout flare (early treatment)0, Gout flare prophylaxis (when initiating urate-lowering therapy)0, Familial Mediterranean fever0, Recurrent pericarditis0, Atherosclerotic cardiovascular risk reduction (low-dose, post-LoDoCo trials)0
Pharmacy
Starting dose
Acute gout: 1.2 mg PO at first symptom, then 0.6 mg 1 hour later (total 1.8 mg in 1 hour, the FDA-revised regimen); prophylaxis 0.6 mg PO daily or BID; FMF 1-2 mg/d; pericarditis 0.5-0.6 mg BID for 3 months; Lodoco 0.5 mg PO daily for CV risk reduction
Preparations
0.6 mg tablets; 0.6 mg/5 mL solution; 0.5 mg tablets (Lodoco)
US FDA Max
1.8 mg in any 1-hour period (acute gout); 1.2 mg/d (prophylaxis with renal/hepatic impairment); much lower with strong CYP3A4 or P-gp inhibitors
Pharmacology
Routes
Oral (IV form withdrawn US 2009 due to fatal toxicity reports)
Onset
Anti-inflammatory effect within 24 hours of gout flare onset; loses effectiveness if delayed
Duration
Hours per dose
Half-life
~27-31 hours; markedly prolonged in renal/hepatic impairment and with CYP3A4 or P-gp inhibitors[1]
Bioavailability
~45% (oral)[1]
Pregnancy
Used in FMF in pregnancy; otherwise weigh against alternatives.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Colchicine binds tubulin and prevents microtubule polymerization, disrupting neutrophil migration, NLRP3 inflammasome assembly, and IL-1β release — the proximal drivers of MSU-crystal-induced gout inflammation.0 Narrow therapeutic window with no antidote; fatal interactions with strong CYP3A4 or P-glycoprotein inhibitors (clarithromycin, certain calcineurin inhibitors, ritonavir) including in patients with renal/hepatic impairment. Symptoms of overdose include severe GI then multi-organ failure with delayed bone marrow suppression[1].
References
edit- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Colcrys (colchicine), Takeda, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/022351s011s012lbl.pdf