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colchicine (cardiovascular)

Brand: Colcrys, Lodoco

Prototype: colchicine
Drug Class: anti-inflammatory (cardiovascular)
Drug Family: anti-inflammatory
Subclass: microtubule polymerization inhibitor
Organ Systems: cardiovascularmusculoskeletal

Mechanism of Action

Inhibits microtubule polymerization preventing neutrophil migration and inflammasome (NLRP3) activation; reduces pericardial and vascular inflammation; LoDoCo2/COLCOT trials demonstrate CV benefit.

tubulin (microtubule polymerization)

Indications

  • ASCVD risk reduction (LoDoCo2, COLCOT)
  • pericarditis (acute and recurrent)
  • gout (acute)
  • Familial Mediterranean Fever

Contraindications

  • severe renal impairment
  • severe hepatic impairment
  • concurrent strong CYP3A4/P-gp inhibitors

Adverse Effects

Common

  • GI toxicity (diarrhea, nausea — dose-limiting)
  • neutropenia (rare)

Serious

  • severe myelosuppression
  • neuromyopathy with prolonged high doses
  • fatal poisoning in overdose

Pharmacokinetics (ADME)

Absorption 45% oral
Distribution large Vd
Metabolism CYP3A4 and P-gp substrate
Excretion biliary 65%, renal 10-20%
Half-life 26-31 hours
Onset 1-2 hours
Peak 0.5-3 hours
Duration 24 hours
Protein Binding 34-44%
Vd 5-8 L/kg

Drug Interactions

Drug / Agent Mechanism Severity
strong CYP3A4 inhibitors (clarithromycin, itraconazole) markedly increases colchicine — toxicity major
P-gp inhibitors (verapamil, cyclosporine) increases colchicine levels major
statins additive myopathy risk moderate

Nursing Considerations

  1. COLCOT: colchicine 0.5 mg daily reduced CV events post-MI
  2. LoDoCo2: reduced CV events in stable coronary disease
  3. Start low (0.6 mg) with renal impairment
  4. GI toxicity is dose-limiting — start low and increase slowly
  5. Avoid with strong CYP3A4 or P-gp inhibitors — fatal colchicine toxicity reported

Clinical Pearls

  • COLCOT trial: 0.5 mg/day reduced CV death, MI, stroke by 23% post-MI
  • LoDoCo2: 0.5 mg/day reduced composite CV events in stable CAD
  • Anti-NLRP3 inflammasome mechanism: reduces IL-1β driven vascular inflammation

Safety Profile

Pregnancy avoid
Lactation avoid
Renal Adjustment Required
Hepatic Adjustment Required
TDM Not required
Guideline Update pending

Concordance Terms

Cross-referenced clinical concepts — click any term to see all content where it appears.

Anti-inflammatory (cardiovascular) ASCVD Risk Reduction (LoDoCo2, COLCOT) Familial Mediterranean Fever Gout (acute) Pericarditis (acute And Recurrent)
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