Colchicine
Colchicine, an alkaloid. Binds β-tubulin at the vinca-site → blocks microtubule polymerisation → inhibits neutrophil chemotaxis, NLRP3… Oral half-life 31 h.
Binds β-tubulin at the vinca-site → blocks microtubule polymerisation → inhibits neutrophil chemotaxis, NLRP3 inflammasome assembly, and intracellular trafficking. Low-dose indication in stable CAD (LoDoCo2 trial 2020) — reduces recurrent MI via inflammasome suppression. Narrow therapeutic index — CYP3A4 and P-gp inhibitors drastically raise exposure and toxicity.
Pharmacokinetics
- Oral — t½ 31 h · F 45% · Vd 490 L
Related compounds
- Cyclosporine — contraindicated
- Statins — caution
- Piperine — caution
Sources: PMID:21111934, PMID:20190787, PMID:15572716