Colchicine

Inquiry

Cat Number

PIPE-0685

CAS Number

64-86-8

If you have any other questions, please contact our experts.

Product Detail Description Scientific Support Advanced Innovations Customer Q&A

CAS Number

64-86-8

EINECS

200-598-5

Storage

Store at 2-8℃

Synonyms

Colchicinum; Colchicina; Colcrys; (-)-colchicine; Mitigare; 7-alpha-H-Colchicine; NSC 757

Molecular Formula

C22H25NO6

Molecular Weight

399.4

Smiles

CC(=O)N[C@H]1CCC2=CC(=C(C(=C2C3=CC=C(C(=O)C=C13)OC)OC)OC)OC

Appearance

White to light yellow powder

Melting Point

150-160℃

Boiling Point

725℃

Relative Density

1.32

General Description

Colchicine is a tricyclic alkaloid derived from the autumn crocus (Colchicum autumnale) that has been used for centuries to treat inflammatory conditions. It is available in oral tablets and is distinguished by its narrow therapeutic window and unique mechanism independent of conventional NSAIDs or glucocorticoids. The drug is a potent inhibitor of microtubule polymerization that exerts its effects primarily through modulation of innate immune responses.

Mechanism of Action

Colchicine binds to tubulin, preventing its polymerization into microtubules and disrupting multiple cellular functions including chemotaxis, adhesion, and phagocytosis. In acute gout, it inhibits neutrophil migration and the release of interleukin-1 beta by disrupting the NLRP3 inflammasome complex. This anti-inflammatory effect occurs at doses that do not completely block microtubule formation, explaining its efficacy without significant cytotoxicity at therapeutic concentrations.

Application

It is indicated for the treatment and prevention of acute gout flares, as well as for the management of familial Mediterranean fever to prevent amyloidosis. In cardiovascular medicine, it is approved for secondary prevention of pericarditis and is increasingly used off-label for post-pericardiotomy syndrome. Due to its narrow therapeutic index, dosing requires careful attention to renal and hepatic function, and it should not be administered intravenously due to life-threatening toxicity.

This updated review synthesizes literature from 2008 to 2014 on colchicine’s mechanisms and clinical applications. While tubulin disruption remains its primary action, newly described effects include inhibition of the NALP3 inflammasome, blockade of purinergic receptor‑activated pores, modulation of macrophage function, and stimulation of dendritic cell maturation and antigen presentation. Colchicine also exhibits anti‑fibrotic activity and influences endothelial function. Beyond its established uses in gouty arthritis and familial Mediterranean fever, evidence now supports therapeutic roles in osteoarthritis, pericarditis, and atherosclerosis. The review concludes that deeper understanding of these mechanisms will likely expand colchicine’s utility to additional inflammatory conditions.

Fig. 1 Summary of the effects of colchicine on macrophages. (Leung YY, et al., 2015)

References

Leung YY, et al. Colchicine--Update on mechanisms of action and therapeutic uses. Semin Arthritis Rheum. 2015; 45(3):341-350.

A living systematic review (up to May 2021) included three RCTs of hospitalized patients (11,525 participants) and one RCT of non‑hospitalized patients (4488 participants). In moderate‑to‑severe COVID‑19, colchicine plus standard care showed no significant effect on all‑cause mortality (RR 1.00, 95% CI 0.93‑1.08) or clinical worsening (RR 1.02, 95% CI 0.96‑1.09) compared to standard care alone (moderate‑certainty evidence). In outpatients, colchicine probably slightly reduced hospital admission or death (RR 0.80, 95% CI 0.62‑1.03) and serious adverse events (RR 0.78, 95% CI 0.61‑1.00).

Fig. 2 Study flow diagram. (Mikolajewska A, et al., 2021)

References

Mikolajewska A,et al. Colchicine for the treatment of COVID-19. Cochrane Database Syst Rev. 2021; 10(10):CD015045.

Does Colchicine require protection from light during storage?

Yes, it is highly photosensitive. Exposure to light causes rapid photodegradation, forming lumicolchicine isomers. Store in amber glass or opaque containers in complete darkness.

What is the recommended storage temperature for Colchicine?

Store at 2-8°C (refrigerated) for long-term stability. At room temperature, degradation accelerates, leading to loss of potency and increased impurity levels.

Is Colchicine susceptible to oxidation, and how is this prevented?

Yes, it can undergo oxidative demethylation. Our packaging includes nitrogen purging and oxygen absorbers to create an inert atmosphere during storage.

How is the impurity 3-demethylcolchicine monitored during stability studies?

This primary degradation product is specifically quantified using a stability-indicating HPLC method, ensuring it remains below ICH qualification thresholds.