Named Bioactive Compounds · Compound
Colchicine
Moderate Evidencecompound7 PubMed Studies
Hermetica Superfood Encyclopedia
Colchicine is an alkaloid derived from Colchicum autumnale that inhibits microtubule polymerization and neutrophil migration. It effectively treats acute gout attacks and prevents cardiovascular events through anti-inflammatory mechanisms.
Colchicine is a toxic alkaloid extracted primarily from Colchicum autumnale (autumn crocus), with concentrations ranging from 0.1% in flowers to 0.8% in bulbs and seeds. This tropolone-containing compound has the molecular formula C₂₂H₂₅NO₆ and is also found in Gloriosa superba (glory lily).
Colchicine has FDA approval since 1961 for acute gout treatment and prophylaxis, with multiple RCTs supporting its efficacy. The LoDoCo trial and extensions demonstrate potential cardiovascular benefits at low doses (0.5 mg daily) in post-MI patients. Note: Specific PubMed PMIDs were not provided in the search results.
Acute gout: 1.2 mg loading dose, then 0.6 mg hourly until relief (maximum 6 mg per flare). Gout prophylaxis: 0.5-1.2 mg daily. Familial Mediterranean Fever: 1-2 mg daily in divided doses. Cardiovascular prevention (emerging): 0.5 mg daily. Consult a healthcare provider before starting any new supplement.
Colchicine is a pharmaceutical alkaloid (C₂₂H₂₅NO₆, MW 399.44 g/mol), not a nutritional compound. It is a tricyclic tropane alkaloid originally derived from Colchicum autumnale (autumn crocus) and Gloriosa superba. It contains no macronutrients, vitamins, minerals, fiber, or protein of nutritional relevance. Key chemical features: • Active compound: Colchicine — a lipophilic alkaloid with three rings (trimethoxyphenyl ring A, seven-membered ring B, tropolone ring C with acetamide group). • Bioavailability: Oral bioavailability approximately 45% (range 24–88%), with rapid gastrointestinal absorption; peak plasma concentration (Cmax) reached in 0.5–2 hours. • Distribution: Large volume of distribution (~5–8 L/kg), extensive tissue binding, particularly to intracellular tubulin. Concentrates in leukocytes (especially neutrophils) at levels 16-fold higher than plasma. • Metabolism: Primarily hepatic via CYP3A4-mediated demethylation; also a substrate of P-glycoprotein (P-gp) efflux transporter. Major metabolite: 2-O-demethylcolchicine and 3-O-demethylcolchicine (both less active). • Elimination half-life: 20–40 hours in plasma; however, leukocyte half-life is substantially longer (~60 hours), contributing to prolonged pharmacodynamic effects. • Enterohepatic recirculation: Significant; 10–20% of dose excreted unchanged in urine, with biliary/fecal excretion accounting for a major elimination route. • Typical therapeutic doses: 0.5–1.2 mg/day for prophylaxis; 1.2 mg followed by 0.6 mg one hour later for acute gout flare. • Narrow therapeutic index: Toxic dose is close to therapeutic dose; doses exceeding 0.5 mg/kg can be fatal. • Natural source concentration: Colchicum autumnale corms contain approximately 0.1–0.8% colchicine by dry weight; seeds contain up to 0.4–1.2%. Gloriosa superba tubers contain 0.7–1.2%. • No caloric value, no essential nutrient content. This is strictly a pharmacologically active compound, not a food or dietary supplement.
Colchicine binds to tubulin and prevents microtubule polymerization, disrupting neutrophil chemotaxis and degranulation. This reduces inflammatory cell recruitment to affected tissues and decreases release of inflammatory mediators like IL-1β and TNF-α. The compound also inhibits NLRP3 inflammasome activation, providing broad anti-inflammatory effects.
Multiple randomized controlled trials demonstrate colchicine's efficacy for acute gout treatment, with 0.6-1.2 mg daily reducing pain by 50% within 24-48 hours. The COLCOT trial (4,745 patients) showed 0.5 mg daily reduced major cardiovascular events by 23% in post-myocardial infarction patients. Long-term prevention studies indicate 0.5-0.6 mg daily reduces gout flare frequency by 70-85% during urate-lowering therapy initiation. Evidence quality is strong for gout applications and moderate for cardiovascular benefits.
Common side effects include gastrointestinal upset (30-40% of users), diarrhea, and nausea, typically dose-dependent. Colchicine is metabolized by CYP3A4 and P-glycoprotein, requiring dose reduction with strong inhibitors like clarithromycin or cyclosporine. Contraindicated in severe renal or hepatic impairment due to accumulation risk and potential toxicity. Pregnancy category C with limited safety data, though short-term use may be acceptable when benefits outweigh risks.
3 documented interactions for Colchicine. Click any row to read the full explanation. Always consult your healthcare provider before combining supplements with medications.
Clarithromycin dramatically increases colchicine levels in your blood. Because colchicine has a very narrow safety margin, this combination has caused deaths, particularly in people with kidney or liver problems.
What to do: Do NOT take these together if you have any kidney or liver problems. If you have normal kidney and liver function and must take both, your colchicine dose needs to be drastically reduced.
Timing: Follow each medication's specific timing instructions. Clarithromycin — check if it requires an empty stomach or should be taken with food. Colchicine follows its normal schedule. Complete the full antibiotic course as prescribed.
Full interaction details →Grapefruit increases colchicine levels significantly. Colchicine toxicity can be fatal — it affects your bone marrow, muscles, and organs.
What to do: Avoid grapefruit entirely while taking colchicine. Colchicine toxicity has no specific antidote and can be fatal.
Timing: Be consistent with how you take Colchicine relative to meals — take it with food or without food consistently each day. Grapefruit — sudden large changes in diet composition can affect how your body processes many medications. Grapefruit, leafy greens, and high-fiber foods are the most common food-drug interaction culprits.
Full interaction details →Fluconazole can increase colchicine levels, and since colchicine has a very narrow safety margin, this raises the risk of serious side effects including multi-organ failure.
What to do: If you take colchicine and need fluconazole, your doctor should reduce your colchicine dose. Report any severe nausea, vomiting, or diarrhea immediately.
Timing: Take Fluconazole as directed (some require food for absorption, others an empty stomach — check the label). Azole antifungals are potent CYP enzyme inhibitors that can dramatically increase blood levels of many medications. Colchicine levels should be monitored during antifungal treatment.
Full interaction details →Educational information only. Always consult a qualified healthcare provider before changing your supplement or medication regimen.
