Brand names:Gloperba,Lodoco,Mitigare
Drug class: Cardiovascular Drugs, Nonsteroidal Anti-inflammatory

Medically reviewed by Drugs.com on Feb 10, 2026. Written byASHP.

Introduction

Antigout, anti-inflammatory, and antimitotic agent.

Uses for Colchicine

Gout Flare

Colchicine 0.6 mg tablets are used for prophylaxis and treatment of acute gout flares in adults; capsules and oral solution used only for prophylaxis of gout flares in adults.

The American College of Rheumatology (ACR) recommends colchicine, nonsteroidal anti-inflammatory agent (NSAIAs), or glucocorticoids as first-line therapy for the treatment of gout flares.

For gout prophylaxis, ACR recommends urate-lowering therapy, with allopurinol as the preferred first-line agent. Anti-inflammatory prophylaxis (e.g., colchicine, NSAIAs, glucocorticoids) is recommended when initiating urate-lowering therapy, with continuation for at least 3 to 6 months.

Familial Mediterranean Fever

Colchicine 0.6 mg tablets are used in the management of Familial Mediterranean Fever (FMF) in adults and children ≥4 years of age.

Colchicine is recommended as the mainstay of therapy for FMF, with initiation of therapy as soon as a diagnosis of FMF is made. For patients who are adherent to colchicine therapy and at maximally tolerated dose who do not respond adequately, a disease-modifying antirheumatic drug (DMARDs, preferably an IL-1 inhibitor) can be added to treatment.

Prevention of Cardiovascular Events

Colchicine 0.5 mg tablets are used to reduce the risk of MI, stroke, coronary revascularization, and cardiovascular death in patients with atherosclerotic disease or with multiple risk factors for cardiovascular disease.

Recommendations for management of patients with chronic coronary disease (CCD) include lifestyle modifications, lipid management, and BP and blood glucose control. Antiplatelet agents, beta-blockers, ACE inhibitors, and/or angiotensin II receptor antagonists are recommended for secondary prevention of major cardiovascular events in patients with CCD or at high risk.

Colchicine is also recommended for secondary prevention of cardiovascular events in patients with CCD; however, use is limited to patients who remain at very high risk despite use of guideline-directed medical therapy.

Acute or Recurrent Pericarditis

Colchicine has been used for treatment of acute or recurrent pericarditis^{† [off-label]}.

Anti-inflammatory therapy is recommended as the mainstay of treatment for acute or recurrent pericarditis. Anti-inflammatory therapies include NSAIAs, usually ibuprofen or indomethacin while aspirin is preferred in patients with coronary artery disease. Colchicine is recommended in patients with acute or recurrent pericarditis in addition to aspirin or an NSAIA.

Post-pericardiotomy Syndrome Prophylaxis

Colchicine has been used in the prevention of post-pericardiotomy syndrome (PPS)^{† [off-label]}.

Guidelines state that colchicine may be considered after cardiac surgery for prevention of PPS with treatment continued for 30 days. An expert review on PPS from the American College of Cardiology (ACC) suggest pretreatment with colchicine may be effective only in select patients at high risk for developing PPS.

Calcium Pyrophosphate Deposition Disease

Colchicine has been used in the treatment of calcium pyrophosphate deposition (CPPD) disease, formerly referred to as pseudogout^{† [off-label]} .

Guidelines on the management of CPPD disease include colchicine and NSAIAs as treatment options for acute episodes, as well as for prevention of frequent recurrent episodes. However, use of either agent may be limited by their side effect profiles and evidence for use is primarily extrapolated from studies on treatment of acute gout flares.

Recurrent Aphthous Stomatitis and Behçet Syndrome

Colchicine has been used for treatment of recurrent oral ulcers, including recurrent aphthous stomatitis (RAS)^{† [off-label]} and oral ulcers associated with Behçet syndrome^{† [off-label]} .

Treatment options for RAS include topical corticosteroids, anti-infective mouthrinses, topical antibiotics, and topical anesthetics. For patients not responding to topical agents or for more severe cases, systemic therapies include corticosteroids (e.g., prednisone) and immunomodulators (e.g., levamisole, colchicine, and dapsone).

For treatment of mucocutaneus lesions associated with Behçet Syndrome, topical treatment, such as topical corticosteroids, is recommended. For prevention of recurrent mucocutaneus lesions, colchicine is recommended. Additional agents such as azathioprine, thalidomide, interferon-alpha, TNF-alpha inhibitors, or apremilast may be considered for select patients.

Colchicine Dosage and Administration

General

Patient Monitoring

• Monitor for colchicine toxicity and, if present, consider temporary interruption or discontinuation.

• Monitor patients with hepatic or renal impairment closely for adverse effects of colchicine. Monitor closely for colchicine toxicity in patients undergoing hemodialysis.

• Monitor closely for signs of toxicity in patients receiving medications that are inhibitors of cytochrome P-450 (CYP) isoenzyme 3A4 and/or the P-gp transport system.

• Monitor for GI side effects in infants of nursing mothers receiving colchicine oral solution.

Dispensing and Administration Precautions

• The 2023 American Geriatrics Society (AGS) Beers Criteria for Potentially Inappropriate Medication (PIM) Use in Older Adults includes colchicine and probenecid on the list of PIMs that are best avoided by older adults in most circumstances or under specific situations, such as certain diseases, conditions, or care settings. The criteria are intended to apply to adults ≥65 years of age in all ambulatory, acute, and institutional settings of care, except hospice and end-of-life care settings. For colchicine, the Beers Criteria Expert Panel specifically recommends to reduce the dosage and monitor for adverse effects (GI, neuromuscular, bone marrow toxicity) in geriatric patients with creatinine clearance (Cl_cr) <30 mL/min; probenecid should be avoided in geriatric patients with Cl_cr<30 mL/min due to loss of effectiveness.

• The Institute for Safe Medication Practices (ISMP) includes colchicine and Cortrosyn (cosyntropin) on their List of Confused Drug Names and recommends using special safeguards to ensure the accuracy of prescriptions for these medications.

Other General Considerations

• Administer prophylactic doses of colchicine before initiation of allopurinol or uricosurics because sudden changes in serum urate concentrations may precipitate acute gout flare. Prophylactic therapy may be beneficial for at least the first 6 months of uric acid-lowering therapy.

• Consider the potential for drug-drug interactions, especially with CYP3A4 and/or P-gp inhibitors, prior to and during treatment with colchicine.

Administration

Oral Administration

Available as tablets or oral capsules (Mitigare) containing 0.6 mg, oral solution (Gloperba) containing 0.12 mg/mL, and tablets (Lodoco) containing 0.5 mg.

Colchicine 0.5 mg is also commercially available in a fixed-dose tablet combination with probenecid 500 mg; refer to full prescribing information for administration of the combination product.

Colchicine 0.6 mg tablets and capsules, and the oral suspension are administered without regard to meals.

Initiate therapy with colchicine 0.6 mg tablets for acute gout flare at the first sign of an attack.

Provide patients with specific instructions to follow in case a dose of colchicine is missed; instructions differ based on formulation and indication.

Dosage

Dosage of 0.6 mg tablet depends on patient age, renal and hepatic function, and recent (within 14 days) or concomitant use of moderate or strong CYP3A4 inhibitors or inhibitors of the P-gp transport system.

Refer to full prescribing information for dosing of the colchicine/probenecid combination product.

Pediatric Patients

Prophylactic Treatment of Recurrent Gout Flares

Oral

Solution— Adolescents ≥16 years of age: 0.6 mg (5 mL) once or twice daily. The maximum recommended dosage is 1.2 mg daily. Prophylactic therapy may be beneficial for at least the first 6 months of uric acid-lowering therapy.

Tablet (0.6 mg)— Adolescents ≥16 years of age may receive adult dosages (see Table 4).

Familial Mediterranean Fever

Oral

Tablet (0.6 mg)— Recommended dosage in children not receiving concomitant therapy with a moderate or strong CYP3A4 inhibitor or a P-gp inhibitor depends on child’s age (see Table 1). See Table 2 for recommended dosage for patients receiving or who have recently received (within 14 days) a moderate or strong CYP3A4 inhibitor or P-gp inhibitor.

Dosage can be increased in increments of 0.3 mg daily to the maximum recommended dosage or decreased in decrements of 0.3 mg daily in individuals who develop intolerable adverse effects.

These maximum recommended dosages are intended for individuals for whom a dosage range of 1.2–2.4 mg daily would be appropriate in the absence of interacting medications (i.e., adolescents >12 years of age); manufacturer makes no specific recommendations regarding maximum colchicine dosage in children 4–12 years of age who are receiving CYP3A4 or P-gp inhibitors.

Adults

Treatment of Acute Gout Flare

Oral

Tablet (0.6 mg)— Recommended dosage of colchicine depends on whether patient is currently receiving, or has received within the past 14 days, a moderate or strong CYP3A4 inhibitor or a P-gp inhibitor (see Table 3).

Use of colchicine for gout flare is not recommended in patients receiving colchicine for prevention of gout flare and also receiving a CYP3A4 inhibitor.

Do not repeat courses of colchicine therapy (see Table 3) until 3 days have elapsed.

Prophylactic Treatment of Recurrent Gout Flares

Oral

Capsule— 0.6 mg once or twice daily. The maximum recommended dosage is 1.2 mg daily.

Solution— 0.6 mg (5 mL) once or twice daily. The maximum recommended dosage is 1.2 mg daily. Prophylactic therapy may be beneficial for at least the first 6 months of uric acid-lowering therapy.

Tablet (0.6 mg) - Recommended dosage of colchicine depends on whether patient is currently receiving or has received within the past 14 days, a moderate or strong CYP3A4 inhibitor or a P-gp inhibitor (see Table 4).

Familial Mediterranean Fever

Oral

Tablet (0.6 mg)— Recommended dosage of colchicine depends on whether patient is currently receiving or has received within the past 14 days, a moderate or strong CYP3A4 inhibitor or a P-gp inhibitor (see Table 5).

Dosage can be increased in increments of 0.3 mg daily to the maximum recommended dosage or decreased in decrements of 0.3 mg daily in individuals who develop intolerable adverse effects.

Prevention of Cardiovascular Events

Oral

Tablet (0.5 mg)— 0.5 mg orally once daily.

Acute or Recurrent Pericarditis†

Oral

Acute pericarditis: Some experts recommend 0.5–1.2 mg daily administered once or in 2 divided doses based on weight for 3 months. European experts recommend 0.5 mg once daily for patients <70 kg or 0.5 mg twice daily for patients ≥70 kg, continued for 3 months. Tapering dosage not mandatory; however, if desired, administer 0.5 mg every other day for patients <70 kg or 0.5 mg once daily for patients ≥70 kg in the last weeks.

Recurrent pericarditis: Some experts recommend 0.5–1.2 mg daily administered once or in 2 divided doses based on weight for ≥6 months. European experts recommend 0.5 mg twice daily, or once daily for patients <70 kg or who are intolerant to higher doses, continued for ≥6 months. Tapering dosage not necessary; however, if desired, administer 0.5 mg every other day for patients <70 kg or 0.5 mg once daily for patients ≥70 kg in the last weeks.

Post-pericardiotomy Syndrome†

Oral

European experts recommend 0.5 mg once daily for patients ≤70 kg or 0.5 mg twice daily for patients >70 kg, without a loading dose, continued for 1 month.

Calcium Pyrophosphate Deposition Disease†

Oral

Treatment of acute calcium pyrophosphate crystal arthritis: European experts recommend 0.5 mg up to 3–4 times daily with or without initial dose of 1 mg.

Prophylaxis against frequent, recurrent acute calcium pyrophosphate crystal arthritis: European experts recommend 0.5–1 mg daily.

Recurrent Aphthous Stomatitis†

Oral

Some experts recommend stepwise dosing of 0.5 mg daily up to 1.8 mg per day.

Special Populations

Hepatic Impairment

Capsule: Consider dosage reduction or alternatives for prophylaxis of gout flares in patients with severe hepatic impairment.

Do not use in patients with hepatic impairment receiving medications that inhibit both CYP3A4 and P-gp. Do not use in patients with both hepatic and renal impairment.

Oral solution: Dosage adjustment not required for prophylaxis of gout flares in patients with mild to moderate hepatic function impairment; however, monitor closely for adverse effects. Consider dosage reduction for prophylaxis of gout flares in patients with severe hepatic impairment.

Do not use in patients with hepatic impairment receiving medications that inhibit both CYP3A4 and P-gp. Do not use in patients with both hepatic and renal impairment.

Tablet (0.5 mg): Contraindicated in severe hepatic impairment.

Contraindicated in patients with any degree of hepatic impairment and receiving strong or moderate CYP3A4 inhibitors or P-gp inhibitors. Monitor patients with any degree of hepatic impairment for adverse effects.

Tablet (0.6 mg): Contraindicated in patients with hepatic impairment who are receiving or have recently received a strong CYP3A4 or P-gp inhibitor.

Treatment of Gout Flare—

Use of colchicine for gout flare is not recommended in patients with hepatic impairment who are receiving the medication for prevention of gout flares.

Mild to moderate hepatic impairment: Dosage adjustment is not needed. Monitor closely for adverse effects.

Severe hepatic impairment: Dosage adjustment is not needed Do not repeat courses of colchicine until 2 weeks have elapsed. Consider alternative therapy for patients requiring treatment.

Prophylactic Treatment of Recurrent Gout Flares —

Mild to moderate hepatic impairment: Dosage adjustment is not needed. Monitor for adverse effects.

Severe hepatic impairment: Consider dosage reduction.

Familial Mediterranean Fever —

Mild to moderate hepatic impairment: Dosage adjustment is not needed. Monitor for adverse effects.

Severe hepatic impairment: Consider dosage reduction.

Renal Impairment

Capsule: Consider dosage reduction or alternatives for prophylaxis of gout flares in patients with severe renal impairment.

Do not use in patients with renal impairment receiving medications that inhibit both CYP3A4 and P-gp. Do not use in patients with both renal and hepatic impairment.

Oral solution: Dosage adjustment is not required for prophylaxis of gout flares in mild (eGFR 60–89 mL/min) to moderate (eGFR 30–59 mL/min) renal impairment; however, monitor closely for adverse effects.

Severe impairment (eGFR 15–29 mL/min): Starting dosage should be 0.3 mg (2.5 mL) per day; perform any increase in dosage with close monitoring.

Patients undergoing dialysis: Starting dosage for prophylaxis of gout flares should be 0.3 mg (2.5 mL) administered twice weekly with close monitoring.

Do not use in patients with renal impairment receiving medications that inhibit both CYP3A4 and P-gp. Do not use in patients with both renal and hepatic impairment.

Tablet (0.5 mg): Contraindicated in renal failure (Cl_cr <15 mL/minute).

Avoid use in patients with moderate renal impairment who are receiving moderate CYP3A4 inhibitors. Monitor patients with renal impairment for adverse effects.

Contraindicated with concurrent strong CYP3A4 or P-gp inhibitors, including in patients with renal impairment.

Tablet (0.6 mg): Contraindicated in patients with renal impairment who are receiving or have recently received therapy with a strong CYP3A4 or P-gp inhibitor.

Treatment of Gout Flare—

Use of colchicine for gout flare not recommended in patients with renal impairment who are receiving colchicine for prevention of gout flares.

Mild to moderate renal impairment (Cl_cr50–80 or 30–50 mL/minute, respectively): Dosage adjustment not needed. Monitor for adverse effects.

Severe renal impairment (Cl_cr <30 mL/minute): Dosage adjustment is not needed. Do not repeat courses of colchicine therapy until 2 weeks have elapsed. Consider alternative therapy for patients requiring treatment.

Dialysis: 0.6 mg at first sign of gout flare. Do not repeat courses of colchicine therapy until 2 weeks have elapsed.

Prophylactic Treatment of Recurrent Gout Flares —

Mild to moderate renal impairment (Cl_cr 50–80 or 30–50 mL/minute, respectively): Dosage adjustment not needed. Monitor for adverse effects.

Severe renal impairment (Cl_cr <30 mL/minute): Initial dosage is 0.3 mg daily; monitor closely if dosage is increased.

Dialysis: Initial dosage is 0.3 mg twice weekly; monitor closely.

Familial Mediterranean Fever —

Mild to moderate renal impairment (Cl_cr 50–80 or 30–50 mL/minute, respectively): Monitor for adverse effects. Dosage adjustment may be needed.

Severe renal impairment (Cl_cr <30 mL/minute) or dialysis: Initial dosage is 0.3 mg daily; dosage can be increased with careful monitoring.

Geriatric Patients

Capsule: Consider dosage reduction because of age-related decreases in renal function and concomitant disease and medication therapy observed in geriatric patients.

Oral solution: Select dosage with caution because of age-related decreases in renal function and concomitant disease and drug therapy observed in geriatric patients.

Tablet (0.5 mg): The manufacturer makes no specific dosage recommendations. Since geriatric patients are more likely to have decreased renal function, it may be useful to monitor renal function.

Tablet (0.6 mg): Select dosage with caution because of age-related decreases in renal function and concomitant disease and drug therapy observed in geriatric patients.

Cautions for Colchicine

Contraindications

• Contraindications with the 0.6 mg Tablets

• Patients with hepatic or renal impairment who are receiving strong CYP3A4 (including all protease inhibitors except fosamprenavir) or P-gp inhibitors; fatal or life-threatening colchicine toxicity has occurred in such patients.

• Contraindications with the 0.5 mg Tablets

• Concurrent use of strong CYP3A4 or P-gp inhibitors, including in patients with hepatic or renal impairment; fatal or life-threatening colchicine toxicity has occurred in such patients.

• Renal failure (Cl_cr <15 mL/minute).

• Severe hepatic impairment.

• Pre-existing blood dyscrasias.

• Hypersensitivity to the medication or any inactive ingredient.

• Contraindications with the Capsules

• Patients with hepatic or renal impairment who are receiving colchicine with concomitant use of CYP3A4 and P-gp inhibitors; fatal or life-threatening colchicine toxicity has occurred in such patients.

• Both hepatic and renal impairment.

• Contraindications with the Oral Solution

• Oral solution: Patients with hepatic or renal impairment who are receiving colchicine with concomitant use of CYP3A4 and P-gp inhibitors; fatal or life-threatening colchicine toxicity has occurred in such patients.

• Both hepatic and renal impairment.

Warnings/Precautions

Blood Dyscrasias

Myelosuppression, leukopenia, granulocytopenia, thrombocytopenia, pancytopenia, and aplastic anemia reported. These blood dyscrasias can be life-threatening or fatal.

The risk of development of blood dyscrasias is increased with concomitant use of medications that reduce the metabolism of colchicine or the presence of hepatic or renal impairment. New GI symptoms should prompt evaluation for colchicine toxicity.

Neuromuscular Toxicity

Neuromuscular toxicity and rhabdomyolysis are reported with long-term use. Individuals with renal impairment and geriatric individuals are at increased risk.

Concomitant use of certain medications may increase the risk of myotoxicity.

If patient develops signs of neuromuscular toxicity during treatment with colchicine, discontinue colchicine therapy, investigate other causes, and treat appropriately.

Fatal Overdosage

Fatal overdoses, both accidental and intentional, have been reported in adults and children.

Keep out of the reach of children.

Drug Interactions

Drug interactions, including life-threatening and fatal cases, have been reported with concomitant use with CYP3A4 and/or P-gp inhibitors.

Consider potential for serious drug-drug interactions prior to and during colchicine therapy. Concomitant use with certain medications is contraindicated or requires particular caution.

Use of Fixed Combination

When colchicine is used in a fixed-dose combination with probenecid, consider the cautions, precautions, and contraindications associated with probenecid.

Specific Populations

Pregnancy

Available data in humans have not identified risks for major birth defects, miscarriage, or adverse maternal or fetal outcomes. Colchicine crosses the placenta in humans. Animal reproduction and development studies have reported embryofetal toxicity, teratogenic effects, and altered postnatal development. The effect on labor and delivery is not known.

Use during pregnancy only if potential benefits outweigh risks. Advise females of child bearing potential to contact their clinician if they become pregnant while taking colchicine.

Lactation

Colchicine is distributed into milk. No adverse events in breastfed infants have been reported following administration to lactating females. However, colchicine may affect GI cell turnover and function, leading to GI or other unknown adverse effects. There are no data on effects on milk production.

The manufacturer states colchicine oral solution is safe during breastfeeding.

Consider developmental and health benefits of breastfeeding along with the mother’s clinical need for colchicine and any potential adverse effects on breastfed child from colchicine or underlying maternal condition.

Females and Males of Reproductive Potential

There are no adequate and well-controlled studies of the effects of colchicine on fertility. Infertility in males reported; may be reversible. Studies have not established a clear relationship between colchicine use and female infertility.

Since the progression of FMF without treatment may result in infertility, weigh the use of colchicine 0.6 mg tablets against potential risks.

Advise females and males of reproductive potential who intend to have children and are receiving colchicine oral solution to contact their clinician before attempting to become pregnant.

Advise females of reproductive potential, and males with partners of reproductive potential, receiving colchicine oral solution and who do not want to become pregnant to use an effective form of contraception.

Pediatric Use

The safety and efficacy of colchicine is not yet established for gout.

The safety and efficacy of 0.6 mg tablets for FMF in children was evaluated in uncontrolled studies. Long-term use did not appear to affect growth in children with FMF.

The safety and efficacy of 0.5 mg tablets in children not established.

Geriatric Use

Clinical studies of colchicine 0.6 mg tablets and oral solution did not include sufficient numbers of patients ≥65 years of age to determine whether geriatric patients respond differently than younger patients.

In clinical studies of colchicine 0.5 mg tablets, no overall differences in safety or effectiveness was observed between geriatric and younger patients. Other reported clinical experience has not identified differences in responses between geriatric and younger patients; however, greater sensitivity of some older individuals cannot be excluded. Monitor renal function in geriatric patients.

Select dosage carefully in geriatric patients with gout; consider the greater frequency of decreased renal function and of concomitant disease and medication therapy observed in geriatric patients.

Hepatic Impairment

Substantial interpatient variability in IV colchicine pharmacokinetics. Decreased clearance and prolonged half-life has been observed in some patients with mild to moderate cirrhosis; however, there are no consistent trends observed in those with primary biliary cirrhosis.

Monitor patients with hepatic impairment closely for adverse effects.

Renal Impairment

Clearance of colchicine and its metabolites is decreased in patients with renal impairment.

End-stage renal disease requiring dialysis: Colchicine clearance is decreased by 75%.

Monitor patients with renal impairment closely for adverse effects. Monitor closely for colchicine toxicity in patients undergoing hemodialysis.

Common Adverse Effects

Most common adverse effects are GI symptoms (nausea, abdominal discomfort/pain, vomiting, and/or diarrhea) and myalgia. Pharyngolaryngeal pain also commonly reported with treatment of gout flares.

Drug Interactions

Metabolized by CYP3A4. Does not inhibit or induce CYP isoenzymes 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, or 3A4.

P-gp substrate.

Commercially available in a fixed-dose combination tablet with probenecid; refer to full prescribing information for drug interactions with the combination product.

Drugs Affecting Hepatic Microsomal Enzymes

CYP3A4 inhibitors: Concomitant use with strong CYP3A4 inhibitors (e.g., atazanavir, clarithromycin, darunavir/ritonavir, indinavir, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, or tipranavir/ritonavir), or with moderate CYP3A4 inhibitors (e.g., amprenavir, aprepitant, diltiazem, erythromycin, fluconazole, fosamprenavir, grapefruit juice, verapamil), may result in substantially increased colchicine plasma concentrations.

Fatal drug interactions reported with concomitant use of a dual inhibitor of CYP3A4 and P-gp (i.e., clarithromycin). Toxicities also reported when used concomitantly with CYP3A4 inhibitors that may not be strong P-gp inhibitors (e.g., grapefruit juice, erythromycin, verapamil), or P-gp inhibitors that may not be strong CYP3A4 inhibitors (e.g., cyclosporine).

Colchicine capsules: Avoid concomitant use with CYP3A4 inhibitors (e.g., clarithromycin, ketoconazole, grapefruit juice, erythromycin, verapamil). If concomitant therapy is necessary, reduce colchicine dosage or dosing frequency and monitor carefully for colchicine toxicity. Do not administer colchicine capsules with medications that inhibit both CYP3A4 and P-gp in patients with hepatic or renal impairment.

Colchicine oral solution: Avoid concomitant use with CYP3A4 inhibitors. If concomitant therapy is necessary, consider reducing daily dosage of colchicine; monitor carefully for colchicine toxicity. Do not administer colchicine oral solution with medications that inhibit both CYP3A4 and P-gp in patients with hepatic or renal impairment.

Colchicine 0.6 mg tablets: If concomitant therapy is necessary, adjust the colchicine dosage if patient is currently receiving, or has received within the last 14 days, a moderate or strong CYP3A4 inhibitor (dosage recommendation varies based on indication). Colchicine treatment may need to be interrupted if used concomitantly with a strong CYP3A4 inhibitor. Concomitant use of colchicine and strong CYP3A4 inhibitors is contraindicated in hepatic or renal impairment.

Colchicine 0.5 mg tablets: Concomitant use with a strong CYP3A4 inhibitor is contraindicated. In patients receiving a moderate CYP3A4 inhibitor, monitor for signs of colchicine toxicity; avoid concomitant use with a moderate CYP3A4 inhibitor in patients with hepatic or renal impairment.

Drugs Affecting P-gp Transport

P-gp inhibitors: Concomitant use with P-gp inhibitors (e.g., cyclosporine, ranolazine) results in substantially increased colchicine plasma concentrations.

Fatal drug interactions have been reported with concomitant use with dual inhibitors of CYP3A4 and P-gp (i.e., clarithromycin). Toxicities have also been reported when used concomitantly with CYP3A4 inhibitors that may not be strong P-gp inhibitors (e.g., grapefruit juice, erythromycin, verapamil), or P-gp inhibitors that may not be strong CYP3A4 inhibitors (e.g., cyclosporine).

Colchicine capsules: Avoid concomitant use with P-gp inhibitors (e.g., clarithromycin, ketoconazole, cyclosporine). If concomitant therapy is necessary, reduce colchicine dosage or dosing frequency; monitor carefully for colchicine toxicity. Do not administer colchicine capsules with medications that inhibit both CYP3A4 and P-gp in patients with hepatic or renal impairment.

Colchicine oral solution: Avoid concomitant use with P-gp inhibitors. If concomitant therapy is necessary, consider reducing colchicine daily dosage; monitor carefully for colchicine toxicity. Do not administer colchicine oral solution with medications that inhibit both CYP3A4 and P-gp in patients with hepatic or renal impairment.

Colchicine 0.6 mg tablets: If concomitant therapy with a P-pg inhibitor is required, adjust colchicine dosage if patient is currently receiving or has received within the past 14 days a P-gp inhibitor; dosage recommendation varies based on indication. Colchicine treatment may need to be interrupted if used concomitantly with a strong P-gp inhibitor. Concomitant use of colchicine and P-gp inhibitors is contraindicated in patients with hepatic or renal impairment.

Colchicine 0.5 mg tablets: Concomitant use with a strong P-gp inhibitor is contraindicated.

Specific Drugs

Colchicine Pharmacokinetics

Absorption

Bioavailability

Absolute bioavailability about 45%.

Mean peak plasma concentrations occur in 1–2 hours after single dose under fasting conditions.

Following oral administration of 0.6 mg twice daily for 10 days, mean peak plasma concentration are reached at 1.3–1.4 hours.

Following administration of single dose of capsule, peak plasma concentrations are reached in 1.3 hours.

Following administration of single dose of oral solution, peak plasma concentrations are reached in 1 hour under fasting conditions.

Following administration of single dose of 0.5 mg tablet, peak plasma concentrations are reached in 1 hour and 1.7 hours under fasting and fed conditions, respectively.

Enterohepatic circulation may occur; secondary peak may be present in some individuals 3–36 hours after the dose.

Exhibits linear pharmacokinetics within dosage range of 0.5–1.5 mg.

Food

Administration with food did not affect rate of absorption, but decreased extent of absorption by 15%; not clinically important.

Slight decrease in peak plasma concentration was observed when oral solution was administered following high-fat, high-calorie meal; however, overall extent of absorption based on AUC similar in fed and fasted conditions.

No significant effect observed following administration of 0.5 mg tablet with a high-fat, high-calorie meal.

Distribution

Extent

Following reabsorption, colchicine is rapidly removed from plasma and distributed to various tissues.

High concentrations of colchicine are found in leucocytes, kidneys, liver, and spleen.

Colchicine crosses the placenta.

Colchicine is distributed into breast milk.

Colchicine crosses the blood-brain barrier and can accumulate in brain.

Plasma Protein Binding

39% (mainly albumin).

Elimination

Metabolism

Demethylated in the liver by CYP3A4.

Glucuronidation is also believed to be metabolic pathway.

P-gp efflux is postulated to have important role in colchicine disposition.

Elimination Route

40–65% recovered unchanged in urine.

Enterohepatic circulation and biliary excretion may occur.

Not removed by hemodialysis.

Half-life

26.6–31.2 hours in healthy young adults receiving colchicine 0.6 mg orally twice daily.

31 hours following administration of capsules and oral suspension in healthy adults.

19 hours following administration of single oral dose of colchicine 0.5 mg daily in healthy volunteers.

Stability

Storage

Oral

Capsules

Store at 20–25°C. Protect from light and moisture.

Solution

Store at 20–25°C (excursions permitted to 15–30°C).

Tablets

0.5 mg tablets: Store at 20–25°C (excursions permitted to 15–30°C). Store in original package to protect from light

0.6 mg tablets: Store at 20–25°C. Protect from light. Dispense in tight, light-resistant container.

Colchicine Mechanism of Action

• Mechanism of principal (antigout) effect not completely known; effectiveness postulated to be due to ability to block neutrophil-mediated inflammatory responses induced by monosodium urate crystals in synovial fluid.

• Appears to disrupt cytoskeletal functions through inhibition of β-tubulin polymerization into microtubules thus preventing activation, degranulation, and migration of neutrophils believed to mediate some gout symptoms.

• May interfere with intracellular assembly of inflammasome complex in neutrophils and monocytes that mediates activation of interleukin-1β.

• Anti-inflammatory effects are consistent with clinical data showing that colchicine reduces high sensitivity C-reactive protein.

• Mechanism of beneficial effects in FMF or in the prevention of major cardiovascular events not fully elucidated.

Advice to Patients

• Advise patients to read the FDA-approved patient labeling (Medication Guide).

• Advise patients to take colchicine as prescribed and to not alter the dosage or discontinue treatment without consulting their clinician. Instruct patients on how to resume colchicine therapy if a dose of colchicine is missed; instructions vary based on colchicine formulation and indication.

• Advise patients of the risk of overdose, which can be fatal. Instruct patients to keep colchicine out of the reach of children.

• Advise patients of the risk for bone marrow depression with agranulocytosis, aplastic anemia, and thrombocytopenia.

• Advise patients of the risk and signs of neuromuscular toxicity (e.g., muscle pain or weakness, tingling or numbness in fingers or toes) when colchicine is used alone or in combination with certain other medications. Inform patients to discontinue colchicine and seek immediate medical attention if they develop signs and symptoms of neuromuscular toxicity.

• Advise patients to inform a clinician if they experience persistent moderate or severe GI symptoms (e.g., abdominal pain, nausea, vomiting or diarrhea), either when taking colchicine or when a new medication is taken with colchicine, since these may be a sign of acute or early colchicine toxicity.

• Advise patients to inform their clinician of existing or contemplated concomitant therapy, including prescription and OTC medications and dietary or herbal supplements, as well as any concomitant illnesses. Advise patients that grapefruit and grapefruit juice may interact with colchicine and should not be used during treatment.

• Advise females of child bearing potential to inform clinicians if they are or plan to become pregnant or plan to breast-feed.

• Advise males of reproductive potential that colchicine may rarely and transiently impair fertility.

• Advise patients of other important precautionary information.

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to theASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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Related/similar drugs

Frequently asked questions

• Can Colchicine be used to treat COVID-19 (coronavirus)?

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