Colchicine: Targeted Relief for Gout and Acute Inflammation
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Synonyms | |||
Colchicine is a time-tested, orally administered medication derived from the autumn crocus (Colchicum autumnale). It is a first-line therapeutic agent for the treatment and prophylaxis of acute gout flares and Familial Mediterranean Fever (FMF). Its primary mechanism of action involves binding to tubulin, inhibiting microtubule polymerization, which subsequently disrupts neutrophil migration, phagocytosis, and the inflammatory response central to gouty arthritis. This profile provides a comprehensive, evidence-based overview for healthcare professionals.
Features
- Active Ingredient: Colchicine.
- Pharmacologic Class: Anti-gout agent, microtubule inhibitor.
- Available Forms: Oral tablets (typically 0.6 mg).
- Mechanism of Action: Binds to tubulin, inhibiting microtubule assembly and neutrophil motility and activity.
- Bioavailability: Approximately 45%; significant first-pass metabolism.
- Half-life: Approximately 27-31 hours; prolonged in patients with hepatic or renal impairment.
- Primary Excretion: Biliary and fecal; ~10-20% renal.
Benefits
- Rapid Onset of Action: Effectively reduces the pain, swelling, and erythema associated with acute gout attacks when administered within 36 hours of symptom onset.
- Prophylactic Efficacy: Low-dose regimens significantly reduce the frequency and severity of subsequent gout flares, particularly during the initiation of urate-lowering therapy.
- Disease-Modifying for FMF: Prevents attacks and the development of systemic amyloidosis in patients diagnosed with Familial Mediterranean Fever.
- Non-NSAID/Narcotic Option: Provides a potent anti-inflammatory alternative for patients with contraindications to NSAIDs or opioids.
- Well-Established Safety Profile: When dosed appropriately and with careful patient selection, the risk-benefit profile is favorable for its indicated uses.
Common use
Colchicine is FDA-approved for the treatment of acute gout flares and for the prophylaxis of gout flares. It is also approved for the treatment of Familial Mediterranean Fever. Its use is predicated on a confirmed diagnosis. Off-label uses include the treatment and prevention of pericarditis, Behçet’s disease, and other crystal-induced arthropathies, though these applications require careful clinical judgment and monitoring.
Dosage and direction
Dosing is critically important due to colchicine’s narrow therapeutic index. Dosing must be adjusted for renal and hepatic function, age, and concomitant medications.
- Acute Gout Flare:
- Loading Dose: 1.2 mg (two 0.6 mg tablets) at first sign of flare.
- Followed by: 0.6 mg one hour later.
- Maximum Total Course Dose: 1.8 mg over 1 hour. Do not repeat for at least three days.
- Gout Flare Prophylaxis:
- Standard Dose: 0.6 mg once or twice daily.
- Maximum Prophylactic Dose: 0.6 mg twice daily. Dose reduction is required in patients with renal or hepatic impairment.
- Familial Mediterranean Fever (FMF):
- Adults: 1.2 to 2.4 mg daily, administered in one or two divided doses.
- Pediatric dosing is weight-based and must be carefully calculated. The dose may be increased or decreased by 0.3 mg per day based on efficacy and tolerability.
Administration: Take with or without food. However, GI upset may be minimized if taken with food.
Precautions
- Hepatic Impairment: Use with extreme caution. Patients with hepatic impairment are at increased risk of toxicity. Dose reduction is mandatory; consider alternative therapy in severe impairment.
- Renal Impairment: Use is contraindicated in patients with severe renal impairment (eGFR <30 mL/min). In patients with mild to moderate impairment (eGFR 30-80 mL/min), dose reduction, extended dosing intervals, and heightened monitoring for adverse effects are required.
- Elderly Patients: Increased susceptibility to myelosuppression, myopathy, and neuropathy. Use the lowest effective dose and monitor closely.
- Blood Monitoring: Periodic monitoring of complete blood count (CBC) and creatine phosphokinase (CPK) is advised during chronic therapy.
- P-Glycoprotein (P-gp) Inhibitors: Concomitant use is a major precaution (see Drug Interactions).
Contraindications
Colchicine is contraindicated in patients with:
- Severe renal impairment (eGFR <30 mL/min).
- Severe hepatic impairment.
- Known hypersensitivity to colchicine or any component of the formulation.
- Concomitant use of potent P-glycoprotein (P-gp) or strong CYP3A4 inhibitors in patients with renal or hepatic impairment, due to the high risk of fatal overdose.
Possible side effect
Adverse effects are often dose-dependent and more common with acute dosing.
- Very Common (>10%): Gastrointestinal effects including diarrhea, nausea, vomiting, and abdominal pain.
- Common (1-10%): Pharyngolaryngeal pain.
- Uncommon (<1%): Myelosuppression (neutropenia, thrombocytopenia, aplastic anemia), myotoxicity (myopathy, rhabdomyolysis, elevated CPK), peripheral neuropathy.
- Rare: Alopecia, dermatological reactions, hepatotoxicity.
Drug interaction
Colchicine is a substrate for both CYP3A4 and P-glycoprotein (P-gp). Concomitant use with inhibitors of these pathways can lead to a profound and dangerous increase in colchicine plasma levels.
- Strong CYP3A4/P-gp Inhibitors (CONTRAINDICATED in renal/hepatic impairment; require dose reduction/prohibition in others): Clarithromycin, ketoconazole, itraconazole, ritonavir, cyclosporine.
- Moderate/Weak CYP3A4/P-gp Inhibitors (Use with caution; dose reduction likely needed): Verapamil, diltiazem, erythromycin, grapefruit juice.
- Statins and Fibrates: Increased risk of myopathy and rhabdomyolysis.
- CNS Depressants: Potential additive effects.
Missed dose
- If a dose is missed for prophylactic treatment, take it as soon as it is remembered.
- If it is almost time for the next scheduled dose, skip the missed dose and resume the normal dosing schedule.
- Do not double the dose to make up for a missed one.
Overdose
Colchicine overdose is a MEDICAL EMERGENCY and can be FATAL. Symptoms occur in three phases:
- 10-24 hours: Severe GI upset (nausea, vomiting, diarrhea, abdominal pain), which may lead to fluid depletion and electrolyte imbalances.
- 24 hours to 7 days: Multi-organ failure, including bone marrow suppression (pancytopenia, sepsis), arrhythmias, respiratory distress, renal failure, and progressive neuromuscular toxicity (myopathy, ascending paralysis).
- >7 days: A rebound leukocytosis and alopecia may occur in survivors. Treatment is supportive and must be conducted in an intensive care setting. There is no specific antidote. Gastric lavage may be considered if presentation is immediate. Aggressive fluid and electrolyte management, vasopressor support, and treatment of infections due to neutropenia are mainstays of care. Granulocyte colony-stimulating factor (G-CSF) may be used for severe marrow suppression.
Storage
- Store at room temperature (20°C to 25°C or 68°F to 77°F).
- Keep in the original container, tightly closed, and protected from light and moisture.
- Keep out of reach of children and pets.
Disclaimer
This information is for educational and professional medical purposes only and is not a substitute for the professional judgment of a qualified healthcare provider in diagnosing and treating patients. The prescribing physician must rely upon their own clinical experience and knowledge of the patient to determine dosages and the best course of treatment. The author assumes no liability for any information contained herein.
Reviews
“Colchicine remains an indispensable tool in our rheumatologic arsenal. Its efficacy in aborting acute gout is remarkable when initiated promptly. The key to its safe use lies in strict adherence to modern, low-dose regimens and vigilant patient selection, particularly regarding renal function and drug interactions.” – Rheumatologist, 15 years experience
“For FMF patients, colchicine is truly a life-saving medication. It prevents not only the painful attacks but also the devastating complication of amyloidosis. Managing the GI side effects is often the biggest challenge, but dose adjustment or splitting usually resolves this.” – Clinical Immunologist
“The narrow therapeutic window demands respect. I have seen cases of toxicity from inappropriate dosing or unsuspected drug interactions. It reinforces the necessity of a thorough medication reconciliation and patient education on the signs of toxicity.” – Clinical Pharmacist, Poison Control Center