Yes: Tablet

Colchicine

Treat acute gouty arthritis attacks and prevent recurrences of such attacks, management of familial Mediterranean fever

C (oral); D (parenteral)

Hypersensitivity to colchicine or any component; serious renal, gastrointestinal, hepatic, or cardiac disorders; blood dyscrasias

Severe local irritation can occur following S.C. or I.M. administration; use with caution in debilitated patients or elderly patients or patients with severe GI, renal, or liver disease

>10%: Gastrointestinal: Nausea, vomiting, diarrhea, abdominal pain

1% to 10%:

Dermatologic: Alopecia

Gastrointestinal: Anorexia

<1%: Rash, azoospermia, agranulocytosis, aplastic anemia, bone marrow suppression, hepatotoxicity, myopathy, peripheral neuritis

Symptoms of overdose include nausea, vomiting, abdominal pain, shock, kidney damage, muscle weakness, burning in throat, watery to bloody diarrhea, hypotension, anuria, cardiovascular collapse, delirium, convulsions

Treatment includes gastric lavage and measures to prevent shock, hemodialysis or peritoneal dialysis; atropine and morphine may relieve abdominal pain

Decreased effect: Vitamin B₁₂ absorption may be decreased

Increased toxicity:

Sympathomimetic agents

CNS depressant effects are enhanced

Protect tablets from light; I.V. colchicine is incompatible with I.V. solutions with preservatives; incompatible with dextrose

Decreases leukocyte motility, decreases phagocytosis in joints and lactic acid production, thereby reducing the deposition of urate crystals that perpetuates the inflammatory response

Onset of effect: Oral: Pain relief begins within 12 hours if adequately dosed

Distribution: Concentrates in leukocytes, kidney, spleen, and liver; does not distribute in heart, skeletal muscle, and brain

Protein binding: 10% to 31%

Metabolism: Partially deacetylated in the liver

Half-life: 12-30 minutes

End-stage renal disease: 45 minutes

Time to peak serum concentration: Oral: Within 0.5-2 hours declining for the next 2 hours before increasing again due to enterohepatic recycling

Elimination: Primarily in the feces via bile; 10% to 20% excreted in the urine

Prophylaxis of familial Mediterranean fever: Oral:

Children:

less than or equal to 5 years: 0.5 mg/day

>5 years: 1-1.5 mg/day in 2-3 divided doses

Adults: 1-2 mg/day in 2-3 divided doses

Gouty arthritis, acute attacks: Adults:

Oral: Initial: 0.5-1.2 mg, then 0.5-0.6 mg every 1-2 hours or 1-1.2 mg every 2 hours until relief or GI side effects (nausea, vomiting, or diarrhea) occur to a maximum total dose of 8 mg; wait 3 days before initiating another course of therapy

I.V.: Initial: 1-3 mg, then 0.5 mg every 6 hours until response, not to exceed 4 mg/day; if pain recurs, it may be necessary to administer a daily dose of 1-2 mg for several days, however, do not administer more colchicine by any route for at least 7 days after a full course of I.V. therapy (4 mg), transfer to oral colchicine in a dose similar to that being given I.V.

Gouty arthritis, prophylaxis of recurrent attacks: Adults: Oral: 0.5-0.6 mg/day or every other day

Dosing adjustment in renal impairment:

Cl_cr <50 mL/minute: Avoid chronic use or administration

Cl_cr <10 mL/minute: Decrease dose by 50% for treatment of acute attacks

Hemodialysis: Not dialyzable (0% to 5%); supplemental dose is not necessary

Peritoneal dialysis: Supplemental dose is not necessary

Alcohol: Avoid use

Food: Cyanocobalamin (Vitamin B₁₂): Malabsorption of the substrate. May result in macrocytic anemia or neurologic dysfunction. May need to supplement with Vitamin B₁₂.

CBC and renal function test

May cause false-positive results in urine tests for erythrocytes or hemoglobin

May cause drowsiness

Rare reports of agranulocytosis; use caution with clozapine and carbamazepine; CNS depressant effects may be enhanced

No information available to require special precautions

No effects or complications reported

Take as directed; do not exceed recommended dosage. Consult prescriber about a low-purine diet. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). Do not use alcohol or aspirin-containing medication without consulting prescriber. You may experience nausea, vomiting, or anorexia (small frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help); hair loss (reversible). Stop medication and report to prescriber if severe vomiting, watery or bloody diarrhea, or abdominal pain occurs. Report muscle tremors or weakness; fatigue; easy bruising or bleeding; yellowing of eyes or skin; or pale stool or dark urine. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Consult prescriber if breast-feeding.

Severe local irritation can occur following S.C. or I.M. administration; extravasation can cause tissue irritation; administer I.V. over 2-5 minutes into tubing of free-flowing I.V. with compatible fluid; administer orally with water and maintain adequate fluid intake

Injection: 0.5 mg/mL (2 mL)

Tablet: 0.5 mg, 0.6 mg

Baud FJ, Sabouraud A, Vicaut E, et al, "Treatment of Severe Colchicine Overdose With Colchicine-Specific Fab Fragments," N Engl J Med, 1995, 332(10):642-5.

Emmerson BT, "The Management of Gout," N Engl J Med, 1996, 334(7):445-51.

Folpini A and Furfori P, "Colchicine Toxicity - Clinical Features and Treatment: Massive Overdose Case Report," J Toxicol Clin Toxicol, 1995, 33(1):71-7.

Heaney D, Derghazarian CB, Pineo GF, et al, "Massive Colchicine Overdose. A Report on the Toxicity," Am J Med Sci, 1976, 271(2):233-8.

Levy M, Spino M, and Read SE, "Colchicine: A State-of-the-Art Review," Pharmacotherapy, 1991, 11(3):196-211.

Majeed HA, Carroll JE, Khuffash FA, et al, "Long-term Colchicine Prophylaxis in Children With Familial Mediterranean Fever (Recurrent Hereditary Polyserositis)," J Pediatr, 1990, 116(6):997-9.

Murray SS, Kramlinger KG, McMichan JC, et al, "Acute Toxicity After Excessive Ingestion of Colchicine," Mayo Clin Proc, 1983, 58(8):523-32.

Pitts FN Jr, "Colchicine Therapy for Palmer Fibromatosis," N Engl J Med, 1995, 333(6):393.

Scherrmann JM, "Antibody Treatment of Toxin Poisoning - Recent Advances," J Toxicol Clin Toxicol, 1994, 32(4):363-75.

Stapczynski JS, Rothstein RJ, Gaye WA, et al, "Colchicine Overdose: Report of Two Cases and Review of the Literature," Ann Emerg Med, 1981, 10(7):364-9.

Valenzuela P, Paris E, Oberpauer B, et al, "Overdose of Colchicine in a Three-Year-Old Child," Vet Hum Toxicol, 1995, 37(4):366-7.