Colchicine

Trade Names:
Colchicine
- Tablets 0.6 mg
- Injection 0.5 mg/mL

Pharmacology

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Inhibits inflammation and reduces pain and swelling associated with gouty arthritis.

Pharmacokinetics

Absorption

Rapidly absorbed. T _max is 0.5 to 2 h.

Distribution

Large amounts present in bile and intestinal secretions. High concentrations also found in kidney, liver, and spleen. About 50% protein bound. Vd is 1 to 3 L/kg.

Metabolism

Undergoes enterohepatic recirculation. Deacetylated primarily by the liver.

Elimination

Plasma t _½ to 10 to 60 min. Excreted via biliary and renal routes; 10% to 20% excreted unchanged in urine.

Indications and Usage

Treatment and relief of pain in attacks of acute gouty arthritis; regular prophylaxis between attacks and is often effective in aborting an attack when taken at the first sign of articular discomfort; colchicine IV is used when rapid response is desired or if GI adverse reactions interfere with oral use.

Unlabeled Uses

Familial Mediterranean fever; hepatic cirrhosis; primary biliary cirrhosis; treatment of Behcet disease; scleroderma; Sweet syndrome

Contraindications

Serious GI, renal, hepatic, or cardiac disorders; blood dyscrasias.

Dosage and Administration

Initial dose (give at first sign of attack) PO 1.2 mg; then 0.6 every h or 1.2 mg every 2 h until pain is relieved or diarrhea ensues. Total dose is usually 4 to 8 mg. Wait 3 days before initiating a second course of therapy. IV Initial dose 2 mg; then 0.5 mg every 6 h until satisfactory response is achieved (max, 4 mg per 24 h or 1 course of treatment).

PO 0.6 mg/day for 3 to 4 days/wk if fewer than 1 attack/yr; if more than 1 attack/yr, 0.6 mg/day. Severe cases may require 1.2 to 1.8 mg/day.

IV 0.5 to 1 mg 1 or 2 times/day; however, oral form is preferable, usually in conjunction with a uricosuric agent.

PO 0.6 mg 3 times daily for 3 days before and 3 days after surgery.

General Advice

• Parenteral
• Reconstitute with sodium chloride 0.9% (without preservatives) only.
• Administer parenterally via IV route only. Considerable irritation and tissue damage may occur if leakage into surrounding tissue occurs.

Storage/Stability

Store tablets in airtight, light-resistant container.

Drug Interactions

None well documented.

Incompatibility

Do not dilute with dextrose 5% in water.

Laboratory Test Interactions

May cause false-positive results in urine tests for RBCs and hemoglobin.

Adverse Reactions

Dermatologic

Dermatoses; purpura; alopecia.

GI

Nausea; vomiting; diarrhea; abdominal pain.

Hematologic

Bone marrow depression with aplastic anemia; agranulocytosis, leukopenia or thrombocytopenia (long-term therapy).

Hepatic

Elevated alkaline phosphatase and AST.

Miscellaneous

Reversible azoospermia; myopathy; peripheral neuritis.

Precautions

Pregnancy

Category C (oral). Category D (parenteral).

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Administer with great caution to elderly and debilitated patients.

Hepatic Function

Increased colchicine toxicity may occur.

GI reactions

Drug may cause nausea, vomiting, diarrhea, and abdominal pain that may aggravate pre-existing peptic ulcer or spastic colon. Discontinue drug if these symptoms appear.

Injection

Severe local irritation occurs if drug is given by subcutaneous or IM route.

Myopathy and neuropathy

Myoneuropathy may occur and cause weakness in patients with impaired kidney function; serum creatine kinase may be elevated. Usually resolves in 3 to 4 wk after drug withdrawal.

Vitamin B ₁₂ malabsorption:

Colchicine induces reversible malabsorption of vitamin B ₁₂ with long-term use.

Overdosage

Symptoms

Nausea, severe abdominal pain, vomiting, diarrhea, shock, ST segment elevation, paralysis, respiratory failure, liver damage, renal failure, leukopenia, thrombocytopenia, coagulopathy, alopecia, stomatitis.

Patient Information

• Instruct patient to take colchicine regularly to prevent acute attacks.
• Instruct patient not to exceed 8 mg in course of therapy for acute attack. To minimize cumulative toxicity, patient should wait 3 days before starting second course.
• Advise patient with gout to drink at least 2,000 mL of fluid daily, unless contraindicated.
• Reinforce health care provider's instructions about weight loss, diet, and alcohol intake.
• Advise patient to have extra supply of drug on hand in case health care provider gives instructions to increase dosage.
• Instruct patient to stop taking drug if nausea, vomiting, diarrhea, or abdominal pain occurs, especially if patient has history of spastic colon or ulcers.

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