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Colchicine/Probenecid

    Brands

    DEA Class; Rx

    Common Brand Names;  ColciGel, Colcrys, GLOPERBA, MITIGARE

    • Uricosuric Agents; 
    • Antigout Agents

    Antigout anti-inflammatory agent
    Used primary for treatment and prevention of acute gout and for familial Mediterranean fever
    Concomitant renal or hepatic dysfunction and the use of P-glycoprotein or strong CYP3A4 inhibitors increase toxicity risk

    Indicated for treatment of chronic gouty arthritis when complicated by frequent, recurrent acute attacks of gout

    Hypersensitivity

    Blood dyscrasias

    Uric acid kidney stones Initiation of therapy during an acute gouty attack

    Probenecid

    • CNS: Headache, dizziness
    • Metabolic: Precipitation of acute gouty arthritis
    • Gastrointestinal: Hepatic necrosis, vomiting, nausea, anorexia, sore gums
    • Genitourinary: Nephrotic syndrome, uric acid stones with or without hematuria, renal colic, costovertebral pain, urinary frequency
    • Hypersensitivity: Anaphylaxis, fever, urticaria, pruritus
    • Hematologic: Aplastic anemia, leukopenia, hemolytic anemia which in some patients could be related to genetic deficiency of glucose-6-phosphate dehydrogenase in red blood cells, anemia
    • Integumentary: Dermatitis, alopecia, flushing

    Colchicine

    • Adverse effects appear to be dose dependent; increased colchicine toxicity may occur with hepatic dysfunction
    • CNS: Peripheral neuritis
    • Musculoskeletal: Muscular weakness
    • Gastrointestinal: Nausea, vomiting, abdominal pain, or diarrhea may be particularly troublesome in the presence of peptic ulcer or spastic colon Hypersensitivity: Urticaria
    • Hematologic: Aplastic anemia, agranulocytosis
    • Integumentary: Dermatitis, purpura, alopecia
    • At toxic doses, may cause severe diarrhea, generalized vascular damage, and renal damage with hematuria and oliguria

    Exacerbation of gout may occur; in such cases additional colchicine or other appropriate therapy required

    Probenecid increases plasma concentrations of methotrexate; if combination must be used, reduce methotrexate dose and monitor methotrexate serum levels

    Salicylates antagonize probenecid’s uricosuric effect

    Rare occurrence of severe allergic reactions and anaphylaxis reported; most within several hours after readministration following prior usage of the drug; discontinue colchicine/probenecid if this occurs

    Hematuria, renal colic, costovertebral pain, and formation of uric acid stones associated with the use may be prevented by alkalization of the urine and a liberal fluid intake

    History of peptic ulcer

    Increased dosage requirements may be needed with renal impairment

    Pregnancy Category: C; While not studied in the treatment of gout, data from a limited number of published studies found no evidence of an increased risk of miscarriage, stillbirth, or teratogenic effects among pregnant women using colchicine to treat familial Mediterranean fever

    Lactation: Colchicine is distributed in breast milk; limited information suggests breastfed infants receive <10% of maternal weight-adjusted dose; caution advised and observe infant for adverse effects if breastfeeding

    Maximum dosages are dependent on indication for use. Do not exceed the maximum dose recommended for the indication for use.

    Adults

    1.8 mg PO per acute gout flare course (tablets); 1.2 mg/day PO for gout prophylaxis (tablets, capsules, oral solution); 2.4 mg/day PO for familial Mediterranean fever (tablets).

    Geriatric

    1.8 mg PO per acute gout flare course (tablets); 1.2 mg/day PO for gout prophylaxis (tablets, capsules, oral solution); 2.4 mg/day PO for familial Mediterranean fever (tablets).

    Adolescents

    2.4 mg/day PO for familial Mediterranean fever (tablets). Rare off-label use for gout prophylaxis has been described, do not exceed 1.2 mg/day PO.

    Children

    4 to 12 years: 1.8 mg/day PO for familial Mediterranean fever (tablets).
    4 years: Safety and efficacy have not been established.

    Infants

    Safety and efficacy have not been established.

    colchicine/probenecid

    tablet

    • 0.5mg/500mg