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 breastfeedingPregnancy Categories A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk. B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available. Mechanism of Action Colchicine: Inhibits leukocyte migration, decreased phagocytosis in joint, decreased lactic acid production by neutrophils resulting in reducing uric acid crystal deposition and decreasing inflammation Probenecid: Uricosuric and renal tubular blocking agent Absorption Bioavailability: 25-50% (colchicine); >90% (probenecid) Onset initial: 12-24 hr (colchicine);1 hr initial (probenecid) Onset maximum: 48-72 hr (colchicine); 3 hr (probenecid) Peak Plasma Time: 0.5-2 hr (colchicine); 1-5 hr (probenecid) Distribution Protein Bound: 10-30% (colchicine); 85-95% to albumin (probenecid) Vd: 2 L (colchicine); 11 L (probenecid) Metabolism Colchicine is metabolized by CYP3A4; partially deacetylated in the liver; undergo enterohepatic circulation Probenecid is metabolized in the liver to hydroxylated metabolites, N-despropyl metabolite, probenecid acylglucuronide Elimination Half-life: 4.4 hr (colchicine); 3-17 hr (probenecid) Dialyzable: No (colchicine) Renal clearance: 0.7 L/hr/kg (colchicine) Excretion: 10-20% feces (colchicine); 75-88% urine (probenecid) No images available for this drug. No images available for this drug.A Patient Handout is not currently available for this monograph.Print FormularyPatient DiscountsAdding plans allows you to compare formulary status to other drugs in the same class.To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.Create Your List of PlansAdding plans allows you to:View the formulary and any restrictions for each plan.Manage and view all your plans together – even plans in different states.Compare formulary status to other drugs in the same class.Access your plan list on any device – mobile or desktop. The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information. View explanations for tiers and restrictions Tier Description 1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs. 2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs. 3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs. 4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products. 5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products. 6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products. NC NOT COVERED – Drugs that are not covered by the plan. Code Definition PA Prior Authorization Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription. 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