Therapeutic Classification: antigout agents
Absorption: 45% absorbed from the GI tract, then re-enters GI tract from biliary secretions, when more absorption may occur.
Distribution: Extensively distributed to tissues.
Metabolism/Excretion: Partially metabolized by the liver by the CYP3A4 isoenzyme; also a substrate for P-glycoprotein. Secreted in bile back into GI tract; eliminated in the feces. 40–65% excreted in the urine as unchanged drug.
Half-life: 19–31 hr.
(anti-inflammatory activity)
Derm: alopecia.
GI: diarrhea, nausea, vomiting, abdominal pain.
Hemat: AGRANULOCYTOSIS, APLASTIC ANEMIA, leukopenia, thrombocytopenia.
MS: myalgia, RHABDOMYOLYSIS.
Neuro: peripheral neuritis.
Treatment of Gout Flares (Colcrys and Generic Tablets Only)
- PO (Adults): 1.2 mg initially, then 0.6 mg 1 hr later (maximum dose of 1.8 mg in 1 hr); Concomitant use of strong CYP3A4 inhibitors in patients with normal renal and hepatic function (atazanavir, clarithromycin, darunavir/ritonavir, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, ritonavir, tipranavir/ritonavir): 0.6 mg initially, then 0.3 mg 1 hr later (do not repeat treatment course for ≥3 days); Concomitant use of moderate CYP3A4 inhibitors (aprepitant, diltiazem, erythromycin, fluconazole, fosamprenavir, grapefruit juice, verapamil): 1.2 mg as single dose (do not repeat for ≥3 days); Concomitant use of strong P-gp inhibitors (cyclosporine, ranolazine) in patients with normal renal and hepatic function: 0.6 mg as single dose (do not repeat for ≥3 days).
Renal Impairment
- PO (Adults): CCr <30 mL/min: 1.2 mg initially, then 0.6 mg 1 hr later; do not repeat treatment course for ≥2 wk; Dialysis: 0.6 mg as single dose; do not repeat treatment course for ≥2 wk.
Prevention of Gout Flares (Gloperba, Mitigare, and Generic Capsules Only)
- PO (Adults): 0.6 mg once or twice daily; Concomitant use of strong CYP3A4 inhibitors (atazanavir, clarithromycin, darunavir/ritonavir, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, ritonavir, tipranavir/ritonavir) or strong P-gp inhibitors (cyclosporine, ranolazine) in patients with normal renal and hepatic function: if original dose was 0.6 mg twice daily, ↓ to 0.3 mg once daily; if original dose was 0.6 mg once daily, ↓ to 0.3 mg every other day; Concomitant use of moderate CYP3A4 inhibitors (aprepitant, diltiazem, erythromycin, fluconazole, fosamprenavir, grapefruit juice, verapamil): if original dose was 0.6 mg twice daily, ↓ to 0.3 mg twice daily or 0.6 mg once daily; if original dose was 0.6 mg once daily, ↓ to 0.3 mg once daily.
Renal Impairment
- PO (Adults): CCr <30 mL/min: 0.3 mg once daily; Dialysis: 0.3 mg twice weekly.
Familial Mediterranean Fever (Colcrys and Generic Tablets Only)
- PO (Adults and Children >12 yr): 1.2–2.4 mg/day (in 1–2 divided doses); may ↑ or ↓ dose in 0.3-mg/day increments based on safety and efficacy; Concomitant use of strong CYP3A4 inhibitors (atazanavir, clarithromycin, darunavir/ritonavir, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, ritonavir, tipranavir/ritonavir) or strong P-gp inhibitors (cyclosporine, ranolazine) in patients with normal renal and hepatic function: Do not exceed 0.6 mg/day (may be given as 0.3 mg twice daily); Concomitant use of moderate CYP3A4 inhibitors (aprepitant, diltiazem, erythromycin, fluconazole, fosamprenavir, grapefruit juice, verapamil): Do not exceed 1.2 mg/day (may be given as 0.6 mg twice daily).
- PO (Children 6–12 yr): 0.9–1.8 mg/day (in 1–2 divided doses).
- PO (Children 4–6 yr): 0.3–1.8 mg/day (in 1–2 divided doses).
Renal Impairment
- PO (Adults): CCr 30–50 mL/min: dose ↓ may be necessary; CCr <30 mL/min or dialysis: 0.3 mg/day.
Reduction in Risk of MI, Stroke, Coronary Revascularization, and Cardiovascular Death
- PO (Adults): 0.5 mg once daily.
Colcrys, Gloperba, Lodoco, Mitigare
