colchicine (Rx)

Brand and Other Names:Colcrys, Mitigare, more...Gloperba
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 0.6mg (Colcrys)

capsule

  • 0.6mg (Mitigare)

oral solution

  • 0.6mg/5mL (Gloperba)

Gout

Treatment of acute gout flares (Colcrys): 1.2 mg PO at first sign of flare, then 0.6 mg 1 hr later; not to exceed 1.8 mg in 1-hr period

Prophylaxis

  • Colcrys, Mitigare, Gloperba
  • Indicated for prophylaxis of gout flares
  • 0.6 mg PO qDay or q12hr; not to exceed 1.2 mg/day; after gout flare, wait 12 hr to continue prophylaxis

Familial Mediterranean Fever

Colcrys: 1.2-2.4 mg/day PO in single daily dose or divided q12hr; increase in 0.3-mg/day increments as necessary to control disease; decrease in 0.3-mg/day increments if intolerable adverse effects develop; not to exceed 2.4 mg/day

Dosage Modifications

Renal impairment (gout)

  • Mild-to-severe (CrCl <80 mL/min): No dosage adjustment necessary; monitor for adverse effects
  • Severe (CrCl <30 mL/min): Do not repeat more frequently than q2Weeks
  • Hemodialysis: 0.6 mg once; do not repeat more frequently than q2Weeks

Renal impairment (familial Mediterranean fever [FMF])

  • Mild-to-moderate (CrCl 30-80 mL/min): Monitor for adverse effects; dosage adjustment may be required
  • Severe (CrCl <30 mL/min): 0.3 mg/day initially; dosage increases should be done with adequate monitoring for adverse effects
  • Hemodialysis: 0.3 mg PO once; dosage increases should be done with adequate monitoring for adverse effects

Hepatic impairment (gout)

  • Mild-to-severe: No dosage adjustment necessary; monitor for adverse effects
  • Severe: Do not repeat more frequently than q2Weeks; consider alternative therapy if repeated courses are required

Hepatic impairment (FMF)

  • Mild-to-moderate: Monitor for adverse effects
  • Severe: Consider dosage reduction; do not repeat more frequently than q2Weeks

Strong CYP3A4 inhibitors

  • Mitigare or Gloperba: Avoid use; if coadministration with strong CYP3A4 inhibitor is necessary, consider reducing the colchicine dose and closely monitor
  • Colcrys
    • Treatment of acute gout flares: 0.6 mg, then 0.3 mg 1 hr later; to be repeated no earlier than 3 days later
    • Prophylaxis of acute gout flares: If original colchicine regimen was 0.6 mg BID, decrease dose to 0.3 mg qDay; if original colchicine regimen was 0.6 mg qDay, decrease dose to 0.3 mg once every other day
    • FMF: Not to exceed 0.6 mg/day; 0.6 mg can be given as 0.3 mg q12hr

Moderate CYP3A4 inhibitors

  • Colcrys
    • Gout: 1.2 mg PO once; to be repeated no earlier than 3 days later
    • FMF: Not to exceed 1.2 mg/day; 0.6 mg can be given as 0.6 mg q12hr

P-gp inhibitors

  • Mitigare or Gloperba: Avoid use; if coadministration with P-gp inhibitor is necessary, consider reducing the colchicine dose and closely monitor
  • Colcrys
    • Gout: 0.6 mg PO once; to be repeated no earlier than 3 days later
    • FMF: Not to exceed 0.6 mg/day; 0.6 mg can be given as 0.3 mg q12hr

Post-STEMI Pericarditis (Off-label)

Treatment of pericarditis after ST-elevation myocardial infarction (STEMI)

0.6 mg PO q12hr

Behcet Syndrome (Orphan)

Orphan sponsor

  • AR Scientific, Inc, 1100 Orthodox Street, Philadelphia, PA 19124

Dosing Considerations

Limitations of use

  • Safety and effectiveness for acute treatment of gout flares during prophylaxis has not been studied
  • Not an analgesic medication and should not be used to treat pain from other causes

Dosage Forms & Strengths

tablet

  • 0.6mg (Colcrys)

capsule

  • 0.6mg (Mitigare)

Gout

<16 years

  • Not recommended

>16 years

  • Treatment of acute gout flares (Colcrys): 1.2 mg PO at first sign of flare, then 0.6 mg 1 hr later; not to exceed 1.8 mg in 1-hr period
  • Prophylaxis (Colcrys, Mitigare): 0.6 mg PO once daily or q12hr; not to exceed 1.2 mg/day; after gout flare, wait 12 hr to continue prophylaxis

Familial Mediterranean Fever

<4 years: Safety and efficacy not established

4-6 years: 0.3-1.8 mg/day PO in single daily dose or divided q12hr

6-12 years: 0.9-1.8 mg/day PO in single daily dose or divided q12hr

>12 years: 1.2-2.4 mg/day PO in single daily dose or divided q12hr

Dosing considerations

  • Increased or decreased in 0.3 mg/day increments as necessary; not to exceed maximum recommended daily dose
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Interactions

Interaction Checker

and colchicine

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            GI effects (eg, diarrhea, nausea, cramping, abdominal pain, vomiting) (26-77%)

            1-10%

            Fatigue (1-4%)

            Gout (0-4%)

            Pharyngolaryngeal pain (2-3%)

            Headache (1-2%)

            Frequency Not Defined

            Neuromuscular toxicity (eg, muscle pain, weakness)

            Myelosuppression

            Disseminated intravascular coagulation Injury to cells in the renal, hepatic, circulatory, and central nervous systems

            Postmarketing Reports

            Neurologic: Sensory motor neuropathy

            Dermatologic: Alopecia, purpura, maculopapular rash, rash

            GI: Lactose intolerance, abdominal cramping, abdominal pain, vomiting, diarrhea, nausea

            Hematologic: Thrombocytopenia, leukopenia, granulocytopenia, pancytopenia, aplastic anemia

            Hepatobiliary: Elevated liver transaminases

            Musculoskeletal: Myotonia, muscle weakness, myopathy, elevated creatine phosphokinase, muscle pain, rhabdomyolysis

            Reproductive: Azoospermia, oligospermia

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            Warnings

            Contraindications

            Coadministration with P-gp or strong CY3A4 inhibitors in patients with hepatic or renal impairment

            Patients with both renal and hepatic impairment

            Cautions

            Long-term use is established for FMF, but safety and efficacy of repeat treatment in gout flares has not been evaluated

            Not to be used to treat pain from other causes; drug is not analgesic

            Must be kept out of reach of children; fatal overdoses reported in both adults and children

            Blood dyscrasias (eg, leukopenia, myelosuppression, thrombocytopenia, pancytopenia, granulocytopenia, aplastic anemia) reported at therapeutic dosages

            Rhabdomyolysis and neuromuscular toxicity reported with long-term treatment at therapeutic dosages; increased risk in renal dysfunction, elderly patients, and concomitant therapy with myotoxic drugs; symptoms generally resolve within 1 week to few months upon discontinuance

            Drug interactions overview

            • Colchicine is a CYP3A4 and P-gp substrate
            • Inhibition of both CYP3A4 and P-gp by dual inhibitors (ie, clarithromycin) reported to produce life-threatening or fatal colchicine toxicity due to significant increases in systemic colchicine levels
            • Coadministration with P-gp and strong CYP3A4 inhibitors may warrant dosage reduction or interruption of therapy
            • HMG-CoA reductase inhibitors and fibrates may increase the risk of myopathy when combined with colchicine; check serum creatinine kinase levels if patient reports muscle pain or weakness
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            Pregnancy & Lactation

            Pregnancy

            Available human data from published literature on colchicine use in pregnancy over several decades have not identified any drug-associated risks for major birth defects, miscarriage, or adverse maternal or fetal outcomes

            Animal data

            • Published animal reproduction and development studies indicate that colchicine causes embryofetal toxicity and altered postnatal development at exposures within or above the clinical therapeutic range

            Lactation

            Colchicine is present in human milk

            No adverse events in breastfed infants in the published literature after administration of colchicine to lactating women

            No data available on the effects of colchicine on milk production

            Consider developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition

            Infertility

            • Case reports and epidemiology studies in males on colchicine therapy indicate that infertility from colchicine is rare and may be reversible

            Pregnancy 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.

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            Pharmacology

            Mechanism of Action

            Gout: Disruption of cytoskeletal functions through inhibition of β-tubulin polymerization into microtubules, which prevents activation, degranulation, and migration of neutrophils

            FMF: Mechanism not established; may interfere with intracellular assembly of inflammasome complex present in neutrophils and monocytes, which mediates activation of interleukin-1β

            Absorption

            Bioavailability: ~45%

            Onset: 18-24 hr

            Time to peak effect: 48-72 hr

            Fasted

            • Peak plasma concentration: 3 ng/mL (Mitigare); 2.16 ng/mL (Gloperba); 2.5-3.6 ng/mL (Colcrys)
            • Peak plasma time: 1 hr (Gloperba); 1.3-1.5 hr (Colcrys)
            • AUC: 19.9 hr·ng/mL (Gloperba)

            Fed

            • Peak plasma concentration: 1.68 ng/mL (Gloperba)
            • Peak plasma time: 2 hr (Gloperba)
            • AUC: 18.47 hr·ng/mL (Gloperba)

            Distribution

            Vd: ~1420L (Colcrys); ~5-8L/kg (Mitigare); 341-1150 L (Colcrys)

            Protein bound: 39%

            Colchicine crosses the placenta (plasma levels in the fetus reported to be ~15% of the maternal concentration)

            Metabolism

            Metabolized by P-gp and CYP3A4

            May also be metabolized by glucuronidation

            Metabolites: Demethylated to 2 primary metabolites and 1 minor metabolite

            Elimination

            Half-life: 31 hr (Mitigare and Gloperba); 26.6-31.2 hr (Colcrys)

            Dialyzable: No (hemodialysis)

            Excretion: Urine (40-65%)

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            Administration

            Oral Administration

            Administered orally, without regard to meals

            Storage

            All formulations: Store at 20-25°C (68-77°F)

            Tablets or capsules: Protect from light

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            Formulary

            FormularyPatient Discounts

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            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.
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            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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