colchicine/probenecid (Rx)

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Dosing & Uses

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Dosage Forms & Strengths

colchicine/probenecid

tablet

  • 0.5mg/500mg
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Chronic Gouty Arthritis

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

1 tablet (0.5 mg/500 mg) PO qDay for 1 week, then increase to 1 tablet BID thereafter

May be increased by 1 tablet q4wk within tolerance (and usually not above 4 tablets/day) if symptoms not controlled or the 24 hour uric acid excretion is <700 mg

Renal Impairment

Dosage requirements may be increased with renal impairment

CrCl <30 mL/min: Probenecid not effective with low urine output

Dosing Considerations

Do not start until an acute gouty attack has subsided; however, if an acute attack is precipitated during therapy, colchicine/probenecid may be continued without changing the dosage, and additional colchicine or other appropriate therapy should be given to control the acute attack

Gastric intolerance may be indicative of overdosage, and may be corrected by decreasing the dosage

As uric acid tends to crystallize out of an acid urine, a liberal fluid intake is recommended and sodium bicarbonate (3-7.5 g/day) or potassium citrate (7.5 g/day) to maintain an alkaline urine

Safety and efficacy not established

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Interactions

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            Adverse Effects

            Frequency Not Defined

            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
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            Warnings

            Contraindications

            Hypersensitivity

            Blood dyscrasias

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

            Cautions

            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

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            Pregnancy & Lactation

            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

            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

            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)

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            Formulary

            FormularyPatient Discounts

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            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.

            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.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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