probenecid (Rx)

Brand and Other Names:Benemid
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 500mg

Gout

250 mg PO twice daily for 1 week; increase to 500 mg PO twice daily to 2 g/day maximum with dosage increases of 500 mg q4weeks

If gout attacks do not occur for 4 months and uric acid levels are within normal may reduce dose by 500 mg q6monts

Dosing Considerations

  • Therapy should not be started until an acute gouty attack has subsided; however, if acute attack is precipitated during therapy, probenecid may be continued without changing the dosage, and full therapeutic dosage of colchicine, or other appropriate therapy, should be given to control the acute attack

Prolong Penicillin Serum Levels

500 mg PO four times daily

Pelvic Inflammatory Disease

1 g PO with 2 g cefoxitin IM as single dose

Gonorrhea

1 g PO with 2 g cefoxitin IM as single dose

Renal Impairment

CrCl<30 mL/min: Avoid use

Dosage Forms & Strengths

tablet

  • 500mg

Prolong Penicillin Serum Levels

<2 years old

  • Contraindicated

>2 years old

  • <50 kg: 25 mg/kg body weight (or 700mg/m2) PO once with PCN; for maintenance, increase to 40 mg/kg body weight (or 1.2 g/m2) per day PO divided q6hr; not to exceed 500 mg/dose  
  • >50 kg: 500 mg PO four times daily

Gonorrhea

<45 kg

  • Safety and efficacy not established

>45 kg

  • 1 g PO with 2 g cefoxitin IM as single dose
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Interactions

Interaction Checker

and probenecid

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Adverse Effects

            1-10%

            Headache

            Nausea

            Vomiting

            Loss of appetite

            GI upset

            Rash

            Flushing

            Dizziness

            Fever

            Aplastic anemia

            Hemolytic anemia

            Leukopenia

            Renal calculi

            Nephrotic syndrome (rare)

            Exacerbation of gout

            Gouty arthritis

            Hepatic necrosis (rare)

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            Warnings

            Contraindications

            <2 years

            Uric acid kidney stones, acute gouty arthritis

            Hypersensitivity

            Blood dyscrasias

            Administration during gouty attack

            Small or large dose aspirin therapy

            Cautions

            Use caution in patients with G6PD deficiency; may increase risk for hemolytic anemia

            Use caution in patients with peptic ulcer disease

            Salicylates may reduce the therapeutic effects of probenecid (effect may be pronounced with high chronic doses

            May cause exacerbation of acute gouty attack; in such cases colchicine or other appropriate therapy is advisable

            May increase serum concentration of methotrexate; if probenecid is given with methotrexate, reduce dosage of methotrexate and monitor serum levels

            Hematuria, renal colic, costovertebral pain, and formation of uric acid stones associated with use of probenecid in gouty patients may be prevented by alkalization of the urine and a liberal fluid intake; in these cases when alkali is administered, the acid-base balance of the patient should be watched

            Rarely, severe allergic reactions and anaphylaxis have been reported with the use of probenecid; most of these have been reported to occur within several hours after readministration following prior usage of the drug; the appearance of hypersensitivity reactions requires cessation of therapy with probenecid; discontinue drug if allergic reaction occurs

            Probenecid has been used in patients with some renal impairment, but dosage requirements may be increased; probenecid may not be effective in chronic renal insufficiency particularly when the glomerular filtration rate is ≤30 mL/minute because of its mechanism of action, probenecid is not recommended in conjunction with penicillin in the presence of known renal impairment

            Drug interaction overview

            • In patients on probenecid the use of salicylates in either small or large doses is contraindicated because antagonizes the uricosuric action of probenecid; the biphasic action of salicylates in the renal tubules accounts for the so-called “paradoxical effect” of uricosuric agents; in patients on probenecid who require a mild analgesic agent the use of acetaminophen rather than small doses of salicylates would be preferred
            • Concomitant administration of probenecid increases mean plasma elimination half-life of a number of drugs which can lead to increased plasma concentrations; these include agents such as indomethacin, acetaminophen, naproxen, ketoprofen, meclofenamate, lorazepam, and rifampin
            • Although clinical significance of this observation has not been established, a lower dosage of the drug may be required to produce a therapeutic effect, and increases a dosage of the drug in question should be made cautiously and in small increments when probenecid is being coadministered
            • Although specific instances of toxicity due to potential interaction have not been observed to date, physicians should be alert to this possibility
            • Probenecid given concomitantly with sulindac had only a slight effect on plasma sulfide levels, while plasma levels of sulindac and sulfone were increased; sulindac was shown to produce a modest reduction in uricosuric action of probenecid, which probably is not significant under most circumstances
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            Pregnancy & Lactation

            Pregnancy

            Probenecid crosses placenta barrier and appears in cord blood; the use of any drug in women of childbearing potential requires that the anticipated benefit be weighed against possible hazards

            Lactation

            Not known if distributed into breast milk, use with caution

            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

            (Uricosuric) inhibits tubular reabsorption of urate; increasing uric acid excretion

            Also inhibits tubular secretion of weak organic acids like PCNs & cephalosporins

            Pharmacokinetics

            Half-Life: 3-17 hr

            Onset: 2 hr (effect on penicillin levels)

            Peak Plasma Time: 2-4 hr

            Bioavailability: >90%

            Protein Bound: 85-95% (albumin)

            Metabolism: Liver

            Metabolites: hydroxylated metabolites, N-despropyl metabolite, probenecid acylglucuronide

            Excretion: Urine

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

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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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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.