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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      Serious - Use Alternative

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            Contraindicated (0)

              Serious - Use Alternative (14)

              • aspirin

                aspirin decreases effects of probenecid by acidic (anionic) drug competition for renal tubular clearance. Avoid or Use Alternate Drug. Aspirin decreases uricosuric action of probenecid.

              • aspirin rectal

                aspirin rectal decreases effects of probenecid by acidic (anionic) drug competition for renal tubular clearance. Avoid or Use Alternate Drug. Aspirin decreases uricosuric action of probenecid.

              • aspirin/citric acid/sodium bicarbonate

                aspirin/citric acid/sodium bicarbonate decreases effects of probenecid by acidic (anionic) drug competition for renal tubular clearance. Avoid or Use Alternate Drug. Aspirin decreases uricosuric action of probenecid.

              • baricitinib

                probenecid will increase the level or effect of baricitinib by decreasing elimination. Avoid or Use Alternate Drug. Coadministration of baricitinib with strong organic anion transporter 3 (OAT3) inhibitors is not recommended.

              • imipenem/cilastatin

                probenecid increases levels of imipenem/cilastatin by decreasing renal clearance. Avoid or Use Alternate Drug. Coadministration increases the plasma level and half-life of imipenem.

              • imipenem/cilastatin/relebactam

                probenecid increases levels of imipenem/cilastatin/relebactam by decreasing renal clearance. Avoid or Use Alternate Drug. Coadministration increases the plasma level and half-life of imipenem.

              • ketorolac

                probenecid increases levels of ketorolac by decreasing renal clearance. Contraindicated.

              • ketorolac intranasal

                probenecid increases levels of ketorolac intranasal by decreasing renal clearance. Contraindicated.

              • meropenem/vaborbactam

                probenecid increases levels of meropenem/vaborbactam by decreasing elimination. Avoid or Use Alternate Drug. Probenecid competes withe meropenem for active tubular secretion.

              • methotrexate

                probenecid increases levels of methotrexate by acidic (anionic) drug competition for renal tubular clearance. Avoid or Use Alternate Drug. If combination must be used, decrease methotrexate dose; also, methotrexate increases uric acid production and risk for uric acid neuropathy.

              • nafcillin

                nafcillin, probenecid. Either increases levels of the other by decreasing renal clearance. Avoid or Use Alternate Drug.

              • pivmecillinam

                pivmecillinam, probenecid. Either increases levels of the other by decreasing renal clearance. Avoid or Use Alternate Drug.

              • temocillin

                temocillin, probenecid. Either increases levels of the other by decreasing renal clearance. Avoid or Use Alternate Drug.

              • ticarcillin

                ticarcillin, probenecid. Either increases levels of the other by decreasing renal clearance. Avoid or Use Alternate Drug.

              Monitor Closely (96)

              • aceclofenac

                aceclofenac will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • acemetacin

                acemetacin will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • acyclovir

                acyclovir will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • aminohippurate sodium

                aminohippurate sodium will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • aspirin/citric acid/sodium bicarbonate

                aspirin/citric acid/sodium bicarbonate decreases effects of probenecid by unknown mechanism. Use Caution/Monitor.

              • balsalazide

                balsalazide will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

                balsalazide decreases effects of probenecid by unknown mechanism. Use Caution/Monitor.

              • bendroflumethiazide

                bendroflumethiazide will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • cabozantinib

                probenecid will increase the level or effect of cabozantinib by Other (see comment). Use Caution/Monitor. MRP2 inhibitors increase cabozantinib toxicity

              • cefaclor

                cefaclor will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • cefadroxil

                cefadroxil will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • cefamandole

                cefamandole will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • cefazolin

                probenecid increases levels of cefazolin by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • cefdinir

                probenecid will increase the level or effect of cefdinir by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • cefditoren

                probenecid will increase the level or effect of cefditoren by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • cefepime

                probenecid will increase the level or effect of cefepime by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • cefixime

                probenecid will increase the level or effect of cefixime by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • cefotaxime

                probenecid will increase the level or effect of cefotaxime by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • cefotetan

                probenecid will increase the level or effect of cefotetan by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • cefoxitin

                probenecid will increase the level or effect of cefoxitin by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • cefpirome

                cefpirome will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • cefpodoxime

                probenecid will increase the level or effect of cefpodoxime by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • cefprozil

                probenecid will increase the level or effect of cefprozil by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • ceftaroline

                probenecid increases levels of ceftaroline by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • ceftazidime

                probenecid will increase the level or effect of ceftazidime by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • ceftazidime/avibactam

                probenecid increases levels of ceftazidime/avibactam by decreasing renal clearance. Use Caution/Monitor. Avoid, coadministration not recommended according to the prescribing information. In vitro, probenecid inhibits uptake of avibactam by OATP1 and OATP3 transporters in the kidney by 56-70%. This may result in decreased renal elimination of avibactam.

              • ceftibuten

                ceftibuten will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • ceftriaxone

                probenecid will increase the level or effect of ceftriaxone by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • cefuroxime

                probenecid will increase the level or effect of cefuroxime by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • celecoxib

                celecoxib will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • cephalexin

                cephalexin will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • chlorothiazide

                chlorothiazide will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • chlorpropamide

                chlorpropamide will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

                probenecid increases levels of chlorpropamide by unspecified interaction mechanism. Use Caution/Monitor. Risk of hypoglycemia.

              • chlorthalidone

                chlorthalidone will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • choline magnesium trisalicylate

                choline magnesium trisalicylate will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

                choline magnesium trisalicylate decreases effects of probenecid by unknown mechanism. Use Caution/Monitor.

              • ciprofloxacin

                probenecid will increase the level or effect of ciprofloxacin by Other (see comment). Use Caution/Monitor. Probenecid interferes with renal tubular secretion of ciprofloxacin and produces an increase in the ciprofloxacin levels in the serum

              • cyclopenthiazide

                cyclopenthiazide will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • deferiprone

                probenecid will increase the level or effect of deferiprone by decreasing metabolism. Use Caution/Monitor. Coadministration with UGT1A6 inhibitors may increase serum concentration of deferiprone.

              • diclofenac

                diclofenac will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • dicloxacillin

                probenecid increases levels of dicloxacillin by decreasing renal clearance. Use Caution/Monitor.

              • diflunisal

                diflunisal will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

                diflunisal decreases effects of probenecid by unknown mechanism. Use Caution/Monitor.

              • ethambutol

                ethambutol decreases effects of probenecid by Other (see comment). Use Caution/Monitor. Comment: Hyperuricemia reported with ethambutol and precipitation of gout reported; uric acid lowering agents may be require dosage adjustment.

              • etodolac

                etodolac will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • famciclovir

                probenecid increases levels of famciclovir by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor. Coadministration of famciclovir with drugs that are significantly eliminated by active renal tubular secretion may increase plasma concentrations of famciclovir's active moiety (ie, penciclovir).

              • fenoprofen

                fenoprofen will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • flurbiprofen

                flurbiprofen will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • ganciclovir

                ganciclovir will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • glimepiride

                probenecid increases levels of glimepiride by unspecified interaction mechanism. Use Caution/Monitor. Risk of hypoglycemia.

              • glipizide

                probenecid increases levels of glipizide by unspecified interaction mechanism. Use Caution/Monitor. Risk of hypoglycemia.

              • glyburide

                probenecid increases levels of glyburide by unspecified interaction mechanism. Use Caution/Monitor. Risk of hypoglycemia.

              • glycerol phenylbutyrate

                probenecid, glycerol phenylbutyrate. decreasing renal clearance. Use Caution/Monitor. Probenecid may inhibit the renal excretion glycerol phenylbutyrate metabolites PAA and PAGN; caution when adjusting doses based on these metabolite levels.

              • hydrochlorothiazide

                hydrochlorothiazide will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • hydroxyurea

                hydroxyurea increases levels of probenecid by Other (see comment). Use Caution/Monitor. Comment: Dosage adjustment of probenecid may be needed.

              • ibuprofen

                ibuprofen will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • ibuprofen IV

                ibuprofen IV will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • indapamide

                indapamide will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • indomethacin

                indomethacin will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • ketoprofen

                ketoprofen will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • ketorolac

                ketorolac will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • ketorolac intranasal

                ketorolac intranasal will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • lornoxicam

                lornoxicam will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • meclofenamate

                meclofenamate will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • mefenamic acid

                mefenamic acid will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • meloxicam

                meloxicam will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • meropenem

                probenecid increases levels of meropenem by decreasing elimination. Use Caution/Monitor.

              • mesalamine

                mesalamine will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

                mesalamine decreases effects of probenecid by unknown mechanism. Use Caution/Monitor.

              • methotrexate

                probenecid will increase the level or effect of methotrexate by Other (see comment). Use Caution/Monitor. Methotrexate plasma levels, therapeutic effects, and toxicity may be enhanced. Monitor methotrexate concentrations and adjust dose accordingly.

              • methyclothiazide

                methyclothiazide will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • metolazone

                metolazone will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • mycophenolate

                probenecid increases levels of mycophenolate by decreasing renal clearance. Use Caution/Monitor. Probenecid may interfere with renal tubular secretion of mycophenolate active metabolites.

              • nabumetone

                nabumetone will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • nafcillin

                probenecid will increase the level or effect of nafcillin by decreasing renal clearance. Use Caution/Monitor.

              • naproxen

                naproxen will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • oseltamivir

                probenecid increases levels of oseltamivir by Other (see comment). Use Caution/Monitor. Comment: Coadministration of probenecid results in a 2-fold increase in exposure to oseltamivir carboxylate because of a decrease in active anionic tubular secretion in the kidney. No dosage adjustments are required with probenecid coadministration.

              • oxaprozin

                oxaprozin will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • parecoxib

                parecoxib will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • penicillin G aqueous

                probenecid increases levels of penicillin G aqueous by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • piperacillin

                probenecid will increase the level or effect of piperacillin by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • piroxicam

                piroxicam will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • pralatrexate

                probenecid increases levels of pralatrexate by decreasing renal clearance. Use Caution/Monitor.

              • pyrazinamide

                pyrazinamide decreases effects of probenecid by unknown mechanism. Use Caution/Monitor.

              • rifampin

                probenecid will increase the level or effect of rifampin by unspecified interaction mechanism. Use Caution/Monitor. Concomitant use with probenecid increase concentration of rifampin which may increase risk of toxicity; monitor for adverse reactions during coadministration

              • rose hips

                rose hips will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • salicylates (non-asa)

                salicylates (non-asa) will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

                salicylates (non-asa) decreases effects of probenecid by unknown mechanism. Use Caution/Monitor.

              • salsalate

                salsalate will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

                salsalate decreases effects of probenecid by unknown mechanism. Use Caution/Monitor.

              • sodium phenylacetate

                probenecid increases levels of sodium phenylacetate by decreasing renal clearance. Use Caution/Monitor.

              • sodium phenylbutyrate

                probenecid increases levels of sodium phenylbutyrate by decreasing renal clearance. Use Caution/Monitor.

              • sulfasalazine

                sulfasalazine will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

                sulfasalazine decreases effects of probenecid by unknown mechanism. Use Caution/Monitor.

              • sulindac

                sulindac will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • tenofovir DF

                probenecid increases levels of tenofovir DF by decreasing renal clearance. Use Caution/Monitor. Potential for increased toxicity. .

              • tolazamide

                probenecid increases levels of tolazamide by unspecified interaction mechanism. Use Caution/Monitor. Risk of hypoglycemia.

              • tolbutamide

                probenecid increases levels of tolbutamide by unspecified interaction mechanism. Use Caution/Monitor. Risk of hypoglycemia.

              • tolfenamic acid

                tolfenamic acid will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • tolmetin

                tolmetin will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • valganciclovir

                probenecid will increase the level or effect of valganciclovir by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

              • willow bark

                willow bark will increase the level or effect of probenecid by acidic (anionic) drug competition for renal tubular clearance. Use Caution/Monitor.

                willow bark decreases effects of probenecid by unknown mechanism. Use Caution/Monitor.

              • zidovudine

                probenecid increases levels of zidovudine by decreasing metabolism. Use Caution/Monitor.

              Minor (22)

              • aztreonam

                probenecid increases levels of aztreonam by decreasing elimination. Minor/Significance Unknown.

              • benazepril

                probenecid increases levels of benazepril by Other (see comment). Minor/Significance Unknown. Comment: Probenecid may decrease the renal excretion of benazepril; monitor blood pressure.

              • captopril

                probenecid increases effects of captopril by unspecified interaction mechanism. Minor/Significance Unknown.

              • dapsone

                probenecid increases levels of dapsone by decreasing elimination. Minor/Significance Unknown.

              • enalapril

                probenecid increases effects of enalapril by unspecified interaction mechanism. Minor/Significance Unknown.

              • ertapenem

                probenecid increases levels of ertapenem by decreasing elimination. Minor/Significance Unknown.

              • fosinopril

                probenecid increases effects of fosinopril by unspecified interaction mechanism. Minor/Significance Unknown.

              • gemifloxacin

                probenecid increases levels of gemifloxacin by decreasing renal clearance. Minor/Significance Unknown.

              • imidapril

                probenecid increases effects of imidapril by unspecified interaction mechanism. Minor/Significance Unknown.

              • lisinopril

                probenecid increases effects of lisinopril by unspecified interaction mechanism. Minor/Significance Unknown.

              • methohexital

                probenecid increases levels of methohexital by unknown mechanism. Minor/Significance Unknown.

              • moexipril

                probenecid increases effects of moexipril by unspecified interaction mechanism. Minor/Significance Unknown.

              • penicillin VK

                probenecid will increase the level or effect of penicillin VK by acidic (anionic) drug competition for renal tubular clearance. Minor/Significance Unknown.

              • perindopril

                probenecid increases effects of perindopril by unspecified interaction mechanism. Minor/Significance Unknown.

              • primaquine

                primaquine, probenecid. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Risk of hemolysis in G6PD deficient pts.

              • quinapril

                probenecid increases effects of quinapril by unspecified interaction mechanism. Minor/Significance Unknown.

              • ramipril

                probenecid increases effects of ramipril by unspecified interaction mechanism. Minor/Significance Unknown.

              • sulfadiazine

                probenecid increases levels of sulfadiazine by unspecified interaction mechanism. Minor/Significance Unknown.

              • sulfamethoxazole

                probenecid increases levels of sulfamethoxazole by unspecified interaction mechanism. Minor/Significance Unknown.

              • sulfisoxazole

                probenecid increases levels of sulfisoxazole by unspecified interaction mechanism. Minor/Significance Unknown.

              • trandolapril

                probenecid increases effects of trandolapril by unspecified interaction mechanism. Minor/Significance Unknown.

              • valacyclovir

                probenecid increases levels of valacyclovir by decreasing renal clearance. Minor/Significance Unknown.

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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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              Images

              BRAND FORM. UNIT PRICE PILL IMAGE
              probenecid oral
              -
              500 mg tablet
              probenecid oral
              -
              500 mg tablet
              probenecid oral
              -
              500 mg tablet

              Copyright © 2010 First DataBank, Inc.

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              Patient Handout

              Patient Education
              probenecid oral

              PROBENECID - ORAL

              (proe-BEN-e-sid)

              COMMON BRAND NAME(S): Benemid

              USES: This medication is used to prevent gout and gouty arthritis. It will not treat a sudden/severe attack of gout and may make it worse. Probenecid belongs to a class of drugs known as uricosurics. It lowers high levels of uric acid in your body by helping the kidneys to get rid of uric acid. When uric acid levels get too high, crystals can form in the joints, causing gout. Lowering uric acid levels may also help your kidneys.Probenecid may be prescribed in combination with certain antibiotics (such as penicillins). It increases the levels of antibiotic in the blood, which helps the antibiotic work better.Probenecid should not be used by children younger than 2 years.

              HOW TO USE: To prevent gout, take this medication by mouth, usually twice daily with food or antacids to reduce stomach upset or as directed by your doctor. It is best to drink a full glass of water with each dose and at least another 8 glasses (8 ounces each) a day while taking this drug in order to prevent kidney stones. If you are on restricted fluid intake, consult your doctor for further instructions. Your doctor may also instruct you on how to decrease acidity in your urine (such as by avoiding large amounts of ascorbic acid/vitamin C) to prevent kidney stones. Your doctor may order other medications (such as sodium bicarbonate, citrate) to make your urine less acidic.Dosage is based on your condition and response to therapy. Your doctor may direct you to take a low dose at first, then adjust your dose based on uric acid levels and your gout symptoms. After you have been symptom-free for several months and your uric acid levels are normal, your doctor may lower your probenecid dose to the lowest effective dose. Follow your doctor's directions carefully.Probenecid should not be started during a sudden/severe gout attack. Wait until your current attack is over before starting this medication. You may experience an increase in the number of gout attacks for several months after starting this medicine while the body removes extra uric acid. If you have a gout attack while taking probenecid, continue taking it along with your medications for gout pain.Probenecid is not a pain reliever. To relieve pain from gout, continue to take your medicines prescribed for pain from gout attacks (e.g., colchicine, ibuprofen, indomethacin) as directed by your doctor.If you are taking this medication to raise the level of antibiotics in your body, follow your doctor's directions for when to take the antibiotic and when to take the probenecid.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day.Inform your doctor if your condition persists or worsens.

              SIDE EFFECTS: Nausea, loss of appetite, dizziness, vomiting, headache, sore gums, or frequent urination may occur as your body adjusts to the medicine. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if any of these unlikely but serious side effects occur: lower back pain, difficult/painful urination, change in amount/color of urine.Tell your doctor right away if any of these rare but very serious side effects occur: easy bruising/bleeding, signs of infection (e.g., fever, sore throat), severe abdominal pain, pale stools, unusual tiredness, dark urine, yellowing eyes/skin.A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

              PRECAUTIONS: Before taking probenecid, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: low blood counts (e.g., aplastic anemia, bone marrow depression), certain type of kidney stone (uric acid).Before using this medication, tell your doctor or pharmacist your medical history, especially of: cancer treatment, a certain enzyme deficiency (G6PD), kidney problems (e.g., kidney stones, obstruction), peptic ulcer disease.This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).Before having surgery, tell your doctor or dentist that you are using this medication.Kidney function declines as you grow older. This medication is removed by the kidneys. Elderly people may be at greater risk for side effects while using this drug, including stomach problems.During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is not known whether this drug passes into breast milk. Consult your doctor before breast-feeding.

              DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: cancer chemotherapy, baricitinib, dyphylline, ketorolac, methotrexate, pyrazinamide, salicylates (e.g., high-dose aspirin), zidovudine, certain drugs removed from your body by the kidneys (such as ceftazidime/avibactam, dapsone, heparin, fosfomycin).Alcohol can decrease this drug's effectiveness. Limit alcohol while taking this medication.This medication may interfere with certain laboratory tests (including urine glucose tests), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.

              OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe vomiting, loss of consciousness, seizures.

              NOTES: Do not share this medication with others.Laboratory and/or medical tests (e.g., uric acid blood levels, liver/kidney function tests, complete blood count) may be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.If you are using this medication to treat gout, your doctor may recommend a low-purine diet. Follow your doctor's instructions carefully.

              MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

              STORAGE: Store at room temperature between 59-86 degrees F (15-30 degrees C) away from light and moisture. Do not store in the bathroom. Keep all medicines away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

              Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

              IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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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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              5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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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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              Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
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              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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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.