Probenecid

What is Probenecid?

• Probenecid (Benemid; Probalan) is a uricosuric and renal tubular transport blocking agent used for the treatment of the hyperuricemia associated with gout and gouty arthritis.
• Probenecid is also used with penicillin or with ampicillin, methicillin, oxacillin, cloxacillin, or nafcillin for elevation and prolongation of plasma levels by whatever route the antibiotic is given.

Probenecid

Probenecid molecule ball

Probenecid molecule spacefill

What are the uses of this medicine?

• Probenecid (Benemid; Probalan) is used for the treatment of the hyperuricemia associated with gout and gouty arthritis.
• Probenecid is also used to make certain antibiotics (penicillin or with ampicillin, methicillin, oxacillin, cloxacillin, or [[]]nafcillin) more effective by preventing the body from passing them in the urine.

How does this medicine work?

• Probenecid is a uricosuric and renal tubular blocking agent.
• It inhibits the tubular reabsorption of urate, thus increasing the urinary excretion of uric acid and decreasing serum urate levels.
• Therapy leads to lowering of serum uric acid levels within a few weeks, and chronic therapy has been shown to decrease uric acid levels and to decrease acute gouty attacks.
• Probenecid inhibits the tubular secretion of penicillin and usually increases penicillin plasma levels by any route the antibiotic is given.
• Probenecid also has been reported to inhibit the renal transport of many other compounds including aminohippuric acid (PAH), aminosalicylic acid (PAS), indomethacin, sodium iodomethamate and related iodinated organic acids, 17-ketosteroids, pantothenic acid, phenolsulfonphthalein (PSP), sulfonamides, and sulfonylureas.

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• Who have Hypersensitivity to probenecid
• Children under 2 years of age
• with known blood dyscrasias or uric acid kidney stones

• Therapy with probenecid should not be started until an acute gouty attack has subsided.

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

• especially aminosalicylic acid
• antibiotics
• aspirin
• cancer chemotherapy agents (methotrexate)
• clofibrate (Atromid-S)
• dapsone
• diflunisal (Dolobid)
• diuretics ('water pills')
• heparin
• indomethacin (Indocin)
• medication for anxiety
• nitrofurantoin (Macrodantin, Macrobid)
• oral diabetes medications
• pyrazinamide
• salsalate (Disalcid)
• vitamins

Is this medicine FDA approved?

• Probenecid was approved for use in the United States in 1951 and is still used for therapy and prevention of gout and hyperuricemia.

How should this medicine be used?

Recommended dosage: Gout:

• Therapy with probenecid should not be started until an acute gouty attack has subsided.
• The recommended adult dosage is 250 mg (1/2 probenecid tablet), twice a day for one week, followed by 500 mg (1 tablet) twice a day thereafter.
• A daily dosage of 1000 mg may be adequate.
• However, if necessary, the daily dosage may be increased by 500 mg increments every 4 weeks within tolerance (and usually not above 2000 mg per day) if symptoms of gouty arthritis are not controlled or the 24 hour uric acid excretion is not above 700 mg.

Probenecid and Penicillin Therapy (General):

• Adults: The recommended dosage is 2000 mg (4 tablets of probenecid) daily in divided doses. This dosage should be reduced in older patients in whom renal impairment may be present.
• Children: 2-14 years of age:
• Initial dose: 25 mg/kg body weight (or 0.7 g/square meter body surface).
• Maintenance Dose: 40 mg/kg body weight (or 1.2 g/square meter body surface) per day, divided into 4 doses.
• For children weighing more than 50 kg (110 lb) the adult dosage is recommended.

Administration:

• Probenecid comes in a tablet to take by mouth.
• It usually is taken two times a day when prescribed for chronic gout or gouty arthritis and four times a day when prescribed with antibiotics to make them more effective.
• Probenecid may increase the frequency of gout attacks during the first 6 to 12 months that you take it, although it will eventually prevent them.
• Another drug, such as colchicine, may be prescribed to decrease this effect.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As tablet for oral administration contains 500 mg of probenecid

This medicine is available in fallowing brand namesː

• Benemid; Probalan

What side effects can this medication cause?

The most common side effects of this medicine include:

• headache
• dizziness
• precipitation of acute gouty arthritis
• hepatic necrosis
• vomiting
• nausea
• anorexia
• sore gums
• nephrotic syndrome
• uric acid stones with or without hematuria
• renal colic
• costovertebral pain
• urinary frequency
• anaphylaxis
• fever
• urticaria
• pruritus
• aplastic anemia
• leukopenia
• hemolytic anemia
• dermatitis
• alopecia
• flushing

What special precautions should I follow?

• Exacerbation of gout following therapy with probenecid may occur; in such cases colchicine or other appropriate therapy is advisable.
• Probenecid increases plasma concentrations of methotrexate in both animals and humans. If probenecid is given with methotrexate, the dosage of methotrexate should be reduced and serum levels may need to be monitored.
• In patients on probenecid the use of salicylates in either small or large doses is contraindicated. In patients on probenecid who require a mild analgesic agent the use of acetaminophen rather than small doses of salicylates would be preferred.
• Rarely, severe allergic reactions and anaphylaxis have been reported with the use of probenecid. The appearance of hypersensitivity reactions requires cessation of therapy with probenecid.
• Use with caution in patients with a history of peptic ulcer.
• Probenecid has been associated with minor serum aminotransferase elevations and very rarely with hypersensitivity reactions which, even more rarely, can be accompanied by acute liver injury.
• Probenecid has been used in patients with some renal impairment, but dosage requirements may be increased.
• Drink at least six to eight full glasses of water a day while taking probenecid to prevent kidney stones, unless directed to do otherwise by your doctor.
• Probenecid may cause an upset stomach. Take with food or antacids.
• If you are having any urine tests done, tell your doctor and the laboratory personnel that you are taking probenecid because it may affect the results of the test.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

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

Can this medicine be used in children?

• Probenecid cannot be used for children under 2 years of age.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• PROBENECID

Inactive ingredients (intravenous):

• CELLULOSE, MICROCRYSTALLINE
• SODIUM LAURYL SULFATE
• SODIUM STARCH GLYCOLATE TYPE A POTATO
• STARCH, CORN
• POVIDONE, UNSPECIFIED
• SILICON DIOXIDE
• MAGNESIUM STEARATE
• POLYVINYL ALCOHOL, UNSPECIFIED
• TITANIUM DIOXIDE
• POLYETHYLENE GLYCOL, UNSPECIFIED
• TALC
• D&C YELLOW NO. 10
• FD&C YELLOW NO. 6
• FD&C BLUE NO. 2
• ALUMINUM OXIDE

Who manufactures and distributes this medicine?

Distributed by:

• Lannett Company, Inc.
• Philadelphia, PA

What should I know about storage and disposal of this medication?

• STORE AT 20°-25°C (68°-77°F).
• PROTECT FROM LIGHT.

The following drugs are considered antigout medications:

• Allopurinol
• Benzbromarone
• Colchicine
• Febuxostat
• Lesinurad
• Pegloticase
• Probenecid
• Rasburicase

• Dailymed label info on Probenecid
• FDA Probenecid

Probenecid Resources
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