Probenecid

Probenecid
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Alberto Plate [2]

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Overview

Probenecid is an antigout, uricosuric and renal tubular transport blocking agent. that is FDA approved for the treatment of hyperuricemia associated with gout and gouty arthritis. Common adverse reactions include {{{adverseReactions}}}.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Gout

Therapy with probenecid should not be started until an acute gouty attack has subsided. However, if an 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.

• Dosage: The recommended adult dosage is 250 mg (½ probenecid tablet), twice a day for one week, followed by 500 mg (1 tablet) twice a day thereafter.

Some degree of renal impairment may be present in patients with gout. 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. As noted, probenecid may not be effective in chronic renal insufficiency particularly when the glomerular filtration rate is 30 mg mL/minute or less.

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, as well as sufficient sodium bicarbonate (3 to 7.5 g daily ), or potassium citrate (7.5 g daily) to maintain an alkaline urine.

Alkalization of the urine is recommended until the serum urate level returns to normal limits and tophaceous deposits disappear, i.e., during the period when urinary excretion of uric acid is at high level. Thereafter, alkalization of the urine and the usual restriction of purine-producing foods may be somewhat relaxed.

Probenecid should be continued at the dosage that will maintain normal serum urate levels. When acute attacks have been absent for 6 months or more and serum urate levels remain within normal limits, the daily dosage may be decreased by 500 mg every 6 months. The maintenance dosage should not be reduced to the point where serum urate levels tend to rise.

Gonnorrhea

Recommended by the Center of Disease Control, U.S Department of Health and Human Services, Public Health Service (Morbidity and Mortality Weekly Report Supplement, Volume 34, Number 4S, October 18, 1985). In uncomplicated gonococcal infections in men and women (urethral, cervical, rectal), 1 g of probenecid should be given orally with 4.8 million units of aqueous procaine penicillin G² (given IM), or 3 g of amoxicillin² (given orally), or 3.5 g of ampicillin² (given orally).

Probenecid and Penicillin Therapy (In 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.
    • Probenecid is contraindicated in children under 2 years of age.

The PSP excretion test may be used to determine the effectiveness of probenecid in retarding penicillin excretion and maintaining therapeutic levels. The renal clearance of PSP is reduced to about one-fifth the normal rate when dosage of probenecid is adequate.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Probenecid in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Probenecid in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding Probenecid FDA-Labeled Indications and Dosage (Pediatric) in the drug label.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Probenecid in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Probenecid in pediatric patients.

Contraindications

There is limited information regarding Probenecid Contraindications in the drug label.

Warnings

There is limited information regarding Probenecid Warnings' in the drug label.

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Probenecid Clinical Trials Experience in the drug label.

Postmarketing Experience

There is limited information regarding Probenecid Postmarketing Experience in the drug label.

Drug Interactions

There is limited information regarding Probenecid Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): There is no FDA guidance on usage of Probenecid in women who are pregnant.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Probenecid in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Probenecid during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Probenecid in women who are nursing.

Pediatric Use

There is no FDA guidance on the use of Probenecid in pediatric settings.

Geriatic Use

There is no FDA guidance on the use of Probenecid in geriatric settings.

Gender

There is no FDA guidance on the use of Probenecid with respect to specific gender populations.

Race

There is no FDA guidance on the use of Probenecid with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Probenecid in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Probenecid in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Probenecid in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Probenecid in patients who are immunocompromised.

Administration and Monitoring

Administration

There is limited information regarding Probenecid Administration in the drug label.

Monitoring

There is limited information regarding Probenecid Monitoring in the drug label.

IV Compatibility

There is limited information regarding the compatibility of Probenecid and IV administrations.

Overdosage

There is limited information regarding Probenecid overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.

Pharmacology

There is limited information regarding Probenecid Pharmacology in the drug label.

Mechanism of Action

There is limited information regarding Probenecid Mechanism of Action in the drug label.

Structure

There is limited information regarding Probenecid Structure in the drug label.

Pharmacodynamics

There is limited information regarding Probenecid Pharmacodynamics in the drug label.

Pharmacokinetics

There is limited information regarding Probenecid Pharmacokinetics in the drug label.

Nonclinical Toxicology

There is limited information regarding Probenecid Nonclinical Toxicology in the drug label.

Clinical Studies

There is limited information regarding Probenecid Clinical Studies in the drug label.

How Supplied

There is limited information regarding Probenecid How Supplied in the drug label.

Storage

There is limited information regarding Probenecid Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Probenecid Patient Counseling Information in the drug label.

Precautions with Alcohol

Alcohol-Probenecid interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Probenecid Brand Names in the drug label.

Look-Alike Drug Names

There is limited information regarding Probenecid Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

Probenecid

File:Probenecid.png
Clinical data
ATC code	M04AB01 (WHO)
Pharmacokinetic data
Protein binding	75-95%
Elimination half-life	6-12 hours
Identifiers
IUPAC name 4-(dipropylsulfamoyl)benzoic acid
CAS Number	57-66-9
PubChem CID	4911
DrugBank	APRD00167
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C13H19NO4S
Molar mass	285.36 g/mol

Probenecid is a uricosuric drug, primarily used in treating gout or hyperuricemia, that increases uric acid removal in the urine. One of its trade names is 'Benuryl.'

Probenecid also decreases the renal excretion of some drugs.

In one study, probenecid was shown to more than double a patient's exposure to oseltamivir (trade name Tamiflu), an antiviral drug used to combat influenza. This is significant because nations are currently stockpiling oseltamivir in anticipation of an influenza pandemic, and there could be supply shortages. During World War II, probenecid was used to extend limited supplies of penicillin, and is still currently used to increase antibiotic concentrations in serious infections. It has also found use as a masking agent by athletes attempting to get away with using performance enhancing drugs.

In the kidneys it is filtered at the glomerulus, secreted in the proximal tubule and reabsorbed in the distal tubule.

Probenecid's exact mechanism of action in the kidneys' nephrons is unknown. (I wish to question this statement. The text Human Physiology by Dee Unglaub Silverthorn explains that gout is caused by elevated levels of uric acid in the plasma, and that the kidney's organic anion transporter (OAT) reclaims uric acid from the urine and returns it to the plasma. If the organic acid probenecid is administered to a patient, the OAT binds to probenecid instead of to uric acid, preventing the reabsorption of uric acid. As a result, more uric acid leaves the body in the urine, lowering the uric acid concentration in the plasma. This is an example of the way in which competition between substrates transported across cell membranes has been put to use in medicine.)

Probenecid reduces the reabsorption of uric acid.

See also

• Gout

References

• Probenecid pharmacology from McGill University