Probenecid Tablets

Name: Probenecid Tablets

Probenecid Tablets Description

Probenecid is a uricosuric and renal tubular transport blocking agent.

The chemical name for probenecid is 4-[(dipropylamino) sulfonyl] benzoic acid. It has the following structural formula:

Probenecid, USP is a white or nearly white, fine, crystalline powder. Probenecid is soluble in dilute alkali, in alcohol, in chloroform, and in acetone; it is practically insoluble in water and in dilute acids.

Each tablet for oral administration contains 500 mg of probenecid and the following inactive ingredients: microcrystalline cellulose, sodium lauryl sulfate, sodium starch glycolate, starch (corn), povidone, colloidal silicon dioxide, magnesium stearate, polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, D&C Yellow #10 Aluminum Lake, FD&C Yellow #6 Aluminum Lake, and FD&C Blue #2 Aluminum Lake.

Warnings

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. In animal studies, increased methotrexate toxicity has been reported. 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 because it 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.

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.

Use 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.

Probenecid Tablets Dosage and Administration

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.

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 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 (see PRECAUTIONS).

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 a 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.

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.

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.

Penicillin Therapy (Gonorrhea)1

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).

For further guidance, see CDC recommendations for definition of regimens of choice, alternative regimens, treatment of hypersensitive patients, and other aspects of therapy.

1 Recommended by the Center for 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). 2 See package circulars of manufacturers for detailed information about CONTRAINDICATIONS, WARNINGS, PRECAUTIONS, and ADVERSE REACTIONS.

How is Probenecid Tablets Supplied

Probenecid Tablets, USP are available containing 500 mg of Probenecid, USP.

The tablets are capsule shaped, film-coated yellow, debossed LCI on one side and 1367 on the other side. They are available as follows:

NDC 0527-1367-01     bottles of 100 tablets

NDC 0527-1367-10     bottles of 1000 tablets

STORE AT 20°-25°C (68°-77°F) [See USP Controlled Room Temperature]

PROTECT FROM LIGHT.

Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.

MANUFACTURED BY
LANNETT COMPANY, INC.
PHILADELPHIA, PA 19136

0527
1367
Revised 10/06

Principal display panel

NDC 0527-1367-10

Lannett

PROBENECID
TABLETS, USP

500 mg

Rx Only

1000 TABLETS

PROBENECID 
probenecid tablet, film coated
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:0527-1367
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
PROBENECID (PROBENECID) PROBENECID 500 mg
Inactive Ingredients
Ingredient Name Strength
CELLULOSE, MICROCRYSTALLINE  
SODIUM LAURYL SULFATE  
SODIUM STARCH GLYCOLATE TYPE A POTATO  
STARCH, CORN  
POVIDONE K29/32  
COLLOIDAL SILICON DIOXIDE  
MAGNESIUM STEARATE  
POLYVINYL ALCOHOL  
TITANIUM DIOXIDE  
POLYETHYLENE GLYCOL  
TALC  
D&C YELLOW NO. 10  
FD&C YELLOW NO. 6  
FD&C BLUE NO. 2  
ALUMINUM OXIDE  
Product Characteristics
Color YELLOW (Yellow) Score no score
Shape OVAL Size 18mm
Flavor Imprint Code LCI;1367
Contains     
Packaging
# Item Code Package Description
1 NDC:0527-1367-01 100 TABLET, FILM COATED (100 TABLET) in 1 BOTTLE
2 NDC:0527-1367-10 1000 TABLET, FILM COATED (1000 TABLET) in 1 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA080966 07/29/1976
Labeler - Lannett Company, Inc. (002277481)
Establishment
Name Address ID/FEI Operations
Lannett Company, Inc. 002277481 MANUFACTURE
Establishment
Name Address ID/FEI Operations
Lannett Company, Inc. 829757603 ANALYSIS, LABEL, MANUFACTURE, PACK
Establishment
Name Address ID/FEI Operations
Lannett Company, Inc. 683520909 ANALYSIS
Revised: 11/2010   Lannett Company, Inc.
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