Source: Medicines and Medical Devices Safety Authority (NZ) Revision Year: 2018 Publisher: AFT Pharmaceuticals Ltd, PO BOX 33203, Takapuna, Auckland, Email: customer.service@aftpharm.com
Probenecid is a uricosuric agent for the treatment of hyperuricaemia in all stages of gout and gouty arthritis except a presenting acute attack. Asymptomatic hyperuricaemia seems to occur in a significant percentage of relatives of gouty patients. Probenecid may be given prophylactically to these people to forestall gouty attacks and urate deposition in tissues. By virtue of its effective uricosuric activity, probenecid may be used to control the hyperuricaemia induced or aggravated by many diuretics employed for the treatment of oedema and hypertension (e.g. thiazides and similar diuretics).
Probenecid is indicated for the elevation and prolongation of plasma levels by whatever route the antibiotic is given. A two-to-fourfold increase in plasma levels has been demonstrated for penicillin G or V, the synthetic penicillins, ampicillin, methicillin, oxacillin, cloxacillin, nafcillin, carbenicillin, and for the cephamycin, cefoxitin sodium, and the cephalosporins, cephalothin, cephalexin and cephaloglycin.
Probenecid therapy should not be initiated until an acute gouty attack has subsided. Should an acute attack be precipitated during therapy, the drug may be continued without changing the dosage, and therapeutic doses of colchicine, indomethacin, or other appropriate therapy may be administered to control the acute attack.
The recommended dose for adults is 250 mg (½ tablet) twice a day for one week, followed by 500 mg (1 tablet) twice a day thereafter. As some degree of renal impairment is common in patients with gout, a daily dosage of 1000 mg may be adequate for many patients. The daily dosage may be increased, if necessary, by increments of 500 mg every four weeks, but usually not beyond 2000 mg daily, if symptoms of gouty arthritis are not controlled or the 24-hour urate excretion is not above 700 mg.
In chronic renal insufficiency particularly when the glomerular filtration rate is 30 mL/minute or less probenecid may not be effective.
Gastric intolerance may be indicative of overdosage. This may be corrected by reducing the dose without losing the required therapeutic response.
Probenecid should be continued at a dosage that will maintain a normal serum uric acid level. When acute attacks have been absent for six months or more and serum uric acid levels remain within normal limits, the daily dosage may be decreased by one tablet every six months to a minimum effective dose. The maintenance dosage should not be reduced to the point where serum uric acid levels tend to rise.
For the treatment of uncomplicated gonorrhoea in men or women, a single 1000 mg dose of Probenecid (2 tablets) may be given with adequate doses of oral ampicillin, intramuscularly injected aqueous procaine penicillin G or cefoxitin. If oral ampicillin is used, probenecid should be administered simultaneously. If a parenteral antibiotic is administered, the dose of probenecid should be given preferably at least 30 minutes before the injection.
The adult recommended dosage is 2000 mg (4 tablets) daily in divided doses, reduced in older patients suspected of having renal impairment. Due to its mechanism of action, Probenecid is not recommended for concurrent use with a β-lactam antibiotic in the presence of known renal impairment.
For two years of age or older the recommended dosage is 25 mg/kg (or 0.7 g/m² body surface) of body weight initially, followed by 40 mg/kg (or 1.2 g/m² body surface) daily in divided doses every six hours. For children weighing more than 50 kilograms the adult dose is recommended.
The phenolsulfonphthalein (PSP) excretion test may be used to determine the effectiveness of probenecid in retarding penicillin excretion and maintaining therapeutic levels. When the dose of probenecid is adequate, the renal clearance of PSP is reduced to about one-fifth of the normal rate.
This product is not able to deliver all approved dose regime.
Tablets for oral administration.
In the event of overdosage, symptomatic and supportive measures should be employed along with gastric lavage. If signs of central nervous excitation are present, a short-acting barbituate may be given parentally.
For advice on the management of overdose please contact the National Poisons Centre on 0800 POISON (0800 764766).
3 years.
Store below 30°C.
Probenecid Tablet 500 mg is packed in Milky White 100 cc HDPE Bottles & Milky White 38 mm HDPE caps with induction wad, which is labeled with Printed Sticker Labels.
Silica Gel Bags is used in packing as a preventive measure to absorb excess of moisture.
Not applicable.
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