Yes

Uricosuric Agent

Prevention of gouty arthritis; hyperuricemia; prolongation of beta-lactam effect (ie, serum levels)

B

Hypersensitivity to probenecid or any component; high-dose aspirin therapy; moderate to severe renal impairment; children <2 years of age

Use with caution in patients with peptic ulcer; use extreme caution in the use of probenecid with penicillin in patients with renal insufficiency; probenecid may not be effective in patients with a creatinine clearance <30 to 50 mL/minute; may cause exacerbation of acute gouty attack

>10%:

Central nervous system: Headache

Gastrointestinal: Anorexia, nausea, vomiting

Neuromuscular & skeletal: Gouty arthritis (acute)

1% to 10%:

Cardiovascular: Flushing of face

Central nervous system: Dizziness

Dermatologic: Rash, itching

Gastrointestinal: Sore gums

Genitourinary: Painful urination

Renal: Renal calculi

<1%: Leukopenia, hemolytic anemia, aplastic anemia, hepatic necrosis, urate nephropathy, nephrotic syndrome, anaphylaxis

Symptoms of overdose include nausea, vomiting, tonic-clonic seizures, coma

Activated charcoal is especially effective at binding probenecid, for GI decontamination

Decreased effect:

Salicylates (high dose) may decrease uricosuria

Nitrofurantoin may decrease efficacy

Increased toxicity:

Increases methotrexate toxic potential; combination with diflunisal has resulted in 40% decrease in its clearance and as much as a 65% increase in plasma concentrations due to inhibition of diflunisal metabolism

Probenecid decreases clearance of beta-lactams such as penicillins and cephalosporins; increases levels/toxicity of acyclovir, thiopental, clofibrate, dyphylline, pantothenic acid, benzodiazepines, rifampin, sulfonamide, dapsone, sulfonylureas, and zidovudine

Avoid concomitant use with ketorolac (and other NSAIDs) since its half-life is increased twofold and levels and toxicity are significantly increased

Allopurinol readministration may be beneficial by increasing the uric acid lowering effect

Pharmacologic effects of penicillamine may be attenuated

Competitively inhibits the reabsorption of uric acid at the proximal convoluted tubule, thereby promoting its excretion and reducing serum uric acid levels; increases plasma levels of weak organic acids (penicillins, cephalosporins, or other beta-lactam antibiotics) by competitively inhibiting their renal tubular secretion

Onset of action: Effect on penicillin levels reached in about 2 hours

Absorption: Rapid and complete from GI tract

Metabolism: In the liver

Half-life: Normal renal function: 6-12 hours and is dose dependent

Time to peak serum concentration: 2-4 hours

Elimination: In urine

Oral:

<2 years: Not recommended

2-14 years: Prolong penicillin serum levels: 25 mg/kg starting dose, then 40 mg/kg/day given 4 times/day

Gonorrhea: <45 kg: 25 mg/kg x 1 (maximum: 1 g/dose) 30 minutes before penicillin, ampicillin or amoxicillin

Adults:

Hyperuricemia with gout: 250 mg twice daily for one week; increase to 250-500 mg/day; may increase by 500 mg/month, if needed, to maximum of 2-3 g/day (dosages may be increased by 500 mg every 6 months if serum urate concentrations are controlled)

Prolong penicillin serum levels: 500 mg 4 times/day

Gonorrhea: 1 g 30 minutes before penicillin, ampicillin, procaine, or amoxicillin

Pelvic inflammatory disease: Cefoxitin 2 g I.M. plus probenecid 1 g orally as a single dose

Neurosyphilis: Aqueous procaine penicillin 2.4 units/day I.M. plus probenecid 500 mg 4 times/day for 10-14 days

Dosing adjustment in renal impairment: Cl_cr <50 mL/minute: Avoid use

Food: Drug may cause GI upset; take with food if GI upset. Drink plenty of fluids.

Administer with food or antacids to minimize GI effects

Uric acid, renal function, CBC

False-positive glucosuria with Clinitest®, a falsely high determination of theophylline has occurred and the renal excretion of phenolsulfonphthalein 17-ketosteroids and bromsulfophthalein (BSP) may be inhibited

May cause dizziness

May rarely cause leukopenia; use caution with clozapine and carbamazepine

No information available to require special precautions

No effects or complications reported

Take as directed; do not discontinue without consulting prescriber. May take 6-12 months to reduce gouty attacks (attacks may increase in frequency and severity for first few months of therapy). Take with food or antacids or alkaline ash foods (milk, nuts, beets, spinach, turnip greens). Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). Avoid aspirin, or aspirin-containing substances. Diabetics should use serum glucose monitoring. If you experience severe headache, contact prescriber for medication. You may experience dizziness or lightheadedness (use caution when driving, changing position, or engaging in tasks requiring alertness until response to drug is known); nausea, vomiting, indigestion, or loss of appetite (small frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help). Report skin rash or itching, persistent headache, blood in urine or painful urination, excessive tiredness or easy bruising or bleeding, or sore gums. Breast-feeding precautions: Consult prescriber if breast-feeding.

An alkaline urine is recommended to avoid crystallization of urates; use of sodium bicarbonate or potassium citrate is suggested until serum uric acid normalizes and tophaceous deposits disappear

Tablet: 500 mg