probenecid

REMS

Prevention of recurrences of gouty arthritis.
Treatment of hyperuricemia secondary to thiazide therapy.
Used to increase and prolong serum levels of penicillin and related anti-infectives.

Inhibits renal tubular reabsorption of uric acid, thus promoting its renal excretion.

Therapeutic Effects:

Reduction of serum uric acid levels.

Absorption: Well absorbed following oral administration.

Distribution: Crosses the placenta.

Protein Binding: 75–95%.

Metabolism/Excretion: Mostly metabolized by the liver; 10% excreted unchanged in the urine.

Half-life: 4–17 hr.

Contraindicated in:

Hypersensitivity
Chronic high-dose salicylate therapy
Pedi: Children <2 yr.

Use Cautiously in:

Peptic ulcer
Blood dyscrasias
Uric acid kidney stones
Renal impairment (dosage ↓ recommended; may not be effective if CCr 30 mL/min)
OB: Has been used safely during pregnancy
Lactation: Safety not established.

CNS: headache, dizziness.

GI: nausea, vomiting, abdominal pain, diarrhea, drug-induced hepatitis, sore gums.

GU: uric acid stones, urinary frequency.

Derm: flushing, rashes.

Hemat: APLASTIC ANEMIA, anemia.

Drug-Drug:

↑blood levels of acyclovir, allopurinol, barbiturates, benzodiazepines, cephalosporins, dapsone, dyphylline, methotrexate, NSAIDs, penicillamine, penicillins, rifampin, sulfonamides, sulfonylureas, or zidovudine.
Large doses of salicylates may ↓ uricosuric activity.

PO (Adults and Children >50 kg): Hyperuricemia — 250 mg twice daily for 1 wk; ↑ to 500 mg twice daily, then may ↑ by 500 mg/day every 4 wk (not to exceed 3 g/day).Augmentation of penicillins/cephalosporins — 500 mg 4 times daily. Single-dose therapy of gonorrhea — 1 g with amoxicillin or penicillin.
PO (Children 2–14 yr and 50 kg): 25 mg/kg (700 mg/m²) initially; then 10 mg/kg (300 mg/m²) 4 times daily.

Probenecid therapy is not used to treat gouty arthritis but, rather, to prevent it. If acute attacks occur during therapy, probenecid is usually continued at full dose along with colchicine or NSAIDs.
PO: Administer with food or antacid to minimize gastric irritation.
- Gradual dosage reduction should be attempted if uric acid levels remain stable following 6 mo of therapy.

Therapeutic Classification: antigout agents, uricosurics

(Generic available)

Tablets: 500 mg;
In combination with: colchicine (Col-Probenecid). See Appendix [not included in this PDA edition].

(effects on serum uric acid levels)

ROUTE	ONSET	PEAK	DURATION
PO	30 min	2–4 hr	8 hr

Gout: Assess involved joints for pain, mobility, and edema throughout course of therapy.
- Monitor intake and output ratios. Fluids should be encouraged to prevent urate stone formation (2000–3000 mL/day). Alkalinization of the urine with sodium bicarbonate, potassium citrate, or acetazolamide may also be used for this purpose.

Lab Test Considerations:

CBC, serum uric acid levels, and renal function should be monitored routinely during long-term therapy.
- Serum and urine uric acid determinations may be measured periodically when probenecid is used to treat hyperuricemia.

Acute pain (Indications).
Impaired physical mobility (Indications).
Deficient knowledge, Relate med (Patient/Family Teaching).

Instruct patient to take medication exactly as directed, not to discontinue without consulting health care professional. Irregular dosage schedules may cause elevation of uric acid levels and precipitate an acute gout attack.
Explain purpose of the medication to patients taking probenecid with penicillin.
Advise patient to follow recommendations of health care professional regarding weight loss, diet, and alcohol consumption.
Caution patient not to take aspirin or other salicylates, because they decrease the effects of probenecid.
Instruct patient to report nausea, vomiting, loss of appetite, abdominal pain, unusual bleeding or bruising, sore throat, fatigue, malaise, or yellowing of the skin or eyes promptly.

Decrease in pain and swelling in affected joints and subsequent decrease in frequency of gout attacks. May require several mo of continuous therapy for maximum effects.
Decrease in serum uric acid levels.
Prolonged serum levels of penicillins and other related antibiotics.

NDC Code^*

0378- Mylan Pharmaceuticals Inc.
0378-0156- Probenecid 0378-0156-01- 100 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (0378-0156-01)

0527- Lannett Company, Inc.
0527-1367- Probenecid 0527-1367-01- 100 TABLET, FILM COATED in 1 BOTTLE (0527-1367-01)

0527- Lannett Company, Inc.
0527-1367- Probenecid 0527-1367-10- 1000 TABLET, FILM COATED in 1 BOTTLE (0527-1367-10)

0591- Actavis Pharma, Inc.
0591-5347- Probenecid 0591-5347-01- 100 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (0591-5347-01)

0591- Actavis Pharma, Inc.
0591-5347- Probenecid 0591-5347-10- 1000 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (0591-5347-10)

10135- Marlex Pharmaceuticals Inc
10135-541- Probenecid 10135-541-01- 100 TABLET, FILM COATED in 1 BOTTLE (10135-541-01)

10135- Marlex Pharmaceuticals Inc
10135-541- Probenecid 10135-541-10- 1000 TABLET, FILM COATED in 1 BOTTLE (10135-541-10)

43353- Aphena Pharma Solutions - Tennessee, LLC
43353-839- Probenecid 43353-839-60- 90 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (43353-839-60)

43353- Aphena Pharma Solutions - Tennessee, LLC
43353-991- Probenecid 43353-991-60- 90 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (43353-991-60)

63629- Bryant Ranch Prepack
63629-8213- Probenecid 63629-8213-1- 30 TABLET, FILM COATED in 1 BOTTLE (63629-8213-1)

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Pronunciation ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Route/Dosage ⬆ ⬇

Implementation ⬆ ⬇

US Brand Names ⬆ ⬇

Canadian Brand Names ⬆ ⬇

Classifications ⬆ ⬇

Availability ⬆ ⬇

Time/Action Profile ⬆ ⬇

Assessment ⬆ ⬇

Pot. Nursing Diagnoses ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

Code ⬆