probenecid

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);
Lactation: Safety not established in breastfeeding.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: flushing, rash

GI: nausea, vomiting, abdominal pain, diarrhea, hepatitis, sore gums

GU: uric acid stones, urinary frequency

Hemat: anemia, APLASTIC ANEMIA

Neuro: headache, dizziness

Interactions ⬆ ⬇

Drug-drug:

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

Availability ⬆ ⬇

(Generic available)

Tablets: 500 mg
In combination with: colchicine.

Route/Dosage ⬆ ⬇

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.

Action ⬆ ⬇

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

Therapeutic effects:

Reduction of serum uric acid levels.
Prolonged serum levels of penicillins and other related antibiotics.

Classifications ⬆ ⬇

Therapeutic Classification: antigout agents, uricosurics

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following oral administration.

Distribution: Unknown.

Protein Binding: 75–95%.

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

Half-Life: 4–17 hr.

Time/Action Profile ⬆ ⬇

(effects on serum uric acid levels)

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

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication exactly as directed and 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.
Rep: Advise females of reproductive potential to notify health care professional if breastfeeding is planned.

Pronunciation ⬆ ⬇

Code ⬆

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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Indications ⬇

Contraind./Precautions ⬆ ⬇