Davis's Drug Guide

probenecid

General

Pronunciation
proe-BEN-e-sid [Audio]

Trade Name(s)

• Benuryl [Canada]

• Probalan

Pregnancy Category
Category B

Ther. class.
antigout agents
uricosurics

Indications

• 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

Action

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

Therapeutic Effect(s):
Reduction of serum uric acid levels

Pharmacokinetics

Absorption: Well absorbed following oral administration

Distribution: Crosses the placenta

Protein Binding: 75–95%

Metabolism and 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)

ROUTEONSETPEAKDURATION
PO30 min2–4 hr8 hr

Contraindication/Precautions

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 C30 mL/min)

• OB: Has been used safely during pregnancy

• Lactation: Safety not established

Adverse Reactions/Side Effects

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.

*CAPITALS indicates life-threatening.
*italic indicates most frequent.

Interactions

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

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 C50 kg): 25 mg/kg (700 mg/m2) initially; then 10 mg/kg (300 mg/m2) 4 times daily.

Availability

Tablets: 500 mg

Assessment

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

Potential Nursing Diagnoses

• Acute pain (Indications)

• Impaired physical mobility (Indications)

• Deficient knowledge , related to medication regimen (Patient/Family Teaching)

Implementation

• 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

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

Evaluation/Desired Outcomes

• Decrease in pain and swelling in affected joints and subsequent decrease in frequency of gout attacks. May require several months of continuous therapy for maximum effects

• Decrease in serum uric acid levels

• Prolonged serum levels of penicillins and other related antibiotics



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