probenecid


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Related to probenecid: allopurinol

probenecid

 [pro-ben´ĕ-sid]
a compound used in treatment of gout to promote excretion of uric acid; also used to increase serum concentration of certain antibiotics and other drugs.

probenecid

Benuryl (CA)

Pharmacologic class: Sulfonamide-derived uricosuric

Therapeutic class: Antigout drug, tubular blocking agent

Pregnancy risk category B

Action

Promotes uric acid excretion from kidney by blocking tubular reabsorption; also inhibits tubular secretion of weak organic acids (most penicillins and cephalosporins, some beta-lactams)

Availability

Tablets: 0.5 g

Indications and dosages

Hyperuricemia caused by gout Adults and children weighing more than 50 kg (110 lb): After acute gout attack subsides, 250 mg P.O. b.i.d. for 1 week, then 500 mg b.i.d.; may increase by 500 mg/day q 4 weeks (not to exceed 3 g/day)

To prolong action or increase blood level of penicillins or cephalosporins

Adults: 500 mg P.O. q.i.d.

Children ages 2 to 14: Initially, 25 mg/kg or 0.7 g/m2, then a maintenance dosage of 40 mg/kg/day or 1.2 g/m2 in four divided doses

Gonorrhea

Adults: 1 g P.O. as a single dose given with or immediately before prescribed ampicillin dose

Dosage adjustment

• Renal impairment

Off-label uses

• Hyperuricemia secondary to thiazide therapy

Contraindications

• Hypersensitivity to drug

• Acute gout attack

• Uric acid calculi

• Blood dyscrasias

• Concurrent salicylate use

• Concurrent penicillin use in patients with renal impairment

• Children younger than age 2

Precautions

Use cautiously in:

• peptic ulcer, renal impairment

• pregnant or breastfeeding patients.

Administration

Don't give until acute gout attack subsides.

• Ensure high fluid intake and alkaline urine during therapy.

Adverse reactions

CNS: headache, dizziness

GI: nausea, vomiting, diarrhea, abdominal pain, anorexia

GU: urinary frequency, uric acid calculi, renal colic, nephrotic syndrome

Hematologic: anemia, hemolytic anemia, aplastic anemia

Hepatic: hepatitis, hepatic necrosis

Metabolic: gout exacerbation

Musculoskeletal: costovertebral pain

Skin: flushing, rash, pruritus

Other: sore gums, fever, hypersensitivity reactions including anaphylaxis

Interactions

Drug-drug. Acyclovir, allopurinol, barbiturates, cephalosporins, pantothenic acid, penicillins: increased blood levels of these drugs, enhanced uric acid-reducing effect of probenecid

Benzodiazepines: faster onset and prolonged effects of these drugs

Clofibrate: increased clofibrate blood level

Dapsone: accumulation of dapsone and its metabolites

Dyphylline: increased half-life and decreased clearance of dyphylline

Methotrexate, nonsteroidal anti-inflammatory drugs, rifampin, sulfonamides: increased blood levels, therapeutic effects, and toxicity of these drugs

Oral hypoglycemics: increased half-life and effects of these drugs

Penicillamine: increased pharmacologic effect of penicillamine

Salicylates: decreased probenecid or salicylate activity

Thiopental: extended anesthetic effect of thiopental

Zidovudine: increased risk of zidovudine toxicity

Drug-diagnostic tests. Urine glucose tests using copper reduction method (such as Clinitest): false-positive result

Patient monitoring

• Monitor kidney and liver function tests, CBC, and blood urea nitrogen level.

• Assess fluid intake and output to ensure good hydration and reduce urinary side effects.

• During first 6 to 12 months of therapy, monitor pattern and severity of acute gout attacks to assess need for additional anti-inflammatory drugs.

Patient teaching

• Advise patient to take with food or milk to minimize GI upset.

• Teach patient about causes of gout and proper use of drug. Stress that he must wait until acute attack subsides and then take drug regularly to prevent further attacks.

• Tell patient drug may exacerbate acute gout attacks for first 6 to 12 months, necessitating colchicine or other anti-inflammatory drug for 3 to 6 months.

• Instruct patient to drink 2 to 3 liters of fluids daily.

• Tell patient with gout to limit foods high in purine (such as anchovies, organ meats, and legumes).

• Instruct diabetic patient to test urine glucose level during therapy.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

pro·ben·e·cid

(prō-ben'ĕ-sid),
A competitive inhibitor of the secretion of penicillin or p-aminohippurate by kidney tubules; a uricosuric agent.

probenecid

(prō-bĕn′ĭ-sĭd)
n.
A uricosuric drug, C13H19NO4S, derived from benzoic acid and used chiefly in the treatment of gout.

probenecid

A drug used to prevent kidney damage during treatment with the antiviral drug cidofovir.

Probenecid

A drug that corrects hyperuricemia by increasing the urinary excretion of urate.
Mentioned in: Gout

pro·ben·e·cid

(prō-ben'ĕ-sid)
A uricosuric agent.

Patient discussion about probenecid

Q. SVT and AF, Hearts that go fast to slow or any others probs with the beats of any kind and Ablation of hearts I have had Ablation done once and I am still having passing out spells and still on 50mg toprol 2 times a day till two days ago, now I am on 150 to 200 aday again. Its not the first time I have had to up meds. I had ablation down 4/22/05. I can breath better now but but it didnt take it away as you can tell. Now Dr Leonardie would like to do it again . This is the big ????! Will it or can it work 100% this time, or will it hit and miss some again???? MTT

A. Well I can understand the frustration of having to go through this procedure yet another time. There are no guarantees in medicine. You should follow your doctor's advice, as another proceudre might be more helpful than the last one. However you should keep in mind that nothing is for sure.

More discussions about probenecid
References in periodicals archive ?
The initial dosage of probenecid is 250 mg twice daily, uptitrated weekly to 1 g twice daily, based on the sUA level.
Regulation of factors Target Mechanism A20/TNFAIP3 [34] NLRP1 Binding with Bcl-2 and Bcl-X(L) miR-223 [38] NLRP3 Acting on a conserved binding site within 3' untranslated region of NLRP3 miR-7 [39] NLRP3 Posttranscriptionally controlled NLRP3 expression Human [CD4.sup.+] NLRP3 Down-regulation of P2X7R memory T cells [41] signaling molecules Caspase-12 [42] Caspase-1 Associated with caspase-1 POM-1 [43] NLRP1 Inhibit the events related with ATP- dependent inflammasome Probenecid [44] NLRP3 Block pannexin 1 channel and high extracellular potassium Type I interferons [86] NLRP1/NLRP3 Via the STAT1 transcription factor A20/TNFAIP3: tumor necrosis factor a-induced protein 3; NLRP1/NLRP3: NOD-like receptors pyrin domain-containing 1 or 3; POM-1: polyoxotungstate-1.
o 24 x [10.sup.6] U/dia en infusion continua durante 10-14 dias Penicilina G Dosis: 2,4 x [10.sup.6] U/dia procainica 2 g/dia Probenecid Administrar: 2,4 x [10.sup.6] U/dia en una sola aplicacion i.m.
To prepare MPR2 inhibitor probenecid stock solution, probenecid was weighed precisely at 0.028 g, and placed in a 25-mL volumetric flask.
CAZ, ceftriaxone via intramuscular injection and oral azithromycin; ZAP, azithromycin, amoxicillin, probenecid.
Stimulation of primary arterial endothelial mesenteric cells and intact mesenteric arteries with the neurotransmitter calcitonin gene-related peptide (CGRP) leads to Panx1 channel opening as shown by ethidium uptake, which was prevented by the specific inhibition of CGRP receptors with the peptide CGRP[sub]8-37 or the blockade of Panx1 channels with probenecid. Furthermore, stimulation of perivascular sensory nerves with capsaicin led to CGRP release and downregulation of endothelial NO synthase (eNOS) expression, linking pro-inflammatory-induced neurotransmitter release to the development of endothelial dysfunction during inflammation through decreased eNOS protein levels.[36]
(5) Newer therapies that require more evidence include substances targeting anti-crystal formation (such as probenecid) as well as anti-inflammatory medications (such as methotrexate) that target interleukin pathways to prevent recurrent attacks.
Medical therapy has very limited role in the treatment of calcinosis cutis but drugs like corticosteroids, probenecid, colchicine, sodium etidronate, diphosphonates, diltiazem, and magnesium and aluminium antacids can be used in order to relieve the symptoms9,10.
Your doctor can give you the anti-gout drug colchicine and the preventive drugs, allopurinol or probenecid.
These drugs include allopurinol (Aloprim, Lopurin, Zyloprim), febuxostat (Uloric), and probenecid (Benemid).
Probenecid is a uricosuric agent and an alternative to allopurinol.