Probenecid

By

Generic Name: Probenecid Brand Name(s): Generics only. No brands available.

Uses

What is Probenecid used for?

Probenecid is used to prevent gout and gouty arthritis. It will not treat a sudden/severe attack of gout and may make it worse. Probenecid belongs to a class of drugs known as uricosurics. It lowers high levels of uric acid in your body by helping the kidneys to get rid of uric acid. When uric acid levels get too high, crystals can form in the joints, causing gout. Lowering uric acid levels may also help your kidneys.

Probenecid may be prescribed in combination with certain antibiotics (such as penicillins). It increases the levels of antibiotic in the blood, which helps the antibiotic work better.

Probenecid should not be used in children younger than 2 years.

How should I take Probenecid?

To prevent gout, take this medication by mouth, usually twice daily with food or antacids to reduce stomach upset or as directed by your doctor. It is best to drink a full glass of water with each dose and at least another 8 glasses (8 ounces each) a day while taking this drug in order to prevent kidney stones. If you are on restricted fluid intake, consult your doctor for further instructions. Your doctor may also instruct you on how to decrease acidity in your urine (e.g., avoid large amounts of ascorbic acid/vitamin C) to prevent kidney stones. Your doctor may order other medications (e.g., sodium bicarbonate, citrate) to make your urine less acidic.

Dosage is based on your condition and response to therapy. Your doctor may direct you to take a low dose at first, then adjust your dose based on uric acid levels and your gout symptoms. After you have been symptom-free for several months and your uric acid levels are normal, your doctor may lower your probenecid dose to the lowest effective dose. Follow your doctor’s directions carefully.

Probenecid should not be started during a sudden/severe gout attack. Wait until your current attack is over before starting this medication. You may experience an increase in the number of gout attacks for several months after starting this medicine while the body removes extra uric acid. If you have a gout attack while taking probenecid, continue taking it along with your medications for gout pain.

Probenecid is not a pain reliever. To relieve pain from gout, continue to take your medicines prescribed for pain from gout attacks (e.g., colchicine, ibuprofen, indomethacin) as directed by your doctor.

If you are taking this medication to raise the level of antibiotics in your body, follow your doctor’s directions for when to take the antibiotic and when to take the probenecid.

Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day.

Inform your doctor if your condition persists or worsens.

How do I store Probenecid?

Probenecid is best stored at room temperature away from direct light and moisture. To prevent drug damage, you should not store Probenecid in the bathroom or the freezer. There may be different brands of Probenecid that may have different storage needs. It is important to always check the product package for instructions on storage, or ask your pharmacist. For safety, you should keep all medicines away from children and pets.

You should not flush Probenecid down the toilet or pour them into a drain unless instructed to do so. It is important to properly discard this product when it is expired or no longer needed. Consult your pharmacist for more details about how to safely discard your product.

Precautions & warnings

What should I know before using Probenecid?

Before taking probenecid, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: low blood counts (e.g., aplastic anemia, bone marrow depression), certain type of kidney stone (uric acid).

Before using this medication, tell your doctor or pharmacist your medical history, especially of: cancer treatment, a certain enzyme deficiency (G6PD), kidney problems (e.g., kidney stones, obstruction), peptic ulcer disease.

This drug may make you dizzy. Alcohol or marijuana can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana.

Before having surgery, tell your doctor or dentist that you are using this medication.

Kidney function declines as you grow older. This medication is removed by the kidneys. Therefore, elderly people may be at greater risk for side effects while using this drug, including stomach problems.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

It is not known whether this drug passes into breast milk. Consult your doctor before breast-feeding.

Is it safe during pregnancy or breast-feeding?

There are no adequate studies in women for determining risk when using this Probenecid during pregnancy or while breastfeeding. Please always consult with your doctor to weigh the potential benefits and risks before taking Probenecid. Probenecid is pregnancy risk category B according to the US Food and Drug Administration (FDA).

FDA pregnancy risk category reference below:

  • A=No risk,
  • B=No risk in some studies,
  • C=There may be some risk,
  • D=Positive evidence of risk,
  • X=Contraindicated,
  • N=Unknown

Side effects

What side effects can occur from Probenecid?

Nausea, loss of appetite, dizziness, vomiting, headache, sore gums, or frequent urination may occur as your body adjusts to the medicine. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if any of these unlikely but serious side effects occur: lower back pain, difficult/painful urination, change in amount/color of urine.

Tell your doctor right away if any of these rare but very serious side effects occur: easy bruising/bleeding, signs of infection (e.g., fever, sore throat), severe abdominal pain, pale stools, unusual tiredness, dark urine, yellowing eyes/skin.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

Not everyone experiences these side effects. There may be some side effects not listed above. If you have any concerns about a side-effect, please consult your doctor or pharmacist.

Interactions

What drugs may interact with Probenecid?

Some products that may interact with this drug include: cancer chemotherapy, ketorolac, dyphylline, methotrexate, pyrazinamide, salicylates (e.g., high-dose aspirin), zidovudine, certain drugs removed from your body by the kidneys (such as ceftazidime/avibactam, dapsone, heparin, fosfomycin).

Alcohol can decrease this drug’s effectiveness. Limit alcohol while taking this medication.

This medication may interfere with certain laboratory tests (including urine glucose tests), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.

Probenecid may interact with other drugs that you are currently taking, which can change how your drug works or increase your risk for serious side effects. To avoid any potential drug interactions, you should keep a list of all the drugs you are using (including prescription drugs, nonprescription drugs and herbal products) and share it with your doctor and pharmacist. For your safety, do not start, stop, or change the dosage of any drugs without your doctor’s approval.

Does food or alcohol interact with Probenecid?

Probenecid may interact with food or alcohol by altering the way the drug works or increase the risk for serious side effects. Please discuss with your doctor or pharmacist any potential food or alcohol interactions before using this drug.

What health conditions may interact with Probenecid?

Probenecid may interact with your health condition. This interaction may worsen your health condition or alter the way the drug works. It is important to always let your doctor and pharmacist know all the health conditions you currently have.

Dosage

The information provided is not a substitute for any medical advice. You should ALWAYS consult with your doctor or pharmacist before using this Probenecid.

What is the dose of Probenecid for an adult?

Usual Adult Dose for Gout

Therapy should not be started until an acute gout attack has subsided:

Initial: 250 mg orally twice a day for 1 week

Maintenance: 500 mg orally twice a day

-If symptoms of gouty arthritis are not controlled or 24-hour uric acid excretion is not above 700 mg, may increase dose in 500 mg increments every 4 weeks as tolerated; continue at dose that maintains normal serum urate levels

Maximum dose: 2 g per day

Comments:

-If an acute attack is precipitated during therapy, this drug should be continued at same dose while appropriate therapy is given to control acute attack.

-To prevent crystallization of uric acid in urine, a liberal fluid intake (2 L/day) and alkalization of the urine should be encouraged; alkalization of urine may be relaxed when serum urate levels return to normal limits and tophaceous deposits disappear.

-Maintenance dose may be decreased in increments of 500 mg every 6 months when acute attacks have been absent for 6 months or more and serum urate levels remain within normal limits; maintenance dosage should not be reduced to the point serum urate levels start to rise.

Use: For the treatment of hyperuricemia associated with gout and gouty arthritis.

Usual Adult Dose for Gouty Arthritis

Therapy should not be started until an acute gout attack has subsided:

Initial: 250 mg orally twice a day for 1 week

Maintenance: 500 mg orally twice a day

-If symptoms of gouty arthritis are not controlled or 24-hour uric acid excretion is not above 700 mg, may increase dose in 500 mg increments every 4 weeks as tolerated; continue at dose that maintains normal serum urate levels

Maximum dose: 2 g per day

Comments:

-If an acute attack is precipitated during therapy, this drug should be continued at same dose while appropriate therapy is given to control acute attack.

-To prevent crystallization of uric acid in urine, a liberal fluid intake (2 L/day) and alkalization of the urine should be encouraged; alkalization of urine may be relaxed when serum urate levels return to normal limits and tophaceous deposits disappear.

-Maintenance dose may be decreased in increments of 500 mg every 6 months when acute attacks have been absent for 6 months or more and serum urate levels remain within normal limits; maintenance dosage should not be reduced to the point serum urate levels start to rise.

Use: For the treatment of hyperuricemia associated with gout and gouty arthritis.

Usual Adult Dose for Adjunct to Antibiotic Therapy

500 mg orally 4 times a day

Comment: The Centers for Disease Control and Prevention (CDC) no longer recommend this drug with oral cephalosporins or ampicillin as a treatment for gonococcal infections.

Use: As an adjuvant to therapy with penicillin or with ampicillin, methicillin, oxacillin, cloxacillin, or nafcillin, for elevation and prolongation of plasma levels by whatever route the antibiotic is given.

Renal Dose Adjustments

Gout:

-Chronic renal insufficiency (CrCl less than 30 mL/min): Not recommended as it may not be effective

-Renal impairment: Use caution; dosage requirements may be increased in some patients with some renal impairment

Adjunct to penicillin:

-Not recommended in conjunction with penicillin in the presence of known renal impairment.

-If used in elderly patients with renal impairment, use caution, dose reduction may be warranted, specific guidelines are not provided

Dose Adjustments

Urine alkalization:

-A liberal fluid intake (2 L/day) and alkalization of the urine is recommended when excretion of uric acid is at a high level; alkalization may be relaxed when serum urate levels return to normal and tophaceous deposits disappear.

-Sodium bicarbonate 3 to 7.5 g/day or potassium citrate 7.5 g/day may be used to maintain an alkaline urine.

-Acid-base balance should be watched carefully when alkali is administered.

Adjunct to antibiotic:

Phenolsulfonphthalein (PSP) excretion test may be used to determine the effectiveness of probenecid in retarding penicillin excretion and maintaining therapeutic levels; the renal clearance of PSP is reduced to about one-fifth the normal rate when dosage of probenecid is adequate.

Other Comments

Administration advice:

Take orally

Gout:

-Maintain adequate hydration (at least 2 L/day) and alkalization of the urine with sodium bicarbonate or potassium citrate as needed.

Storage requirements:

-Protect from light

General:

-Gastric intolerance may be indicative of toxicity and can be corrected by decreasing dosage.

-This drug should not be started until an acute gouty attack has subsided; if an acute attack is precipitated during therapy, this drug should be continued at same dose while appropriate therapy is given to control acute attack.

-This drug inhibits the tubular secretion of penicillin and usually increases penicillin plasma levels 2 to 4 fold.

Monitoring:

Gout:

-Monitor serum urate levels as needed to determine adequacy of treatment

-Monitor acid-base balance in patients administered alkali.

Patient advice:

-Instruct patients on the need for adequate hydration, alkalization of the urine, and/or dietary restrictions appropriate to their care.

-Inform patients that salicylates may diminish the uricosuric effect of this drug; if a mild analgesic agent is needed, acetaminophen should be used.

What is the dose of Probenecid for a child?

Usual Pediatric Dose for Adjunct to Antibiotic Therapy

Age: 2 to 14 years and weight less than 50 kg:

Initial: 25 mg/kg (or 0.7 g/m2 ) orally once

Maintenance: 40 mg/kg (or 1.2 g/m2/) per day orally administered in 4 equally divided doses 4 times a day

Weight greater than 50 kg:

500 mg orally 4 times a day

Comment: The Centers for Disease Control and Prevention (CDC) no longer recommend this drug with oral cephalosporins or ampicillin as a treatment for gonococcal infections.

Use: As an adjuvant to therapy with penicillin or with ampicillin, methicillin, oxacillin, cloxacillin, or nafcillin, for elevation and prolongation of plasma levels by whatever route the antibiotic is give.

Precautions

Contraindicated in children less than 2 years of age

How is Probenecid available?

Probenecid is available in the following dosage forms and strengths:

  • Oral tablet.

What should I do in case of an emergency or overdose?

In case of an emergency or an overdose, call your local emergency services or go to your nearest emergency room.

What should I do if I miss a dose?

If you miss a dose of Probenecid, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and take your regular dose as scheduled. Do not take a double dose.

Hello Health Group does not provide medical advice, diagnosis or treatment.

Sources

Review Date: April 21, 2018 | Last Modified: April 21, 2018

Want to live your best life?
Get the Hello Doktor Daily newsletter for health tips, wellness updates and more.
You might also like