Probenecid

Yes

Probenecid blocks excretion of some drugs by the kidney and, therefore, may increase blood levels and side effects of methotrexate (Rheumatrex, Trexall) and nonsteroidal antiinflammatory drugs (NSAIDs), for example, ibuprofen (Advil), naproxen (Aleve), indomethacin (Indocin), ketorolac (Toradol) and others. Aspirin may reduce the action of probenecid through unknown mechanisms.

Probenecid has not been adequately studied in pregnant women.

Probenecid has not been adequately studied in nursing mothers.

Tablets: 0.5 g

Probenecid should be stored at room temperature, 15 C - 30 C (59 F - 86 F).

Mechanism of Action

(Uricosuric) inhibits tubular reabsorption of urate; increasing uric acid excretion

Also inhibits tubular secretion of weak organic acids like PCNs & cephalosporins

Pharmacokinetics

Half-Life: 3-17 hr

Onset: 2 hr (effect on penicillin levels)

Peak Plasma Time: 2-4 hr

Bioavailability: >90%

Protein Bound: 85-95% (albumin)

Metabolism: Liver

Metabolites: hydroxylated metabolites, N-despropyl metabolite, probenecid acylglucuronide

Excretion: Urine

Serious side effects have been reported with probenecid. See the "Probenecid Precautions" section.

Common side effects of probenecid include the following:

• headache
• dizziness
• worsening of a gouty arthritis attack
• vomiting
• nausea
• loss of appetite
• sore gums
• increased urination
• fever
• itching
• hair loss
• skin rash

This is not a complete list of probenecid side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effect that bothers you or that does not go away.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Uricosuric and renal tubular transport blocking agent.b

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For probenecid, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to probenecid or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Probenecid has been tested in children 2 to 14 years of age for use together with antibiotics. It has not been shown to cause different side effects or problems than it does in adults. Studies on the effects of probenecid in patients with gout have been done only in adults. Gout is very rare in children.

Geriatric

Many medicines have not been studied specifically in older people. Therefore, it may not be known whether they work exactly the same way they do in younger adults. There is no specific information comparing use of probenecid in the elderly with use in other age groups.

Pregnancy

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking probenecid, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using probenecid with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

• Ketorolac

Using probenecid with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Avibactam
• Baricitinib
• Cephalexin
• Citalopram
• Deferiprone
• Doripenem
• Indomethacin
• Methotrexate
• Naproxen
• Pegloticase
• Zalcitabine

Using probenecid with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Amoxicillin
• Aspirin
• Bismuth Subsalicylate
• Cefditoren Pivoxil
• Cefotaxime
• Cefpodoxime Proxetil
• Cefprozil
• Choline Magnesium Trisalicylate
• Ciprofloxacin
• Enprofylline
• Ertapenem
• Gatifloxacin
• Lorazepam
• Magnesium Salicylate
• Meropenem
• Norfloxacin
• Phenprocoumon
• Piretanide
• Pralatrexate
• Sodium Salicylate
• Sodium Thiosalicylate
• Zidovudine
• Zomepirac

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of probenecid. Make sure you tell your doctor if you have any other medical problems, especially:

• Blood disease or
• Cancer being treated by antineoplastics (cancer medicine) or radiation (x-rays) or
• Kidney disease or stones (or history of) or
• Stomach ulcer (history of)—The chance of side effects may be increased

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Dizziness.
• Headache.
• Not hungry.
• Upset stomach or throwing up.
• Swollen or sore gums.
• Hair loss.
• Flushing.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.

NDC 10135-541-10
Probenecid
TABLETS, USP 
500 mg
1000 TABLETS
Rx Only 

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Generic: 500 mg