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probenecid

 
Dictionary: pro·ben·e·cid   (prō-bĕn'ĭ-sĭd) pronunciation
n.
A uricosuric drug, C13H19NO4S, derived from benzoic acid and used chiefly in the treatment of gout.

[PRO(PYL) + BEN(ZOIC) (A)CID.]


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Food and Fitness: probenecid
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A drug sometimes misused by athletes to alter the integrity of a urine sample and escape detection by dope tests. Probenecid affects the transport of chemicals across tissue barriers, such as that between the blood and the kidneys. In medicine, this effect is taken advantage of to treat gout by reducing the amount of uric acid in the blood. However, the same effect is misused by athletes to reduce the amount of drugs, such as anabolic steroids, released into the urine, making them much more difficult to detect by conventional dope tests. Because of misuse, probenecid is listed among the banned drugs of the International Olympic Committee. Fortunately, its presence is easily detected in a urine sample.

Dental Dictionary: probenecid
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n

trade names: Benemid, Probalan; drug class: uricosuric; action: inhibits tubular reabsorption of urates, with increased excretion of uric acids; uses: hyperuricemia in gout, gouty arthritis, adjunct to cephalosporin or penicillin treatment by reducing excretion and maintaining high blood levels of medication.

Drug Info: Probenecid
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Chemical formula:



Probenecid tablets

What are probenecid tablets?

PROBENECID (Benemid®, Probalan®) helps to remove excess uric acid from the body. Uric acid can cause gout or gouty arthritis. Probenecid is not a cure for gout, but can help to prevent recurring gouty attacks. It is not for use in treating an attack of gout, and can make an attack worse. Certain illnesses or medications can cause an increase in uric acid. Probenecid can help to reduce the risk of complications (such as kidney stones) that may arise as a result of an increase in uric acid levels (hyperuricemia). Probenecid can also help to prolong the action of certain antibiotics and make them more effective. Generic probenecid tablets are available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• blood disorders or disease
• kidney disease, or kidney stones
• recent radiation therapy
• stomach ulcers
• an unusual or allergic reaction to probenecid, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I take this medicine?

Take probenecid tablets by mouth. Follow the directions on the prescription label. Swallow the tablets with a drink of water. Take your doses at regular intervals. Do not take your medicine more often than directed.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What if I miss a dose?

If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.

What drug(s) may interact with probenecid?

• alcohol
allopurinol
• antiinflammatory drugs (NSAIDs, such as ibuprofen)
• antibiotics including penicillins
• antiviral medicines such as acyclovir, famciclovir, ganciclovir
• aspirin and aspirin-like medicines
clofibrate
diazoxide
entacapone
ethambutol
heparin
lorazepam
• mecamylamine
methotrexate
nitrofurantoin
pyrazinamide, PZA
• water pills

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking probenecid?

It may take several months before you see the full effect of probenecid. Do not stop taking except on your prescriber or health care professional;s advice. Probenecid is only effective if you keep taking it regularly even if you have an attack of gout. Your prescriber or health care professional will prescribe other tablets to treat an acute attack.

Aspirin and non-steroidal antiinflammatory drugs like ibuprofen can make probenecid less effective. Do not treat yourself for headaches or pain; ask your prescriber or health care professional for advice.

Alcohol can increase the amount of uric acid in your body and aggravate gout. Alcohol can also make probenecid less effective. Avoid alcoholic drinks.

Drink 10 or more full glasses of water a day while taking probenecid. This will help to prevent formation of kidney stones and other possible kidney problems by removing excess uric acid. Probenecid works best when the urine is alkaline (non-acidic). Ask your prescriber or health care professional about which foods or juices to avoid, and about other foods, beverages or antacids that may help to make the urine alkaline.

Probenecid can interfere with the results of copper sulfate urine tests (Clinitest®), but not with glucose enzymatic urine sugar tests (Clinistix®). Diabetic patients may get false results.

What side effects may I notice from taking probenecid?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• blood in urine
• difficulty breathing, wheezing or shortness of breath
• fever, chills or sore throat
• lower back or side pain
• mouth sores
• pain or difficulty passing urine
• skin rash and itching (hives)
• swelling of the feet, ankles, face or lips
• unusual weakness or tiredness
• unusual bleeding or bruising

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• dizziness
• flushing
• frequent passing of urine
• hair loss
• headache
• loss of appetite
• nausea, vomiting
• painful or swollen joints

Where can I keep my medicine?

Keep out of the reach of children in a container that small children cannot open.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Keep container tightly closed. Throw away any unused medicine after the expiration date.


Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

A drug used to treat gout by reducing levels of uric acid in the blood. Probenecid inhibits the transport of organic acids and antibodies across some tissue barriers, such as the barrier between the blood and the kidney tubule. It has two very important effects on other drugs: first, it can increase the concentration of another drug or antibody within the blood; secondly, it can reduce the amount of drug (e.g. anabolic steroid) released into the urine, making a banned drug much more difficult to detect. Because probenecid may be used to alter the integrity of a urine sample and avoid detection in dope tests, it is categorized as a masking agent by the World Anti-Doping Agency. Probenecid is relatively easy to detect in a urine sample.

Veterinary Dictionary: probenecid
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Used in the treatment of gout to promote excretion of uric acid; also used with certain antibiotics such as penicillin G and ampicillin to delay excretion and prolong their action.

Wikipedia: Probenecid
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Probenecid
Systematic (IUPAC) name
4-(dipropylsulfamoyl)benzoic acid
Identifiers
CAS number 57-66-9
ATC code M04AB01
PubChem 4911
DrugBank APRD00167
Chemical data
Formula C13H19NO4S 
Mol. mass 285.36 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding 75-95%
Metabolism  ?
Half life 2-6 hours (dose: 0.5-1 g)

4-12 hours (dose: >2 g)

Excretion renal (77-88%)
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes oral

Probenecid (Benuryl) is a uricosuric drug that increases uric acid excretion in the urine. It is primarily used in treating gout and hyperuricemia.

Probenecid competitively inhibits the renal excretion of some drugs, thereby increasing their plasma concentration and prolonging their effects.

It was developed as an alternative to caronamide.[1]

Contents

Uses

In one study, probenecid was shown to more than double blood concentrations of oseltamivir (trade name Tamiflu), an antiviral drug used to combat influenza.[2] This is significant because nations are currently stockpiling oseltamivir in anticipation of an influenza pandemic, and there could be supply shortages.[citation needed] During World War II, probenecid was used to extend limited supplies of penicillin,[3] and is still currently used to increase antibiotic concentrations in serious infections.

It has also found use as a masking agent.[4]

Mechanism

In the kidneys probenecid is filtered at the glomerulus, secreted in the proximal tubule and reabsorbed in the distal tubule.

Probenecid's exact mechanism is explained as follows. The kidney's organic anion transporter (OAT) reclaims uric acid from the urine and returns it to the plasma. Probenecid interferes with these systems.[5] If probenecid (an organic acid) is administered to a patient, the OAT binds to probenecid instead of to uric acid, preventing the reabsorption of uric acid. As a result, more uric acid leaves the body in the urine, lowering the uric acid concentration in the plasma. This is an example of the way in which competition between substrates transported across cell membranes has been put to use in medicine.

See also

References


 
 
Learn More
Probenecid tablets
Tabletas de probenecid
Antidiabetic Drugs: Interactions

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Dictionary. The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2009. Published by Houghton Mifflin Company. All rights reserved.  Read more
Food and Fitness. Food and Fitness: A Dictionary of Diet and Exercise. Copyright © 1997, 2003 by Oxford University Press. All rights reserved.  Read more
Dental Dictionary. Mosby's Dental Dictionary. Copyright © 2004 by Elsevier, Inc. All rights reserved.  Read more
Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
Sports Science and Medicine. The Oxford Dictionary of Sports Science & Medicine. Copyright © Michael Kent 1998, 2006, 2007. All rights reserved.  Read more
Veterinary Dictionary. Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.  Read more
Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Probenecid" Read more