- March 15, 2022
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Brand Name :
Benemid
Synonyms :
probenecid
Class :
Uricosuric Agents
Dosage forms and strengths
tablet
500mg
Administer 250 mg orally two times daily one week
The recommended dosage increment involves raising the oral intake to 500 mg twice daily, with a maximum daily dose of 2 grams each day
The dosage should be increased by 500 mg every four weeks
In the absence of gout attacks for 4 months and with uric acid levels in the normal range, a reduction of 500 mg every six months may be considered
Administer 1 gram orally along with a single dose of 2 grams of cefoxitin via intramuscular injection
Administer 1 gram orally along with a single 2-gram dose of cefoxitin intramuscularly
Dosage forms and strengths
tablet
500mg
For individuals weighing over 45 kg, an oral dose of 1 gram and a single intramuscular dose of 2 grams of cefoxitin should be administered
Refer adult dosing
may enhance the concentration of serum when combined with acetaminophen
Decrease renal clearance.
may increase the serum concentration
may enhance the serum concentration of acetaminophen
may enhance the serum concentration when combined
may enhance the serum concentration of OAT1/3 substrates
choline magnesium trisalicylate
The therapeutic efficacy of probenecid could be reduced by salicylates
probenecid: they may enhance the serum concentration of ketorolac
probenecid: they may increase the anticoagulant effect of Antiplatelet agents
probenecid: they may increase the anticoagulant effect of Antiplatelet agents
probenecid: they may increase the anticoagulant effect of Antiplatelet agents
probenecid: they may increase the anticoagulant effect of Antiplatelet agents
probenecid: they may increase the anticoagulant effect of Antiplatelet agents
nafcillin or probenecid, both increase the levels of other action by decreasing renal clearance.
Decrease renal clearance.
avoid interaction, as it may increase hepatotoxicity and serum concentration of methotrexate
avoid interaction, as it may increase hepatotoxicity and serum concentration of trimetrexate
may enhance the serum concentration of OAT1/3 substrates
may enhance the serum concentration of cephalosporins
baricitinib's effect can be enhanced by the concurrent administration of probenecid, as it reduces the elimination process
probenecid enhances the concentrations of meropenem/vaborbactam by reducing its elimination from the body
probenecid's uricosuric effect is lessened by aspirin
probenecid may increase the serum concentration of penicillins
probenecid may increase the serum concentration of penicillins
probenecid may increase the serum concentration of penicillins
probenecid may increase the serum concentration of penicillins
probenecid may increase the serum concentration of penicillins
it increases the concentration of cephalosporins in the serum
it increases the concentration of cephalosporins in the serum
it increases the concentration of cephalosporins in the serum
it increases the concentration of cephalosporins in the serum
it increases the concentration of cephalosporins in the serum
may enhance the serum concentration when combined with ganciclovir-valganciclovir
may diminish the excretion when combined with quinolones
may diminish the excretion when combined with quinolones
it may enhance the metabolism when combined with aripiprazole lauroxil
It may diminish the excretion when combined with dexamethasone
It may enhance the serum concentration when combined with pegloticase
The therapeutic effectiveness of nitrofurantoin may be reduced by probenecid
may enhance serum concentrations when combined with agents of urea cycle disorder
It may enhance the levels when combined with sodium phenylbutyrate by diminishing renal clearance
The effectiveness of loop diuretics could be reduced by the presence of probenecid
The effectiveness of loop diuretics could be reduced by the presence of probenecid
The effectiveness of loop diuretics could be reduced by the presence of probenecid
probenecid could potentially lead to an elevation in the concentration serum of sulfonylureas
probenecid could potentially lead to an elevation in the concentration serum of sulfonylureas
probenecid could potentially lead to an elevation in the concentration serum of sulfonylureas
probenecid could potentially lead to an elevation in the concentration serum of sulfonylureas
probenecid could potentially lead to an elevation in the concentration serum of sulfonylureas
probenecid will increase the effect of piperacillin by acidic drug competition.
when both drugs are combined, there may be an increased effect of cabozantinib
when both drugs are combined, there may be a decreased effect of probenecid by acidic drug competition for renal tubular clearance
when both drugs are combined, there may be an increased effect of cefotaxime by acidic (anionic) drug competition for renal tubular clearance
the interaction may increase the therapeutic effects of cefprozil
the interaction may increase the therapeutic effects of cefaclor
when both drugs are combined, there may be an increased risk of adverse effects
the interaction may increase the therapeutic effects of cefepime
the interaction may increase the therapeutic effects of cefuroxime
it decreases renal excretion of quinolones
Interaction with pivmecillinam may enhance the serum concentration of methotrexate
may enhance the effect of the other by cationic drug competition for renal tubular clearance.
may decrease the therapeutic effect of antibiotics
imipenem/cilastatin/relebactam
may decrease the therapeutic effect of antibiotics
may increase the serum concentration of cephalosporins
may enhance the serum concentration of meropenem
By competing with acidic (anionic) drugs for renal clearance, aceclofenac will raise the amount of probenecid
By competing with acidic (anionic) drugs for renal clearance, acemetacin will raise the amount of probenecid
By competing with acidic (anionic) drugs for renal clearance, acyclovir will raise the amount of probenecid
By competing with acidic (anionic) drugs for renal clearance, cefpirome will raise the amount of probenecid
amoxicillin and clavulanate potassium
probenecid has the potential to elevate the concentration serum of Beta-lactamase Inhibitors
probenecid has the potential to elevate the concentration serum of Beta-lactamase Inhibitors
probenecid has the potential to elevate the concentration serum of Beta-lactamase Inhibitors
Probenecid may enhance serum concentrations of ampicillin.
When bacampicillin and probenecid combine the plasma concentrations of bacampicillin increase by inhibition of renal tubular secretion.
The increase plasma levels, and half-life of penicillin increases by inhibiting renal tubular secretion.
it increases the concentration of lorazepam in serum
probenecid may enhance the effects of lisinopril through an unidentified interaction mechanism
Actions and Spectrum:
Action:
Uricosuric Action: The Drug exerts its primary action as a uricosuric agent. It Inhibits uric acid’s reabsorption in the kidneys’ proximal renal tubules. By blocking the reabsorption, probenecid increases the excretion of uric acid in the urine, thereby lowering its concentration in the blood. This action is beneficial in treating conditions associated with high levels of uric acid, such as gout and hyperuricemia.
Renal Action: Drug affects the renal system by altering the normal renal tubular transport processes. It inhibits the active reabsorption of organic acids, such as penicillin and cephalosporins, in the renal tubules. This action prolongs the presence of these drugs in the urine, leading to increased urinary concentrations. As a result, probenecid is often used as an adjunct therapy with certain antibiotics to enhance their effectiveness and extend their duration of action.
Spectrum:
Gout: The Drug is commonly used to manage gout, By increasing uric acid’s urinary excretion, the drug helps reduce uric acid levels in the body, thereby preventing the formation of new uric acid crystals and promoting the dissolution of existing crystals.
Hyperuricemia: The drug is used to treat hyperuricemia, particularly when it is associated with conditions such as gout, kidney stones, and certain types of kidney disorders. By enhancing uric acid excretion, probenecid helps to normalize blood uric acid levels and prevent the complications associated with hyperuricemia.
Frequency defined
1-10%
Hepatic necrosis (rare)
Gouty arthritis
Exacerbation of gout
Nephrotic syndrome (rare)
Renal calculi
Leukopenia
Hemolytic anemia
Aplastic anemia
Fever
Dizziness
Flushing
Rash
GI upset
Loss of appetite
Vomiting
Nausea
Headache
None
Contraindication/Caution:
Allergy or hypersensitivity: Drugs should not be used in individuals with a known allergy or hypersensitivity to probenecid or any of its components.
Acute gout attack: Drug is not effective in treating acute gout attacks. It is a preventive medication and should not be initiated during an acute attack.
Uric acid kidney stones: Drug is contraindicated in individuals with a history of uric acid kidney stones. It may increase the risk of stone formation.
Kidney disease: Drug is primarily excreted through the kidneys. Therefore, it is not recommended for individuals with severe kidney impairment or a history of kidney disease.
Blood disorders: Drugs may affect blood cell production and cause certain blood disorders. It should be used with caution or avoided in individuals with a history of blood disorders such as anemia or bone marrow suppression.
Peptic ulcer disease: Drug may increase the risk of peptic ulcer disease or worsen existing ulcers. It should be used with caution in individuals with a history of peptic ulcer disease.
Pregnancy warnings:
Pregnancy category: AU TGA pregnancy category: B2
US FDA pregnancy category: B
Lactation: Excreted into human milk is known
Pregnancy Categories:
Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.
Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology:
probenecid is a medication that belongs to a class of drugs known as uricosuric agents. It is primarily used in the treatment of gout, a type of arthritis caused by the accumulation of uric acid crystals in the joints.
Pharmacodynamics:
probenecid acts on the kidneys to inhibit the reabsorption of uric acid, thereby increasing its excretion in the urine. It achieves this by blocking the activity of specific transporters in the renal tubules, such as the organic anion transporter 1 (OAT1) and organic anion transporter 3 (OAT3). These transporters are responsible for reabsorbing uric acid from the urine back into the bloodstream. By inhibiting their activity, probenecid prevents the reabsorption of uric acid, leading to its increased elimination from the body.
Pharmacokinetics:
Absorption
Drug is well absorbed orally after administration. The absorption mainly occurs in the stomach and the small intestine. Food does not significantly affect its absorption.
Distribution
Drug is extensively distributed throughout the body. It binds extensively to plasma proteins, primarily albumin. The drug crosses the placental barrier and is also present in breast milk.
Metabolism
Drug undergoes minimal metabolism in the liver. The major metabolic pathway involves conjugation with glucuronic acid, resulting in the formation of glucuronide metabolites. These metabolites are mainly excreted in the urine.
Excretion and Elimination
Drug and its metabolites are primarily eliminated via the kidneys. The drug undergoes both glomerular filtration and tubular secretion. It inhibits the reabsorption of uric acid and other drugs in the renal tubules, leading to increased excretion of these substances. probenecid has a prolonged half-life, ranging from 5 to 12 hours in healthy individuals.
Administration:
The dosage of probenecid can vary depending on the individual and the condition being treated. It is typically taken orally in tablet form. The duration of probenecid treatment varies depending on the condition being treated.
Patient information leaflet
Generic Name: probenecid
Why do we use probenecid?
Gout: The drug is commonly prescribed for the treatment of gout,It helps lower uric acid levels in the blood, preventing the formation of new crystals and reducing the frequency and severity of gout attacks.
Hyperuricemia: The drug may be used to manage hyperuricemia which can lead to gout or kidney stones.
Kidney Stones: The drug is sometimes used with other medications to prevent the formation of certain kidney stones, such as uric acid stones. By increasing the excretion of uric acid, drug reduces the likelihood of stone formation.
Antibiotic Therapy: Drug has another important use in medicine. It can be used as an adjunctive therapy in combination with certain antibiotics, such as penicillin or cephalosporins. drug helps increase the concentration of antibiotics in the blood and tissues, enhancing their effectiveness against bacterial infections.
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