benzbromarone

Action and Spectrum

Actions and Spectrum: 

benzbromarone is a medication primarily used to treat gout, characterized by elevated levels of uric acid in the blood, which can leads to painful joint inflammation. benzbromarone affects the body’s uric acid metabolism, primarily through its actions on the kidneys and liver. 

• Uric Acid Reduction: benzbromarone is a uricosuric agent promoting uric acid excretion in the urine. It inhibits the reabsorption of the uric acid in the renal tubules, leading to increased uric acid elimination and lower blood levels of uric acid. This helps avert the formation of uric acid crystals in the joints, which might cause gout attacks. 
• Liver Enzyme Inhibition: benzbromarone can inhibit certain liver enzymes in uric acid production. Doing so reduces the overall production of uric acid in the body. 
• Anti-inflammatory Properties: While benzbromarone’s primary role is to lower uric acid levels, it may also have some anti-inflammatory properties that can help alleviate the pain and inflammation associated with gout attacks. 

Spectrum: benzbromarone is typically used in the following situations: 

• Gout Treatment: It is prescribed to individuals with gout who do not respond well or tolerate other urate-lowering medications such as allopurinol. 
• Chronic Gout Management: benzbromarone may be a long-term treatment to maintain lower uric acid levels and prevent recurrent gout attacks. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Uric acid renal calculi  

Renal colic 

It may cause liver damage 

An acute attack of gout 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Hypersensitivity or Allergy: Individuals with a previous hypersensitivity reaction or allergy to benzbromarone or its components should not use this medication. 
• Severe Liver Impairment: benzbromarone can potentially cause liver damage, and its use is generally contraindicated in individuals with severe liver impairment or liver disease. 
• Kidney Impairment: People with severe kidney impairment may need dose adjustments or may not be suitable candidates for benzbromarone therapy. It should be used with caution in patients with moderate kidney impairment. 
• History of Drug-Induced Liver Injury: Individuals with a history of drug-induced liver injury should avoid benzbromarone due to the risk of exacerbating liver problems. 
• Porphyria: benzbromarone is contraindicated in patients with porphyria, an infrequent genetic disorder affecting the nervous system and skin. 
• Pregnancy and Breastfeeding: The safety of benzbromarone during pregnancy and breastfeeding is not well-established, and its use is generally discouraged in pregnant or breastfeeding women unless the potential benefits outweighs the risks. Alternative medications may be considered. 
• Concurrent Use of Hepatotoxic Drugs: Combining benzbromarone with other drugs known to have the potential for causing liver toxicity should be avoided, as it may increase the risk of liver damage. 
• History of Blood Dyscrasias: Patients with a history of blood dyscrasias (abnormalities in blood cell counts) should use benzbromarone cautiously, as it may exacerbate these conditions. 
• Pediatric Use: benzbromarone is not typically used in children and adolescents due to limited safety and efficacy data in this age group. 
• Alcohol Abuse: Individuals with a history of alcohol abuse or dependence should be cautious when using benzbromarone, as alcohol consumption can potentially exacerbate liver-related side effects. 

Caution 

• Liver Function: benzbromarone has been associated with rare cases of liver toxicity, including severe liver injury. Therefore, individuals taking benzbromarone should have regular liver function tests (such as liver enzyme measurements) to monitor for any signs of liver problems. If there are significant changes in liver function, the medication may need to be discontinued. 
• Kidney Function: benzbromarone can increase the excretion of uric acid through the kidneys. Monitoring kidney function regularly when using benzbromarone is essential, especially in individuals with pre-existing kidney disease. Dose adjustments may be necessary. 
• Drug Interactions: benzbromarone can interact with other medications. It may increase the levels of certain drugs in the blood, potentially leading to adverse effects or toxicity. Therefore, healthcare providers should be aware of all medications and supplements a patient is taking to assess potential interactions. 
• Allergic Reactions: Although rare, allergic reactions to benzbromarone can occur. If an individual experiences symptoms such as rash, itching, swelling, severe dizziness, or difficulty breathing, they should seek immediate medical attention and discontinue the medication. 
• Porphyria: benzbromarone is contraindicated in individuals with porphyria, a rare group of genetic disorders that affect heme production in the body. 
• Pregnancy and Breastfeeding: The safety of benzbromarone during pregnancy and breastfeeding is not well-established, and it should be used with caution in these situations. Pregnant and breastfeeding women should discuss the potential risks and benefits with their healthcare provider. 
• Alcohol Use: Individuals should be cautious about alcohol consumption while taking benzbromarone, as excessive alcohol use can potentially exacerbate liver-related side effects. 
• Regular Monitoring: Regularly monitoring uric acid levels, liver function, and kidney function is crucial while using benzbromarone. This helps ensure that the medication is generally effective and safe for the individual. 
• Dosage Adjustments: Dose adjustments may be necessary for individuals with impaired kidney function or those taking other medications that interact with benzbromarone. A healthcare provider should determine the appropriate dosage based on the individual’s circumstances. 
• Patient Education: Patients should be educated about the potential risks and benefits of benzbromarone and encouraged to report any unusual or concerning symptoms to their healthcare provider promptly. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not assigned. 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• 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

Pharmacology: 

benzbromarone is a uricosuric agent used in gout treatment, acting primarily on uric acid metabolism’s renal and hepatic pathways. It generally inhibits the reabsorption of uric acid in the renal tubules, leading to increased uric acid excretion and a decrease in blood uric acid levels. Additionally, benzbromarone can inhibit liver enzymes in uric acid production, reducing uric acid synthesis.

These combined actions effectively lower uric acid levels, helping to avert the formation of uric acid crystals in the joints and the recurrence of painful gout attacks. However, it is essential to exercise caution with benzbromarone due to potential liver toxicity, and regular monitoring of liver function is often required during its use. 

Pharmacodynamics: 

Mechanism of action: benzbromarone affects the body’s metabolism and excretion of uric acid. benzbromarone is primarily used to treat gout, which can leads to painful joint inflammation and the formation of the uric acid crystals in joints.  

• Inhibition of Uric Acid Reabsorption: benzbromarone primarily acts on the kidneys. It generally inhibits the reabsorption of uric acid in the renal tubules, specifically in the proximal convoluted tubules of the nephrons. In a healthy kidney, uric acid is filtered from the blood into the urine, but some can be reabsorbed back into the bloodstream. benzbromarone reduces this reabsorption, increasing uric acid excretion in the urine. 
• Increased Uric Acid Excretion: By inhibiting uric acid reabsorption, benzbromarone effectively increases the elimination of uric acid from the body through urine. This helps lower the concentration of uric acid in the bloodstream, reducing the risk of uric acid crystal formation in the joints and the subsequent gout attacks. 
• Inhibition of Liver Enzymes: Additionally, benzbromarone can inhibit certain liver enzymes involved in uric acid production. This further contributes to reducing the overall production of uric acid in the body. 

Pharmacokinetics: 

Absorption 

benzbromarone is administered orally, typically in tablet form. After ingestion, it is absorbed in the gastrointestinal tract, primarily in the small intestine. The rate and extent of absorption may vary among individuals and may be affected by factors such as food intake. 

Distribution 

Once absorbed into the bloodstream, benzbromarone is distributed throughout the body. It binds to plasma proteins, primarily to albumin. The distribution of benzbromarone to various tissues and organs allows it to exert its effects on uric acid metabolism, primarily in the liver and kidneys. 

Metabolism 

benzbromarone undergoes extensive hepatic (liver) metabolism. Various cytochrome P450 enzymes, including CYP2C9, metabolize it. These metabolic pathways leads to the formation of several metabolites, some of which are pharmacologically active. The metabolism of benzbromarone can vary among individuals and can be influenced by genetic factors. 

Elimination and Excretion 

benzbromarone and its metabolites are eliminated primarily through renal (kidney) excretion. They are excreted in urine, with some metabolites appearing alongside the unchanged drug. The excretion rate can be influenced by factors such as renal function, urinary pH, and other characteristics. 

Adminstartion

Administration: 

The administration of benzbromarone, like any medication, should follow the prescribed dosage and also instructions provided by the healthcare provider. benzbromarone is typically available in tablet form, and here are some general guidelines for its administration: 

• Dosage: The specific dosage of benzbromarone can vary based on the  condition and your healthcare provider’s recommendations. Typically, it is taken once daily, often in the morning. 
• Timing: benzbromarone is usually taken with or immediately after a meal to enhance absorption and minimize the risk of stomach upset.  
• Swallow Whole: Take the benzbromarone tablet whole with a full glass of water. Do not crush, break/chew the tablet unless your healthcare provider instructs. 
• Follow Recommendations: Always follow your healthcare provider’s recommendations regarding the dosage and duration of treatment. Do not change the dosage or stop taking the medication without consulting your healthcare provider. 
• Monitoring: Regular monitoring of your uric acid levels, liver function, and kidney function might be necessary while you are on benzbromarone. Your healthcare provider will schedule these tests and determine the appropriate frequency based on your needs. 
• Compliance: Taking benzbromarone as prescribed is essential, even if you start feeling better. Gout is a chronic condition that requires ongoing management, and discontinuing the medication prematurely may lead to gout attacks. 
• Interaction with Other Medications: Inform your healthcare provider about all other medications, supplements, or herbal products you are taking. benzbromarone can interact with other drugs, so your healthcare provider can assess potential interactions and adjust your treatment plan if necessary. 
• Lifestyle Modifications: In addition to medication, your healthcare provider may recommend lifestyle changes to help manage gout. This may include dietary modifications (such as reducing purine-rich foods and alcohol intake), staying hydrated, and maintaining a healthy weight. 
• Adverse Effects: Be aware of any potential side effects of benzbromarone, and promptly report any unusual or concerning symptoms to your healthcare provider. 
• Regular Follow-Up: Maintain regular follow-up appointments with your healthcare provider to assess your progress, discuss any concerns, and adjust your treatment plan as needed. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: benzbromarone 

Why do we use benzbromarone? 

benzbromarone is a medication primarily used to treat gout, a condition characterized by elevated levels of uric acid in the blood, which might generally lead to painful joint inflammation and the formation of uric acid crystals in the joints.  

• Gout Treatment: benzbromarone is used to lower uric acid levels in the body, which helps avert gout attacks and alleviate the symptoms of acute gout flares. It is often prescribed to individuals with gout who do not respond well to or cannot tolerate other urate-lowering medications, such as allopurinol. 
• Chronic Gout Management: In addition to treating acute gout attacks, benzbromarone may be used as a long-term or maintenance therapy to keep uric acid levels within the normal range and prevent recurrent gout episodes. It benefits patients with severe gout or those who do not achieve adequate uric acid control with other medications.