(British Approved Name, US Adopted Name, rINN)
What Is Benzbromarone?
Benzbromarone is a medication used to treat gout, a type of arthritis that occurs when uric acid crystals accumulate in the joints. It belongs to a class of drugs known as uricosurics, which work by increasing the excretion of uric acid from the body, thereby reducing uric acid levels in the blood and preventing the formation of urate crystals in the joints.
Benzbromarone works by inhibiting the reabsorption of uric acid in the kidneys, promoting its excretion in the urine. This helps lower the levels of uric acid in the blood.
It primarily treats hyperuricemia (elevated uric acid levels) associated with gout.
By increasing the excretion of uric acid, benzbromarone helps prevent the formation of urate crystals in the joints, reducing the frequency and severity of gout attacks.
The onset of action of benzbromarone is typically within a few days to weeks.
Benzbromarone may be associated with liver-related side effects and liver function should be monitored regularly during treatment.
Common side effects may include gastrointestinal symptoms, skin rash, and liver enzyme abnormalities. Serious but rare side effects may include severe liver injury, and immediate medical attention is needed if symptoms such as jaundice or persistent nausea occur.
Benzbromarone is contraindicated in individuals with severe liver impairment, kidney impairment, and certain conditions affecting the bile ducts.
As with any medication, benzbromarone should be used under the supervision of a healthcare professional. Following the prescribed dosage and undergoing regular monitoring is essential to assess its efficacy and detect potential side effects.
Pharmacokinetics
Benzbromarone is only partially absorbed from the gastrointestinal tract, reaching peak plasma concentrations about 2 to 4 hours after oral administration. Benzbromarone is extensively bound to plasma proteins. It is metabolized in the liver and is excreted mainly in the feces; a small amount appears in the urine.
Uses and Administration
Benzbromarone is a uricosuric drug that reduces plasma concentrations of uric acid by blocking renal tubular reabsorption. It has been suggested that benzbromarone may also increase the intestinal elimination of uric acid. It has been used to treat hyperuricemia, including that associated with chronic gout, although it has been withdrawn in many countries due to reports of hepatotoxicity.
Benzbromarone is not used to treat acute gout attacks and may exacerbate and prolong them if given during an attack; treatment should not start until an acute attack has subsided.
The usual oral dose has been 50 to 200 mg daily. An NSAID or colchicine should be given initially to reduce the risk of precipitating acute gout. An adequate fluid intake should be maintained. Lower doses of benzbromarone (20 mg) have also been used as a combination product with allopurinol.
Adverse Effects
Benzbromarone may cause gastrointestinal adverse effects, especially diarrhea. It may precipitate an acute gout attack and cause uric acid, renal calculi, and renal colic. Hepatotoxicity has occurred, and monitoring of liver function has been recommended.
Effects on the Liver
Benzbromarone-induced liver damage has been reported.
Precautions
Benzbromarone should be avoided in patients with moderate or severe renal impairment, those with uric acid renal calculi, and those with urinary uric acid excretion rates greater than 700 mg per 24 hours. Like other uricosurics, treatment with benzbromarone should not be started during an acute gout attack. Similarly, an adequate fluid intake should be maintained to reduce the risk of uric acid renal calculi; additionally, alkalinization of the urine may be considered.
Porphyria
Benzbromarone is considered to be unsafe in patients with porphyria because it is porphyrin-ogenic in in-vitro systems.
Interactions
Benzbromarone, like many medications, can interact with other drugs, potentially affecting their effectiveness or increasing the risk of side effects. It’s important to inform your healthcare provider about all the medications, supplements, and herbal products you are taking to avoid potential interactions. Some factors to consider include:
- Warfarin (Anticoagulant): Benzbromarone may enhance the anticoagulant effects of warfarin, potentially increasing the risk of bleeding. Regular monitoring of the International Normalized Ratio (INR) is recommended in individuals taking both medications.
- Ciclosporin: Benzbromarone may increase the levels of ciclosporin, a medication used to suppress the immune system. Dose adjustments may be needed.
- Tacrolimus: Benzbromarone may increase the levels of tacrolimus, another immunosuppressive medication. Dose adjustments may be necessary.
- Contraceptives: Benzbromarone may decrease the effectiveness of hormonal contraceptives. Additional or alternative contraceptive methods may be needed.
- Antacids: The absorption of benzbromarone may be reduced when taken concomitantly with antacids. It is advisable to separate the administration of benzbromarone and antacids.
- Probenecid: Probenecid, another uricosuric medication, may enhance the uricosuric effects of benzbromarone.
- Other Medications: Inform your healthcare provider about all medications you are taking, including over-the-counter medications and herbal supplements, as interactions can occur.
It’s crucial to follow your healthcare provider’s instructions regarding the use of benzbromarone and to communicate any concerns or changes in your medication regimen. Your healthcare provider can provide guidance on potential interactions and adjust your treatment plan accordingly to ensure its safety and efficacy.
Drug Nomenclature
International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):
Synonyms: Bensbromaron; Bentsbromaroni; Benzbromaron; Benzbromarona; Benzbromaronas; Benzbromaronum; L-2214; MJ-10061
BAN: Benzbromarone
USAN: Benzbromarone
INN: Benzbromarone [rINN (en)]
INN: Benzbromarona [rINN (es)]
INN: Benzbromarone [rINN (fr)]
INN: Benzbromaronum [rINN (la)]
INN: Бензбромарон [rINN (ru)]
Chemical name: 3,5-Dibromo-4-hydroxyphenyl 2-ethyl benzofuran-3-yl ketone
Molecular formula: C17H12Br2O3 =424.1
CAS: 3562-84-3
ATC code: M04AB03
Pharmacopoeias. In Europe and Japan.
European Pharmacopoeia, 6th ed., 2008 and Supplements 6.1 and 6.2 (Benzbromarone). A white or almost white crystalline powder. Practically insoluble in water, sparingly soluble in alcohol, and freely soluble in acetone and dichloromethane. Protect from light.
Preparations
Single-ingredient Preparations
The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.
Argentina: Max Uric¤;
Austria: Uricovac;
Belgium: Desuric¤;
Brazil: Narcaricina;
France: Desuric¤;
Germany: Azubromaron¤; Harolan¤; Narcaricin¤; Uricovac¤;
Hong Kong: Narcaricin¤;
Hungary: Harpagin;
Japan: Urinorm;
Malaysia: Harpagin¤;
Mexico: Desuric¤;
Netherlands: Desuric;
South Africa: Minuric¤;
Singapore: Narcaricin¤;
Spain: Urinorm;
Switzerland: Desuric¤; Obaron¤;
Thailand: Narcaricin;
Multi-ingredient Preparations
Austria: Allobenz; Duovitan¤; Gichtex plus; Uroplus¤;
Belgium: Comburic;
France: Anurate¤; Desatura¤;
Germany: Acifugan¤; Allo.comp.; Allomaron¤; Harpagin; Uricovac comp¤;
Italy: Urifugan¤;
Portugal: Acifugan¤;
South Africa: Allomaron;
Spain: Acifugan¤; Facilit¤;
Switzerland: Acifugan¤;
Thailand: Allomaron
Jennifer is a clinical pharmacologist. She helps doctors of all medical specialties choose medications. Jennifer consults about drug dosage, interactions, and side effects.