Approval Date: December 21, 2006
Revision Date: May 13, 2010
October 01, 2010
October 01, 2012
June 30, 2015
December 01, 2015
March 13, 2017
2019**Month**
Benzbromarone Tablets Instructions
Please read the instructions carefully and use under the guidance of a physician
[Drug Name].
Generic name: Benzbromarone Tablets
English name: Benzbromarone Tablets
Hanyu Pinyin: Benxiumalong Pian
Ingredients
The main ingredient of this product is benzbromarone.
Chemical name: (3,5-dibromo-4-hydroxyphenyl)-(2-ethyl-3-benzofuranyl)methanone.
Chemical structure formula.
Molecular formula: C17H12Br2O3
Molecular weight: 424.08
Properties
This product is white or off-white tablet.
Indications
It is suitable for primary hyperuricemia and intermittent gouty arthritis.
Specification
50mg
Dosage
Adults take 50mg (one tablet) orally once a day after breakfast. Check the serum uric acid concentration after 1 week, or take 100mg (two tablets) orally after breakfast at the beginning of treatment, and then change to 50mg (one tablet) daily when the blood uric acid drops to normal range.
[Adverse Reactions].
General adverse reactions
Gastrointestinal discomfort, such as nausea, vomiting, feeling of fullness in the stomach and diarrhea, may sometimes occur.
Rarely, urticaria (rubella) may occur.
Inflammation of the conjunctiva (conjunctivitis), short-term impotence, localized eczema (rash), headache and increased urinary frequency may occur in some cases.
Abnormal liver function and, in some cases, aggravation of liver disease (cytolytic hepatitis), which in some cases is acute and more difficult to control, are also observed.
Pruritus, facial redness, erythema, photosensitivity, swelling, and cardiac discomfort have been reported with benzbromarone.
Serious Adverse Reactions
Severe liver injury (frequency unknown): There is a possibility of severe liver injury such as fulminant hepatitis and jaundice, so adequate observation must be made by regular liver function tests, etc., and when abnormalities are detected, the drug should be stopped and appropriate measures taken.
If adverse reactions occur that are not mentioned in the product’s instructions, please inform your doctor or pharmacist immediately.
Contraindications
This product is contraindicated in the following patients.
1. Those with known hypersensitivity to this product.
2. Pregnant or potentially pregnant women and nursing mothers.
3. Patients with moderate to severe renal impairment (glomerular filtration below 20 ml/min) and patients with kidney stones.
Precautions]
1. should not be taken during acute attacks of gout, as the disease may be aggravated with the leaching of uric acid from the tissues during the beginning of the treatment phase.
2. usually take benzbromarone according to the prescribed dosage and method, gout will not attack in the early stage of treatment, but if it does, it is recommended to reduce the amount of medication used by half, and also use colchicine or anti-inflammatory and analgesic drugs to relieve pain as needed.
3. During the treatment period, it is necessary to drink a lot of water to increase the amount of urine (the amount of water drunk at the beginning of treatment should not be less than 1.5-2 liters). The pH of urine should be measured regularly. To promote urine alkalinization, sodium bicarbonate or citrate combination may be given as appropriate, and the acid-base balance should be noted. The patient’s urine pH should be adjusted between 6.2 and 6.8.
4. A large amount of uric acid is excreted in the urine at the beginning of treatment, so the dose of medication at this time should be small (starting dose).
5. Liver function should be checked regularly when using the drug for a long time.
6. Pay close attention to loss of appetite, nausea, vomiting, general feeling of lethargy, abdominal pain, diarrhea, fever, concentrated urine staining, yellow staining of conjunctiva and other phenomena during the course of medication.
7. For patients with hyperuricemia caused by hematopoietic system diseases (i.e. secondary hyperuricemia caused by blood diseases), this product should be taken only after consulting a doctor.
8. Avoid concomitant use with other drugs for liver damage.
Pregnant women and nursing mothers
It is contraindicated in pregnant women, women at risk of pregnancy, and women who are breastfeeding.
For Children
The safety and efficacy of use in children (<18 years) has not been established.
Geriatric Use]
The elderly generally have reduced physiological functions, so reduce the dosage or follow medical advice.
Drug Interactions
1. The effect of benzbromarone to promote uric acid excretion may be weakened by salicylate and benzosulfone.
2. The antituberculosis drug pyrazinamide can inhibit the secretion of uric acid in the renal tubules, thus weakening the effect of benzbromarone.
3. Combination with other potentially hepatotoxic drugs should be avoided.
4.Benzbromarone may increase the anticoagulant effect of coumarin-based anticoagulants, so if coumarin-based anticoagulants are combined with this product, patients should be closely monitored for prothrombin time (Quick value or INR value).
Drug overdose]
Not yet known.
Pharmacology and Toxicology
Pharmacological effects
Benzbromarone is a benzofuran derivative, which is a pro-uric acid excretory drug. It reduces the concentration of uric acid in blood by inhibiting the reabsorption of uric acid in the renal tubules.
Toxicological study
Reproductive toxicity
Animal tests have shown that benzbromarone has teratogenic effects on animals.
Genotoxicity
The results of Ames test, DNA repair test in rat hepatocytes, chromosome aberration and sister chromatid interchange test in mouse lymphocytes were all negative for benzbromarone.
Carcinogenicity
Hepatic tumor nodules were seen in rats given benzbromarone orally for 102 weeks at a dose of 2.0 mg/kg or 50 mg/kg, and one case of hepatocellular carcinoma (HCG) was seen in the 50 mg/kg (equivalent to 17 times the clinical dose) group, suggesting that this product has some hepatic tumor-inducing effects. In addition, rat studies have shown that this product has the effect of promoting liver growth and liver peroxisome proliferation, which may be related to tumor formation. In vitro studies have shown that this product also has the effect of promoting peroxisome proliferation in isolated rat hepatocytes, but not in human hepatocytes, and the relevance of this finding to clinical humans is unclear.
Pharmacokinetics
Healthy adult oral 50mg, about 2~3 hours after peak blood concentration, 4~5 hours uric acid profile reached the maximum, half-life of 12~13 hours, the product mainly as a prototype drug single halide, complete dehalogenation from the urine, feces and bile excretion.
Storage】Store under light and seal.
Package】Packaged in aluminum foil/polyvinyl chloride solid pharmaceutical rigid tablets, 10 tablets/box, 30 tablets/box.
Expiration date】18 months
Execution Standard
Approval Number】State Drug Administration H20040348
【Manufacturing enterprise
Company Name: Yichang East Sunshine Yangtze River Pharmaceutical Co.
Address: No. 38, Binjiang Road, Yidu City, Yichang, Hubei Province
Postal Code: 443300
Medical consultation telephone number: 4006707855
Sales phone number：0769-85370280 Fax number：0769-85370206
Web address: Http://www.hecpharma.com
If you have any questions, you can contact with the manufacturer.