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Pyrazinamide Capsules (0.25g)
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Pyrazinamide Capsules (0.25g)

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Pyrazinamide Capsule Instructions
 Please read the instructions carefully and use under the guidance of a doctor
 
 
【Drug Name】
Generic name: Pyrazinamide capsules
English name: Pyrazinamide Capsules 
Chinese Pinyin: Biqinxian'an Jiaonang
【Ingredients】
Chemical name: Pyrazinamide
Chemical Structure:
 
 
Molecular formula: C 5 H 5 N 3 O
Molecular weight: 123.12
【Properties】
This product is a capsule, and the content is white or off-white powder.
【Indications】
This product is only effective against mycobacteria and is used in combination with other anti-tuberculosis drugs (such as streptomycin, isoniazid, rifampicin and ethambutol) in the treatment of tuberculosis.
【Specifications】0.25g
【Dosage】
oral. Common dosage for adults, combined with other anti-tuberculosis drugs, 15-30mg/kg a day, or 50-70mg/kg, 2-3 times a week; daily maximum 2g daily, 3 times a week maximum 3g each time, up to 4g each time for 2 times a week.
【Adverse reactions】
Higher incidence: arthralgia (due to hyperuricemia, often mild, self-limiting); lower incidence: loss of appetite, fever, fatigue or weakness, yellow eyes or skin (hepatotoxicity) , Chills.
【Taboo】
The experiment has not been carried out and there is no reliable reference.
【Precautions】
1. Cross allergy, patients allergic to ethionamide, isoniazid, niacin or other drugs with similar chemical structure may also be allergic to this product.
2. Interference with diagnosis: This product can react with sodium nitrocyanide to produce reddish brown, which affects the results of urine ketone determination; it can increase the measured values ​​of alanine aminotransferase, aspartate aminotransferase, and blood uric acid concentration.
3. Use with caution for those with diabetes, gout or severe liver function decline.
4. Serum uric acid often increases during the course of treatment with this product, which can cause acute gout attacks, and serum uric acid must be measured.
5. This product can also be administered intermittently, twice a week, 50mg/kg each time.
[Medicine for pregnant women and lactating women]
Pregnant women with tuberculosis can be treated with isoniazid, rifampicin and ethambutol for 9 months first. Those who are resistant to any of the above drugs and may be sensitive to this product may consider using this product. This product belongs to FDA category C of pregnancy drugs.
【Children's Medication】
This product is highly toxic and should not be used by children. When it must be applied, it must be decided after weighing the pros and cons.
【Geriatric Medication】
The experiment has not been carried out and there is no reliable reference.
【medicine interactions】
1. Combining this product with allopurinol, colchicine, probenecid, and sulfopridone can increase the blood uric acid concentration and reduce the efficacy of the above drugs on gout. Therefore, the dose should be adjusted when combined to control hyperuricemia and gout.
2. It can enhance adverse reactions when combined with ethionamide.
3. The blood concentration of cyclosporine and pyrazinamide may decrease when the former is used together, so blood concentration should be monitored and the dosage adjusted accordingly.
【Overdose】
The experiment has not been carried out and there is no reliable reference.
【Pharmacology and Toxicology】
This product has a good antibacterial effect on human tuberculosis bacillus. It has the strongest bactericidal effect at pH 5 to 5.5. It is especially the best bactericidal drug for the tuberculosis bacteria in the phagocytes that grow slowly in an acidic environment. The inhibitory concentration of this product in the body is 12.5μg/ml, up to 50μg/ml can kill Mycobacterium tuberculosis. The concentration of this product to inhibit Mycobacterium tuberculosis in the cell is 10 times lower than that in the outside of the cell, and it has almost no antibacterial effect in a neutral and alkaline environment. The mechanism of action may be related to pyrazinic acid. After pyrazinamide penetrates into the phagocytes and enters the Mycobacterium tuberculosis, the amidase in the bacteria removes the amide group and converts it into pyrazinic acid to exert antibacterial effects. In addition, because pyrazinamide is similar in chemical structure to nicotinamide, it interferes with dehydrogenase by replacing nicotinamide, prevents dehydrogenation, hinders the use of oxygen by Mycobacterium tuberculosis, and affects the normal metabolism of bacteria, causing death.
【Pharmacokinetics】
After oral administration, it is absorbed quickly and completely in the gastrointestinal tract. It is widely distributed in body tissues and body fluids, including liver, lung, cerebrospinal fluid, kidney and bile. The drug concentration in the cerebrospinal fluid can reach 87%-105% of the blood concentration. The protein binding rate is about 10% to 20%. The plasma concentration can reach the peak 2 hours after oral administration, and the t1/2 is 9-10 hours. It may be prolonged when the liver and kidney function decline. It is mainly metabolized in the liver, hydrolyzed into pyrazinic acid, which is a metabolite with antibacterial activity, and then hydroxylated into an inactive metabolite, which is excreted through glomerular filtration. 70% is excreted as metabolites within 24 hours (of which pyrazinic acid is about 33%), and 3% is excreted in its original form. 4 hours of hemodialysis can reduce the blood concentration of pyrazinamide by 55%, and the blood pyrazinic acid can be reduced by 50% to 60%.
【Storage】
Shading, sealed and preserved.
【package】
Packed in plastic bottle, 100 capsules/bottle.  
【Validity Period】
36 months
【Executive Standard】
"Chinese Pharmacopoeia" 2015 Edition Two
【Approval Number】
National Medicine Standard H21022352
【manufacturer】
Company Name: Shenyang Hongqi Pharmaceutical Co., Ltd.  
Production address: No. 6, Xinluo Street, Hunnan New District, Shenyang City    
Postal Code: 110179        
Phone number: (024) 23786260 23786261  
Fax number: (024) 23786263
Website: www.hongqipharma.com
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