keyword :
分类
Products
  • Name: Rifampin Isoniazid and Pyrazinamide Capsules
  • Add time: 2015-05-15
  • Views : 120

 

[Drug Name]
Generic Name:异福酰胺胶囊
English name:Rifampin Isoniazid and Pyrazinamide Capsules
Pinyin:Yifuxian’an Jiaonang
Ingredient
This product is compound, the group were as follows: each containing rifampicin (C43H58N4O12) 0.075g, isoniazid (C6H7N3O) 0.05g and pyrazinamide (C5H5N3O) 0.25g.
[Character]
This product capsules, the contents of brick red, orange or red powder.
Indications
Mainly used to strengthen the short-course chemotherapy of tuberculosis.
[Specification]
0.375g (C43H58N4O12 0.075g, C6H7N3O 0.05g and C5H5N3O 0.25g)
Dosage
Oral. 33 ~ 55kg weight patients 6 daily, 1 hour before or 2 hours after meals Dayton clothing. Weighing more than 55kg patient, doctor.
This product is used to strengthen short-term therapy of anti-TB treatment phase, namely the first 2 months of treatment. According to WHO recommendations, the initial stage of treatment, to use ethambutol or streptomycin as the four kinds of therapy, after which the stage with rifampicin and isoniazid continue therapy for at least four months.
Adverse reactions
Foreign clinical research data shows that:
Rifampin tolerated, rarely severe reactions, side reactions occur daily or intermittent program is as follows:
Mild skin reactions and self-healing, typically include skin flushing, may be associated with pimples or without pimples, more severe allergic reactions are extremely rare.
Gastrointestinal effects include nausea, vomiting, abdominal discomfort and diarrhea. Pseudomembranous colitis has been reported.
It can cause hepatitis, liver function should be checked regularly (see note).
Thrombocytopenia with or without purpura, often occurs in a batch program, immediately after stopping often return purpura, purpura occurred after continued use may cerebral haemorrhage have been reported. Small number of patients increased eosinophils, neutrophils decreased, edema, muscle weakness and myopathy.
The following adverse reactions occurred in a batch program, more concerned with immunity.
- Flu-like syndrome, including fever, chills, headache, dizziness and pain, occurred in the treatment of the first 3-6 months. The frequency varies greatly, rifampicin 25 mg / kg or more, administered once a week, 50% of patients the reaction can occur.
A shortness of breath and wheezing.
- Blood pressure and shock.
An acute hemolytic anemia.
- Due to acute tubular necrosis or acute interstitial nephritis induced acute renal failure.
Long-term women receiving rifampicin-containing regimen may be irregular menstruation. Patients should be told in advance rifampicin urine, stool, sputum and tears into red, contact lenses may be colored.
There may be a serious and sometimes fatal hepatitis isoniazid isoniazid therapy. Isoniazid-induced polyneuritis, manifested as numbness, muscle weakness, tendon reflexes and the like. Rifampicin, pyrazinamide capsule using different recommended doses do not appear in multiple cell deficiency, thrombocytopenia, or anemia. Gastrointestinal system reactions include nausea, vomiting, and abdominal discomfort. Large doses of isoniazid can cause convulsions, conventional doses does not cause other neurological toxicity such as toxic encephalopathy, optic neuritis and optic atrophy, memory loss and poison neuropathy. Isoniazid can increase the number of seizures epilepsy patients.
Pyrazinamide pyrazinamide-induced side effects (except liver reactions) have active gout (pyrazinamide may reduce the excretion of uric acid), sideroblastic anemia, joint pain, loss of appetite. Hepatic reactions are most common side effects. Only liver function abnormalities may be asymptomatic or manifested as mild fever, fatigue and liver tenderness, clinical also can be severe jaundice, rare individual cases of acute jaundice, liver atrophy and death.
Taboo
Rifampin, isoniazid, pyrazinamide history of allergies were banned.
[Precautions]
1. any component of this product can cause liver damage, during the administration should be careful to check liver function.
Rifampicin patients with impaired liver function, only when necessary and in use under the close supervision of medical personnel, these patients should be every 2 to 4 weeks and carefully check liver function before treatment and treatment periods, particularly SGPT and SGOT, when found any tendency to liver cell damage should be immediately discontinued.
In some cases, due to the rifampicin and bilirubin in hepatocytes competition discharge, early treatment can occur hyperbilirubinemia. Case Report moderately elevated bilirubin, transaminases at this time not as an interrupt treatment indications, should be more checks, pay attention to the trend, and clinical manifestations considered.
Because of the possibility of intermittent immune response treatment should be closely observed, and tell the patient not to interrupt therapy, interruption of treatment may occur due to the reaction.
Rifampin has enzyme induction effects, including induction - within aminolevulinic acid synthase. Case reports make use of rifampicin porphyria worse.
Isoniazid patients with chronic liver disease and kidney dysfunction should be used with caution isoniazid.
Serious or even fatal hepatitis can occur in patients starting isoniazid therapy may also occur for several months after treatment. The occurrence of hepatitis and age. Where the early symptoms of hepatitis, such as fatigue, weakness, fatigue, loss of appetite, nausea and vomiting should be careful to check the patient follow-up, where the above symptoms or signs of liver damage, isoniazid should immediately stop using it. Continued use can cause serious consequences.
When pyrazinamide have gout This product should be used with caution, if there excess uric acid accompanied by acute gouty arthritis, patients should be free to use pyrazinamide regimen.
2. mental illness or epilepsy with caution.
3. carcinogenic, mutagenic, fertility damage.
Rifampicin so far no information on the potential long-term carcinogenic effects on people, mutagenic, fertility damage, only a few case reports of accelerated growth of lung cancer, but it does not determine causality. Rifampicin in man-days 2 to 10 times the average dose given to mice 60 weeks, found that female mice of hepatocellular carcinoma increased in the next four to six weeks observation. Under the same experimental conditions, it was not found in male mice or rabbits or other species of mice have carcinogenic effects.
Rifampicin has immunosuppressive effects, are being reported in rabbits, rats, guinea pigs and human experiment, too, rifampicin also have anticancer effects.
No rifampin in bacteria, fruit flies or mice mutagenic effect was not found rifampicin induced chromosomal aberrations in lymphocytes in vitro wife. Whole blood cell cultures treated with rifampicin and found an increase in chromosome breakage.
Isoniazid Isoniazid many strains of mice can induce lung tumors have been reported.
[Pregnant women and lactating women drug]
When high doses of rifampicin, rodents can cause deformities, No controlled studies in pregnant women report. Use of rifampicin in late pregnancy weeks, can cause bleeding postpartum mothers and babies. Given vitamin K can be corrected.
Isoniazid isoniazid mice pregnancy can cause embryonic death have been reported. But no reports of isoniazid-induced abnormalities produced.
Pyrazinamide no controlled studies in pregnant women report.
Pregnant women can use after weighing the benefit outweigh the potential risk to the fetus. Due to rifampin and isoniazid can pass through the placenta into the milk, it should not breast-feeding, unless your doctor has considered the benefit outweigh the potential risk to the baby.
Pediatric Use
Not to proceed with the experiment and no reliable references.
[Geriatric medicine]
Not to proceed with the experiment and no reliable references.
Drug interactions
Rifampicin rifampicin induce liver enzymes features, you can decrease the effect of many drugs, such as anticoagulants, adrenocorticotropic hormone, cyclosporine, digitalis preparations, quinidine, oral contraceptives, oral hypoglycemic agents , dapsone, anesthesia and painkillers. It is reported that rifampicin and methadone, barbiturates, diazepam, verapamil set, adrenal blockers, Clofibrate, progesterone, disopyramide, mexiletine, theophylline, chloramphenicol and anti- while taking anticonvulsants, may reduce its role. As required while taking should focus on improving dose, usually in the application of rifampicin, the patient should be switched to a non-hormonal method of contraception. Acid drugs can affect the absorption of rifampicin.
When use of rifampicin and halothane, increased liver toxicity; and ketoconazole use of two drugs can reduce serum concentration, it can be patient clinical dose adjustment. Rifampicin inhibit standard microbiological method to detect serum folic acid and vitamin B12, can make sulfa titanium sodium (BSP) and transient increase in serum bilirubin, so the above test should be carried out before the morning service rifampin.
Isoniazid may reduce the excretion of phenytoin to enhance its role. The dose should be adjusted anti-seizure drugs, the daily drinking can increase isoniazid hepatitis, the elderly and malnourished patient treatment, isoniazid with vitamin B6 serving a total.
Overdosage
If overdose of this product should immediately stop using the drug, gastric lavage, activated carbon injection and symptomatic treatment measures (including hemodialysis).
Pharmacology and Toxicology
Pharmacological effects
This product is anti-TB drugs, is compound formulation consists of rifampin, isoniazid and pyrazinamide composition. It has been confirmed that, rifampin, isoniazid and pyrazinamide in the therapeutic levels of intracellular and extracellular M. tuberculosis have antibacterial activity.
Mechanism of action: inhibition by rifampicin sensitive Mycobacterium tuberculosis RNA polymerase, especially the interaction of the bacteria with the antimicrobial activity reached RNA polymerase, but no inhibitory effect on mammals. Mycobacterium tuberculosis Isoniazid by inhibiting cyclic fatty acid biosynthesis, which affects cell wall synthesis of Mycobacterium tuberculosis. The exact role of pyrazinamide suppress the growth of Mycobacterium tuberculosis mechanism is not clear, but the body, studies show outside, pyrazinamide is only active at a slightly acidic (pH5.5) environment.
Toxicology
Different, rifampicin, pyrazinamide
Genetic Toxicity: Use of the compound from the patient's lymphocytes in vitro study shows that the rate of increase of chromosomal aberrations. Other information may refer to the relevant information provided by a single drug.
Currently there is no genetic toxicity of the compound, and reproductive toxicity and carcinogenicity studies, toxicology each single agent can refer to the following related information.
Rifampicin
Genetic Toxicity: Bacteria Drosophila or in mice not found this product has mutagenic effects; human lymphocyte chromosomal aberration test was negative, but during the whole blood cell culture of the material and found that an increase in chromosome breakage.
Reproductive toxicity: rodent study found that the goods in large doses have teratogenic effects.
Carcinogenicity: There is no long-term use of this product about people reported to have carcinogenic potential, there are a few cases of clinical reports of patients taking this cancer grow faster, but its correlation with the drug has not been determined. People daily average of 2 to 10 times the dose administered to the mice 60 weeks, can be observed increased incidence of liver cancer in females, but not found carcinogenic in male mice and other strains of mice or rabbits.
Other: A number of studies suggest that the goods on rabbits, rats, mice, guinea pigs and human potential immunosuppressive effects.
Isoniazid
Genetic Toxicity: no report.
Reproductive toxicity: In pregnant rats and rabbits experiments, the product can cause embryonic death.
Carcinogenicity: It has been reported, isoniazid can cause a variety of lung tumors in mice.
Pyrazinamide
Genetic Toxicity: Ames test of this product was negative, but in vitro tests showed that the product can induce chromosome aberrations in human lymphocytes.
Reproductive toxicity: Reproductive toxicity studies have not been reported on this product.
Carcinogenicity: Lifetime test results in rats and male mice suggest that the product non-carcinogenic, but female mice carcinogenicity inconclusive.
Pharmacokinetics
Rifampicin:
Rifampicin easily absorbed from the gastrointestinal tract. Peak plasma concentration between adults and children are quite different, press 10 mg / kg body weight empty stomach, 2 to 4 hours peak plasma concentration of about 10 micrograms / ml. As with food, reduce the absorption of rifampicin. Normal service 600 mg rifampicin, biological half-life of 3 hours average blood; 900 mg after serving an average half-life of 5.1 hours. Repeated administration, the half-life decreased, the average of 2 to 3 hours. When daily doses of 600 mg, no patients with kidney failure half-life difference, so no need to adjust the dose, while taking isoniazid, rifampicin half-life is reduced.
After rifampicin absorbed quickly in the biliary clearance, carried enterohepatic circulation. At this point deacetylation rifampin, so all was the presence of about six hours in this form bile. Metabolite retains antibacterial effect. Deacetylation reduce the intestinal absorption of the drug and then promote drug clearance. About 30% of the drug (half of the prototype) from the urine. Rifampicin is widely distributed throughout the body in many organs and body fluids including cerebrospinal fluid was effective concentration. Rifampicin about 80% and protein binding, most unbound partially electrically ionized, so freely dispersed in the tissue.
Isoniazid:
Isoniazid effect on the activity of the growth of Mycobacterium tuberculosis, 1 to 2 hours after oral administration to reach peak blood concentration, within six hours reduced to 50%. Easy dispersed to various body fluids (cerebrospinal fluid, chest and abdominal fluid), tissues, organs and excreta (saliva, sputum and stool). Isoniazid is also through the placenta into the milk at concentrations similar to plasma. About 50% to 70% of isoniazid excreted in the urine within 24 hours.
In the metabolism of isoniazid acetylation and off the main hydrazine, acetylation rate of genetic, about 50 percent of blacks and Europeans as "slow inactivated by" most Asians as "fast does not activate those."
Serving large doses of vitamin B6 deficiency can occur isoniazid, the results may be due to competition with pyridoxal phosphate alcohol off the enzyme tryptophan.
Pyrazinamide
Ease of absorption from the gastrointestinal tract and rapidly distributed in the body, two hours of peak blood concentration. Pyrazine acid hydrolysis, and then metabolized into serotonin pyrazine acid discharged from the glomerular filtration rate. And in the acidic environment of the intracellular TB bactericidal effect.
In normal volunteers Pharmacokinetic studies showed that the bioavailability of rifampicin, pyrazinamide capsule three different components simultaneously with the three-drug combination with a single dose similar.
Domestic research results are consistent with studies abroad.
[Storage]
Shading, sealed and stored in a dry place.
[Packaging]
(1) blister packaging, 6 / plate; composite bag, 5 boards / bag; carton packaging, 2 bags / boxes.
(2) blister packaging, 6 / plate; composite bag, 5 boards / bag; carton, 3 bags / boxes.
[Validity]
24 months.
[Executive standard]
"Chinese Pharmacopoeia" 2010 edition Third Supplement
Approval Number
Zhunzi H20020465
Manufacturer
Company Name: Shenyang Hongqi Pharmaceutical Co., Ltd.
Production Address: Shenyang Hunnan New District envelope 6th Street
Postal Code: 110179
Phone Number: (024) 2,378,626,023,786,261
Fax: (024) 23786263

 

The above is for reference
If you have questions can contact the manufacturer