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  • Name: Rifampin and Isoniazid Capsules
  • Add time: 2015-05-15
  • Views : 62

 

[Drug Name]
Generic Name:异福胶囊
English name:Rifampin and Isoniazid Capsules
Pinyin:Yifu Jiaonang
Ingredient
This product is compound, the group were as follows: each containing rifampicin (C43H58N4O12) 0.15g, isoniazid (C6H7N3O) 0.1g.
[Character]
This product capsules, the contents of the orange-red to dark red powder.
Indications
Suitable for tuberculosis four months early treatment and non-drug-resistant TB patients multiplicity maintenance phase treatment.
[Specification]
0.25g (C43H58N4O12 0.15g and C6H7N3O 0.1g)
Dosage
This product is only suitable for those weighing less than 50kg (not including 50kg) adults. Adult usual dose: Oral, weight <50kg person, an oral rifampin 0.45g, isoniazid 0.3g, once a day. 30 minutes before meals or two hours after a meal taken, the general course of four months. Or compliance.
Adverse reactions
1. The most common gastrointestinal reactions, may occur after oral administration of fear of food, nausea, vomiting, abdominal discomfort, diarrhea and other gastrointestinal reactions.
2. The main side effects of liver toxicity based products, in the first few weeks of treatment, few patients can occur in serum aminotransferase, hepatomegaly and jaundice, mostly asymptomatic serum aminotransferase a transient increase, self-healing in the course of treatment, the elderly, alcoholics, malnutrition, liver disease, or other factors existing liver dysfunction are more likely to occur. Adverse reactions manifested as poor appetite, unusual fatigue or weakness, nausea or vomiting (liver toxicity of prodromal symptoms) and dark urine, yellowing of the eyes or skin (liver toxicity).
3. allergy include fever, polymorphous rash, lymphadenopathy, vasculitis, purpura, asthma, anaphylactic shock. Even after high-dose intermittent therapy can be a "flu-like syndrome", manifested as chills, chills, fever, malaise, difficulty breathing, dizziness, drowsiness and muscle pain, and dose size and frequency of intermittent time clearly related. It can occur even acute hemolysis or renal failure, now that the case of an allergic reaction which produces the mechanism.
4. The nervous system toxicity: peripheral neuropathy is more common in slow acetylation, and a clear relationship between dose. More patients showed unsteady gait, numbness tingling, burning or pain in the hands and feet. Such reactions lead poisoning, atherosclerosis, hyperthyroidism, diabetes, alcoholism, malnutrition and pregnant women are more prone. B610 ~ 50mg daily doses of vitamins can prevent or relieve symptoms. Other adverse reactions such as excitement, euphoria, insomnia, loss of self-main, toxic encephalopathy or toxic psychosis are belong to rare, serious toxicity optic neuritis and atrophy occasionally reported.
5. The blood system can have neutropenia, increased eosinophils, thrombocytopenia, methemoglobinemia and the like.
6. Others such as prothrombin time shortened, headache, dizziness, dry mouth, hypertension, vitamin B6 deficiency, hyperglycemia, metabolic acidosis, endocrine dysfunction occasionally reported.
Taboo
1. Disable to isoniazid, rifampicin and rifamycin antimicrobial drug allergies.
2. severe liver failure, biliary obstruction, and within three months pregnancy.
[Precautions]
1. alcoholism, mental illness, epilepsy, liver dysfunction caution. Baby, three months or more pregnant and lactating women with caution.
2. Cross-allergic reactions to B isonicotinoyl amine, pyrazinamide, nicotinic acid or other chemical structure of drug allergies may be allergic to the chemicals.
3. The diagnosis of interference: may cause direct antiglobulin test (Coombs test) positive; interference serum folate concentrations were measured and the measurement results of serum vitamin B12 concentrations; phthalocyanine sodium methyl bromide can cause false positive test retention; may interfere with the use of spectrophotometric The results of the urine analysis test meter or color changes carried out; make the blood urea nitrogen, serum alkaline phosphatase, serum alanine aminotransferase, aspartate aminotransferase, serum bilirubin and serum The measurement results uric acid concentration increased; performed using copper sulfate urine assay false positive reaction can be presented, but does not affect the enzymatic assay results.
4. Rifampicin can cause liver dysfunction, jaundice associated deaths have been reported with other hepatotoxic drugs when the same clothes in the original patients with liver disease or the goods and therefore the original liver disease, only in case there is a clear indication before caution, before the start of treatment, the treatment of close observation of changes in liver function, liver damage occur, immediate withdrawal.
5. Vitamin B6 isoniazid structure similar to large doses, vitamin B6 can make a lot with the urine, inhibition of glutamate in the brain become γ- aminobutyric acid decarboxylation lead to seizures, but also can cause peripheral nervous system multiple lesions. Therefore, while daily oral vitamin B650 ~ 100mg help prevent or mitigate peripheral neuritis and (or) vitamin B6 deficiency symptoms. Such as mild tingling hands and feet, dizziness, you can take vitamin B1 or B6, or if there is severe vomiting phenomenon, should be discontinued immediately.
6. rifampicin may cause neutropenia and thrombocytopenia and bleeding gums and lead to infection, delayed wound healing and so on. You should avoid tooth extraction surgery, and pay attention to oral hygiene, brushing and flossing are required to carefully until the blood return to normal. Peripheral blood should be checked regularly during the treatment.
7. The Department of hyperbilirubinemia liver cells and bile retention hybrid, medication in patients with mild self-limiting, weight are required to observe the withdrawal. Serum bilirubin may be the result of rifampicin compete with bilirubin excretion. Early treatment for 2 to 3 months, hepatic function should be closely monitored.
8. Patients with liver dysfunction require dose reduction, severe renal dysfunction required reductions.
9. The product of therapeutic use of anti-TB drugs continue chemotherapy, the general application of four months, treatment should adhere to the sputum negative conversion, clinical symptoms improved through the maximum extent so far.
10. The treatment of optic neuritis symptoms, the need for eye examination immediately, and regularly reviewed.
11. Patients with slow acetylation easier to produce adverse reactions, it is appropriate to lower doses.
12. After taking urine, saliva, sputum, tears, sweat and other excretions could significantly orange.
[Pregnant women and lactating women drug]
1. rifampin and isoniazid can cross the placenta, animal experiments confirmed teratogenic and can cause stillbirth. Although not confirmed human problems, but pregnant women should be avoided, if there are indications when applications must fully weigh.
2. rifampin and isoniazid can be secreted through breast milk, although in humans has not been proven there is a problem, the application should still be fully weigh the nursing period, if the medication are advised to suspend breast-feeding.
Pediatric Use
This product safety in children under 5 years old application has not been determined.
[Geriatric medicine]
Elderly patients have decreased liver function, the dosage should reduce it.
Drug interactions
1. The alcohol may cause increased incidence of liver toxicity of this product increased metabolism of the product, the need to adjust the dose, and close observation of patients with and without liver toxicity appear.
2. aminosalicylates may affect the absorption of the product, resulting in reduced plasma concentrations of rifampicin; such as when applications must be united, the two take at least 6 hours.
3. The goods and acetic isonicotinoyl amine, pyrazinamide, or other anti-TB drugs may increase the adverse reactions. In combination with other hepatotoxic drugs may increase the liver toxicity of this product, should be avoided.
4. chlorophenol hydrochloride can reduce the absorption of rifampicin, the peak time delay and half-life.
5. and miconazole or ketoconazole can both reduce the plasma concentration, so the product should not be combined with imidazole.
6. adrenocorticotropic hormone (glucocorticoid, mineralocorticoid), anticoagulants, aminophylline, theophylline, chloramphenicol, clofibrate, cyclosporine, verapamil (verapamil), duly Carney, propafenone, trimethoprim, or indandione coumarin derivatives, oral hypoglycemic agents, corticotropin, dapsone, digitalis glycosides, disopyramide, quinidine and When combined with the product, since rifampicin induces hepatic microsomal enzyme activity, it can weaken the efficacy of these drugs, so in addition to dapsone digoxin and outside, in front of the FDA and the course of treatment need to adjust the dose of these drugs . The goods and coumarin or indane ketones should be combined daily or periodically measuring prothrombin time, according to adjust the dose.
7. It can promote the metabolism of estrogen or reduce its enterohepatic circulation, reduce the role of oral contraceptives, resulting in irregular menstruation, menstrual bleeding between periods and unplanned pregnancy. Therefore, patients using this service, you should use other contraceptive methods.
8. The product can induce hepatic microsomal enzymes, increased antitumor dacarbazine (dacarbazine), cyclophosphamide metabolism, the formation of alkylated metabolites induce leukocyte reduced, and therefore the need to adjust the dose.
9. diazepam (Valium) combined to increase the elimination of the latter to reduce the plasma concentration, and therefore need to adjust the dose.
10. The product can increase phenytoin metabolism in the liver, so the two combined phenytoin plasma concentrations should be measured and adjust the dosage.
11. The product can increase levothyroxine degradation in the liver, so the dose of L-thyroxine should be increased when the two combined.
12. This product can also increase methadone, mexiletine metabolized in the liver, causing methadone withdrawal symptoms mexiletine plasma concentrations reduced, so after two in combination require dose adjustment.
13. probenecid can compete with rifampicin uptake by liver cells, so that increased plasma concentration of rifampicin and produce toxicity. But instability in the action, it is usually not added with probenecid to increase the plasma concentration of this product.
14. isoniazid antagonists vitamin B6, and vitamin B6 may increase by renal excretion, prone to cause the occurrence of peripheral neuropathy. While taking vitamin B6, the need to increase the amount of discretion.
15. This product should not be combined with other nerve poisons, so as not to increase neurotoxicity.
16. to increase the central nervous system in combination with cycloserine adverse reactions (such as dizziness or drowsiness), the need to adjust the dose, and closely observe the signs of toxicity in the central nervous system, especially the need for high sensitivity work in patients.
17. The product can inhibit the metabolism of carbamazepine, making plasma concentration increased, causing toxicity; carbamazepine isoniazid may induce microsomal metabolism, intermediate metabolite increased liver toxicity.
18. In the combination of acetaminophen, since isoniazid may induce hepatic cytochrome P450, that the former is formed to increase the amount of toxic metabolites, increase liver toxicity and kidney toxicity.
19. When combined with alfentanil, since the drug isoniazid liver enzyme inhibitor, extended alfentanil effect; with disulfiram can be combined to enhance its role in the central nervous system, resulting in dizziness, incoordination, irritability, insomnia; and enflurane combined form can increase inorganic fluoride nephrotoxic metabolites.
20. Not with ephedrine, belladonna while taking to avoid adverse reactions or increased.
21. The aluminum-containing antacids may delay and reduce the absorption of isoniazid after oral administration, plasma concentration reduced, should avoid the use of, or prior to oral antacid at least 1 hour using this service.
Overdosage
1. Drug overdose of performance: eye or facial edema, generalized itching, Reds syndrome (skin and mucous membranes and sclera red or orange), convulsions, unconsciousness, and coma. With primary liver disease, alcoholism, or liver toxicity with taking other drugs that could cause death.
2. overdose treatment:
(1) withdrawal.
(2) keep the airway open.
(3) use of short-acting barbiturate preparations and vitamin B6 in the intravenous administration. Vitamin B6 1mg dose of isoniazid with each 1mg of vitamin B6, such as taking a dose of isoniazid is unknown, may be given vitamin B65g, every 30 minutes, until the convulsions stopped, the patient regained conscious. Followed by gastric lavage, gastric lavage should be within 2 to 3 hours after taking this be, given after gastric lavage activated charcoal paste the gastrointestinal tract to absorb the remnants of the goods; severe nausea and vomiting antiemetic agent.
(4) immediately measured blood gas, electrolytes, blood urea nitrogen, blood sugar.
(5) immediately intravenous sodium bicarbonate to correct metabolic acidosis, repeated administration when needed.
(6) the use of osmotic diuretics, and continue to apply after the clinical symptoms have improved, promote the excretion of the product, prevent recurrence of symptoms.
(7) severe poisoning patients should be early with blood, ready to do hemodialysis, can not be performed hemodialysis, peritoneal dialysis can be performed at the same time combined with diuretics.
(8) severe liver dysfunction for more than 24 to 48 hours, could be considered for bile drainage to cut off rifampicin enterohepatic circulation.
Pharmacology and Toxicology
This product is anti-TB drugs, rifampicin and isoniazid compound preparation. Rifampicin and outside the host cell significantly bactericidal effect against Mycobacterium tuberculosis and some non-tuberculous mycobacteria (including Mycobacterium leprae, etc.). Isoniazid to all types of Mycobacterium tuberculosis has a highly selective bactericidal effect, growth and reproduction of Mycobacterium effect on strong, weak and slow quiescent role. The two combined can enhance the antibacterial activity, and reduce the generation of resistant strains.
Rifampicin and DNA-dependent RNA polymerase β subunit strongly binding, inhibit the synthesis of bacterial RNA, preventing the enzyme and ligated DNA, thus blocking transcription of RNA, DNA and protein synthetic stopped. Mechanism of Isoniazid may inhibit sensitive bacteria meromycolic leaving the cell wall synthesis break.
Pharmacokinetics
This product is well absorbed orally, 1 to 2 hours after taking isoniazid peak plasma concentration (Cmax), 1.5 ~ 4 小时 rifampicin peak plasma concentration (Cmax). After the adult oral rifampicin 0.6g peak plasma concentration (Cmax) of 7 ~ 9mg / L, 6 months to 5 years old children an oral rifampicin 10mg / kg, peak plasma concentration (Cmax) of 11mg / L . Distributed in the body after absorption of most tissues and body fluids, you can cross the placenta. Rifampicin protein binding rate of 80% to 91% protein binding rate isoniazid 0 to 10%. Rifampicin plasma elimination half-life (t1 / 2β) of 3 to 5 hours, after repeated administration has been shortened, from 2 to 3 hours; Fast acetylation of isoniazid blood elimination half-life (t1 / 2β) is 0.5 to 1.6 hours, slow acetylation of isoniazid blood elimination half-life (t1 / 2β) is from 2 to 5 hours. In the liver by itself induced microsomal oxidase rapidly deacetylated, rifampicin metabolite 25- deacetyl having antimicrobial activity of rifampicin, isoniazid metabolite and no antibacterial activity.
Rifampicin the biliary and intestinal excretion, may enter the enterohepatic circulation, but its active metabolite deacetylation no enterohepatic circulation, 60% to 65% of the dose excreted by 6% to 15% of the drug In the prototype, 15% active metabolites excreted in the urine, 7% places no active 3-formyl derivatives discharge, also discharged through milk; isoniazid in 70% of the dose excreted by the kidneys within 24 hours, Most of inactive metabolites, fast acetylation 93% to acetylation from the urine, slow acetylation of 63%, can be discharged from the milk, saliva, sputum and faeces. Rifampin can not clear by hemodialysis or peritoneal dialysis. A considerable amount of isoniazid can be cleared by hemodialysis and peritoneal dialysis.
Pharmacokinetic study of healthy volunteers showed that two components of the product whether it is at the same time taking each dose is administered in complex formulations, its bioavailability is similar.
[Storage]
Shading, sealed and stored in a dry place.
[Packaging]
Blister packaging, 12 / plate; composite bag, 5 boards / bag; carton packaging, bag / box.
[Validity]
24 months
[Executive standard]
"Chinese Pharmacopoeia" 2010 edition Third Supplement
Approval Number
Zhunzi H21023354
Manufacturer
Company Name: Shenyang Hongqi Pharmaceutical Co., Ltd.
Production Address: Shenyang Hunnan new network on the 6th Street Postcode: 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 manufacture