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  • Name: Ethambutol Hydrochloride, Rifampicin and Isoniazid Tablets
  • Add time: 2015-05-14
  • Views : 84

 

[Drug Name]
Generic Name:乙胺利福异烟片
English name:Ethambutol Hydrochloride, Rifampicin and Isoniazid Tablets
Pinyin:Yi’an Lifu Yiyan Pian
Ingredient
This product is compound, the group were as follows: Each tablet contains rifampicin 0.12g, isoniazid 0.12g, ethambutol hydrochloride 0.25g.
[Character]
This product is film-coated tablets, were removed after coating red.
Indications
This product is applicable to all types of adult retreatment sputum smear-positive TB patients continue on treatment.
Regimens: retreatment sputum smear-positive patients: intensive treatment of 2H3R3Z3E3S3 / continuation phase 6H3R3E3.
[Specification]
Each containing rifampicin 0.12g, isoniazid 0.12g, ethambutol hydrochloride 0.25g.
【Dosage】
Oral.
This product is used in patients with sputum smear positive retreatment of patients who continued, medication once every two days, a total of six months, the drug 90 times. Adult, weighing more than 50kg each patient fasting Dayton clothing amine Lifestyle isonicotinoyl sheet 5, 50kg underweight patients under doctor's orders to reduce it, one hour before meals or two hours after a meal Dayton clothing.
Press the specification or compliance to the FDA, the treatment of the whole process can not be interrupted or unauthorized changes medication regimen. In the event of adverse reactions, shall obey the physician orders.
【Adverse reactions】
Rifampicin: more common transient transaminase elevation, and occasionally nausea, vomiting, drug fever, rash, thrombocytopenia, asthma, severe cases can cause jaundice, renal function.
Isoniazid: occasionally peripheral neuritis and memory loss, headaches, insomnia, drowsiness, severe mental disorders induced epilepsy. Large doses or long-term use cause liver damage, may also have a rash, rash, drug fever and other allergic reactions.
Ethambutol: visual impairment, reduced vision, optic neuritis, occasional liver dysfunction and peripheral neuritis.
Taboo
1. Rifampin, isoniazid, ethambutol hydrochloride allergies were banned;
2. Liver dysfunction, biliary obstruction, pregnant women, patients with gout, mental illness, epilepsy, diabetes retinopathy were banned. Elderly and diabetic patients with caution. Alcoholism, liver dysfunction, optic neuritis, kidney dysfunction in patients with caution.
【Precautions】
1. The diagnosis of interference: make blood urea nitrogen, serum alkaline phosphatase, serum alanine aminotransferase, aspartate aminotransferase, bilirubin and serum measurement results of serum uric acid concentration increased. Where rifampicin can cause direct antiglobulin test (Coombs test) positive; measured serum folate concentrations and interfere with the measurement results of serum vitamin B12 concentrations; make methyl bromide phthalocyanine sodium retention test false positive; can interfere with the use of a spectrophotometer or color changes were the result of the urine analysis test. Isoniazid urine determination of copper sulfate method showed a false positive reaction, but does not affect the results of the enzymatic assay. Isoniazid can increase serum bilirubin measurement results.
2. Cross-allergy: The B isonicotinoyl amine, nicotinic acid or other similar chemical structure of the drug in patients with allergy to the chemicals may have allergies.
3. Since the product can make the serum uric acid concentration increased, causing gout attacks, so the treatment should be measured regularly.
4. During the treatment should be checked: eye, vision, vision, red-green discrimination, etc., before treatment, treatment of daily checks, optic neuritis symptoms, eye examination should be carried out immediately, and periodic review.
5. rifampicin
(1) baby, three months or more pregnant and lactating women with caution.
(2) rifampicin can cause liver dysfunction, jaundice associated deaths have been reported in patients with liver disease or when the original of this product with other hepatotoxic drugs with the service, and therefore the original patients with liver disease, only in case there is a clear indication below It can be used with caution, before the start of treatment, the treatment of close observation of changes in liver function, liver damage occur, immediate withdrawal.
(3) Department of hyperbilirubinemia liver cells and bile retention of mixed type, in patients with mild medication subside on their own weight are required to observe the withdrawal. Blood bilirubin may also be the result of competition rifampin and bilirubin excretion. Early treatment for 2 to 3 months should be closely monitored changes in liver function.
(4) rifampicin may cause neutropenia and thrombocytopenia and bleeding gums and lead to infection, delayed wound healing and the like. 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.
(5) after taking the urine, saliva, sweat and other excretions could significantly orange. Interstitial nephritis may occur.
[Pregnant women and lactating women drug]
Rifampicin: can cross the placenta, pregnant women should be the FDA ban within three months, more than three months pregnant women should be used with caution. Although unproven in humans against the harmful effects of fetal, maternal drug use should remain fully weigh; by milk excretion, although not confirmed in humans there is a problem, but lactating women should still be fully weighed.
Ethambutol: You can cross the placenta, although not confirmed in humans there is a problem, but the application must fully weigh pregnant women; may be secreted into milk, concentration and plasma concentration are similar, although not confirmed in humans have problems breast-feeding Women must be weighed against the drug.
Isoniazid: can cross the placenta, causing fetal blood concentrations higher than the maternal plasma concentration in humans did not confirm there is a problem, but the application must be fully weighed against pregnant women; similar to the product concentration in breast milk and plasma concentration, although In humans did not confirm there is a problem, the application should be fully weigh during lactation.
Pediatric Use
This product is not for children.
[Geriatric medicine]
Ethambutol hydrochloride: the elderly often accompanied by physiological renal dysfunction, renal function should therefore adjust the dosage.
Drug interactions
Rifampicin:
1. Lifestyle usually taking rifampicin daily drinking can lead to increased incidence of liver toxicity, and increased metabolic rifampicin, the need to adjust the dose of rifampicin, and closely monitor patients with and without liver toxicity symptoms appear.
2. adrenocorticotropic hormone (glucocorticoid, mineralocorticoid), anticoagulants, or indandione coumarin derivatives, oral hypoglycemic agents, corticotropin, dapsone, digitalis glycosides, disopyramide When amines, quinidine and rifampin, as the latter stimulating effect on the liver microsomal enzyme activity, can reduce the efficacy of these drugs, so in addition to dapsone digoxin and outside, with rifampicin flat front and the course of treatment of these drugs need to adjust the dose. The goods and coumarin or indane ketones should be combined daily or periodically measuring prothrombin time, to adjust the dose.
3. aminosalicylates may affect the absorption of rifampicin, resulting in reduced plasma concentration of rifampicin; for patients taking aminosalicylates and Lifestyle usual, separated by at least 6 hours between the two drugs.
4. Rifampicin can stimulate estrogen metabolism or decrease its enterohepatic circulation, reduce the role of oral contraceptives, resulting in irregular menstruation, menstrual bleeding and unplanned pregnancy period, usually patients taking rifampicin, should use other contraceptive methods ʱ??
5. rifampicin may induce hepatic microsomal enzymes, an increase of antineoplastic agents dacarbazine (dacarbazine), the metabolism of cyclophosphamide, an alkylating metabolites formed to promote leukocyte reduced, and therefore need to adjust the dose.
6. isoniazid and rifampin, or miconazole (intravenous), ketoconazole increase the risk of liver toxicity, especially liver dysfunction original fast and isoniazid acetylation patients. In addition, isoniazid or rifampicin and miconazole or ketoconazole, after both can reduce blood concentration, so this product and isoniazid should not be combined with imidazole.
7. rifampicin and diazepam (Valium) combined to increase the elimination of the latter, so that the plasma concentration decreased, so the need to adjust the dose.
8. rifampin and isoniazid amine B sulfur can be combined to aggravate the adverse reactions.
9. rifampicin increase levothyroxine degradation in the liver, so the dose of L-thyroxine should be increased when the two combined. Rifampin can increase methadone, mexiletine metabolized in the liver, causing methadone withdrawal symptoms mexiletine plasma concentrations reduced, so after two in combination require dose adjustment. Phenytoin rifampin may increase the metabolism in the liver, so the two combined phenytoin plasma concentrations should be measured and adjust the dosage.
10. probenecid can compete with rifampicin uptake by liver cells, so that increased plasma concentration of rifampicin and produce toxicity. But instability in the role, it is usually not added with probenecid to increase plasma concentrations of rifampicin.
11. rifampin trimethoprim may increase the elimination of increased metabolic xanthine, so eliminate the increase of theophylline.
Ethambutol hydrochloride:
1. isonicotinoyl amine and acetic combined increase adverse reactions.
2. with the use of aluminum hydroxide can reduce the absorption of ethambutol.
3. with neurotoxic drug combination can increase the neurotoxicity of this product, such as optic neuritis or peripheral neuritis.
Isoniazid:
1. while taking isoniazid daily drinking can lead to liver toxicity induced by isoniazid, isoniazid and accelerate metabolism, and therefore need to adjust the dose of isoniazid and closely observe signs of liver toxicity, the patient should be advised Avoid alcoholic beverages while taking this medicine.
2. The aluminum-containing antacids may delay and reduce the absorption of isoniazid after oral administration, the blood concentration reduced, it should be taken to avoid both, or prior to oral antacids for at least 1 hour before taking isoniazid.
3. anticoagulants (such as coumarin or indane diketone derivative) simultaneously with the application of isoniazid, due to inhibition of the enzyme metabolism of anticoagulants, so anticoagulation effects.
4. and cycloserine with taking the central nervous system to increase the side effects (such as dizziness or drowsiness), the need to adjust the dose, and closely observe the signs of central nervous system toxicity, especially in the need for higher working sensitivity patients.
5. rifampin and isoniazid in combination can increase the risk of liver toxicity, and in particular liver dysfunction or fast acetylation of isoniazid, so in the first three months whether the course should be closely followed signs of liver toxicity occurs.
6. isoniazid vitamin B6 antagonists, and increase the amount of vitamin B6 excreted by the kidneys, which may lead to peripheral neuritis, thus increasing requirement of vitamin B6 when combined with isoniazid.
7. When combined with adrenocorticotropic hormone (especially prednisolone), increase isoniazid in liver metabolism and excretion, causing the latter to reduce the plasma concentration affect efficacy in fast acetylation more significant, should appropriate dose adjustment.
8. When combined with alfentanil (alfentanil), due to liver enzyme inhibitors isoniazid, extend alfentanil role; with disulfiram (disulfiram) combined to increase the role of the central nervous system, resulting in dizziness, incoordination, irritability, insomnia; increase combined form of inorganic fluorine nephrotoxic metabolite and enflurane.
9. B sulfur isoniazid or other anti-TB drugs, adverse reactions may increase both. Increase the liver toxicity of this product in combination with other hepatotoxic drugs, and therefore should be avoided.
10. isoniazid not with ketoconazole or miconazole in combination, can reduce both due after the plasma concentration.
11. When combined with phenytoin inhibits the latter in the liver metabolism, which led to increased phenytoin plasma concentrations, it has both an application or combination, phenytoin dose should be adjusted appropriately.
Overdosage
Rifampicin: a gastric lavage, because patients often experience nausea, vomiting, is not appropriate to induce vomiting; give activated charcoal paste after gastric lavage to absorb the remnants of rifampicin in the gastrointestinal tract; severe nausea and vomiting antiemetic agent. 2. Give diuretics promote drug excretion. 3. severe liver dysfunction of 24-48 hours or more may be considered for biliary drainage.
. Isoniazid: 1 to maintain airway patency; 2 using short-acting barbiturate internal preparations and intravenous administration of vitamin B6, vitamin B6 dose of isoniazid with each 1mg 1mg, followed by gastric lavage, gastric lavage should take another. performed within 2-3 hours after smoke hydrazine; 3. Determination of immediate blood gas analysis, dielectric, urea nitrogen, blood sugar; 4 immediate intravenous administration of sodium bicarbonate, correction of metabolic acidosis, repeated administration when necessary; 5. using osmotic diuretics, and continue to apply after the clinical symptoms have improved, promote excretion of isoniazid to prevent recurrence; when 6 severe poisoning patients should be early with blood, ready to do hemodialysis, hemodialysis can not be performed peritoneal dialysis, while combined with a diuretic; 7 to take effective measures to prevent hypoxia, hypotension and aspiration pneumonia.
Pharmacology and Toxicology
Rifampicin: a broad-spectrum antimicrobial effect on Mycobacterium tuberculosis, non-tuberculous mycobacteria, M. leprae, Gram-positive and Gram-negative bacteria have a bactericidal effect.
Ethambutol: growth and reproduction of various states have a role TB, strains resistant to isoniazid and streptomycin resistance is also effective, combination of isoniazid, rifampicin, pyrazinamide can delay and reduce tuberculosis resistant to its effects it produces, with no cross-resistance to other anti-TB drugs.
Isoniazid: Mycobacterium tuberculosis to various growth states have a strong bactericidal effect, is a wholly-potent bactericidal drug, Kansas mycobacteria are also inhibitory effect in a variety of non-tuberculous mycobacteria.
【Pharmacokinetics】
Rifampicin: Good oral absorption, after taking 1.5 to 4 hours of peak plasma concentration. After the adult oral 600mg peak plasma concentration (Cmax) of 7 ~ 9mg / L, 6 months to 5 years old children an oral 10mg / kg, peak plasma concentration (Cmax) of 11mg / L. The goods diffuse systemic absorption of most tissues and body fluids, including cerebrospinal fluid, when there is inflammation of the meninges increase in drug concentration in the cerebrospinal fluid; in saliva can achieve effective therapeutic concentrations; the product can pass through the placenta. The apparent volume of distribution (Vd) is 1.6L / kg. Protein binding rate of 80% to 91%. Medication after eating can reduce by 30% the absorption of drugs, the drug blood elimination half-life (t1 / 2) is 3 to 5 hours, after repeated administration has been shortened, from 2 to 3 hours. This product may be self-induced liver microsomal oxidase action quickly deacetylation, become metabolites have antimicrobial activity deacetylation rifampin, forming inactive metabolites excreted in the urine after hydrolysis. This product is mainly excreted via the bile and gut, may enter the enterohepatic circulation, but its active metabolite deacetylation no enterohepatic circulation. 60% to 65% of the dose through the feces, 6% to 15% of the drug to the prototype, 15% of active metabolites excreted in the urine, 7% places no active 3-formyl derivative discharged. Also excreted through breast milk. Patients with renal dysfunction in this product is no accumulation; because of their role in induction of hepatic microsomal oxidase, taking rifampicin 6 to 10 days after its excretion rate increased; After high doses of biliary excretion due to saturation, the product of excretion may be delayed. Rifampicin not clear by hemodialysis or peritoneal dialysis.
Isoniazid: This product after oral rapidly absorbed from the gastrointestinal tract and distributed in body tissues and fluids, including cerebrospinal fluid, pleural effusion, ascites, skin, muscle, milk and cheese-like tissue. You can cross the placental barrier. Protein binding rate 0 to 10%. Orally 1 to 2 hours up to the peak plasma concentration, but 4 to 6 hours after the plasma concentration of acetylated according to the patient rather than the speed of a fast acetylation, t1 / 2 0.5 to 1.6 hours, slow acetylation of 2 to 5 hours, liver and kidney dysfunction may be extended. Metabolism acetylation mainly in the liver from an inactive metabolites, some of which have liver toxicity. The rate of acetylation is determined by heredity. Liver often slow acetylation N- acetyltransferase enzyme deficiency, acetylation of isoniazid may not be part of the combination. This product is mainly by renal excretion (approximately 70%), discharge within 24 hours, mostly inactive metabolites. Fast acetylation of 93% to acetylation excreted in the urine, slow acetylation of 63%. Fast acetylation of isoniazid 7% in the urine in free or combined form, and slow acetylation was 37%. This product is easy through the blood-brain barrier, can be discharged from the milk, a small amount can be from saliva, sputum and feces. A considerable amount of isoniazid may be hemodialysis and peritoneal dialysis.
Ethambutol: gastrointestinal tract after oral absorption of 75% to 80%. Widely distributed in body tissues and fluids (except cerebrospinal fluid). Within the red blood cell concentration and plasma concentration equal to or for the 2-fold, and sustainable 24 hours; kidneys, lungs, saliva and the urine drug concentration is high inside; however, pleural effusion and ascites in very low concentrations. This product can not penetrate normal meninges, but tuberculous meningitis cerebrospinal fluid of patients may have trace. Its volume of distribution of 1.6L / kg. Protein binding rate of about 20% to 30%. Oral administration of 2 to 4 hours up to the peak plasma concentration, t1 / 2 of 3 to 4 hours, renal dysfunction may be extended to eight hours. Mainly by the liver, about 15% of the dose is metabolized to inactive metabolites. By glomerular filtration and tubular secretion discharge; after administration about 80% within 24 hours of discharge, at least 50% of the prototype excretion, approximately 15% to inactive metabolites. Excreted unchanged in the feces of about 20%. Milk in concentrations approximately equivalent to maternal plasma concentration. A considerable amount of ethambutol can be cleared from the body by hemodialysis and peritoneal dialysis.
[Storage]
Sealed and kept in a cool dark place (dark and not more than 20 ℃) and dry place.
[Packaging]
(1) Blister Packing, 5 / plate; composite bag, 5 boards / bag; carton, 3 bags / boxes.
(2) blister packaging, 10 / plate; composite bag, 5 boards / bag; carton packaging, 2 bags / boxes.
(3) blister packaging, 10 / plate; composite bag, 5 boards / bag; carton, 3 bags / boxes.
(4) blister packaging, 10 / plate; composite bag, 5 boards / bag; carton packaging, 6 bags / box.
[Validity]
12 months.
[Executive standard]
China Food and Drug Administration standards YBH03422014
【Approval Number】
Zhunzi H20080078
【manufacturer】
Company Name: Shenyang Hongqi Pharmaceutical Co., Ltd.
Production Address: Shenyang Hunnan New District envelope Street on the 6th
Postal Code: 110179
Telephone number: 024-23786260 024-23786261
Fax: 024-23786263

 

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