Maiser - instructions for use, doses, side effects, contraindications

Composition of gelatin capsule: [gelatin (capsule cap 83.432% / capsule body 83.160%), purified water (capsule cap 14.3% / capsule body 14.3%), dye azorubin (capsules lid 0.112%), dye crimson [Ponso 4R] (capsule cap 0.384%), dye sunset yellow (capsule capsule 0.072%), titanium dioxide (capsule cap 1,400% / capsule body 2,240%),povidone (0.1 capsule capsule capsule 0.100% capsule), bronopol (capsule cap 0,100% / capsule body 0,100%), sodium lauryl sulfate (capsule cap 0,100% / capsule body 0,100%)] - 76,0 mg.

Description:

Hard gelatin capsules No. 1 with a red lid and a white casing. The contents of the capsules are almost white or white with a yellowish tinge of granular powder.

Pharmacotherapeutic group:Antibiotic

ATX: & nbsp

J.04.A.B Antibiotics

J.04.A.B.01 Cycloserine

Pharmacodynamics:Cycloserine is a broad-spectrum bactericidal antibiotic. Cycloserine violates the synthesis of the cell wall, acting as a competitive antagonist of D-alanine, suppresses the enzymes responsible for the synthesis of the cell wall of sensitive strains of gram-positive and gram-negative bacteria. Retards the growth of mycobacterium tuberculosis (active against Mycobacterium tuberculosis, Mycobacterium avium).It is active against gram-negative microorganisms in a concentration of 10-100 mg / l - Rickettsia spp., Treponema spp., the minimum inhibitory concentration in relation to M. tuberculosis is 3-25 mg / l on liquid and 10-20 mg / l and more - on a dense nutrient medium. Drug resistance appears slowly (after 6 months of treatment it develops in 20-60% of cases).

Pharmacokinetics:

After oral administration, quickly and almost completely (70-90%) is absorbed from the gastrointestinal tract. Time to reach the maximum concentration (C_max) in blood plasma - 3-4 hours Proportionally accepted dose of 0.25 g, 0.5 g, 1 g of C_max in blood plasma is 6.24 μg / ml and 30 μg / ml, respectively. After taking 250 mg every 12 hours C_max is 25-30 μg / ml.

It penetrates well into body fluids and tissues, including cerebrospinal fluid, breast milk, bile, sputum, lymphatic tissue, lungs, ascites and synovial fluid, pleural effusion, passes through the placenta. In the abdominal and pleural cavity contains 50-100% of the concentration of the drug in the blood serum. Virtually does not bind to plasma proteins. Half-life with normal kidney function is 10 hours. It is excreted by glomerular filtration in unchanged form: 50% after 12 hours, 65-70% within 24-72 hours, small amounts through the gastrointestinal tract. With chronic renal failure, after 2-3 days, cumulation phenomena may occur.

Indications:

Treatment of the active form of pulmonary tuberculosis and extrapulmonary form of tuberculosis (including kidney damage) in the case of sensitivity of microorganisms to the drug and after an unsuccessful adequate treatment with basic medicinesstreptomycin, isoniazid, rifampicin, ethambutol), only in combination with other antituberculosis drugs; chronic forms of tuberculosis.

The combination of tuberculosis with acute urinary tract infections caused by sensitive strains of gram-positive and gram-negative bacteria, in particular Klebsiella spp., Enterobacter spp., Escherichia coli with ineffectiveness of essential medicines. Use cycloserine for the treatment of these infections should only after all the usual means for treatment have been exhausted and the sensitivity of the microorganisms to it has been determined.

Atypical mycobacterial infections (including those caused by Mycobacterium avium), urinary tract infections.

Contraindications:

Hypersensitivity to cycloserine or any other component of the drug, organic diseases of the central nervous system, epilepsy, epileptic seizures (including in the anamnesis), mental disorders (anxiety, psychosis, depression, including in history), chronic heart failure , chronic renal failure (creatinine clearance less than 25 ml / min), alcoholism, pregnancy, lactation, children under 3 years.

Carefully:

Children's age (from 3 to 18 years), chronic renal failure (creatinine clearance greater than 25 mL / min).

Pregnancy and lactation:

Application during pregnancy: not set whether causes cycloserine damage to the fetus when used in pregnant women. Cycloserine should be given to pregnant women only in cases of extreme necessity.

Application in the period of breastfeeding: concentrations in human milk are close to the concentrations found in the mother's blood serum. The decision to abort breastfeeding or to stop treatment with the drug should be taken in consideration of the value of treatment with the drug for the mother.

Dosing and Administration:

Inside, immediately before meals (with irritation of the mucous membrane of the gastrointestinal tract - after eating).

Adults: The usual dose is from 500 mg to 1 g per day. The initial dose for adults is often 250 mg 2 times a day with 12-hour intervals for the first two weeks, then, if necessary, taking into account the tolerance dose carefully increased to 250 mg every 6-8 hours under control serum concentration of the drug.The daily dose should not exceed 1 g.

Children (over 3 years old): the usual dose of cycloserine is from 10 mg / kg of body weight per day in 2-3 doses, after which it varies depending on the concentration of the drug in the blood and the therapeutic effect. A large dose is given only in the acute phase of the tuberculosis process or with insufficient effectiveness of smaller doses. The daily dose for children should not exceed 750 mg.

Adults: patients older than 60 years, as well as with a body weight of less than 50 kg, the drug is prescribed 250 mg twice a day.

Side effects:

Most side effects observed during treatment with cycloserine are associated with impaired central nervous system function, the use of high doses of the drug (more than 500 mg / day) or is a manifestation of hypersensitivity to the drug.

Allergic reactions: skin rash, itching.

From the central nervous system: epileptic convulsions, drowsiness, insomnia, sopor, headache, tremor, dysarthria, dizziness, confusion and disorientation accompanied by loss of memory; anxiety, peripheral neuritis, psychosis, possibly with suicide attempts,changes in character, euphoria, depression, increased irritability, aggressiveness, paresis, hyperreflexia, paresthesia, large and small seizures of clonic convulsions and coma.

From the digestive system: nausea, heartburn, diarrhea, especially in elderly people with pre-existing liver disease.

From the hematopoiesis: megaloblastic and sideroblastic anemia.

From the cardiovascular system: exacerbation of chronic heart failure in patients (at doses of 1000-1500 mg / day).

Laboratory indicators: increased activity of liver aminotransferases.

Other: fever, coughing.

Overdose:

Symptoms. Acute overdose can occur with cycloserine at a dose of more than 1 g. Overdose phenomena can occur with a plasma cycloserine concentration of 25-30 mg / ml (high doses if daily 500 mg of cycloserine is injected into the body, impaired renal clearance).

Usually, toxic effects occur from the central nervous system. They can include headache, dizziness, confusion, increased irritability, paresthesia, dysarthria and psychosis.When high doses are used, paresis, convulsions and coma may occur. Ethanol may increase the risk of epileptic seizures.

Treatment. It is recommended that symptomatic and supportive treatment be provided. With cramps - antiepileptic drugs. For the prevention of neurotoxic effects are introduced pyridoxine in a dose of 200-300 mg / day, preparations of benzodiazepine series (diazepam), nootropic drugs (piracetam, glutamic acid). Activated carbon may be more effective in reducing absorption than induction of vomiting and gastric lavage. Carrying out of a hemodialysis deduces cycloserine from the blood, but does not exclude the development of life-threatening intoxication.

Interaction:

Cycloserine promotes a decrease in resistance to isoniazid, streptomycin and paraaminosalicylic acid (PASC). Patients receiving cycloserine and isoniazid, should be controlled, as these drugs have a combined toxic effect on the central nervous system.

Increases the rate of excretion of pyridoxine by the kidneys (may cause the development of anemia and peripheral neuritis, an increase in the dose of pyridoxine is required).

Simultaneous administration of ethionamide potentiates neurotoxic side effects, increases the risk of side effects from the central nervous system, especially convulsive syndrome.

Ethanol increases the risk of epileptic seizures.

Special instructions:

Before starting treatment with cycloserine, isolate cultures of microorganisms and determine the sensitivity of strains to cycloserine. Patients who receive more than 500 mg of cycloserine per day should be under the direct supervision of a doctor because of the possible development of side effects from the central nervous system.

Treatment with cycloserine should be canceled or the dose should be reduced if the patient develops allergic dermatitis or symptoms of intoxication of the central nervous system, for example: convulsions, psychosis, drowsiness, oppression or confusion, hyperreflexia, headache, tremor, dizziness, paresis or dysarthria.

The risk of developing convulsive syndrome increases in patients with chronic alcoholism, so the use of cycloserine in this condition is contraindicated.Anticonvulsants or sedatives can be effective in preventing neurotoxic reactions, for example: seizures, arousal or tremor.

When taking the drug should be monitored hematological indicators, excretory function of the kidneys, the concentration of cycloserine in the blood and the state of liver function. The concentration of cycloserine in the blood should not exceed 30 mg / l.

In the treatment of patients with reduced renal function, taking a daily dose of more than 500 mg and who are suspected to have signs and symptoms of an overdose, the level of the drug in the blood should be monitored at least once a week. The dose needs to be adjusted in such a way as to maintain the level of the drug in the blood below 30 mg / l. Such patients should be under the direct supervision of a doctor because of the possible development of symptoms of toxicity.

In some cases, the use of cycloserine and other anti-tuberculosis drugs can cause a deficiency of cyanocobalamin (vitamin B₁₂) and folic acid in the body, the development of megaloblastic anemia. In case of anemia during treatment, it is necessary to conduct an appropriate examination and treatment of the patient.It is possible to prevent or reduce the toxic effect of cycloserine by prescribing glutamic acid 500 mg 3-4 times daily (before meals) during the treatment period, and daily intramuscular administration of sodium salt of adenosine triphosphate (1 ml of 1% solution), pyridoxine 200-300 mg / day.

It is necessary to limit the mental tension of patients and exclude possible factors of overheating (exposure to the sun with an uncovered head, hot shower).

Effect on the ability to drive transp. cf. and fur:

During treatment with cycloserine, it is necessary to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Capsules, 250 mg.

Packaging:

For 40 or 100 capsules per bottle of high-density polyethylene with a screw cap made of polypropylene with embedded moisture absorber (1 or 2 bags of silica gel) and cotton wool. The neck of the bottle is additionally tightened with aluminum foil. The bottle together with the instruction for use is placed in a cardboard box. *

10 capsules per strip of aluminum foil. 10 strips together with instructions for use are placed in a cardboard box. **

Specify the release form:

* - for production at the site located at Malpur, Buddy, Solan Dist. (H.P.) - 173205, India.

** - in production at the site located at B-1 / E-12, Mohan Koop. Ind. Estate, Mathura Road, New Delhi, 110044, India.

Storage conditions:

In dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N014870 / 01

Date of registration:25.03.2009 / 05.11.2015

Expiration Date:Unlimited

The owner of the registration certificate:Panacea Biotech Co., Ltd.Panacea Biotech Co., Ltd. India

Manufacturer: & nbsp

PANACEA BIOTEC, Ltd. India

Representation: & nbspKORAL-MED, CJSCKORAL-MED, CJSC

Information update date: & nbsp25.03.2018

Illustrated instructions

Instructions

Maiser (Myser)