Universal reference book for medicines
Product name: MAIZER (MYZER)

Active ingredient: cycloserine

Type: Anti-TB drug

Manufacturer: PANACEA BIOTEC (India)
Composition, form of production and packaging
Capsules
1 caps.

cycloserine 250 mg

10 pieces.
- Packings without cell contour (10) - packs cardboard.
10 pieces.
- Packings without glue contour (3) - packs cardboard.
10 pieces.
- Packings without cell contour (5) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2010.

PHARMACHOLOGIC EFFECT

Anti-tuberculosis drug.
Cycloserin is a broad-spectrum bactericidal antibiotic. Cycloserin inhibits the synthesis of the cell membrane of sensitive strains of Gram-positive and Gram-negative bacteria and Mycobacterium tuberculosis. It is active against gram-negative microorganisms, in the concentration of 10-100 mg / l - Rickettsia spp., Treponema spp., The minimal suppressing concentration in relation to Mycobacterium tuberculosis is 3-25 mg / l in liquid and 10-20 mg / l and more - on a dense nutrient medium. Drug resistance is slow.
PHARMACOKINETICS

Cycloserin is rapidly absorbed from the digestive tract after ingestion, creating detectable levels of drug concentration in the plasma for one hour, absorption of 70-90%.
Virtually does not bind to plasma proteins. The time to reach C max in the blood is 3-4 h; Proportionally accepted dose 0.25, 0.5 and 1.0 g C max is 6.24 and 30 μg / l, respectively. After taking 250 mg every 12 hours C max 25-30 μg / ml. It is distributed loosely to fluids and body tissues.
Cycloserine penetrates the blood-brain barrier, levels in the cerebrospinal fluid are about the same as in plasma.
In patients with tuberculosis, Cycloserin is found in sputum, as well as in pleural and lecithic fluids, in bile, in amniotic fluid and in fetal blood, in breast milk, lung tissue and in lymphoid tissue.
Cycloserine is excreted in the urine, in which it is detected 30 minutes after the dose.
About 66% of the dose is found unchanged in the urine within 24 hours. The other 10% are excreted within the next 48 hours. Minor amounts are excreted with feces. About 35% is metabolized, but metabolites have not been identified to date. T1/2 cycloserine fluctuates within 8-12 hours.
Cycloserine passes through the placenta.
In the abdominal and pleural cavity contains 50-100% of the concentration of the drug in the blood serum. With chronic renal failure, after 2-3 days, cumulation phenomena may occur.
INDICATIONS

- treatment of pulmonary tuberculosis in active form;

- treatment of extrapulmonary tuberculosis (including kidney disease), provided that microorganisms are sensitive to this drug and after an unsuccessful adequate treatment with the main drugs (streptomycin, isoniazid, rifampicin and ethambutol);

Like all antituberculosis drugs, cycloserine should be used in combination with other chemotherapeutic agents, and not as monotherapy.

- is also used for atypical bacterial infections (including those caused by Mycobacterium avium);

- can be effective for the treatment of acute urinary tract infections caused by sensitive strains of Gram-positive and Gram-negative bacteria, especially Klebsiella / 'Enterobacter and Escherichia coli species;

- treatment of urinary tract infections caused by bacteria, except for mycobacteria.

Use Cycloserin for the treatment of these infections should only after all conventional means of treatment have been exhausted and when the sensitivity of the microorganisms to this drug has been determined.

DOSING MODE

Cycloserine is administered orally, immediately before meals (with irritation of the gastrointestinal mucosa after eating).

Adults .
The usual dose is from 500 mg to 1 g / day. The initial dose for adults is often 250 mg 2 times / day with a 12-hour interval during the first two weeks.Periodically (after several receptions, the level of the drug in the blood is controlled). The daily dose should not exceed 1 g.
Children .
The usual initial dose is from 10 mg / kg of body weight / day, after which it varies depending on the level of the drug in the blood and the therapeutic effect. The daily dose for children is 0.01-0.02 g / kg of body weight (not more than 0.75 g / day).
The elderly .
It is prescribed as well as for adults , but the dose is reduced in case of impaired renal function . Patients older than 60 years, and also with a body weight of less than 50 kg - 0.25 g 2 times / day.
SIDE EFFECT

From the side of the central nervous system: associated with high doses of the drug, i.e.
more than 500 mg per day: convulsions, drowsiness, sleeplessness, nightmares, co-morbid state, headache, tremor, dysarthria, dizziness, confusion and disorientation accompanied by memory loss, anxiety, peripheral neuritis, psychoses, possibly with suicide attempts, changes character, euphoria, depression, increased irritability, aggressiveness, paresis, hyperreflexia, parasthesia, large and small seizures of clonic convulsions and coma.
From the digestive system: nausea, heartburn, diarrhea.

Other: fever, increased cough.

Other established side effects include: allergic reactions, pruritus, megaloblastic anemia and an increase in aminotransferases in the serum, especially in elderly patients with pre-existing liver disease.
Perhaps sudden development of congestive heart failure in patients taking 1 to 1.5 g of cycloserine / day.
CONTRAINDICATIONS

- organic diseases of the central nervous system;

- epilepsy, epileptic seizures (including in the anamnesis);

- Depression;

- marked excitement or psychosis;

- heart failure;

- severe renal insufficiency;

- Abuse of alcohol (including in the anamnesis);

- Pregnancy;

- lactation period;

- Hypersensitivity to cycloserine.

With caution, prescribe Cycloserin in childhood.

PREGNANCY AND LACTATION

It is not established whether cycloserine causes fetal damage when administered to pregnant women or whether it affects reproductive capacity.
Cycloserine should be given to pregnant women only in cases of extreme necessity.
Concentrations in human milk approach the concentrations found in the mother's blood serum.
The decision on the abolition of breastfeeding or the cessation of drug treatment should be taken taking into account the value of treatment with the drug for the mother.
APPLICATION FOR FUNCTIONS OF THE LIVER

Contraindicated:

- severe renal failure.

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 poisoning, the level of the drug in the blood should be monitored at least once a week.
The dose should be adjusted in such a way as to maintain the level of the drug in the blood below 30 mg / ml.
APPLICATION FOR CHILDREN

With caution is prescribed in childhood.

The usual initial dose is from 10 mg / kg of body weight / day, after which it varies depending on the level of the drug in the blood and the therapeutic effect.
The daily dose for children is 0.01-0.02 g / kg of body weight (not more than 0.75 g / day).
APPLICATION IN ELDERLY PATIENTS

It is prescribed as well as for adults, but the dose is reduced in case of impaired renal function.
Patients older than 60 years, and also with a body weight of less than 50 kg - 0.25 g 2 times / day.
SPECIAL INSTRUCTIONS

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

Neurotoxic effect is usually observed at drug levels in the blood of more than 30 mg / ml (which may be the result of an overdose or impaired creatinine clearance).The danger of developing convulsive syndrome increases in patients with chronic alcoholism.
When taking the drug should be monitored hematological indicators, excretory function of the kidneys, the level of the drug in the blood and the state of liver function.
Before starting treatment with cycloserine, it is necessary to isolate cultures of microorganisms and determine the sensitivity of strains to this preparation.
In the case of tuberculosis infection, it is necessary to determine the sensitivity of the strain to other anti-tuberculosis drugs.
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 poisoning, the level of the drug in the blood should be monitored at least once a week.
The dose should be adjusted in such a way as to maintain the level of the drug in the blood below 30 mg / ml.
Anticonvulsants or sedatives can be effective in preventing neurotoxic reactions.

Patients who receive more than 500 mg of cycloserine per day should be directly monitored because of the possible development of such symptoms.
The importance of pyridoxine in the prevention of neurotoxic reactions has not been established.
In rare cases, the use of cycloserine and other anti-tuberculosis drugs can cause the development of vitamin B deficiency and / or folic acid, megaloblastic and sideroblastic 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 0.5 g 3-4 times / day (before meals) during the treatment period, and daily iv injection with sodium salt ATP (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).

In connection with the rapid development of resistance with monotherapy with cycloserine, it is recommended that it be combined with other anti-tuberculosis drugs.

Impact on the ability to drive vehicles and manage mechanisms

Not installed.

OVERDOSE

Symptoms: Acute poisoning can occur if the adult patient has taken inside more than 1 g. Overdose phenomena can occur with a plasma cycloserine concentration of 25-30 mg / ml (high doses if daily more than 500 mg of cycloserine is injected into the body, a violation of creatinine clearance ).
Usually, toxic effects occur from the side of the central nervous system. They may include headache, dizziness, a semi-unconscious condition, confusion, increased irritability, paresthesia, dysarthria and psychosis. At the use of high doses paresis, convulsions and coma can be observed. Ethanol may increase the risk of epileptic seizures.
Treatment: Symptomatic and supportive treatment is recommended.
Antiepileptic means. For the prevention of neurotoxic effects, anticonvulsants and sedatives.Activated charcoal may be more effective in reducing absorption of the drug than causing vomiting and gastric lavage. In adults, neurotoxic effects can be treated and prevented by the administration of 200-300 mg of pyridoxine / day. Conducting hemodialysis removes Cycloserin from the blood, but does not exclude the development of poisoning life-threatening.
DRUG INTERACTION

Cycloserin increases the rate of excretion of pyridoxine by the kidneys (can 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.

Alcohol and cycloserine are incompatible, especially when treated with high doses of cycloserine.
Alcohol increases the possibility and danger of epileptic seizures.
Patients receiving cycloserine and isoniazid should be monitored because these drugs have a combined toxic effect on the CNS.
A dose adjustment may be required.
Ethionamide increases the risk of side effects from the central nervous system, especially convulsive syndrome.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

Keep the drug out of the reach of children at a temperature of no higher than 25 ° C.

Shelf life - 2 years.

Do not use after the date shown on the package.

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