CYCLOSERINUM

General characteristics. Structure:

Active ingredient: Cycloserinum - 250 mg.

Excipients: talc, structure of capsules: dye sunset yellow E110 (ER), dye quinolinic yellow E104 (ER), titanium E171 dioxide (ER), gelatin (ER).

Description. Solid gelatin capsules No. 0 of white color with a lid of orange color. Contents of capsules - white or almost white powder.

Pharmacological properties:

Pharmacodynamics. Cycloserinum is a bactericidal antibiotic of a broad spectrum of activity. Cycloserinum inhibits synthesis of a cellular cover of sensitive strains of gram-positive and gram-negative bacteria and Mycobacterium tuberculosis. It is active concerning gram-negative microorganisms, in concentration of 10-100 mg/l - Rickettsia spp., Treponema spp. MPK in relation to Mycobacterium tuberculosis makes 3-25 mg/l on liquid and 10-20 mg/l and more - on a dense medium. Medicinal stability arises slowly (after 6 months of treatment it is observed in 20-60% of cases).

Pharmacokinetics. Cycloserinum is quickly soaked up from a GIT after intake, reaching the defined concentration in plasma within one hour, is freely distributed in liquids and body tissues. Cycloserinum gets through GEB, concentration in cerebrospinal liquid approximately same, as well as in a blood plasma. Cycloserinum is found in TB patients in a phlegm, and also in pleural and ascitic liquids, in bile, amniotic liquid and in fruit blood, in breast milk, tissues of lungs and in an adenoid tissue. About 66% of a dose of drug are removed with urine in an invariable look within 24 hours. 10% - within the next 48 hours. With a stake are removed in insignificant quantities. About 35% are metabolized, but metabolites are not identified so far. The elimination half-life of Cycloserinum is in limits of 8-12 hours. Cycloserinum gets through a placenta. The abdominal and pleural cavity contains 50-100% of concentration of drug in blood serum. T1/2 at normal function of kidneys - 10 h. At HPN in 2-3 days there can be cumulation phenomena.

Indications to use:

Pulmonary tuberculosis in an active form; extra pulmonary tuberculosis (including a disease of kidneys) on condition of sensitivity of microorganisms to this drug and after inefficient treatment by adequate doses of the main medicines (streptomycin, an isoniazid, rifampicin and Ethambutolum). Drug should be used in combination with other chemotherapeutic means, but not as monotherapy. Atypical bacterial infections (including the caused Mycobacterium avium). Acute infections of the urinary ways caused by sensitive strains of gram-positive and gram-negative bacteria, in particular types of Klebsiella/Enterobacter and Escherichia coli. At treatment of infections of the urinary tract caused by bacteria except for mycobacteria, Cycloserinum is usually effective the same as other antimicrobic drugs. It is necessary to apply Cycloserinum to treatment of these infections only after all usual remedies and when it is established chuvstvitelnostmikroorganizm to this medicine are exhausted.

Route of administration and doses:

Inside, just before meal (at irritation of a mucous membrane of a GIT - after food), the adult - on 0,25 g each 12 h during the first 12 h, then if necessary taking into account portability carefully increase a dose to 250 mg each 6-8 h under control of concentration of drug in blood serum. The maximum daily dose - 1 g. To patients 60 years, and also with body weight less than 50 kg - on 0,25 g 2 times a day are more senior. A daily dose for children - 0,01-0,02 g/kg (it is not higher than 0,75 g/days).

Features of use:

It is possible to warn or reduce toxic action of Cycloserinum, appointing during treatment glutaminic acid on 0,5 g 3-4 times a day (to food), and daily administration of the ATP sodium salt in oil (1 ml of 1% of solution), a pyridoxine of 200-300 mg/days. It is necessary to limit the mental tension of patients and to exclude possible factors of an overheat (stay to the bare-headed sun, a hot shower). Due to the bystry development of stability at monotherapy by Cycloserinum recommends its combination to other antitubercular drugs. Influence on ability of driving of the car and use of mechanisms. It is not established.

Side effects:

The majority of the side effects observed during treatment by Cycloserinum was connected with a nervous system or was manifestations of hypersensitivity to drug. From a nervous system (in connection with high doses of drug (more than 500 mg a day)): spasms, drowsiness, sleeplessness, dreadful dreams, semiconscious condition, headache, tremor, dysarthtia, dizziness, confusion of thoughts and disturbance of the orientation which is followed by memory loss, uneasiness, peripheral neuritis, psychoses character change, euphoria, a depression, an acrimony, aggression, paresis, a hyperreflexia, paresthesia, big and small attacks of clonic spasms and a lump is possible with suicide attempts. From the alimentary system: nausea, heartburn, diarrhea. Allergic reactions, an itch, megaloblastny anemia and increase in aminotransferases in serum, in particular at elderly patients with earlier existing liver diseases belong to other established side effects. Sudden development of congestive heart failure in the patients accepting from 1 to 1,5 g of Cycloserinum a day was noted. Other: fever, strengthening of cough.

Contraindications:

Hypersensitivity to Cycloserinum;

Epilepsy, epileptic seizures (including in the anamnesis);

 Depression;

The expressed conditions of excitement or psychosis;

Heart failure;

Heavy renal failure;

Alcohol abuse;

Children's age up to 3 years.

Overdose:

At overdose the symptomatic treatment is recommended. Interaction with other medicines. Cycloserinum increases the speed of removal of a pyridoxine kidneys (can cause development of anemia and peripheral neuritis that demands increase in a dose of a pyridoxine). Alcohol and Cycloserinum are incompatible, in particular at treatment by high doses of Cycloserinum. Alcohol increases an opportunity and danger of epileptic seizures. The patients receiving Cycloserinum and an isoniazid have to be under control concerning symptoms of poisoning of TsNS, for example, of dizziness and drowsiness as these drugs have the combined toxic effect on TsNS. Etioniamidum increases risk of emergence of side effects from TsNS, especially convulsive syndrome.

Storage conditions:

List B. In the dry, protected from light place, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

Capsules of 250 mg. On 100 capsules in a bottle from polyethylene of high density with the screwed cover (with the image of the schematical drawing - instructions for opening of a bottle) supplied with protection of the first opening in the form of a ring and an induction zapayky foil. On 1 bottle together with the application instruction in a pack from a cardboard.