Cycloserinum

General characteristics. Structure:

Active ingredient: 250 mg of Cycloserinum (in terms of active agent).

Excipients: magnesium stearate, silicon dioxide colloid, calcium phosphate, talc.

The cover of the capsule contains: titanium dioxide, dye crimson Ponso 4R, dye quinoline yellow, gelatin, water.

Antibiotic of a broad spectrum of activity.

Pharmacological properties:

Pharmacodynamics. Works bacteriostatically or bakteritsidno depending on concentration in the center of an inflammation and sensitivity of microorganisms.

Breaks synthesis of a cell wall, working as the competitive antagonist of D-alanine. Suppresses activity of the enzymes responsible for synthesis of a cell wall. 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 develops in 20-60% of cases).

Pharmacokinetics. Absorption after oral administration - 70-90%. Practically does not contact proteins of plasma.

TCmax is 3-4 h; in proportion to the accepted dose 0,25; 0,5 and 1 g of Cmax make 6, 24 and 30 mkg/l respectively. After reception of 250 mg each 12 h Cmax - 25-30 mkg/ml.

Well breast milk, bile, a phlegm, lymphatic fabric, lungs, ascitic and synovial liquids, a pleural exudate gets into liquids and body tissues, including SMZh, passes through a placenta. Belly and pleural cavities contain 50-100% of concentration of drug in blood serum.

About 35% of the entered dose are metabolized. T ½ at normal function of kidneys are 10 h. It is removed by glomerular filtering in not changed look: 50% in 12 h, 65-70% within 24-72 h, small amounts - with a fecal masses. At HPN in 2-3 days there can be cumulation phenomena.

Indications to use:

Tuberculosis (chronic forms, reserve drug, as a part of a combination therapy).

Atypical mikobakterialny infections (including the caused Mycobacterium avium), infections of urinary tract.

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:

Before therapy it is necessary to mark out with Cycloserinum cultures of microorganisms and to define sensitivity of strains to this drug. In case of a tuberculosis infection it is necessary to define sensitivity of a strain to other antitubercular drugs.

Treatment by Cycloserinum needs to be cancelled or it is necessary to reduce a dose if at the patient allergic dermatitis or symptoms of damage of the central nervous system develop, namely: headache, dizziness, drowsiness, confusion of consciousness, tremor, peripheral paresis, dysarthtia, spasms and psychosis. In view of a low therapeutic index of Cycloserinum danger of development of spasms increases at patients with an alcoholism.

Poisoning is usually observed at concentration of drug in blood more than 30 mg/l that can be result of overdose or the broken clearance of kidneys. At administration of drug it is necessary to control hematologic indicators, function of kidneys (concentration of creatinine and an urea nitrogen in blood), concentration of drug in blood and function of a liver.

At treatment of patients with reduced function of the kidneys accepting a daily dose more than 500 mg and in which presumably signs and symptoms of overdose are found drug level in blood needs to be controlled, at least, once a week. The dose needs to be adjusted so that to support drug level in blood lower than 30 mg/l. For prevention of symptoms of damage of the central nervous system, in particular, of spasms, conditions of excitement or a tremor, use of anticonvulsant or sedative drugs is possible. The patients receiving more than 500 mg of Cycloserinum a day have to be under direct observation of the doctor because of possible development of similar symptoms. It is possible to warn or reduce toxic action of Cycloserinum, appointing during treatment glutaminic acid on 500 mg 3-4 times a day (to food), and daily administration of the ATP sodium salt in oil (1 ml of 1% of solution), and also a pyridoxine in a dose of 200-300 mg/days. For prevention of side neurotoxic effects appoint psychotropic drugs of a benzodiazepine row diazepam (5 mg) or Phenazepamum (1 mg) to night, and also piracetam in a dose of 800 mg 2 times a day.

In certain cases use of Cycloserinum can cause development of insufficiency of B12 vitamin and/or folic acid, megaloblastny and sideroblastny anemias. In case of developing of anemia during treatment it is necessary to conduct the corresponding examination and treatment of the patient.

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 HP.

Influence of reception of Cycloserinum on ability of driving of the car and use of mechanisms is not established.

Use at pregnancy and in the period of a lactation. It is applied only in cases of the vital need.

Side effects:

From a nervous system: headache, dizziness, sleeplessness or drowsiness, "dreadful" dreams, uneasiness, irritability, decrease in memory, paresthesia, peripheral neuritis, tremor, euphoria, depression, suicide mood, psychosis, epileptiform spasms.

From cardiovascular system: an exacerbation of chronic heart failure at the patients accepting from 1 to 1,5 g of Cycloserinum a day.

From the alimentary system: nausea, heartburn, diarrhea.

Allergic reactions (skin rash, itch), megaloblastny anemia and increase in level of aminotransferases of a liver, nausea, heartburn, diarrhea in particular at elderly patients with earlier existing liver diseases.

Others: fever, strengthening of cough.

Interaction with other medicines:

Increases the speed of removal of a pyridoxine kidneys (can cause development of anemia and peripheral neuritis, increase in a dose of a pyridoxine is required).

Ethanol increases risk of development of epileptic seizures, especially at the persons suffering from an alcoholism.

Etioniamidum increases risk of emergence of side effects from TsNS, especially convulsive syndrome.

The isoniazid increases the frequency of developing of dizziness, drowsiness.

Contraindications:

Hypersensitivity, organic diseases of TsNS, epilepsy, epileptic seizures (including in the anamnesis), disturbances of mentality (uneasiness, psychosis, a depression, including in the anamnesis), HSN, HPN (clearance of creatinine less than 50 ml/min.), alcoholism.

With care. Children's age.

Overdose:

The overdose is observed at concentration of Cycloserinum in plasma of 25-30 mg/ml as a result of reception of Cycloserinum in high doses and/or disturbances of renal clearance.

Acute poisoning can arise at intake more than 1 g/days. Symptoms of chronic intoxication at long reception in a dose more than 500 mg/days: headache, dizziness, confusion of consciousness, acrimony, paresthesias, psychosis, dysarthtia, paresis, spasms, coma.

Treatment: symptomatic, absorbent carbon, antiepileptic HP. For prevention of neurotoxic effects enter a pyridoxine in a dose of 200-300 mg/days, anticonvulsant and sedative HP.

Storage conditions:

List B. To store in the dry, protected from light place, at a temperature not above 25 °C. To store in the places unavailable to children. Not to use after a period of validity. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

Capsules on 250 mg. On 10 capsules in the AL/PVH blister. On 1, 5, 10 blisters in a cardboard pack together with the application instruction.