Cycloserinum

General characteristics. Structure:

Active ingredient: 250 mg of Cycloserinum.

Bactericidal antibiotic of a broad spectrum of activity, with the expressed activity against mycobacteria.

Pharmacological properties:

Pharmacodynamics. Breaks synthesis of a cell wall, working as the competitive antagonist of D-alanine, suppresses the enzymes responsible for synthesis of a cell wall.

Cycloserinum possesses a wide range of antibacterial action: inhibits synthesis of a cell wall of sensitive strains of gram-positive and gram-negative bacteria. Growth of mycobacteria of tuberculosis detains (Mycobacterium avium is active concerning Mycobacterium tuberculosis). On activity concedes to streptomycin, an isoniazid and Ftivazidum, but works on tuberculosis mycobacteria, steady against these drugs and p-aminosalicylic acid.

Medicinal stability arises slowly (after 6 months of treatment develops in 20-60% of cases).

Pharmacokinetics. Cycloserinum is quickly soaked up from digestive tract. Well breast milk, bile, a phlegm, lymphatic fabric, lungs, ascitic and synovial liquids, a pleural exudate gets into liquids and body tissues, including cerebrospinal fluid, passes through a placenta. At a chronic renal failure 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 digestive tract - after food).

Adults. The initial dose for adults most often makes 250 mg twice a day from 12 an hour interval within the first two weeks. The usual dose makes from 500 mg to 1 g a day for several receptions, under control of level of drug in blood. The daily dose should not exceed 1 g (4 capsules).

Children. The usual initial dose makes from 10 mg/kg of weight bodies/days for several receptions then it changes depending on drug level in blood and therapeutic effect. The daily dose should not exceed 750 mg (3 capsules).

Elderly. To patients 60 years, and also with body weight less than 50 kg - on 250 mg 2 times a day are more senior.

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.

During treatment it is necessary to control function of kidneys (concentration of creatinine and an urea nitrogen in blood), a liver, hematologic indicators and concentration of Cycloserinum in blood (should not exceed 30 mkg/ml). 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 medicines. It is necessary to stop treatment or to lower a dose at development of allergic dermatitis or symptoms of toxicity from the central nervous system, such as spasms, psychosis, drowsiness, depression, confusion of consciousness, hyperreflexia, headache, tremor, вертиго, paresis or a dysarthtia. The risk of development of spasms increases at an alcoholism.

In certain cases use of Cycloserinum and other antitubercular drugs can cause development of insufficiency of B12 vitamin and/or folic acid in an organism, 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.

Influence on ability to driving of motor transport and to control of potentially dangerous mechanisms: for treatment it is necessary to be careful when driving and potentially dangerous to mechanisms because of possible emergence of dizziness, drowsiness, decrease in memory.

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 the alimentary system: nausea, heartburn, diarrhea.

From cardiovascular system: an exacerbation of chronic heart failure at reception of 1 - 1,5 g a day.

Allergic reactions: skin rash, itch.

Others: fever, strengthening of cough, megaloblastny anemia, increase in level of aminotransferases of a liver.

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 the central nervous system, especially convulsive syndrome.

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

Contraindications:

Hypersensitivity, organic diseases of the central nervous system, epilepsy, epileptic seizures (including in the anamnesis), disturbances of mentality (uneasiness, psychosis, a depression, including in the anamnesis), chronic heart failure, a chronic renal failure (clearance of creatinine less than 50 ml/min.), alcoholism, pregnancy, the lactation period.

With care: children's age.

Overdose:

The overdose is observed at concentration of Cycloserinum in plasma of 25-30 mg/ml - reception of high doses, disturbance 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 medicines. For prevention of neurotoxic effects enter a pyridoxine in a dose of 200-300 mg/days, anticonvulsant and sedatives.

Issue conditions:

According to the recipe

Packaging:

Capsules of 250 mg in a blister strip packaging No. 10х3.