Directory of medicines. Instructions for medical use

Cycloserine belongs to the group reserve antibiotics. Its use is characterized by the slow development of drug resistance.

The active substance of the drug is cycloserine. Auxiliary elements include:

• colloidal silicon dioxide;
• talc;
• stearic acid in combination with magnesium salt;
• calcium phosphate.

The formation of the active substance occurs during the life of certain types of actinomycetes. The principle of the bactericidal action of the drug is based on changes in the synthesis of peptidoglycan in the bacterial cell. The structural formula of the drug is as follows - C 3 H 6 N 2 O 2.

Mechanism of action of Cycloserine

Cycloserine penetrates into bacterial cells and destroys them from the inside. It effectively eliminates the inflammatory process. Shows the greatest activity in relation to gram-negative bacteria. Used to treat chronic tuberculosis. It works effectively even when other drugs fail. Combination with second-line anti-tuberculosis drugs is possible.

Plasma protein binding is low. The maximum percentage of active substance concentration is achieved in 240 minutes after reception.

The drug is able to penetrate body fluids. The main amount is in the pleural cavity, the rest is concentrated in sputum, bile and breast milk. The half-life is 10 hours. The drug is excreted by the kidneys.

An overdose of the drug is a dangerous condition for health and life. The maximum daily dose is 500 mg. When an excess amount of Cycloserine enters the body, psychosis develops, headaches and confusion appear, and convulsions occur. It is possible to fall into a coma. To eliminate the symptoms of overdose use sorbents, pyridoxine and antiepileptic drugs.

Important! In case of chronic renal failure, the drug is taken with caution. During treatment, it is advisable to monitor the condition of the kidneys.

Release forms

The medicine is produced in the format of capsules and tablets. Capsules are sold in packages 10 and 30 pieces. One blister contains 10 capsules. One capsule includes 250 grams active substance. Tablets are produced according to 1200, 700, 50, 40, 30 and 10 pieces. The concentration of Cycloserine in one tablet is 250 grams.

Tradename

In pharmacies, Cycloserine is found under the following trade names:

• Mycloserine;
• Serocycline;
• Duplocycline;
• Oksamycin;
• Tebemycin;
• Gloxin.

Manufacturers

Cycloserine is produced in the following countries: Russia, China, India, UK, Switzerland and South Korea. The drug is produced by the following companies:

• "Pharmasintez" (Russia);
• "Atoll" (Russia);
• "Routek Ltd" (Great Britain);
• "Promed Exports Pvt. Ltd" (India);
• “Jinzhou Jizhong Amino Acid Co. Ltd. (China);
• Dong-A Pharmaceutical Co. Ltd. (South Korea);
• "Eli Lili Vostok S.A" (Switzerland).

The drug is dispensed from pharmacies with a prescription from a doctor.

Photo 1. Cycloserine capsules, 250 mg, manufacturer - The Chao Center.

In what cases is it used?

Cycloserine is used for infectious diseases. It is used as part of complex therapy and as an independent remedy. The instructions indicate the following indications for use:

• infectious pathologies of the excretory system;
• tuberculosis;
• infectious diseases caused by yellow bacilli.

At the initial stage of tuberculosis, the drug is not used. During this period, drugs with less effectiveness are used. Cycloserine is prescribed for recurrent stage diseases in combination with other anti-tuberculosis drugs. At this stage, the symptoms of the disease become more pronounced. People with weakened immune systems and untreated tuberculosis are at risk.

Cycloserine helps with chronic tuberculosis. The course of therapy is long. In some cases it can reach 14 months. Compliance with the prescribed treatment regimen will ensure the prevention of complications in the future.

Attention! You cannot combine Cycloserine with alcohol and sour fruit juices. Otherwise, the effect of the drug neutralized.

Analogues and effectiveness

Cycloserine belongs to the group of potent drugs. Its effectiveness in the fight against tuberculosis has been proven by many years of experience in use in medicine.

The drug eliminates not only the symptoms of the disease, but also foci of inflammation.

Hemoptysis gradually disappears, the functioning of the cardiovascular system normalizes, and the intensity of pain in the chest area decreases.

The effect of taking Cycloserine meets expectations, subject to the recommendations of a phthisiatrician.

If the drug is not suitable due to individual intolerance, it is replaced with an analogue drug. Suitable analogues - Mizer, Coxerine, Cycloserine-Ferein, Coxamine.

Useful video

Watch a video that explains how the drug is used and what its mechanism of action is in the treatment of tuberculosis.

Capsules No. 0, opaque, white body, light brown cap; the contents of the capsules are powder or a mixture of powder and granules from white or almost white to light yellow. It is allowed to compact the contents of the capsule according to the shape of the capsule, disintegrating when pressed.

Excipients: lactose 162 mg, colloidal silicon dioxide 3 mg, magnesium stearate 5 mg.

Composition of the capsule body: titanium dioxide 2%, gelatin up to 100%.
Composition of the capsule cap: iron oxide dye black 0.1%, iron oxide red dye 0.12%, iron oxide dye yellow 0.3%, titanium dioxide 2%, gelatin up to 100%.

10 pieces. - contour cellular packaging (aluminum/PVC) (1) - cardboard packs.
10 pieces. - contour cellular packaging (aluminum/PVC) (2) - cardboard packs.
10 pieces. - contour cellular packaging (aluminum/PVC) (3) - cardboard packs.
10 pieces. - contour cellular packaging (aluminum/PVC) (4) - cardboard packs.
10 pieces. - contour cellular packaging (aluminum/PVC) (5) - cardboard packs.
10 pieces. - contour cellular packaging (aluminum/PVC) (6) - cardboard packs.
10 pieces. - contour cellular packaging (aluminum/PVC) (8) - cardboard packs.
10 pieces. - contour cellular packaging (aluminum/PVC) (10) - cardboard packs.
30 pcs. - contour cellular packaging (aluminum/PVC) (1) - cardboard packs.
30 pcs. - contour cellular packaging (aluminum/PVC) (2) - cardboard packs.
30 pcs. - contour cellular packaging (aluminum/PVC) (3) - cardboard packs.
30 pcs. - contour cellular packaging (aluminum/PVC) (4) - cardboard packs.
30 pcs. - contour cellular packaging (aluminum/PVC) (5) - cardboard packs.
30 pcs. - contour cellular packaging (aluminum/PVC) (6) - cardboard packs.
30 pcs. - contour cellular packaging (aluminum/PVC) (8) - cardboard packs.
30 pcs. - contour cellular packaging (aluminum/PVC) (10) - cardboard packs.

20 pcs. - polymer jars (1) - cardboard packs.
30 pcs. - polymer jars (1) - cardboard packs.
40 pcs. - polymer jars (1) - cardboard packs.
50 pcs. - polymer jars (1) - cardboard packs.

Capsules hard gelatin, size No. 1, with a white or almost white body and a red cap; the contents of the capsules are white to light yellow powder.

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

Composition of the capsule shell: titanium dioxide, crimson dye Ponceau 4R, quinoline yellow dye, gelatin, water.

10 pieces. - blisters (10) - cardboard packs.

7 pcs. - cellless contour packages (1) - cardboard packs.
7 pcs. - cellless contour packages (2) - cardboard packs.
7 pcs. - cellless contour packages (3) - cardboard packs.
10 pieces. - cellless contour packages (1) - cardboard packs.
10 pieces. - cellless contour packages (2) - cardboard packs.
10 pieces. - cellless contour packages (3) - cardboard packs.
10 pieces. - cellless contour packages (10) - cardboard packs.
7 pcs. - cellless contour packages (10) - cardboard packs.
7 pcs. - cellless contour packages (50) - cardboard packs.
7 pcs. - cellless contour packages (54) - cardboard packs.
7 pcs. - cellless contour packages (60) - cardboard packs.
7 pcs. - polymer jars (1) - cardboard packs.
10 pieces. - cellless contour packages (50) - cardboard packs.
10 pieces. - cellless contour packages (54) - cardboard packs.
10 pieces. - cellless contour packages (60) - cardboard packs.
100 pieces. - polymer jars (1) - cardboard packs.
10 pieces. - polymer jars (1) - cardboard packs.

100 pieces. - polyethylene bottles (1) - cardboard packs.

Capsules hard gelatin No. 1, with an opaque white body and an opaque red cap.

Excipients: lactose 120 mg, purified talc 10 mg, colloidal silicon dioxide (aerosil) 3 mg, magnesium stearate 10 mg.

Composition of the capsule shell: Capsule body: gelatin up to 100%, titanium dioxide (E 171) 2.11%; Capsule cap: gelatin up to 100%, crimson dye Ponceau 4R (E 124) 0.49%, quinoline yellow dye (E 104) 0.00999%, titanium dioxide (E 171) 2.16%.

10 pieces. - aluminum strips (1) - cardboard packs.
10 pieces. - aluminum strips (5) - cardboard packs.
10 pieces. - aluminum strips (10) - cardboard packs.

Indications

Tuberculosis (as part of combination therapy), atypical mycobacterial infections (MAC infections).

— tuberculosis (chronic forms, reserve drug, as part of combination therapy);

- atypical mycobacterial infections (including those caused by Mycobacterium avium);

- urinary tract infections.

Use in elderly patients

Patients over 60 years old - 0.25 g 2 times a day.

Dosage regimen

When taken orally for adults, the dose is 0.25-1 g/day in several divided doses. Maximum dose- 1 g/day.

For children - 10-20 mg/kg/day in divided doses.

Orally, immediately before meals (if irritation of the gastrointestinal mucosa - after meals), adults- 0.25 g every 12 hours for the first 12 hours, then, if necessary, taking into account tolerability, the dose is carefully increased to 250 mg every 6-8 hours under monitoring the concentration of the drug in the blood serum.

The maximum daily dose is 1 g. Patients over 60 years old, and also with body weight less than 50 kg- 0.25 g 2 times/day. Daily dose for children- 0.01-0.02 g/kg (not higher than 0.75 g/day).

Side effect

From the central nervous system and peripheral nervous system: headache, dizziness, drowsiness, anxiety, confusion, depression, difficulty speaking, nightmares, muscle twitching, tremors, restlessness, peripheral neuropathy, seizures.

Allergic reactions: possible skin rash.

From the nervous system: headache, dizziness, insomnia or drowsiness, nightmares, anxiety, irritability, memory loss, paresthesia, peripheral neuritis, tremor, euphoria, depression, suicidal ideation, psychosis, epileptiform convulsions.

From the cardiovascular system: exacerbation of chronic heart failure in patients taking 1 to 1.5 g of cycloserine per day.

From the digestive system: nausea, heartburn, diarrhea.

Allergic reactions:(skin rash, itching), megaloblastic anemia and increased levels of liver aminotransferases, nausea, heartburn, diarrhea, especially in elderly patients with pre-existing liver disease.

Others: fever, increased cough.

Contraindications for use

Depression, psychosis, alcoholism, renal dysfunction, epilepsy, organic diseases of the central nervous system, history of seizures, pregnancy, hypersensitivity to cycloserine.

- hypersensitivity;

— organic diseases of the central nervous system;

- epilepsy;

— epileptic seizures (including in history);

— mental disorders (anxiety, psychosis, depression, including a history);

— chronic heart failure;

— chronic renal failure (creatinine clearance less than 50 ml/min);

- alcoholism.

Carefully apply in childhood.

Use during pregnancy and breastfeeding

Contraindicated for use during pregnancy.

Cycloserine is excreted in breast milk, so if it is necessary to use it during lactation, the issue of stopping breastfeeding should be decided.

Used only in cases of vital necessity.

Use in children

Application is possible according to the dosage regimen.

Carefully apply in childhood.

special instructions

With monotherapy with cycloserine, rapid development of mycobacterial resistance is possible, so only combination therapy should be used.

Careful monitoring of patients receiving cycloserine at doses above 500 mg/day is necessary to identify signs of CNS toxicity.

During the treatment period, avoid drinking alcohol.

Before starting cycloserine therapy, it is necessary to isolate cultures of microorganisms and determine the sensitivity of the strains to this drug. In the case of tuberculosis infection, it is necessary to determine the sensitivity of the strain to other anti-tuberculosis drugs.

Treatment with cycloserine should be discontinued or the dose should be reduced if the patient develops allergic dermatitis or symptoms of central nervous system damage, namely headache, dizziness, drowsiness, confusion, tremor, peripheral paresis, dysarthria, convulsions and psychosis. Due to the low therapeutic index of cycloserine, the risk of developing seizures increases in patients with chronic alcoholism.

Poisoning usually occurs at blood drug concentrations greater than 30 mg/L, which may result from overdose or impaired renal clearance. When taking the drug, hematological parameters, renal function (creatinine and urea nitrogen concentrations in the blood), drug concentrations in the blood and liver function should be monitored.

When treating patients with reduced renal function who are taking a daily dose of more than 500 mg and who are suspected of showing signs and symptoms of overdose, drug levels in the blood should be monitored at least once a week. The dose must be adjusted so as to maintain the drug level in the blood below 30 mg/l.

To prevent symptoms of damage to the central nervous system, in particular, seizures, agitation or tremor, it is possible to use anticonvulsants or sedatives. Patients receiving more than 500 mg of cycloserine per day should be under the direct supervision of a physician due to the possible development of such symptoms. The toxic effect of cycloserine can be prevented or reduced by prescribing glutamic acid 500 mg 3-4 times a day (before meals) during treatment, and daily intramuscular administration of the sodium salt of ATP (1 ml of 1% solution), as well as pyridoxine in a dose 200-300 mg/day.

To prevent side neurotoxic effects, psychotropic benzodiazepine drugs diazepam (5 mg) or phenazepam (1 mg) are prescribed at night, as well as piracetam at a dose of 800 mg 2 times a day. In some cases, the use of cycloserine can cause the development of vitamin B12 and/or folic acid deficiency, megaloblastic and sideroblastic anemia. If anemia occurs during treatment, it is necessary to conduct appropriate examination and treatment of the patient.

It is necessary to limit the mental stress of patients and exclude possible factors of overheating (staying in the sun with bare head, hot shower).

Due to the rapid development of resistance during monotherapy with cycloserine, its combination with other anti-tuberculosis drugs is recommended.

The effect of taking cycloserine on the ability to drive a car and use machinery has not been established.

Overdose

Overdose is observed when the concentration of cycloserine in plasma is 25-30 mg/ml as a result of taking cycloserine in high doses and/or impaired renal clearance. Acute poisoning can occur when more than 1 g/day is ingested. Symptoms chronic intoxication with long-term use at a dose of more than 500 mg/day: headache, dizziness, confusion, increased irritability, paresthesia, psychosis, dysarthria, paresis, convulsions, coma.

International name

Group affiliation

Dosage form

pharmachologic effect

A broad-spectrum bactericidal antibiotic that disrupts cell wall synthesis, acting as a competitive antagonist of D-alanine, and inhibits enzymes responsible for cell wall synthesis.

Active against gram-negative microorganisms, at a concentration of 10-100 mg/l - Rickettsia spp., Treponema spp. The MIC in relation to Mycobacterium tuberculosis is 3-25 mg/l in liquid and 10-20 mg/l or more in solid nutrient medium. Drug resistance occurs slowly (after 6 months of treatment it develops in 20-60% of cases).

Indications

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

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

Contraindications

Side effects

From the nervous system: headache, dizziness, insomnia or drowsiness, nightmares, anxiety, irritability, memory loss, paresthesia, peripheral neuritis, tremor, euphoria, depression, suicidal ideation, psychosis, epileptiform convulsions.

From the digestive system: nausea, heartburn, diarrhea.

Other: fever, increased cough.

Application and dosage

Orally, immediately before meals (if irritation of the gastrointestinal mucosa - after meals), adults - 0.25 g every 12 hours for the first 12 hours, then, if necessary, taking into account tolerability, the dose is carefully increased to 250 mg every 6-8 hours under supervision concentration of the drug in blood serum.

The maximum daily dose is 1 g. Patients over 60 years of age, as well as with a body weight of less than 50 kg, take 0.25 g 2 times a day. The daily dose for children is 0.01-0.02 g/kg (not higher than 0.75 g/day).

special instructions

The toxic effect of cycloserine can be prevented or reduced by prescribing glutamic acid 0.5 g 3-4 times a day (before meals) during treatment, and daily intramuscular administration of the sodium salt of ATP (1 ml of 1% solution), pyridoxine 200-300 mg /day

During treatment, it is necessary to monitor renal function (the concentration of creatinine and urea nitrogen in the blood) and the concentration of cycloserine in the blood (should not exceed 30 mcg/ml).

It is necessary to limit the mental stress of patients and exclude possible factors of overheating (staying in the sun with bare head, hot shower).

Due to the rapid development of resistance during monotherapy with cycloserine, its combination with other anti-tuberculosis drugs is recommended.

Interaction

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).

Ethanol increases the risk of developing epileptic seizures, especially in people suffering from chronic alcoholism.

Ethionamide increases the risk of CNS side effects, especially seizures.

Isoniazid increases the incidence of dizziness and drowsiness.

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Composition and release form

1 capsule contains cycloserine 250 mg; in a blister pack 100 pcs.

pharmachologic effect