Cycloserine

Cycloserine is an antibiotic of bactericidal type of action; has an antibacterial effect. The drug has a fairly wide range of therapeutic activity - many pathogenic bacteria are sensitive to it.

The drug demonstrates high medicinal efficacy in the treatment of tuberculosis of a chronic nature. It is often used in situations where the bacteria that cause the pathology show resistance to other anti-tuberculosis drugs. [ 1 ]

Indications Cycloserine

It is used for mycobacterial infections of atypical nature, as well as for chronic tuberculosis (as a reserve drug).

Release form

The drug is released in the form of capsules with a volume of 0.25 g - 100 pieces per package.

Pharmacodynamics

The medicinal substance is formed during the life of Streptomyces orchidaceus or is obtained artificially. The principle of medicinal influence is based on the destruction of the processes of binding of cell membranes (inhibits enzymes that are responsible for their binding).

The drug demonstrates activity against treponemas and rickettsiae, and also against tuberculosis mycobacteria. Therapeutic resistance develops quite slowly. [ 2 ]

Pharmacokinetics

The absorption rate is 70-90%. The drug is practically not involved in protein synthesis. Cmax values are noted after 4 hours.

The active element is found in bile, sputum, breast milk, body fluids and pleural effusion. 60-100% of the serum drug level is found in the pleural cavity. 35% of the dosage is involved in metabolic processes. [ 3 ]

The half-life is 10 hours. Excretion is mainly via the kidneys; a small amount is excreted in feces. In case of chronic renal failure, accumulation of the drug is possible.

Dosing and administration

Cycloserine is taken orally, before meals. If there are signs of irritation in the gastrointestinal mucosa, it should be taken after meals.

For adults, the dosage is 0.25 g at 12-hour intervals; if necessary and there are no complications from taking this dosage, it can be used with a 6-hour break. The daily dose is 1000 mg; for a child - a maximum of 750 mg.

The toxic effect can be reduced by prescribing oral glutamic acid and intramuscular pyridoxine with ATP. In case of alcoholism, the likelihood of seizures increases. During therapy, it is necessary to monitor the liver and kidney function, as well as peripheral blood values. In case of allergic dermatitis or signs of neurotoxicity, therapy is discontinued.

Use for monotherapy causes the development of resistance, which makes it necessary to combine the drug with other anti-tuberculosis drugs.

• Application for children

In pediatrics, use with caution.

Use Cycloserine during pregnancy

Cycloserine is contraindicated during pregnancy.

Contraindications

Main contraindications:

• severe intolerance to the drug;
• epilepsy;
• diseases affecting the central nervous system that are organic in nature;
• mental disorders;
• alcoholism;
• breastfeeding period.

The medication should be used with extreme caution in cases of chronic renal failure.

Side effects Cycloserine

Side effects include:

• headaches, psychosis, convulsions (also clonic type), confusion and dysarthria, paresis and aggressiveness;
• itching and rashes on the epidermis;
• diarrhea, nausea and heartburn;
• megaloblastic anemia;
• active form of CHF.

Overdose

Acute intoxication develops when more than 1000 mg of the drug is used per day. In the chronic form of poisoning, which develops as a result of prolonged use of doses over 0.5 g per day, confusion, psychosis, headaches, convulsions, paresthesia, dizziness, paresis and irritability are observed. A comatose state may develop.

Symptomatic actions are performed - the use of anticonvulsants and activated carbon. Pyridoxine is used to prevent the development of neurotoxic symptoms.

Interactions with other drugs

The effect of the medication is neutralized by acidic fruit juices.

When combined with ethyl alcohol, the risk of developing epileptic seizures increases.

Combining Cycloserine with Isoniazid results in drowsiness and dizziness.

Use with ethionamide increases side effects associated with the central nervous system.

Storage conditions

Cycloserine must be stored at temperatures no higher than 25°C.

Shelf life

Cycloserine can be used within a 2-year period from the date of manufacture of the therapeutic element.

Analogues

Analogues of the drug are the medications Coxamin, Coxerine with Cycloserine-Ferein and Mizer.

Reviews

Cycloserine receives mixed reviews. Patients' comments note the drug's high toxicity - mainly hemato- and neurotoxicity. Its use often leads to the appearance of peripheral neuritis and anemia. But in this case, it should be taken into account that it is extremely rare for resistant types of tuberculosis to be treated with drugs that do not lead to the appearance of negative symptoms.

Reviews also indicate that long-term use of the drug leads to a deficiency of pyridoxine, cyanocobalamin and vitamin B9.