Cycloserine

Cycloserine is a bactericidal antibiotic; 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 efficiency in the treatment of chronic tuberculosis. It is often used in situations where the bacteria that are the causative agent of the pathology show resistance to other anti-tuberculosis drugs.[1]

Indications Cycloserine

It is used for atypical mycobacterial infections, as well as for chronic tuberculosis (as a backup medication).

Release form

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

Pharmacodynamics

The drug substance is formed during the vital activity of Streptomyces orchidaceus, or it is obtained artificially. The principle of the medicinal effect is based on the destruction of the binding processes of cell membranes (inhibits the enzymes that are responsible for their binding).

The drug demonstrates activity against treponemes with rickettsia, and in addition against mycobacterium tuberculosis. Therapeutic resistance develops rather slowly.[2]

Pharmacokinetics

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

The active element is found within bile, sputum, breast milk, body fluids and pleural effusion. Inside the pleural cavity, 60-100% of the serum value of the drug is observed. In the exchange processes, 35% of the dosage is involved.[3]

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

Dosing and administration

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

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

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

Use for monotherapy causes the emergence of resistance, which is why it is necessary to combine the medication with other anti-tuberculosis drugs.

• Application for children

Used with caution in pediatrics.

Use Cycloserine during pregnancy

Cycloserine should not be prescribed during pregnancy.

Contraindications

The main contraindications:

• severe drug intolerance;
• epilepsy;
• diseases affecting the central nervous system, which are organic in nature;
• mental disorders;
• alcoholism;
• lactation period.

With extreme caution, the medication is used for chronic renal failure.

Side effects Cycloserine

Among the side symptoms:

• headaches, psychosis, seizures (also of the clonic type), confusion and dysarthria, paresis and aggressiveness;
• itching and rashes on the epidermis;
• diarrhea, nausea, and heartburn;
• anemia of the megaloblastic type;
• 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 dosages over 0.5 g per day, confusion, psychosis, headaches, convulsions, paresthesias, dizziness, paresis and irritability are noted. Coma 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 likelihood of developing epileptic seizures increases.

The combination of Cycloserine with isoniazid leads to drowsiness and dizziness.

The use together with ethionamide increases the side effects associated with the work of the central nervous system.

Storage conditions

Cycloserine is required to be stored at temperatures not exceeding 25 ° C.

Shelf life

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

Analogs

Analogues of the drug are the medicines Coxamine, Coxerin with Cycloserine-Ferein and Maizer.

Reviews

Cycloserine has received conflicting reviews. In the comments of patients, there is a high toxicity of the drug - mainly hemato- and neurotoxicity. Often its use leads to the appearance of a peripheral form of neuritis and anemia. But in this case, it should be borne in mind that it is extremely rare for the treatment of resistant types of tuberculosis to find drugs that do not lead to the appearance of negative symptoms.

The reviews also indicate that prolonged use of the medication leads to a deficiency of pyridoxine, cyanocobalamin and B9-vitamin.