Sodium para-aminosalicylate

Sodium para-aminosalicylate is included in the category of synthetic antibacterial drugs. It has bacteriostatic and anti-tuberculosis properties.

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Indications Para-aminosalicylate sodium

It is used for drug-resistant tuberculosis (any location and in different forms) in combination with other additional drugs with an anti-tuberculosis effect.

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Release form

It is produced in tablets of 0.5 or 1 g, in granules – inside packages of 4, 5 or 100 g, and also in the form of a lyophilisate for infusion solutions – in vials.

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Pharmacodynamics

The drug is a competitor of PABA in the fight for the active center of the enzyme that converts PABA into DHF, and in addition, it slows down the binding of folic acid inside bacterial cells. The tuberculostatic effect of the drug is weaker than the similar effect of streptomycin and isoniazid. The drug effectively affects Mycobacterium tuberculosis - it has a bacteriostatic effect (the size of the MIC in vitro is 1-5 μg / ml).

The drug reduces the risk of bacterial resistance to isoniazid with streptomycin. Its mechanism of action is due to the suppression of folic acid binding processes, as well as the formation of mycobactin (an element of the microbial wall), resulting in a decrease in the level of iron capture by the Mycobacterium tuberculosis bacterium.

It also affects mycobacteria that are in the stage of active reproduction, but has almost no effect on mycobacteria that are in a dormant state. The drug has a rather weak effect on intracellular pathogenic bacteria. The drug has no effect on other non-tuberculous mycobacteria.

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Pharmacokinetics

After oral administration, it is absorbed fairly quickly. The maximum value after oral administration of 4 g of the drug is 75 mcg/ml.

It undergoes hepatic metabolism and is excreted by glomerular filtration – 80% with urine (more than 50% of the substance is in the form of an acetylated derivative). The substance passes into the cerebrospinal fluid only in the case of inflammation in the meninges.

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Dosing and administration

The drug is taken orally with water. It should be taken after meals. The daily dose for adults is 9-12 g (3-4 g three times a day). Exhausted patients (weight less than 50 kg) or those who have poor tolerance to the drug, need to take 6 g / day. The dose for children is 0.2 g / kg / day, the dose is taken in 3-4 doses (a maximum of 10 g is allowed per day).

Persons undergoing outpatient treatment are allowed to take the entire daily dose at one time, but if a person has poor tolerance, it is necessary to divide the dose into 2-3 uses.

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Use Para-aminosalicylate sodium during pregnancy

Pregnant women can take the drug only in cases where the possible benefit from treatment exceeds the likelihood of complications and the fetus.

Breastfeeding is prohibited during therapy.

Contraindications

Among the contraindications:

• presence of hypersensitivity to the drug;
• severe stages of liver or kidney diseases;
• decompensated stage of heart failure;
• ulcer in the gastrointestinal tract;
• epileptic seizures;
• aggravated enterocolitis;
• exacerbated hypothyroidism.

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Side effects Para-aminosalicylate sodium

The use of drugs may lead to the following side effects:

• damage to the gastrointestinal tract: the appearance of vomiting with nausea, loss or weakening of appetite, diarrhea or constipation and abdominal pain;
• allergy symptoms: fever, bronchial spasms, enanthem, and also dermatitis in the form of purpura or urticaria;
• Others: joint pain, development of eosinophilia. Rarely, thrombocytopenia or leukopenia or agranulocytosis occurs, and in addition, drug-induced hepatitis or crystalluria develops.

After prolonged use of high doses of drugs, goiter or myxedema may develop.

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Interactions with other drugs

The drug increases the isoniazid levels in the blood, interferes with the absorption of erythromycin, rifampicin, and lincomycin, as well as the absorption of cyanocobalamin (this can lead to anemia). The drug also potentiates the properties of indirect anticoagulants (derivatives of indandione or coumarin).

Antacids do not affect the absorption of sodium para-aminosalicylate.

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Storage conditions

The medicine Sodium para-aminosalicylate should be kept in a dark place, protected from moisture. Temperature values are no more than 25°C.

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Shelf life

Sodium para-aminosalicylate tablets can be used for a period of 2 years from the date of manufacture of the drug, granules - for 3 years, and lyophilisate - for 4 years.

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