Sodium para-aminosalicylate

Sodium para-aminosalicylate belongs to the category of antibacterial drugs of synthetic type. It has bacteriostatic and anti-tuberculosis properties.

[1], [2], [3], [4]

Indications of the sodium para-aminosalicylate

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

[5], [6], [7],

Release form

The release occurs in tablets with a volume of 0.5 or 1 g, in granules - inside packages of 4, 5 or 100 g, and also as a lyophilizate for infusion solutions - in vials.

[8], [9], [10], [11]

Pharmacodynamics

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

The drug reduces the risk of bacterial resistance to isoniazid with streptomycin. The mechanism of its effect is due to the suppression of folic acid binding processes, and besides the formation of mycobacterium (this is an element of the microbial wall), resulting in a decrease in the level of iron capture of Mycobacterium tuberculosis bacteria.

Influences and on mycobacteria, which are at the stage of active reproduction, but it almost does not affect the mycobacteria, staying in a calm state. Quite weakly, the drug acts on intracellular pathogens. The drug has no effect on other non-tuberculosis mycobacteria.

[12], [13], [14], [15]

Pharmacokinetics

After ingestion, it absorbs quickly enough. The maximum value after oral administration of 4 g of the drug is 75 μg / ml.

Exposed to hepatic metabolism, and excreted by filtration of glomeruli - by 80% in urine (more than 50% of the substance - in the form of an acetylated derivative). Inside the liquor the substance passes only in the case of the development of inflammation in the area of the membranes of the brain.

[16], [17], [18]

Dosing and administration

The drug is taken orally with water. Follow the course after eating. The daily portion for adults is 9-12 g (intake of 3-4 g three times per day). Exhausted patients (weight less than 50 kg) or those with a poor tolerance of drugs, you need to use 6 g / day. The dose for children is 0.2 g / kg / day, the dose is taken in 3-4 times (for a day it is allowed to take a maximum of 10 g).

Persons who are on an outpatient treatment are allowed to take the entire daily portion for 1 time, but if a person has a bad tolerance, it is necessary to divide the dose into 2-3 uses.

[27], [28], [29], [30]

Use of the sodium para-aminosalicylate during pregnancy

Pregnant medicine can be taken only in cases where the possible benefits of treatment will exceed the likelihood of complications and fetus.

Breastfeeding during the period of therapy is prohibited.

Contraindications

Among the contraindications:

• the presence of hypersensitivity to the drug;
• severe stages of hepatic or renal diseases;
• decompensated stage of heart failure;
• an ulcer in the gastrointestinal tract;
• seizures of epilepsy;
• exacerbated enterocolitis;
• exacerbated hypothyroidism.

[19], [20], [21], [22],

Side effects of the sodium para-aminosalicylate

The use of drugs can lead to such side effects:

• lesions of the digestive tract: the occurrence of vomiting with nausea, weakening or loss of appetite, diarrhea or constipation and abdominal pain;
• symptoms of allergy: a state of fever, spasms of bronchi, enanthema, and in addition dermatitis in the form of purpura or urticaria;
• Other: pain in the joints, the development of eosinophilia. Occasionally there is thrombocyto- or leukopenia or agranulocytosis, and in addition, drug-induced hepatitis or crystalluria develops.

After prolonged use of large doses of drugs, there may be a goiter or myxedema.

[23], [24], [25], [26]

Interactions with other drugs

The drug increases the indices of isoniazid inside the blood, interferes with the absorption of erythromycin, rifampicin, and lincomycin, and the assimilation of cyanocobalamin (this can lead to anemia). Also, the drug potentiates the properties of indirect anticoagulants (derivatives of indandion or coumarin).

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

[31], [32], [33], [34]

Storage conditions

Medication Sodium para-aminosalicylate must be kept in a dark place, protected from moisture. The temperature should not exceed 25 ° C.

[35]

Shelf life

Sodium para-aminosalicylate in tablets can be used in the period of 2 years from the date of manufacture of the medicament, granules - for 3 years, and lyophilizate - for 4 years.

[36], [37], [38]