Project Description

Granules “PASA sodium salt”

 Granulae natrii para-аminosalicylas.

international nonproprietary name

Sodium аminosalicylate.

Ref

BP-0101

Pharmacotherapeutic group

Preparations active to mycobacteria. Antituberculous preparations. Aminosalicylic acid and its derivatives.

Composition of the preparation

Each package contains an agent– sodium aminosalicylate (translated in 100 %) – 5,52 g that makes 4,0 g of para-aminosalicylic acid (PASA); auxiliary substance — sugar.

Pharmacological action

Pharmacodynamics

The preparation has a bacteriostatic action in relation to tuberculous mycobacteria and constitutes one of the main antituberculous preparation. The effect is conditioned by competitive interaction with para-aminobenzoic and pantothenic acids, as well as with biotin in the microbal cell. Resistance is rapidly developed on administration in the monotherapy. The preparation tuberculostatic activity is less than that of isoniazid and streptomycin, therefore the preparation shall be combined with more active anti-tuberculous preparations (comprising isoniazid or other preparations of isonicotinic acid hydrazide, cycloserine, kanamycin). The combined therapy slows down the development of resistance to the preparation and intensifies the treatment effectiveness.

Besides antibacterial activity the preparation has a antisensitizing and anti-inflammation action, slightly modifies the character of tissue reactions to lesion and contributes to partial resorption of caseous masses.

Pharmacokinetics

The preparation is well absorbed on oral administration. In case of the single dose 4 g max.content in the blood is determined in 1 – 2 hours. Bounding with blood proteins is 50-60%. It is distributed rapidly in the organs and tissues and moderately penetrates into the cerebrospinal fluid (only on membrane inflammation). The preparation metabolizes, half of the dose is contained in the urine in the form of acetylated derivative. The half-period is 30 minutes.  Small quantity is secreted with bile, breast milk and saliva. Kidney elimination is slow in elderly patients and in patients with kidney failure.

Indications 

Tuberculosis (various forms and localisations).

special indication

The preparation shall be prescribed in combination with more active anti-tuberculous medications.

In case of proteinuria and hematuria development the treatment shall be suspended.

The preparation does not affect the ability to drive and work with the machines.

special warning

Not established

Dosage and method of administration

The preparation is prescribed for oral administration in 0,5-1  hour after the meals. The content of the package is diluted while stirring in 100 ml of water. The prepared solution may be taken with milk, alkaline mineral water, sodium hydrocarbonate solution 0,5-2 %.  For adults the dose is calculated on the basis of para-aminosalicylic acid 12 g (PASA) per day (1 package 3 times a day), for children — 0,2 g/kg per day (1/2 of the package 3 – 5 times a day). Max.daily PASA dose for children is 10 g.

For emaciated, elderly patients and on a bad tolerance of the preparation the dose shall constitute 6 g of PASA per day (1/2 of the package per day).

Max.shelf-life of the prepared solution till its administration is not more than 1 hour.

Duration of treatment is 1 – 2 months.

overdosage

Symptoms: intensification of side effects is possible.

Treatment: cessation of therapy, symptomatic therapy.

safety measures

The preparation shall be prescribed with care in patients with epilepsy and moderate pathology of gastrointestinal tract, kidney and liver failure.

A systematic monitoring of urine and blood and liver function shall be carried out.

Side effects

Loss of appetite, nausea, vomiting, meteorism, pain in the stomach, diarrhea or constipation, hypokaliemia, hepatosplenomegaly, increased liver transaminase activity, hyperbilirubinemia, proteinuria, hematuria, crystalluria, kidney failure, allergic reactions (fever, dermatitis, eosinophilia, arthralgia, bronchospasm). Rarely – thrombocytopenia, leucopenia (to the extent of agranulocytosis), medical hepatitis, lymphadenopathy, B12-deficit megaloblastic anemia, psychosis, and on prolonged administration in elevated doses – hypothyroidism, goiter.

Contraindications

Hypersensitivity to aminosalicylic acid and its salts, kidney and/or liver failure, hepatitis, cirrhosis, visceras amyloidosis, stomach and duodenum peptic ulcer, enterocolitis (acute condition), myxedema, nephritis, decompensated chronic heart failure trombophlebitis, hypocoagulation, epilepsy, pregnancy, lactation.

Interactions with other medicinal preparations

It is compatible with other anti-tuberculous preparations. On simultaneous use with isoniazid the preparation increases its concentration in the blood. It worsens absorption of rifampicin, erythromycin and lincomycin. It impairs vitamin B12 uptake (risk of anemia development).

Probenecid increases the preparation toxicity through impairment of its kidney excretion and increasing its concentration in the blood.

Side effects of the preparation and salicylates have an additive character.

The form of release

12 g in the package. 10 packages with administration data sheet in each package.

Packaging for hospitals: 42 packages with administration data sheet in each box.