Project Description

Frozen-dried powder “PASA sodium salt”

3 g for infusion solution Natrii para-аminosalicylas 3.0g

international nonproprietary name

Sodium aminisalicylate

Ref

BP-0102

Pharmacotherapeutic group

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

Composition of the preparation

Sodium aminosalicylate

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

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.

Intravenous administration of the preparation solution shall be controlled by the doctor. To prevent haematoma and phlebit a fine needle shall be used, as well as the veins for administration shall be alternated.

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

special warning

Not established

Dosage and method of administration

Recommendations for preparation and administration of intravenous infusion solution

To prepare the infusion solution the content of 1 vial containing 3 g (PASA sodium salt) shall be diluted in 100 ml of water for injections. The prepared solution contains 3 g of PASA sodium salt in 100 ml of water (solution 3 %).

The content of the bottle shall be completely dissolved. Only freshly prepared solutions shall be administered. The solution prepared for intravenous administration shall be kept not more than 12 hours. When blurred on storing or dissolving, the solution shall not be administered.

For intravenous injections 3 % solution is used. The preparation can be administered with injection pump with regulated feed. It is administered intravenously drop-by-drop. The administration starts with 30 drops per minute and, in absence of any local or general reactions, in 15 minutes the infusion speed shall be increased up to 40 – 60 drops per minute. For the first infusion not more than 200 ml of the solution shall be administered, and in absence of any side effects – up to 400 ml of the solution. The infusion is made 5 – 6 times a week or every other day alternating with oral administration of PASA sodium salt.

The PASA sodium salt dose for adults constitutes 10-12 g per day, for children – 0,2 g/kg per day (max.daily dose for children –10 g).

For emaciated, elderly patients and on a bad tolerance of the preparation the dose shall constitute 6 g per day.

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.

Local reactions: haematoma and phlebit are possible. In case of non-observance of the infusion technique (rapid infusion, insufficient washing of the system used for administration, remains of the prior administration solution in the system), shock cases are possible.

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 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

3 g in a glass bottle for blood, capacity of 100 ml. Each bottle with administration data sheet is placed into the individual package.

Packaging for hospitals: 56 bottles with corresponding number of application data-sheets are placed into the corrugated cardboard box.