medicalmeds.eu Medicines Drugs, active concerning mycobacteria. Sodium salt of p-aminosalicylic acid

Sodium salt of p-aminosalicylic acid

Producer: JSC Himfarm Republic of Kazakhstan

Code of automatic telephone exchange: J04AA01

Release form: Firm dosage forms. Powder for suspension preparation.

Indications to use: Pulmonary tuberculosis. Tuberculosis.

General characteristics. Structure:

Active agent - dihydrate aminosalicylate sodium 5.52g (it is equivalent to p-aminosalicylic acid) (4.00).

Excipients: lactoses monohydrate, aspartame.

Pharmacological properties:

Pharmacokinetics. It is well soaked up at intake. When using a single dose of 4 g the maximum content in blood is defined in 1-2 hours. Linkng with proteins of a blood plasma low – 15%.

It is quickly distributed on bodies and fabrics, moderately gets into cerebrospinal liquid (only at an inflammation of covers). It Biotransformirutsya in a liver, more than 50% are acetylated to inactive metabolites. It is removed by kidneys: to 85% of a dose it is quickly removed within 7-10 hours by glomerular filtering and canalicular secretion, 14-33% are removed in not changed view with urine, 50% in a look – metabolites. The elimination half-life makes 30 minutes. A small amount cosecretes with bile, breast milk, saliva. At a renal failure and at people of advanced age renal elimination of drug is slowed down.

Pharmacodynamics. Sodium salt of p-aminosalicylic acid has bacteriostatic activity concerning only Mycobacterium tuberculosis. The effect is caused by competitive interaction with paraaminobenzoic and pantothenic acids, and also biotin in a microbic cell. In addition to bacteriostatic activity drug has the desensibilizing and antiinflammatory effect, changes the nature of fabric reactions to damage and promotes a partial resorption of caseous masses.

In comparison with other antituberculous remedies has weaker effect therefore it is combined with more active antituberculous remedies (including, with an isoniazid or other drugs of hydrazide of isonicotinic acid, Cycloserinum, Kanamycinum). At use in the form of monotherapy stability quickly develops. The combination therapy slows down development of medicinal stability and increases efficiency of treatment.

Indications to use:

- a pulmonary tuberculosis and other bodies as a part of a combination therapy with other antituberculous remedies for the prevention of development of resistance of mycobacteria.

Route of administration and doses:

Appoint inside in 0,5-1 h after food. Contents of a bag are dissolved, constantly mixing, in 100 ml of water. The prepared solution of drug can be washed down with milk, alkaline mineral water, 0,5-2% hydrosodium carbonate solution. The adult drug is appointed at the rate of 12 g of p-aminosalicylic acid (PASK) a day (on 1 bag 3 times a day), to children – on 0,2 g/kg a day (but no more than 10 g) in 3-4 receptions.

To the exhausted patients (with body weight it is less than 50 kg), elderly patients and at bad portability of drug appoint 6 g a day (1/2 bags 3 times a day).

In out-patient practice it is possible to appoint a daily dose in 1 reception, however at bad portability the daily dose is divided into 2 - 3 receptions. The maximum period of storage of the prepared solution before its use – no more than 1 hour.

The quantity of courses and the general duration of treatment are defined individually.

Features of use:

With extra care apply at patients with disturbances of functions of kidneys and a liver. In the course of treatment it is necessary to investigate systematically urine and blood and to check a functional condition of a liver.

In high doses of PASK has anti-thyroid effect, at prolonged use it can be observed, зобогенньй effect. This feature of PASK needs to be considered if TB patients have a hypofunction of a thyroid gland.

It is necessary to be careful at patients with moderately expressed digestive tract pathology.

In the presence of aminosalicylates carrying out tests for a glucosuria in which the reagents containing copper are used is broken.

Development of a proteinuria and hamaturia, allergic reactions demand temporary drug withdrawal.

Considering side effects of drug it is necessary to be careful at control of vehicles or work with the mechanisms demanding concentration of attention.

Side effects:

- decrease or loss of appetite, the increased salivation, nausea, vomiting, a meteorism, an abdominal pain, diarrhea or a lock

- increase in activity of "hepatic" transaminases, hyperbilirubinemia, jaundice

- proteinuria, hamaturia, crystalluria

- rash (a small tortoiseshell, a purpura, an enantema, exfoliative dermatitis, the syndrome reminding an infectious mononucleosis or a lymphoma), fever, a bronchospasm, an arthralgia, an eosinophilia.

Seldom:

- medicinal hepatitis (including with a lethal outcome)

- thrombocytopenia, a leukopenia (up to an agranulocytosis), B12-scarce anemia, hemolitic anemia with positive test of Koombs

Others: in high doses - anti-thyroid action; at prolonged use - goitrogenic effect, a medicinal hypothyroidism, a myxedema; a pericardis, a hypoglycemia, an optic neuritis, encephalopathy, Leffler's syndrome (eosinophilic pneumonia, the migrating pulmonary infiltrate), a vasculitis, decrease in a prothrombin.

Interaction with other medicines:

Let's combine with other antitubercular drugs. When sharing with an isoniazid increases its concentration in blood and extends an elimination half-life. Breaks absorption of rifampicin, erythromycin and lincomycin. Breaks digestion of B12 vitamin (risk of development of anemia).

PASK at simultaneous use with the anticoagulants derivative of coumarin or an indandion, strengthens action of the last because of decrease in synthesis in a liver of blood-coagulation factors. Therefore in time and after treatment of PASK can be required dose adjustment of anticoagulants.

Simultaneous use of PASK with aminobenzoates is not recommended since the last can be soaked up more preferably by bacteria, thereby interfering with bacteriostatic effect of the last.

Probenetsid or Sulfinpyrazonum can increase toxicity of drug by disturbance of its renal excretion and increase in concentration in a blood plasma.