Pask sodium salt

Pask sodium salt is an anti-tuberculosis drug that has bacteriostatic activity against Mycobacterium tuberculosis bacteria; it belongs to the subcategory of reserve anti-tuberculosis drugs.

The bacteriostatic effect of the drug is provided by the competitive activity that aminosalicylic acid exhibits in relation to the B10 vitamin, which is similar in structure. This activity develops during the binding of the B9 vitamin, which is required for stable reproduction and growth of tuberculosis mycobacteria.

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Indications Pasc sodium salt

It is used in complex treatment of actively progressing stages of tuberculosis – mainly in pulmonary tuberculosis of a fibrous-cavernous nature (chronic phase).

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Release form

The component is released in the form of a lyophilisate for oral liquid - inside 12.5 g sachets. The pack contains 25 or 300 such sachets.

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Pharmacodynamics

Aminosalicylic acid replaces PABA when binding B9 vitamin, which causes the destruction of normal DNA synthesis with RNA, as well as proteins of tuberculosis mycobacteria. To displace PABA with the help of the drug, it is necessary to use it in large portions.

PAS sodium salt does not affect other bacteria. Its activity against tuberculosis mycobacteria is lower compared to the activity demonstrated by drugs from the main category of anti-tuberculosis drugs. Because of this, it is used in combination with other drugs that have a more powerful effect.

In the case of monotherapeutic use of the drug, tuberculosis mycobacteria quickly develop resistance to it. In complex treatment, this happens much more slowly.

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Pharmacokinetics

When administered orally, the drug is well absorbed in the gastrointestinal tract. Its absorption is better than that of PAS. After oral administration of a drug dose equivalent to 4 g of PAS, plasma Cmax values are approximately 75 mg/ml and are noted after 30-60 minutes. Only 15% of the administered portion is synthesized with intraplasmic blood protein.

The active ingredient spreads at high speed inside tissues with fluids (including pleural and peritoneal fluids, as well as synovium); there its values are approximately equal to the plasma level. The component values inside the cerebrospinal fluid are low, and they increase only with inflammation of the meninges. The drug can cross the placenta and be excreted with breast milk. About 50% of the active ingredient is involved in intrahepatic metabolism by acetylation - as a result, inactive metabolic components are formed.

The half-life of the drug is 1 hour. In case of renal dysfunction, this period is prolonged to 23 hours. 85% of the portion is excreted with urine – through the secretion of tubules and CF, over 7-10 hours. 14-33% of the drug is excreted unchanged, and another 50% – in the form of metabolic components.

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Dosing and administration

The medication should be used only in combination with other anti-tuberculosis agents.

To reduce the irritating effect on the gastric mucosa, it is recommended to take the medicine after meals. To prepare the medicine, dissolve the powder from the bag in plain water, stirring (half a glass of liquid is required - 0.1 l); the prepared solution should be drunk immediately.

An adult should consume 8-12 g of the substance per day. This portion should be divided into 2-3 uses.

For people weighing less than 50 kg, and in case of severe intolerance, the portion is reduced to 4-8 g per day.

For children, the dosage is 0.2-0.3 g/kg per day; the portion should be divided into 2-4 doses. A maximum of 12 g of the medicine can be taken per day.

Individuals with renal insufficiency (creatinine clearance values <30 ml per minute) should be administered a maximum of 8 g of the drug (in 2 doses).

People with liver failure do not require dosage reduction, but it is necessary to monitor liver function values during therapy.

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Use Pasc sodium salt during pregnancy

The medication should not be used during lactation or pregnancy.

Contraindications

Main contraindications:

• severe intolerance to the active element of the drug or its auxiliary components;
• hepatitis, severe liver failure, and liver cirrhosis;
• severe renal failure;
• highly intense left ventricular myocardial hypertrophy;
• Heart failure in the decompensation phase;
• myxedema or ulcer affecting the gastrointestinal tract;
• amyloidosis.

PAS sodium salt contains a food additive - the component aspartame. This substance should not be used by people with phenylketonuria.

Side effects Pasc sodium salt

Side effects include:

• disorders in the nervous system: dizziness, anxiety, hepatic encephalopathy (this includes drowsiness with confusion), paresthesia, headaches, and in addition, neuritis affecting the optic nerve and a metallic taste in the mouth;
• lesions of the lymph and blood system: eosinophilia, leukopenia or thrombocytopenia, hemolytic anemia (in individuals with a deficiency of the G6PD element), agranulocytosis and prothrombin binding disorder occasionally occur;
• immune manifestations: signs of intolerance (bronchial spasm, eosinophilic pulmonary infiltrate, increased temperature and Loeffler syndrome) are occasionally observed, as well as anaphylaxis;
• endocrine disorders: prolonged administration of large portions leads to hypothyroidism;
• problems with the heart: development of pericarditis;
• symptoms related to the function of the vascular system: occasionally, an increase in blood pressure or its fluctuations, and vasculitis are observed;
• gastrointestinal disorders: often there is a weakening or loss of appetite, vomiting, dyspeptic symptoms, pain in the stomach or epigastrium, nausea, as well as bloating, abdominal discomfort, constipation or diarrhea and changes in stool;
• lesions of the biliary tract and liver: hepatitis or jaundice are occasionally observed, as well as pain in the liver and its enlargement;
• disorders of the urinary tract and kidneys: crystalluria appears sporadically;
• problems with the function of the subcutaneous layer and epidermis: occasionally, exanthema, enanthem, dermatitis (purpura or urticaria), rash and exfoliative dermatitis occur;
• disorders of connective and musculoskeletal tissues: occasionally myalgia or pain affecting the joints appears;
• nutritional and metabolic disorders: hypokalemia (occurs in case of prolonged use by people with cardiovascular diseases);
• systemic lesions: general pain throughout the body or asthenia;
• laboratory test results: increased activity of intrahepatic transaminases.

If such negative effects develop, you should stop taking the drug for a short period of time or reduce the dosage.

Negative symptoms are less intense if the patient eats properly, 3 times a day.

If you experience any allergy symptoms, you should consult your doctor to decide whether to discontinue the medication.

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Overdose

Signs of poisoning: diarrhea and vomiting with nausea; psychosis may occur.

Symptomatic measures are taken. Activated carbon is used to delay absorption; gastric lavage is also performed and vital functions of the body are monitored.

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Interactions with other drugs

In tuberculosis, several medications with different principles of influence on tuberculosis mycobacteria are used simultaneously. Complex treatment inhibits the development of mycobacterial resistance and leads to mutual potentiation of the effect of drugs.

PAS sodium salt inhibits the development of resistance of tuberculosis mycobacteria to streptomycin with isoniazid. When combined with isoniazid, its blood counts increase, and there is a risk of hemolytic anemia.

The activity of the drug is weakened when combined with aminobenzoate.

Administration together with anticoagulants potentiates their effect, because the drug inhibits intrahepatic binding of prothrombin.

The uricosuric substance probenecid delays the excretion of the drug with urine, which increases its plasma levels and increases the likelihood of developing toxicity (requires a reduction in the dose).

The drug can disrupt the absorption of cyanocobalamin and lead to vitamin deficiency. Therefore, in such combinations, the parenteral form of the latter should be used.

Combination of drugs with antidiabetic substances potentiates blood hypoglycemia.

The combination of the drug and capreomycin or the administration of large doses of the drug to elderly people with peripheral edema and elevated blood pressure may lead to hypokalemia.

The drug interferes with absorption and weakens the effect of erythromycin and rifampicin with lincomycin.

The drug reduces blood digoxin levels by 40%.

When using iodine-containing thyroid hormones, as well as their antagonists (also antithyroid drugs) and analogues, it is necessary to take into account that the introduction of Pask sodium salt leads to a change in the blood values of TSH and T4.

Ammonium chloride increases the likelihood of crystalluria.

Combined use with ethionamide increases the likelihood of developing hepatotoxicity.

The therapeutic activity of aminosalicylic acid is weakened when combined with diphenhydramine.

The negative effects of drugs and salicylates are additive.

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Storage conditions

Pask sodium salt should be stored in a place closed to children. Temperature values - not higher than 25°C.

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Shelf life

Pask sodium salt can be used for a period of 36 months from the date of manufacture of the therapeutic substance.

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Application for children

There are no data regarding restrictions on the use of drugs in pediatrics.

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Analogues

The analogs of the drug are Rifabutin, Rifampicin, PAS-Akri with Ethambutol and Isoniazid with Terizidone.

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