Pask Sodium Salt

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

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

[1], [2], [3], [4], [5]

Indications Sodium salt salts

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

[6], [7]

Release form

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

[8], [9], [10]

Pharmacodynamics

Aminosalicylic acid replaces PABA upon binding of B9-vitamin, which causes the destruction of normal DNA synthesis with RNA, as well as proteins of tuberculosis mycobacteria. To displace PABK with a medication, it is required to use it in large portions.

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

In the case of monotherapeutic use of the drug, tuberculosis mycobacteria rapidly develop resistance to it. With complex treatment, this is much slower.

[11], [12], [13], [14]

Pharmacokinetics

In oral administration, the drug is well absorbed inside the gastrointestinal tract. Its absorption is better than that of PAS. After oral administration of a dosage equivalent to 4 g of PASK, plasma Cmax values are about 75 tons of mg / ml and are noted after 30-60 minutes. Only 15% of the applied portion is synthesized with intraplasma blood protein.

The acting element at high speeds spreads inside the tissues with fluids (among them pleural and peritoneal, as well as synovia); there his performance is approximately equal to the plasma level. The values of the component inside the cerebrospinal fluid are low, and they increase only with inflammation of the lining of the brain. The drug can cross the placenta and be excreted with the mother's milk. About 50% of the active element is involved in intrahepatic metabolism using acetylation - as a result, inactive metabolic components are formed.

The half-life of drugs is equal to the 1st hour. In case of disorder of renal activity, this period is prolonged up to 23 hours. Together with the urine, 85% of the portion is excreted - through the secretion of the tubules and KF, for 7-10 hours. In unchanged condition, 14-33% of the drug is excreted, and another 50% - in the form of metabolic components. 

[15], [16]

Dosing and administration

The drug should be used exclusively in combination with other anti-TB substances.

To alleviate the irritating effect on the gastric mucosa, it is recommended to use the medicine after a meal. For the preparation of drugs you need to dissolve the powder from the bag in ordinary water, mixing (it takes half a glass of liquid - 0.1 l); ready solution should be drunk immediately.

An adult should consume 8-12 g of a substance per day. Divide this portion should be 2-3 use.

People with a weight below 50 kg, and in addition, with a strong 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 is required to be divided into 2-4 uses. A maximum of 12 g of medication is allowed per day.

Persons with kidney failure (CC values - <30 ml per minute) should be administered a maximum of 8 g of drugs (for 2 uses).

People with liver failure do not need to reduce the dosage, but it is necessary to monitor the values of its work during therapy.

[18], [19], [20], [21]

Use Sodium salt salts during pregnancy

When lactation or pregnancy drug can not be used.

Contraindications

The main contraindications:

• severe intolerance to the active drug element or its auxiliary components;
• hepatitis, severe liver failure, and hepatic cirrhosis;
• lack of function of the kidneys of a severe nature;
• severe intensity of left ventricular myocardium;
• CH in decompensation phase;
• Myxedema or ulcers affecting the digestive tract;
• amyloidosis.

PASK sodium salt contains a dietary supplement component aspartame. This substance can not be used by people with phenylketonuria.

Side effects Sodium salt salts

Among the side effects are:

• disorders in the NA: dizziness, fear, hepatic encephalopathy (this includes drowsiness with confusion), paresthesia, headaches, and in addition neuritis, affecting the optic nerve, and taste of metal in the mouth;
• lesions of the lymph and blood system: rarely eosinophilia, leuko- or thrombocytopenia, hemolytic anemia (in people with a deficient G6PD element), agranulocytosis and prothrombin binding disorder;
• immune manifestations: occasionally signs of intolerance (bronchial spasm, eosinophilic pulmonary infiltration, fever and Leffler syndrome), and anaphylaxis;
• endocrine disruption: prolonged administration of large portions leads to hypothyroidism;
• problems with the work of the heart: the development of pericarditis;
• symptoms associated with the function of the vascular system: rarely there is an increase in blood pressure values or their fluctuation, and vasculitis;
• disorders of the gastrointestinal tract: often there is a weakening or loss of appetite, vomiting, dyspeptic symptoms, pain in the stomach area or epigastria, nausea, and also bloating, abdominal discomfort, stasis or diarrhea and changes in stool;
• damage to the liver and the liver: rarely there is hepatitis or jaundice, as well as pain in the liver and its increase;
• disruption of the urethra and kidneys: crystalluria appears singly;
• problems with the function of the subcutaneous layer and the epidermis: occasionally exanthema, enanthema, dermatitis (purpura or urticaria), rash and exfoliative dermatitis occur;
• disorders of the connective and musculoskeletal tissues: rarely appears myalgia or pain affecting the joints;
• disorders of nutritional and metabolic functions: hypokalemia (occurs in the case of prolonged use by persons with CVD diseases);
• systemic lesions: general body aches or asthenia;
• readings of laboratory tests: an increase in the activity of intrahepatic transaminases.

In the event of the development of such negative phenomena, it is necessary to discontinue the drug for a short time or reduce the dosage.

Negative symptoms have a weaker intensity if the patient is fed in the correct mode, 3 times a day.

If allergy symptoms occur, a doctor should be consulted to decide on the possible cancellation of the medication.

[17]

Overdose

Signs of poisoning: diarrhea and vomiting with nausea; possible appearance of psychosis.

Symptomatic interventions are carried out. To delay absorption, use activated carbon; gastric lavage is also performed and observation of vital body functions is provided.

[22], [23], [24], [25],

Interactions with other drugs

In case of tuberculosis, several medications with different principles of influence are used regarding tuberculosis mycobacteria. Comprehensive treatment inhibits the development of mycobacterial resistance and leads to mutual potentiation of the effects of drugs.

PASK sodium salt inhibits the emergence of tuberculosis mycobacteria resistance to Streptomycin with isoniazid. When combined with isoniazid, its blood counts increase, and the likelihood of hemolytic anemia appears.

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

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

Urikozuricheskoe substance probenecid delays the excretion of drugs with urine, which increases its plasma values and increases the likelihood of toxicity (requires a decrease in portions).

The drug can interfere with the absorption of cyanocobalamin and lead to vitamin deficiency. Therefore, with such combinations, it is necessary to apply the parenteral form of the latter.

Combining drugs with antidiabetic substances potentiates blood hypoglycemia.

The combination of the drug and capreomycin or the introduction of large portions of the drug in elderly people with peripheral edema and increased blood pressure values can lead to hypokalemia.

The drug impairs absorption and weakens the effects of erythromycin and rifampicin with lincomycin.

The drug reduces the blood levels of digoxin by 40%.

When using thyroid hormones containing iodine, and besides their antagonists (also thyroid drugs) and analogues, it is necessary to take into account that the introduction of Pask Na salt leads to a change in 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.

Negative manifestations of drugs and salicylates have an additive character.

[26], [27], [28], [29], [30]

Storage conditions

Pask sodium salt should be stored in a place that is closed to children. Temperature values are not higher than 25 ° С.

[31], [32], [33], [34], [35]

Shelf life

Pask sodium can be used for a 36-month period from the time the therapeutic substance is manufactured.

[36], [37], [38], [39], [40]

Application for children

Data on the limitations of the use of drugs in pediatrics are not available.

[41], [42], [43],

Analogs

Analogues of drugs are the means Rifabutin, Rifampicin, PASK-Acri with Ethambutol and Isoniazid with Terizidone.

[44], [45], [46], [47], [48], [49], [50], [51], [52],