Pasin

Pasin is an anti-tuberculosis drug with a combined therapeutic composition; it is part of a group of substances that have a medicinal effect on the activity of mycobacteria. The composition of this drug contains the components isoniazid, as well as sodium para-aminosalicylate.

Thanks to complex treatment, the process of tuberculosis mycobacteria becoming accustomed to isoniazid with streptomycin is delayed, and at the same time, the activity of anti-tuberculosis drugs is potentiated.

Indications Pasina

It is used for the prevention and treatment of various forms of tuberculosis (any localization).

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Release form

The medicinal element is released in granules, 100 g each inside sachets. The container contains 1 such sachet, as well as a measuring spoon with a capacity of 5 g.

Pharmacodynamics

Sodium para-aminosalicylate has a bacteriostatic effect on tuberculosis mycobacteria. The effect of the substance leads to the suppression of the binding of vitamin B9 or the suppression of the synthesis of the element of the cell wall of mycobacteria. As a result, the absorption of iron by tuberculosis mycobacteria is weakened.

Isoniazid has an effect on actively reproducing tuberculosis mycobacteria; it is less effective against other bacteria. It acts by inhibiting the binding of long-chain mycolic acids, which are elements of the mycobacterial cell membrane. The drug slows the growth of mycobacteria when administered at a dosage concentration of 0.03 mcg/ml.

In comparison with other common microbes that cause various infections, the drug does not have a significant chemotherapeutic effect.

Pharmacokinetics

After 2-3 hours from the moment of drug administration, the indicators of active components in the blood plasma are 50%; the maximum time interval for achieving this result is 6 hours.

The substance passes at high speed into fluids (pleural, cerebrospinal fluid and ascitic), organs with tissues, and secretions (sputum with saliva and feces). At the same time, the drug crosses the placenta and is found in mother's milk (the indicator is similar to plasma). Approximately 50-70% of the portion of both components is excreted with urine within 24 hours.

Metabolic processes mostly occur inside the liver – through dehydrosination and acetylation (the latter is determined by genetic factors). It is possible to distinguish between “slow” and “fast” inactivators. The rate of inactivation generally does not have a significant effect on drug activity, but people with “slow” inactivators may have elevated blood levels of isoniazid and, therefore, an increased likelihood of developing toxic effects.

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Dosing and administration

The drug is administered in combination with other anti-tuberculosis agents. It should be taken 60 minutes before or after meals. Before starting therapy, it is necessary to determine the sensitivity of bacteria to the drug.

The portion is calculated based on isoniazid. The medicine box contains 1 measuring spoon with a capacity of 5 g, which has divisions for 1 g (1 such spoon contains about 116.5 mg of isoniazid, thus, 1 g of this spoon contains approximately 23.3 mg of the substance).

The dosage is calculated in the proportion of 10-15 mg/kg per day. It should be taken daily, in 1 dose; the portion is up to 0.3 g (2.5 measuring spoons). A dosage of 20-40 mg/kg can also be used - up to 0.9 g (corresponds to 7.5 measuring spoons) per day in 1 dose, 2-3 times a week.

For children aged 3 years and over, a dose of 5 mg/kg – up to 0.3 g (equivalent to 2.5 measuring spoons) per day in 1 dose, daily is required; or 10 mg/kg – up to 0.9 g (equivalent to 7.5 measuring spoons) per day in 1 dose, 2-3 times per week is used.

The medicine should be taken with tomato juice or milk.

The serving size for children weighing 15 kg is 75 mg (corresponds to 3/5 of a measuring spoon) of LS, 1 time per day.

For children weighing up to 20 kg – 0.1 g (4/5 teaspoon) of medication once a day.

For children weighing up to 30 kg – 0.15 g (1 + about 1/5 teaspoon) of the substance once a day.

For children weighing up to 40 kg – 0.2 g (1 + about 2/5 teaspoon) LS 1 time per day.

For children weighing up to 50 kg – 0.25 g (2+about 1/5 teaspoon) of medication once a day.

If there is a strong sensitivity to the drug, the dose should be reduced.

Therapy for pulmonary types of tuberculosis.

The course is often conducted using one of the 3 schemes described below.

1. The medication is used over a 2-month period, daily or 2-3 times a week. Streptomycin or ethambutol is administered together with it (until the desired effect regarding mycobacterial sensitivity is achieved).

2. Daily use of Pasin with pyrazinamide, rifampicin, and ethambutol or streptomycin (for a 2-week period), and then 2 times a week for 1.5 months. After that, the medicine is used 2 times a week for 4 months.

3. The drug is used together with streptomycin or ethambutol, pyrazinamide and rifampicin 3 times a week for a period of six months.

Therapy for extrapulmonary tuberculosis.

The basic model of therapy is similar to the schemes used for pulmonary tuberculosis. It is not necessary to monitor the course of treatment of extrapulmonary pathology as carefully, but clinical data allow us to conclude that short treatment cycles lasting 6-9 months give the required result.

Due to limited data in the treatment of bone or miliary tuberculosis and tuberculous meningitis, and also in children, in these cases therapy should be continued for 1 year.

Preventive procedures.

Before starting preventive measures, it is necessary to exclude the possibility of the presence of an active form of tuberculosis. For this, radiological and bacteriological diagnostic methods are used.

For children weighing over 30 kg and adults, 1 serving of 0.3 g of the substance is required per day.

Children weighing less than 30 kg require 5 mg/kg of the drug daily, once a day (up to 0.3 g). If it is impossible to strictly follow the preventive treatment regimen, use 10 mg/kg (maximum 0.9 g per dose) 2 times a week. In this case, the use of the drug should be supervised by a physician.

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Use Pasina during pregnancy

It is prohibited to prescribe to pregnant women in a dose that, when calculated as isoniazid, is more than 10 mg/kg.

Contraindications

Main contraindications:

• the presence of severe intolerance to any of the medicinal elements;
• drug-induced hepatitis;
• liver failure and aggravated liver pathologies.

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Side effects Pasina

Usually, negative manifestations develop from the nervous system – in the form of polyneuropathy, which is expressed through paresthesia in the limbs. This disorder usually depends on the portion size and often develops in people with “slow” inactivators. Among other signs from the nervous system, occurring sporadically (when using average medicinal doses) are atrophy or neuritis affecting the optic nerve, seizures, memory impairment, encephalopathy or psychosis, which are toxic in nature. Epileptics may experience more frequent epileptic seizures.

Liver damage includes increased transaminase levels, bilirubinemia with hyperbilirubinemia, as well as jaundice and, occasionally, hepatitis. Such side effects mainly develop during the first 3 months of the course; they disappear on their own, without requiring discontinuation of therapy. If serum transaminase values are three to five times higher than normal, the need to continue treatment should be carefully assessed. In older patients, negative symptoms associated with the liver occur more often.

Digestive disorders include vomiting with stomach pain and nausea.

Signs of allergy may be observed - lymphadenopathy, fever, rash (maculopapular, exfoliative, morbiliform or purpuric) and vasculitis.

Hematological manifestations include aplastic, hemolytic or sideroblastic forms of anemia, agranulocytosis, eosinophilia or thrombocytopenia.

It is possible that cardiovascular disorders may develop – pain in the chest area, palpitations and increased blood pressure.

Occasionally, disorders such as SLE, menorrhagia, rheumatic syndrome, and in addition, a tendency to bleeding and gynecomastia appear.

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Overdose

In case of poisoning with Pasin, negative manifestations develop 0.5-3 hours after consuming a large portion. Among the signs are vomiting with nausea and dysarthria, hallucinations that have a visual form, visual clouding, suppression of the cardiovascular system, problems with liver function, and in addition, RDS, hyperglycemia, metabolic acidosis, polyneuropathy, ketonuria, comatose state and convulsions. An overdose develops after consuming a portion of 80-150 mg/kg.

Gastric lavage and activated carbon are used. People who do not have noticeable signs of intoxication (with a known volume of the drug taken) should be given pyridoxine intravenously, at a dosage of 1 mg of the substance per 1 mg of Pasin. With an unknown volume of the dose taken that caused the poisoning, an initial dosage of pyridoxine of 5 mg (adults) or 80 mg/kg (children) is used, over 0.5-1 hour.

People with noticeable signs of poisoning are prescribed treatment that supports vital functions of the body. In addition, pyridoxine is administered by bolus method (if the size of the dose taken is unknown, 5 mg (for adults) or 80 mg/kg (for children)) over 3-5 minutes. If the dose taken is known, pyridoxine is administered in a proportion of 1 mg of the substance per 1 mg of the drug taken. If there is no improvement, pyridoxine can be administered again. A dose of 10 g is often sufficient. There is no information regarding the maximum permissible safe dose of pyridoxine in case of intoxication.

Diazepam may be used if necessary. In addition, phenytoin may be used, but with extreme caution, because it can slow down the metabolism of isoniazid. Procedures are carried out to eliminate the metabolic form of acidosis. If the patient's condition cannot be controlled, peritoneal dialysis or hemodialysis may be used.

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Interactions with other drugs

Para-aminosalicylate Na increases blood levels of isoniazid, competing with it for general metabolic processes, and in addition, it disrupts the absorption of erythromycin with rifampicin and lincomycin. The substance also disrupts the absorption of cyanocobalamin, which can cause anemia.

The absorption of isoniazid within the digestive tract is reduced when combined with antacids.

Pasin can be used together with other anti-tuberculosis drugs.

In case of mixed infection, the drug is combined with other antibacterial substances: sulfonamides, antibiotics with a wide range of activity, and also fluoroquinolones.

Isoniazid inhibits the biotransformation of diphenin with carbamazepine, which is why, when used in combination, their plasma levels increase and the toxic effect is potentiated.

The toxic activity of isoniazid is enhanced when combined with MAOIs.

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Storage conditions

Pasin should be stored in a place closed to small children. Temperature – no more than 25°C.

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Shelf life

Pasin can be used for a period of 36 months from the date of sale of the medicinal substance.

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Application for children

Not used in pediatrics - in children under 3 years of age.

Analogues

Analogues of the drug are the drugs Akurit-3, Tubavit, Paramin with Combitub, Rifampicin plus and Mayrin with Rucox, as well as Mili-cox and Forecox track.

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