Aminosalicylic Acid

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Aminosalicylic acid: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Drug interactions
14. Analogs
15. Terms and conditions of storage
16. Terms of dispensing from pharmacies
17. Reviews
18. Price in pharmacies

Latin name: Aminosalicylic acid

ATX code: J04AA01

Active ingredient: aminosalicylic acid (Aminosalicylic acid)

Producer: PJSC "Kraspharma" (Russia), Sanjivani Paranteral Limited (India), LLC "Skopinsky pharmaceutical plant" (Russia), LLC "Makiz-Pharma" (Russia)

Description and photo update: 2019-10-07

Solution for infusion Aminosalicylic acid

Aminosalicylic acid is an anti-tuberculosis drug.

Release form and composition

Dosage forms:

enteric-coated tablets: pink, oval; core - white with a cream shade or white (dosage 1 g: 10 pcs. in blisters, in a cardboard box 2, 5, 10, 50, 100 packages; 5, 10, 15, 20, 25 pcs. in plastic bags, in a container, 1 bag; 50 or 100 pcs. in polymer cans, in a cardboard box 1, 5, 10, 20 or 50 cans; 500 pcs. in polymer cans, in a cardboard box 1 can; dosage 0, 5 g: 500 pcs. In polymer cans, in a cardboard box 1, 4, 6, 10 cans - for hospitals);
solution for infusion: clear liquid, light yellow or colorless (in bottles: 200 ml - in a cardboard box 1 bottle, in a cardboard box 24 bottles; 400 ml - in a cardboard box 1 bottle, in a cardboard box 12 or 24 bottles);
lyophilisate for the preparation of a solution for infusion: powder from white to light gray (13.49 g each: in vials, in a cardboard box of 1 or 5 bottles; in bottles for blood substitutes, in a cardboard box of 10 bottles).

Each pack also contains instructions for the use of Aminosalicylic Acid.

1 tablet contains:

active substance: sodium para-aminosalicylate - 0.5 or 1 g;
auxiliary components: colloidal silicon dioxide, microcrystalline cellulose, citric acid monohydrate, povidone, stearic acid;
enteric coating: methacrylic acid and ethyl acrylate copolymer, aluminum varnish based on azorubin dye, aluminum varnish based on crimson dye (Ponso 4R), aluminum varnish based on indigo carmine dye, aluminum varnish based on quinoline yellow dye, titanium dioxide, sodium bicarbonate, silicon colloidal, sodium lauryl sulfate, triethyl acetate, talc.

100 ml of solution for infusion contains:

active substance: sodium para-aminosalicylate - 3 g;
auxiliary components: disodium edetate dihydrate - 0.05 g; sodium sulfite - 0.5 g; water for injection - up to 100 ml.

The active ingredient of the lyophilisate for the preparation of a solution for infusion is sodium para-aminosalicylate, its content in 1 bottle is 13.49 g.

Pharmacological properties

Pharmacodynamics

Aminosalicylic acid is an anti-tuberculosis drug that has a bacteriostatic effect. Its active ingredient - sodium salt of aminosalicylic acid, is active against only Mycobacterium tuberculosis [MIC (minimum inhibitory concentration) in vitro is 1–5 μg / ml].

The mechanism of tuberculostatic action is to compete with PABA (para-aminobenzoic acid) for the active site of dihydropteroate synthetase - an enzyme that converts PABA into dihydrofolic acid and suppresses the synthesis of components of the cell wall of microbacteria (inhibits the formation of mycobactin), reducing the uptake of iron by the latter, and / or the synthesis of folic acid microbial cell. It has an effect on mycobacteria in a state of active reproduction and practically does not affect mycobacteria in the resting stage. Weakly acts on the intracellular pathogen. Does not affect other mycobacteria. Primary resistance is rare, secondary resistance develops slowly. Resistance to sodium aminosalicylate develops rapidly against the background of monotherapy, in contrast to other anti-tuberculosis drugs, its therapeutic effect is less pronounced. Therefore, Aminosalicylic acid is used only in combination with other anti-tuberculosis drugs, which helps to slow the development of resistance to them, in particular to streptomycin and isoniazid. It has an irritating effect on the mucous membrane of the gastrointestinal tract (gastrointestinal tract).

Pharmacokinetics

After sodium enters the body, para-aminosalicylate is well absorbed. Easily overcoming histohematogenous barriers, it is actively distributed in tissues. In caseous masses it reaches high concentrations. With inflammation of the meninges, it penetrates into the cerebrospinal fluid to a moderate extent. It is determined in breast milk. After oral administration in a dose of 4 g, C _max (maximum concentration of the substance), which is 75 μg / ml, is reached in 1.5–2 hours. Communication with plasma proteins - 50-60% (when using the drug infusion) or 15% (when using oral aminosalicylic acid).

Undergoes active metabolism (the main pathway is acetylation). It is partially metabolized in the stomach, to a greater extent in the liver (over 50% is acetylated to inactive metabolites).

It is excreted by the kidneys through glomerular filtration (80%), 50% of the dose is determined in the urine as an acetylated derivative. The total clearance of the drug depends on the rate of metabolism of the active substance and excretion by the kidneys. The half-life (T _1/2) in the absence of impaired renal function is 0.5-1 hour, in the presence of chronic renal failure it increases to 23 hours.

Indications for use

The use of Aminosalicylic acid is indicated for the treatment of various forms and localizations of tuberculosis as part of a combination therapy with other anti-tuberculosis drugs.

Most often, the drug is prescribed to patients with multidrug resistance to other anti-tuberculosis drugs, as well as in cases when the appointment of other, stronger anti-tuberculosis drugs is impossible.

Contraindications

Absolute:

kidney disease (severe renal failure, nephritis of non-tuberculous etiology);
liver disease (severe liver failure, hepatitis, liver cirrhosis);
peptic ulcer of the stomach and duodenum;
inflammatory process in the intestine in the acute stage;
edema due to hypernatremia;
arterial hypertension;
decompensated chronic heart failure;
decompensated hypothyroidism;
amyloidosis of internal organs;
myxedema in the stage of decompensation;
epilepsy;
hypocoagulation;
thrombophlebitis;
deficiency of glucose-6-phosphate dehydrogenase;
breast-feeding;
children under 3 years of age (for tablets);
hypersensitivity to aminosalicylic acid or its salts, as well as to other components that make up the drug.

Relative (it is recommended to use Aminosalicylic acid with extreme caution):

dysfunction of the kidneys and / or liver of mild to moderate severity;
a history of gastrointestinal diseases;
chronic heart failure;
acute hepatitis;
compensated hypothyroidism;
diabetes;
period of pregnancy.

Aminosalicylic acid, instructions for use: method and dosage

Pills

Aminosalicylic acid tablets are taken orally 30-60 minutes after a meal.

Recommended dosage:

adults: daily dose - 9-12 g, it is divided into 3 doses;
children from 3 years old: daily dose - at the rate of 0.2 g per 1 kg of the child's weight, it is divided into 3-4 doses.

The maximum daily dose for children should not exceed 10 g, for malnourished adult patients (weighing less than 50 kg) - 6 g.

With good tolerance of the drug, the daily dose in outpatient treatment can be taken in one dose, with poor tolerance, it must be divided into several doses.

Solution for infusion and lyophilisate for preparation of solution for infusion

Intravenous (IV) administration is indicated by infusion over 2-4 hours. The initial rate is 30 drops per minute, in the absence of general and local reactions, it can be increased to 40-60 drops per minute.

Recommended daily dosage:

patients over the age of 14: 10-15 g each;
children aged 7 to 14 years: at the rate of 0.2 g per 1 kg of the child's weight;
children under 7 years of age (including premature infants): 0.2–0.3 g per 1 kg of the child's weight.

The maximum daily dose for children should not exceed 10 g, for malnourished adult patients (weighing less than 50 kg) - 6 g.

At the first infusion, no more than 250 ml of the drug is administered. In the future, if there are no side reactions, increase to 500 ml 5-6 times a week or every other day (alternating with taking the tablet form of Aminosalicylic acid). The course can be from 1 to 2 months or more. The doctor determines the total duration of treatment and the number of courses individually, taking into account the severity of the disease.

If the use of the drug is required for a long period of time, measures should be taken to maintain the electrolyte balance. For this purpose, potassium salts are prescribed orally or by adding the required amount of an appropriate potassium preparation for infusion, based on the results of a preliminary assessment of the plasma potassium concentration.

Side effects

Pills

cardiovascular system and blood system (hematopoiesis, hemostasis): impaired prothrombin synthesis, hemolytic anemia (in patients with glucose-6-phosphate dehydrogenase deficiency), eosinophilia, thrombocytopenia, leukopenia (up to agranulocytosis), B ₁₂ -deficient megaloblastic anemia;
digestive system: nausea, vomiting, loss / deterioration of appetite, flatulence, diarrhea / constipation, abdominal pain, increased activity of hepatic transaminases, hyperbilirubinemia, hepatomegaly, drug hepatitis, jaundice;
genitourinary system: crystalluria, hematuria, proteinuria;
allergic reactions: urticaria, purpura, enanthema, drug fever, bronchospasm, arthralgia, a syndrome similar to infectious mononucleosis;
others: hypothyroidism, goiter, myxedema (with prolonged use in high doses), hypokalemia, renal failure, arthralgia, lymphadenopathy, hepatosplenomegaly, encephalitis; in isolated cases - psychosis.

Solution for infusion and lyophilisate for preparation of solution for infusion

Adverse reactions from systems and organs (listed according to the following frequency of occurrence: very often - ≥ 1/10; often - ≥ 1/100 and <1/10; infrequently - ≥ 1/1000 and <1/100; rarely - ≥ 1/10 000 and <1/1000; very rare - <1/1000; unknown frequency - the frequency cannot be determined from the available data):

blood and lymphatic system: rarely - neutropenia, thrombocytopenia, leukopenia (up to agranulocytosis), megaloblastic anemia, eosinophilia, hemolytic anemia with a positive Coombs test, B ₁₂ deficiency anemia, lymphocytosis (the effect on the blood is allergic and toxic; these phenomena reversible); unknown frequency - an increase in prothrombin time with petechiae or hemorrhagic purpura (with repeated or prolonged use of aminosalicylic acid);
endocrine system: very often - hypothyroidism (especially with the introduction of aminosalicylic acid in conjunction with prothionamide / ethionamide in patients with HIV infection), antithyroid action, myxedema; often - suppression of the function of the thyroid gland with the formation of diffuse goiter (in particular, when taking high doses of aminosalicylic acid);
nervous system: unknown frequency - psychosis, paralysis symptoms, clonic-tonic convulsions;
respiratory system, chest and mediastinal organs: unknown frequency - Leffler's syndrome (allergic pulmonary infiltration, eosinophilic pneumonia);
immune system: often - allergic reactions, mainly skin reactions, such as itching, rash (urticaria, exfoliative dermatitis, purpura, lymphoma-like syndrome or infectious mononucleosis, enanthema); rarely - severe allergic reactions [Stevens-Johnson syndrome, exudative erythema multiforme, toxic epidermal necrolysis (Lyell's syndrome)], lupus-like syndrome involving the spleen, kidneys, liver, gastrointestinal tract and nervous system (for example, stiff neck, radicular pain), joint swelling, angioedema, arthralgia, bronchospasm, drug fever [allergic reactions may occur after a few days, although they generally appear between the second and seventh weeks of therapy (most often in the fourth or fifth week)], anaphylactic shock;
liver and biliary tract: rarely - increased activity of hepatic transaminases without / with jaundice, hyperbilirubinemia; unknown frequency - drug hepatitis, liver failure (approximately 25% of patients with an allergic reaction to aminosalicylic acid have liver damage, which in 10% of cases can lead to liver failure and death);
kidneys and urinary tract: often - microhematuria, cylindruria, albuminuria (are temporary and mild); infrequently - hyperglycemic / normoglycemic glucosuria; unknown frequency - an increase in the plasma concentration of urea (especially in patients with impaired renal function and acidosis; renal function must be monitored), crystalluria, proteinuria;
Gastrointestinal tract: very often - nausea, vomiting, heartburn, excessive salivation, stomach discomfort, flatulence, diarrhea, loss / decrease in appetite (as a rule, they occur mildly and quickly disappear after completion of therapy; often develop when taking high doses of aminosalicylic acid due to partial excretion through the intestine, including during infusion); infrequently - colicky abdominal pain (with excessive infusion rate); unknown frequency - bleeding from a peptic ulcer;
metabolism and nutrition: rarely - serious violations of the water and electrolyte balance, mainly in the form of hypokalemia (with the introduction of high doses of Aminosalicylic acid, especially in elderly patients with arterial hypertension and edema, as well as in patients with meningitis; the administration of large doses of the drug leads to loss of cations, which can cause the appearance of acidosis, which is most often observed in children);
infections and parasitic diseases: unknown frequency - superinfections (with repeated or prolonged use of aminosalicylic acid);
others: pericarditis, hypoglycemia, optic neuritis, encephalopathy, vasculitis, decreased prothrombin.

Overdose

Symptoms: Possible aggravation of dose-related adverse events.

Treatment: if an overdose is detected, the use of Aminosalicylic acid should be discontinued and symptomatic therapy should be prescribed. In case of an overdose of tablets, an urgent gastric lavage is indicated.

special instructions

Aminosalicylic acid is recommended to be prescribed in combination with other anti-tuberculosis drugs.

Please note that the presence of aminosalicylates interferes with the results of glucosuria tests if the reagents used contain copper.

When the first signs indicating an allergic reaction appear, you should immediately stop taking the drug and conduct desensitizing therapy. During treatment, it is recommended to regularly conduct blood and urine tests and check the functional state of the liver. In the course of treatment, it is important to control the activity of hepatic transaminases. If, against a background of specific lesions and tuberculous intoxication, renal function decreases, this is not a contraindication to the appointment of aminosalicylic acid. If hematuria / proteinuria develops, the drug should be temporarily discontinued.

With an increase in the activity of hepatic transaminases, the appearance of jaundice, fever or other symptoms of liver dysfunction, it is necessary to interrupt therapy with Aminosalicylic acid and perform a study of the functional state of the liver, since liver damage may be irreversible.

Patients with severe renal / hepatic insufficiency are contraindicated to use the drug due to the possible accumulation of acetyl metabolites.

Aminosalicylic acid must be used with caution in patients with liver damage, for example, acute hepatitis (caused by reduced tolerance to aminosalicylic acid) and impaired hepatic function (due to lack of data on the use in patients with pre-existing liver damage), a history of gastrointestinal diseases, for example, gastritis, gastric and duodenal ulcers (increased risk of exacerbation), as well as patients with impaired renal function [increased risk of uremic acidosis (accumulation of acetyl metabolites)].

To prevent crystalluria, it is necessary to alkalize urine, especially acidic urine.

Patients with diabetes mellitus need to monitor the concentration of glucose in the blood plasma.

While taking aminosalicylic acid, hypothyroidism may develop. The risk of this disease is especially increased when the drug is administered simultaneously with prothionamide / ethionamide to patients with HIV infection. It is necessary to monitor the functional state of the thyroid gland before therapy and regularly during treatment with Aminosalicylic acid, especially when taken in combination with protionamide / ethionamide.

To avoid complications at the injection site, it is recommended to alternate the veins.

The use of aminosalicylic acid can give false positive results in the non-enzymatic determination of glucose and urobilinogen in urine.

Influence on the ability to drive vehicles and complex mechanisms

The effect of aminosalicylic acid on the ability to drive vehicles and perform other actions requiring a high concentration of attention and speed of psychomotor reactions has not been studied. Patients should be warned about the possibility of seizures, paralysis. When the described undesirable phenomena appear, it is necessary to refrain from performing the above activities.

Application during pregnancy and lactation

There are suggestions that the aminosalicylates used in the first trimester of pregnancy can cause birth defects in the fetus. In this regard, the use of aminosalicylic acid during gestation is allowed only if the intended benefit to the mother exceeds the possible risk to the fetus.

The drug is excreted in breast milk, therefore it is contraindicated during lactation.

Pediatric use

Aminosalicylic acid tablets are not used in children under 3 years of age due to the solid dosage form.

Solution for infusion and lyophilisate for preparation of solution for infusion are used in pediatrics using age-appropriate dosages.

With impaired renal function

The use of aminosalicylic acid is contraindicated for the treatment of patients with severe renal failure.

Special care should be taken for mild to moderate renal impairment.

For violations of liver function

The use of Aminosalicylic acid is contraindicated for the treatment of patients with severe hepatic insufficiency, hepatitis, and cirrhosis of the liver.

Special care should be taken for mild to moderate liver dysfunctions.

Drug interactions

isoniazid: sodium para-aminosalicylate, when used simultaneously with isoniazid, increases its plasma concentration and T _1/2 due to competition for common metabolic pathways (if combined use with aminosalicylic acid is necessary, control of a possible increase in isoniazid toxicity should be monitored);
capreomycin: it is possible to reduce the concentration of potassium and pH, increase electrolyte disturbances;
antacids: the absorption of aminosalicylic acid is not impaired;
barbiturates, estrogens, sulfonamides, which reduce blood glucose: the tuberculostatic effect of aminosalicylic acid is weakened;
insulin: the tuberculostatic effect of aminosalicylic acid increases;
probenecid: the excretion of aminosalicylic acid decreases, which can lead to an increase in the toxicity of the drug (due to impaired renal excretion and an increase in plasma concentration);
digoxin: when taken orally with aminosalicylic acid, its absorption from the gastrointestinal tract is reduced by 40% (the relevance of this interaction for intravenous administration is unknown, but is estimated as low);
cyanocobalamin (vitamin B ₁₂): when taken orally with aminosalicylic acid, its absorption is impaired, due to which B ₁₂ deficiency anemia may develop (the relevance of this interaction for intravenous administration is unknown; when symptoms of B ₁₂ deficiency anemia appear, the introduction of cyanocobalamin is recommended);
erythromycin, rifampicin, lincomycin: their effectiveness decreases (due to malabsorption);
phenytoin: an increase in its plasma concentration is possible (if combined use with aminosalicylic acid is necessary, a possible increase in phenytoin toxicity should be monitored);
ethionamide: the risk of side effects of aminosalicylic acid increases, especially from the gastrointestinal tract, as well as liver toxicity and hypothyroidism (it is necessary to monitor the functional state of the liver / thyroid gland; if the severity of side effects worsens, ethionamide therapy should be discontinued);
salicylates, phenylbutazone and other anti-inflammatory drugs with the ability of high binding to blood plasma proteins: the concentration increases and the duration of the presence of aminosalicylic acid in the blood plasma increases; with the combined use of salicylates with acetylsalicylic acid, the additive nature of the side effects of each drug should be taken into account;
folic acid: aminosalicylic acid reduces the absorption of folic acid, which contributes to an increase in the toxicity of folic acid antagonists, for example, methotrexate (if combined use is necessary, it is necessary to monitor possible toxicity);
indirect anticoagulants - derivatives of indandione and coumarin: their effect is enhanced (it is required to adjust the dose of anticoagulants);
iodine-containing thyroid hormones, their analogues and antagonists (including antithyroid drugs): while taking aminosalicylic acid, the plasma concentration of thyroid stimulating hormone and thyroxine changes;
diphenhydramine: the effectiveness of aminosalicylic acid decreases;
ammonium chloride: the risk of developing crystalluria increases;
solutions of protionamide and rifampicin: pharmaceutically incompatible with acetylsalicylic acid (it is contraindicated to enter them in the same mixture simultaneously with aminosalicylic acid; these solutions should be administered separately).

Aminosalicylic acid is compatible with other anti-tuberculosis drugs.

Analogs

Analogues of Aminosalicylic acid are: PASK-Acri, Sodium para-aminosalicylate, Pasconat, Sodium para-aminosalicylate, Aquapask, Verpas-SR, PASK sodium salt, PASK, Paser, PAS-Fatol N, PAS Sodium, Monopas, Simpas, Amiktobin, Sodium aminosalicylate dihydrate, Faminosalk, MAK-PAS, Sodium para-aminosalicylate-Binergy.

Terms and conditions of storage

Keep out of the reach of children.

Store at a temperature: tablets - up to 25 ° C in a place protected from moisture and light, solution - up to 15 ° C in a dark place (do not freeze), lyophilisate for preparation of solution for infusion - up to 25 ° C in a dark place …

Shelf life: tablets, solution - 2 years, lyophilisate - 4 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Aminosalicylic acid

There are no reviews of Aminosalicylic acid on social networks.

Price for Aminosalicylic acid in pharmacies

The price of Aminosalicylic acid for a package containing 1 bottle of infusion solution (200 ml) can be from 640 rubles, 400 ml - from 1281 rubles; for 1 bottle of lyophilisate for preparation of solution for infusion - from 2200 rubles; for 1 can (500 pcs.) of tablets - from 16 308 rubles.

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!