Aminosalicylic acid - instructions for use, dose, side effects, contraindications

Composition: active substance: sodium aminosalicylate in terms of dry matter - 3000 mg; Excipients: sodium sulfite - 500 mg; disodium edetate dihydrate -50 mg; water for injection - up to 100 ml.

Description:colorless or light yellow transparent liquid.

Pharmacotherapeutic group:antiviral [HIV] agent

ATX: & nbsp

J.04.A.A.01 Aminosalicylic acid

Pharmacodynamics:

Aminosalicylic acid has a bacteriostatic effect against Mycobacterium tuberculosis..This reduces the probability of development of bacterial resistance to streptomycin and isoniazid, mechanism of action associated with inhibition of folate synthesis and suppression of formation mikobaktina, mycobacterial component wall, which leads to a reduction of iron capture M. tuberculosis.

Aminosalicylic acid acts on the mycobacteria that are in the active state propagation, and virtually no effect on Mycobacterium in the resting stage. Slightly affects the pathogen, located intracellularly.

Aminosalicylic acid is active only in relation to M. tuberculosis. Does not affect other non-tuberculous mycobacteria.

Pharmacokinetics:

Features of clinical pharmacology amino salicylic acid - a quick education in the acidic environment of toxic inactive metabolite and short half-life in the blood serum were unrelated to the drug one hour.

Metabolised in the liver and partially in the stomach. 80% of aminosalicylic acid is excreted in urine, and more than 50% is excreted in acetylated form. Process Acetylation is not genetically determined, as is the case with isoniazid. Sodium para-aminosalicylate is excreted by glomerular filtration.

In the cerebrospinal fluid the drug penetrates only with inflammation of the meninges.

About 50 - 60% of aminosalicylic acid binds to proteins.

Indications:Different forms and localization of tuberculosis in combination with other anti-TB drugs. Most often, aminosalicylic acid is prescribed for patients with multiple drug resistance to other anti-tuberculosis drugs.

Contraindications:Hypersensitivity to aminosalicylic acid (including other salicylates), other components of the drug; severe kidney and liver diseases (renal and / or liver failure, non-tuberculous etiology nephritis, hepatitis, liver cirrhosis); uncompensated chronic heart failure; peptic ulcer, stomach and duodenum; inflammatory bowel disease in the acute stage; decompensated hypothyroidism, epilepsy.

Carefully:

Hepatic insufficiency of medium degree, deficiency of glucose-6-phosphate dehydrogenase, compensated hypothyroidism.

Pregnancy and lactation:Use during pregnancy is possible if the expected benefit for the mother exceeds potential risk to the fetus. For the duration of the drug should stop breastfeeding.

Dosing and Administration:

Intravenously (intravenously), drip: adults and children over 14 years 10-15 g / day; children under 14 years of age - 200-300 mg / kg / day.

Begin with 30 drops per minute and after 15 minutes, in the absence of local and general reactions increase to 40 - 60 drops per minute.

At the first injection, inject no more than 250 ml of the drug, in the absence of side effects - 500 ml of the drug, 5 - 6 times a week or every other day (alternating with ingestion of the tablet form). The course of treatment is 1-2 months or more. The number of courses and the total duration of treatment are determined individually, depending on the severity of the disease.

Side effects:

From the digestive system: decrease or loss, appetite, increased salivation, nausea, vomiting, flatulence, abdominal pain, diarrhea, or constipation; rise activity of "hepatic" transaminases, hyperbilirubinemia, jaundice; drug hepatitis (including fatal).

From the hematopoiesis: thrombocytopenia, leukopenia (up to agranulo-cytosis), B 12-deficiency anemia, hemolytic anemia with a positive breakdown of Coombs.

From the genitourinary system: proteinuria, hematuria, crystalluria.

Allergic reactions: rash (hives, purpura, enanthema, exfoliative dermatitis, a syndrome reminiscent of infectious mononucleosis or lymphoma), fever, bronchospasm, arthralgia, eosinophilia.

Other: antithyroid action; zobogenic effect, drug hypothyroidism, myxedema; pericarditis, hypoglycemia, optic neuritis, encephalopathy, Leffler's syndrome (eosinophilic pneumonia, migratory pulmonary infiltrate), vasculitis, a decrease in prothrombin content.

If any of the side effects listed in the manual are aggravated, or any other side effects not indicated in the instructions are noted, the doctor should be informed immediately.

Overdose:

Symptoms: may increase dose-related side effects.

Treatment: withdrawal of the drug, symptomatic therapy.

Interaction:

Aminosalicylic acid disrupts the absorption of rifampicin, erythromycin and lincomycin. Aminosalicylic acid violates the absorption of vitamin B12, resulting in the possible development of anemia. The use of the drug together with isoniazid or phenytoin leads to an increase in the duration, the presence of isoniazid or phenytoin in the blood plasma. The use of the drug along with salicylates, phenylbutazone or other anti-inflammatory drugs with increased ability to bind proteins, leads to an increase in the concentration and increase in the duration of the presence of aminosalicylic acid in the blood plasma. The use of the drug together with diphenhydramine leads to a decrease in the concentration of aminosalicylic acid in the blood plasma.

Aminosalicylic acid inhibits the absorption of folic acid and can enhance the toxicity of folic acid antagonists, such as, for example, methotrexate.

Reduces the concentration of digoxin in the blood by 40%. Strengthens the effect of indirect anticoagulants - derivatives of coumarin and indanedione (correction of the dose of anticoagulants is required). When using iodine-containing hormones of the thyroid gland, their analogs and antagonists (including antithyroid agents)that against a background of para-aminobenzoic acid the concentration of thyroxine and thyroid-stimulating hormones in the blood changes. Ammonium chloride increases the risk of developing crystalluria. Simultaneous use with ethionamide increases the risk of hepatotoxicity.

Incompatibilities with other drugs: Aminosalicylic acid should not be administered simultaneously with solutions of rifampicin and protionamide in the total mixture; this medication should be administered separately.

Special instructions:

During treatment, it is necessary to regularly perform blood and urine tests, monitor liver function (activity of "liver" transaminases). To prevent the formation of crystals, it is necessary to "alkalize" the urine, especially having an acid reaction. Sometimes a non-enzymatic determination of glucose and urobilinogen in the urine can give erroneous positive results.

After the expiry date of the drug, unused bottles should be carefully opened, the contents drained into the sewerage system.

Effect on the ability to drive transp. cf. and fur:There is no data on the study of adverse effects of aminosalicylic acid on the ability to drive vehicles and engage in potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Solution for infusions 30 mg / ml.

Packaging:

A solution for infusions of 30 mg / ml on 200 ml, 400 ml in bottles glass. Bottle from instructions for use in a pack of cardboard.

For hospitals:

24 bottles of 200 ml, 12 bottles of 400 ml without packs with an equal number of instructions for use in a box of corrugated cardboard;

1 bottle from instructions for use (from 1 to 24 bottles of 200 ml, from 1 to 12 bottles of 400 ml with an equal number of instructions for use) without a bundle in a box of corrugated cardboard.

Storage conditions:In the dark place at a temperature of no higher than 15 FROM. Do not freeze.

Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-001571

Date of registration:06.03.2012

The owner of the registration certificate:KRASFARMA, JSC KRASFARMA, JSC Russia

Manufacturer: & nbsp

KRASFARMA, JSC Russia

Information update date: & nbsp06.03.2012

Illustrated instructions

Instructions

Aminosalicylic acid (Aminosalicylic asid)