Lysine acetylsalicylate - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Included in the formulation

АТХ:

N.02.B.A Salicylic acid and its derivatives

Pharmacodynamics:

The anti-inflammatory effect of the drug is explained by its effect on the processes taking place in the inflammatory focus: a decrease in the permeability of capillaries, a decrease in the activity of hyaluronidase, a restriction of the energy supply of the inflammatory process by inhibiting the formation of adenosine triphosphate,

The drug inhibits cyclooxygenase-1 and cyclooxygen-2, reduces the synthesis of prostaglandins and thromboxane A2 from arachidonic acid, including in platelets. In small doses, the only selective irreversible cyclooxygenase-1 inhibitor in platelets, which reduces platelet aggregation.

The anti-inflammatory effect of acetylsalicylic acid is due to inhibition of cyclooxygenase-2 activity, which leads to a decrease in the production of inflammatory mediators - PGD2, E2 and I2.

The analgesic effect is associated with a decrease in the synthesis of PGE2, which prevents sensitization of pain receptors to bradykinin, histamine, and other chemicals synthesized or released in the inflammatory focus.

Antipyretic effect is also caused by the disruption of the production of eicosanoide PGE2, which, when inflamed, stimulates the thermoregulatory center in the anterior parts of the hypothalamus. Acetylsalicylic acid and other non-steroidal anti-inflammatory drugs reduce febrile body temperature by increasing heat transfer as a result of increased sweating and widening of peripheral vessels, while normal body temperature does not decrease.

Pharmacokinetics:

When ingested quickly and fairly fully absorbed in the gastrointestinal tract. Binding to plasma proteins - 80-90%. Penetrates into most body tissues. In the blood it hydrolyzes, forming acetylsalicylic acid and lysine. Acetylsalicylic acid in the liver turns into salicylic. PElimination half-life (half-life) of the drug Acetylsalicylic acid - 15-20 minutes, salicylic acid and its active metabolites from 3-6 hours (small doses) to 15-30 hours (high doses).

Biotransformation of salicylates occurs in the liver. Elimination by the kidneys, in the form of free salicylic acid and conjugated metabolites.

Indications:Feverish syndrome with infectious and inflammatory diseases; pain syndrome of different genesis, incl. rheumatic pain, toothache, neuralgia, myalgia, arthralgia, pain in the postoperative period,algodismenorea; thrombosis and thromboembolism (prophylaxis), myocardial infarction (secondary prevention).

ICD-10

XIII.M05-M14.M05 Seropositive rheumatoid arthritis

XVIII.R50-R69.R50 Fever of unknown origin

XVIII.R50-R69.R52.9 Pain, unspecified

XVIII.R50-R69.R52.0 Acute pain

IX.I20-I25.I25.2 Postponed myocardial infarction

IX.I80-I89.I82.9 Embolism and thrombosis of unspecified vein

IX.I70-I79.I74.9 Embolism and thrombosis of unspecified arteries

XIII.M20-M25.M25.5 Pain in the joint

XIII.M70-M79.M79.1 Myalgia

XIII.M70-M79.M79.2 Neuralgia and neuritis, unspecified

Contraindications:Hypersensitivity; erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation), gastrointestinal bleeding; complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including in anamnesis); Hemophilia, hemorrhagic vasculitis, hypoprothrombinemia, portal hypertension; avitaminosis K; kidney failure; deficiency of glucose-6-phosphate dehydrogenase, children's age (up to 15 years - the risk of developing Reye's syndrome in children with hyperthermia in the presence of viral diseases), pregnancy (I and III trimester), breast-feeding.

Carefully:

Gout, erosive-ulcerative diseases of the gastrointestinal tract in the anamnesis, menorrhagia, presence of intrauterine contraceptive.

When used in large doses close to the maximum, especially when administered intravenously to people with a high risk of thrombosis, it is possible to increase the aggregation activity of platelets, in this regard, it is more appropriate to intramuscular administration of the drug.

Pregnancy and lactation:

Category of recommendations for Food and Drug Administration (US Food and Drug Administration) not determined.

Contraindicated in the I and III trimesters of pregnancy and lactation (breastfeeding). In the second trimester of pregnancy, one-time administration is possible on strict indications.

Dosing and Administration:

Inside, intravenously, intramuscularly, rectally. The dose, route of administration and duration of administration are determined individually, depending on the indications, the effectiveness of the therapy, the tolerability of the drug, the age of the patient,

Inside (in terms of acetylsalicylic acid), adults - 500-1000 mg (the contents of 1-2 bags are dissolved in a small amount of water) 2-3 times a day (maximum daily dose - 6 g).Children - 25-50 mg / kg per day in 4-6 receptions (maximum daily dose: at the age of 30 months - 80 mg / kg, from 30 months to 15 years - 100 mg / kg).

Intravenous (jet or drip) and intramuscularly (deep): adults - 500-1000 mg (1-2 bottles) 1-2 times a day (the maximum daily dose is 4 g). Children under the age of 6 years - 10-25 mg / kg per day, from 6 to 10 years - 250-500 mg per day, over 11 years - 500-1000 mg per day.

As an antiaggregant - 1 packet of 100 (pediatric form) or 250 mg once a day for a long time.

Suppositories: rectally; as an antiaggregant drug, adults - 0.2-0.6 g once a day, the course of treatment - up to 2 weeks, then switch to oral intake. In gynecology - 0.6 g for 5-10 days.

Side effects:

From the digestive system: gastropathy associated with the use of non-steroidal anti-inflammatory drugs (dyspepsia, epigastric pain, nausea and vomiting, diarrhea, gastrointestinal bleeding), exacerbation of peptic ulcer of stomach and duodenum, decreased appetite, hepatotoxicity.

From the cardiovascular system and blood: hemorrhagic syndrome.

From the central nervous system: when used in high doses or long-term use - there may be a noise in the ears, a decrease in the severity of hearing, severe headaches.

Allergic reactions: rarely - angioedema, urticaria, bronchospasm, anaphylactic shock.

Other: rarely - hemorrhagic syndrome (nosebleeds, bleeding gums, up to vomiting blood, melena), iron deficiency anemia (as a consequence of hidden or obvious bleeding from the gastrointestinal tract), exacerbation of bronchial asthma, nephrotoxicity, Reye syndrome in children, metabolic acidosis.

Overdose:

Symptoms: confusion, diarrhea, abdominal pain, headache, dizziness, drowsiness, rapid or deep breathing, nausea, vomiting, visual impairment, tinnitus, hearing loss.

Severe overdose: blood in the urine, convulsions, hallucinations, increased excitability, agitation, confusion, shortness of breath or excruciating breath, fever, respiratory alkalosis, metabolic acidosis, hyperglycemia, hypoglycemia, ketonuria, hyponatremia, hypokalemia.

Treatment is symptomatic; hemodialysis, peritoneal dialysis, hemoperfusion, correction of the acid-base state (infusion of solutions of sodium bicarbonate, sodium citrate).

Interaction:

Strengthens the effect of methotrexate, oral hypoglycemic agents (derivatives of sulfonylureas), weakens - uricosuric agents. It potentiates the ulcerogenic effect of corticosteroids, other non-steroidal anti-inflammatory drugs and reserpine. The risk of bleeding increases with simultaneous application with direct and indirect anticoagulants, fibrinolytic agents and antiaggregants.

Vancomycin increases the risk of development of ototoxicity. Probenecid, sulfinpyrazone increase the toxicity lysine acetylsalicylate.

Funds alkalinizing urine (inhibitors of carbonic anhydrase, citrates, sodium bicarbonate, antacids, especially calcium and / or magnesium-containing), with prolonged use - accelerate excretion and decrease efficiency lysine acetylsalicylate.

Cefamandol, cefoperazone, cefotetan, plikamycin, valproic acid - increase the risk of bleeding, the toxicity of valproic acid.

Ciprofloxacin, lomefloxacin, norfloxacin, ofloxacin, enoxacin, itraconazole, ketoconazole, tetracycline - lysine acetylsalicylate reduces their absorption and effectiveness. It is necessary to separate the reception in time.

Do not mix the injectable solution of lysine acetylsalicylate with solutions of other drugs.

Special instructions:

1.8 g of lysine acetylsalicylate corresponds to 1 g of acetylsalicylic acid. Preparations containing lysine acetylsalicylate in an amount corresponding to 1 g of acetylsalicylic acid, are intended only for adults and children over 6 years of age.

If there is any history of gastric ulcer and duodenal ulcer or bleeding from the gastrointestinal tract, the expected benefit of therapy and the potential risk should be compared.

When using lysine acetylsalicylate, an increase in the bleeding time is observed, which persists for 4-8 days after discontinuation, this must be taken into account when performing a surgical procedure.

Overdose should be avoided, especially in young children and in elderly patients.

Instructions

Lysine acetylsalicylate (Lysini acetylsalicylas)