Acetylsalicylic acid + Caffeine - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

NSAIDs - Salicylic acid derivatives

Included in the formulation

Aspirate® plus

pills inwards

VALENTA PHARM, PAO Russia

АТХ:

N.02.B.A.71 Acetylsalicylic acid in combination with psycholeptics

Pharmacodynamics:

Combined drug, the effect of which is due to its constituent components. Acetylsalicylic acid has anti-inflammatory, antipyretic and analgesic effect, inhibits the aggregation of platelets. Caffeine increases the reflex excitability of the spinal cord, excites the respiratory and vasomotor centers, dilates the blood vessels of skeletal muscles, brain, heart, kidneys, reduces platelet aggregation; reduces drowsiness, a feeling of fatigue, increases mental and physical performance.

Pharmacokinetics:

Acetylsalicylic acid

Absorption is complete, fast. During absorption, it undergoes presystemic elimination in the intestinal wall and in the liver (deacetylated). Half-Elimination (half-life) - 15-20 minutes, quickly hydrolyzed to salicylates (in the gastrointestinal tract, liver and blood). In the body it circulates (75-90% in association with albumin) and is distributed in tissues as an anion of salicylic acid. Concentration of the substance in plasma (serum) of blood is reached in about 2 hours. When biotransformation in the liver formed metabolites, found in many tissues and urine. Excretion of salicylates is carried out mainly by active secretion in the tubules of the kidneys in unmodified form and in the form of metabolites. Excretion of unchanged substance and metabolites depends on the pH of the urine (urine alkalinization increases the ionization of salicylates, their reabsorption deteriorates and the excretion increases significantly).

Caffeine

Caffeine and its water-soluble salts are well absorbed in the intestine (including fat). The half-elimination (half-life) period is about 5 hours, in some individuals - up to 10 hours. The main part is demethylated and oxidized. About 10% is excreted by the kidneys unchanged.

Indications:

Moderately or mildly expressed pain syndrome of various origins (headache, toothache, migraine, neuralgia, arthralgia, lumbago, radicular syndrome, muscle pain, menstruation pain).

The raised temperature of a body at cold and other infectious-inflammatory diseases (at adults and children is more senior 15 years).

ICD-10

VI.G40-G47.G43 Migraine

X.J10-J18.J10 Influenza caused by an identified influenza virus

XIII.M50-M54.M54.4 Lumbago with sciatica

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

XIV.N80-N98.N94.6 Dysmenorrhea, unspecified

XVIII.R50-R69.R50.0 Fever with chills

XVIII.R50-R69.R51 Headache

Contraindications:

Hypersensitivity to acetylsalicylic acid, other non-steroidal anti-inflammatory drugs, xanthines and other components of the drug;

Erosive-ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation).

Gastrointestinal bleeding.

Hemophilia, hemorrhagic diathesis, hypoprothrombinemia.

Bronchial asthma induced by the intake of salicylates and other non-steroidal anti-inflammatory drugs.

Complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid.

Organic diseases of the cardiovascular system (including acute myocardial infarction, atherosclerosis, exfoliating aortic aneurysm).

Hypertension, portal hypertension.

Glaucoma.

Renal failure.

Anxiety disorders, increased excitability, sleep disturbance.

Lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Simultaneous reception with methotrexate in a dose of more than 15 mg per week.

Children under 6 years of age with pain syndrome (for this dosage form).

Children and adolescents under the age of 15 years (when used as an antipyretic) with acute respiratory infections caused by viral infections, due to the risk of developing Reye's syndrome (encephalopathy and acute fatty liver disease with acute development of liver failure).

Pregnancy (I and III trimester).

Lactation period.

Carefully:

With caution appoint for gout, hyperuricemia, tk. acetylsalicylic acid in small doses can provoke a gout attack in patients with predisposition to develop gout (with reduced excretion of uric acid from the body). Care should be taken in the presence of an anamnesis of ulcerative lesions of the gastrointestinal tract, gastrointestinal bleeding, renal and hepatic insufficiency. Also, care should be taken with vitamin K deficiency and glucose-6-phosphate dehydrogenase deficiency.

Simultaneous intake of acetylsalicylic acid with methotrexate in doses less than 15 mg per week can lead to an increased incidence of side effects from the hematopoiesis.

The use of acetylsalicylic acid can cause bronchospasm in patients with bronchial asthma, hay fever, polyposis of the nasal mucosa, chronic diseases of the respiratory tract, allergic reactions to other medicines.

It should be borne in mind that with simultaneous use with acetylsalicylic acid, the action of heparin and indirect anticoagulants is enhanced.

Care should be taken for persons with epilepsy and who are prone to seizures, in view of the fact that caffeine reduces the protective effect of antiepileptic drugs.

Pregnancy and lactation:

Recommendations Food and Drug Administration (The US Food and Drug Administration isThe category is not defined.

It has a teratogenic effect: when applied in the first trimester of pregnancy, the fetal splitting of the upper sky occurs, in the third trimester it causes inhibition of labor (suppression of the synthesis of prostaglandins), premature closure of the arterial duct in the fetus,hyperplasia of pulmonary vessels and hypertension in a small circle of blood circulation. Reception of the drug in the II trimester is possible if the potential benefit to the mother exceeds the risk to the fetus.

Salicylates and their metabolites penetrate into breast milk in small amounts, breastfeeding should be stopped for the duration of treatment.

Dosing and Administration:

Inside. To reduce the irritant effect on the gastrointestinal tract, the drug should be taken after meals, washed down with water, milk, alkaline mineral water.

For treatment of pain and increased body temperature adults and children over 15 years of 1-2 tablets; maximum single dose of 2 tablets; the maximum daily dose of 6 tablets.

For the treatment of pain, except for conditions with acute respiratory infections caused by viral infections (risk of developing Reye's syndrome), children aged 6 to 12 years, 1/2 tablet, 12 to 15 years 1 / 2-1 tablet.

If necessary, take a single dose 3-4 times a day with an interval of at least 4 hours. The duration of treatment (without consulting a doctor) should not exceed 7 days when prescribed as an anesthetic and 3 days - as an antipyretic.

Side effects:

From the gastrointestinal tract: nausea, decreased appetite, gastralgia, diarrhea.

From the hemopoietic system: thrombocytopenia, anemia, leukopenia. Allergic reactions: skin rash, angioedema, bronchospasm.

From the central nervous system: insomnia.

From the cardiovascular system: tachycardia, increased blood pressure.

Other: impaired liver and / or kidney function; Reye syndrome (encephalopathy and acute fatty liver dystrophy with rapid development of liver failure).

With prolonged use, dizziness, headache, vomiting, erosive and ulcerative lesions of the gastrointestinal tract, hypocoagulation, bleeding (including in the gastrointestinal tract), visual impairment, decreased ear aches, tinnitus, bronchospasm, interstitial nephritis, prerenal azotemia with hypercreatinemia and hypercalcemia, papillary necrosis, acute renal failure, nephrotic syndrome, aseptic meningitis, increased symptoms of chronic heart failure, edema, increased activity of "liver" transaminases.

Overdose:

Symptoms: with mild poisoning - salicylism syndrome (nausea, vomiting, tinnitus, visual impairment, dizziness, severe headache, general malaise, fever - poor prognostic sign in adults).

With a significant overdose - confusion, drowsiness, convulsions and coma, tremor, noncardiogenic pulmonary edema, dyspnea, choking, water-electrolyte balance disorders, renal failure, collapse and shock.

The greatest risk of chronic intoxication is observed in the elderly with a dose of more than 100 mg / kg per day for several days. In children and elderly patients, the initial signs of salicylism are not always noticeable, so it is advisable to periodically determine the salicylate content in the blood: a concentration above 70 mg% indicates moderate or severe poisoning; above 100 mg% - about extremely severe, prognostically unfavorable. With moderate and severe poisoning, hospitalization is necessary.

Treatment: provocation of vomiting, the appointment of activated carbon and laxatives, alkalinization of urine (shown at salicylate concentrations above 40 mg%intravenous infusion of sodium bicarbonate - 88 meq per 1 liter of 5% dextrose solution, at a rate of 10-15 ml / kg per hour), recovery of circulating blood volume and induction of diuresis (achieved by adding sodium bicarbonate solution at the same dose and dilution, repeat 2 -3 times); it should be borne in mind that intensive fluid infusion of the elderly can lead to pulmonary edema. We do not recommend the use of acetazolamide for alkalinization urine (acidosis can cause toxic effects and enhance salicylates). Hemodialysis is indicated in salicylate concentration of 100-130 mg%, and in patients with chronic poisoning - 40 mg% or less when indicated (refractory acidosis, progressive deterioration severe damage to the central nervous system, lung edema and renal failure). It is shown in pulmonary edema artificial ventilation with a mixture enriched in oxygen at a positive pressure mode at the end of the exhalation; To treat edema of the brain, hyperventilation and osmotic diuresis are used.

Caffeine in doses of more than 300 mg per day (including the abuse of coffee - more than 4 cups of natural coffee at 150 ml) can cause anxiety, tremor, headache, confusion, extrasystole.

Treatment: provocation of vomiting, reception of activated charcoal.

Interaction:

Acetylsalicylic acid increases the toxicity of methotrexate, reducing its renal clearance, the effects of narcotic analgesics, other non-steroidal anti-inflammatory drugs, oral hypoglycemic drugs, heparin, indirect anticoagulants, thrombolytic agents and antiaggregants; reduces the effect of uricosuric medicines (benzbromarone, sulfinpyrazone), antihypertensive drugs, diuretics (spironolactone, furosemide); increases the concentration of digoxin, barbiturates, lithium salts in plasma. Glucocorticosteroids, ethanol and ethanol-containing drugs increase the negative effect on the mucous membrane of the gastrointestinal tract and increase the risk of developing gastrointestinal bleeding. Antatsida containing magnesium and / or aluminum, slow down and worsen the absorption of acetylsalicylic acid. Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

Caffeine reduces the effect of narcotic analgesics and hypnotic drugs, reduces the absorption of Ca2 + preparations in the gastrointestinal tract,increases the excretion of Li + in the urine, accelerates absorption and enhances the action of cardiac glycosides, increases their toxicity. Joint use of caffeine with beta-blockers can lead to mutual suppression of therapeutic effects. Mexiletin - reduces caffeine withdrawal to 50%; nicotine - Increases the speed of caffeine removal.

Special instructions:

Before surgical intervention to reduce bleeding during surgery and in the postoperative period, you should cancel taking the drug for 5-7 days and inform the doctor.

It should be borne in mind that in predisposed patients acetylsalicylic acid (even in small doses) reduces the excretion of uric acid from the body and can lead to the development of an acute attack of gout.

During treatment, you should stop using alcohol (increased risk of gastrointestinal bleeding).

Excessive consumption of caffeinated products (coffee, tea) on the background of treatment can cause symptoms of caffeine overdose.

Children should not be prescribed medications containing acetylsalicylic acid, since in the case of a viral infection they can increase the risk of developing Reye's syndrome.Symptoms of Reye's syndrome include prolonged vomiting, acute encephalopathy, and enlargement of the liver.

With continued use of the drug, control of peripheral blood and the functional state of the liver is necessary.

Patients with hypersensitivity or with asthmatic reactions to salicylates or their derivatives acetylsalicylic acid can be prescribed only with special precautions (in emergency care settings).

Instructions

Acetylsalicylic acid + Caffeine (Acidum acetylsalicylicum + Coffeinum)