Active substanceAcetylsalicylic acid + CaffeineAcetylsalicylic acid + Caffeine
Similar drugsTo uncover
  • Aspirate® plus
    pills inwards 
    VALENTA PHARM, PAO     Russia
  • Dosage form: & nbsppills
    Composition:

    One tablet contains:

    active substances: Acetylsalicylic acid - 500 mg; caffeine 50 mg;

    Excipients: lactose monohydrate 35 mg, corn starch 84 mg, povidone 10 mg, stearic acid 7 mg, crospovidone 14 mg.

    Description:

    Tablets white or white with a yellowish or kremovatym tinged color, flat-cylindrical, with a facet and a risk.

    Pharmacotherapeutic group:Analgesic combined (non-steroidal anti-inflammatory drug + psychostimulating agent)
    ATX: & nbsp

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

    Pharmacodynamics:
    Combined drug, the effect of which is determined by the components that make up its composition. The combination of the components of the drug provides better tolerability of symptoms of malaise and fever in "cold" and other infectious inflammatory diseases, reducing pain syndrome of various origins. Acetylsalicylic acid has anti-inflammatory, analgesic and antipyretic effects associated with the suppression of cyclooxygenase 1 and 2, regulating the synthesis of prostaglandins. As a result, prostaglandins are not formed, which provide the formation of edema and hyperalgesia.Reduction of the content of prostaglandins (mainly E1) in the center of thermoregulation leads to a decrease in body temperature due to the expansion of the vessels of the skin and increased sweating. The analgesic effect is due to both central and peripheral action. Reduces aggregation, platelet adhesiveness and thrombus formation by suppressing the synthesis of thromboxane A2 in platelets. Antiaggregant effect persists for 7 days after a single dose (more pronounced in men than in women).

    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 and fatigue, increases mental and physical performance.

    Pharmacokinetics:

    Acetylsalicylic acid during the absorption is systemically eliminated in the intestinal wall and in the liver (deacetylated). The absorbed part is rapidly hydrolyzed by plasma cholinesterases and albumin esterase, so the period half-life (T1 / 2) - no more than 15-20 minutes.In the body it circulates (75-90% in association with albumin) and is distributed in tissues as an anion of salicylic acid. Maximum concentration Cmax salicylic acid is reached after about 2 hours. Easily penetrates into many tissues and body fluids including into the cerebrospinal fluid, peritoneal and synovial fluid. Penetration into the joint cavity is accelerated in the presence of hyperemia and edema and slows down in the proliferative phase of inflammation. In small amounts, salicylates are found in the nervous tissue, traces in bile, sweat, feces.

    When acidosis occurs, most of the salicylate is converted to a non-ionized acid that penetrates well into the tissue, including the brain. Rapidly passes through the placenta, in small quantities is excreted in breast milk. Metabolized mainly in the liver with the formation of 4 metabolites, found in many tissues and urine. It is excreted mainly by active secretion in the renal tubules in the form of salicylic acid proper (60%) and its metabolites. Removal of unchanged salicylate depends on the pH of the urine (with alkalization of urine ionization of salicylates increases, their reabsorption worsens and the excretion increases significantly).The rate of excretion depends on the dose: when taking small doses of T1 / 2 - 2-3 hours, with an increase in the dose may increase to 15-30 hours.

    Absorption of caffeine occurs mainly due to simple diffusion. Cmax - is reached approximately in 50-75 minutes after intake. Quickly distributed in all organs and tissues of the body; easily penetrates the blood-brain barrier and the placenta. Communication with blood proteins (albumins) is 25-36%. Metabolized mainly in the liver. In adults, about 80% of the dose of caffeine is metabolized to paraxanthin, about 10% to theobromine and about 4% to theophylline. These compounds are subsequently demethylated into monomethylxanthines, and then to methylated derivatives of uric acid. T1 / 2 in adults - 3.9 - 5.3 hours (sometimes up to 10 hours). The excretion of caffeine and its metabolites is carried out by the kidneys.

    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).

    Contraindications:

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

    - erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation);

    - gastrointestinal bleeding;

    - hemophilia, hemorrhagic diathesis, hypoprothrombinemia;

    - The bronchial asthma, induced by the intake of salicylates and other NSAIDs;

    - 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);

    - arterial hypertension, portal hypertension;

    - glaucoma;

    - kidney 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 with pain syndrome (for this dosage form);

    - children and adolescents under the age of 15 years (when used as an antipyretic agent) with acute respiratory infections caused by viral infections,in connection with the risk of developing Reye's syndrome (encephalopathy and acute fatty liver disease with acute, development of hepatic insufficiency).

    -Birth (I and III trimester);

    -period of lactation.

    Carefully:

    With gout, hyperuricemia, because. 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 when there is a history of ulcerative lesions of the gastrointestinal tract (GI 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:

    Has a teratogenic effect: when applied in the first trimester of pregnancy leads to the fetal cleavage of the upper palate, in the third trimester - causes inhibition of labor (suppression of prostaglandin synthesis), premature closure of the arterial duct in the fetus, hyperplasia of pulmonary vessels and hypertension in the small 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 in 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.

    On the part of the hematopoiesis system: thrombocytopenia, anemia, and leukopenia.

    Allergic reactions: skin rash, angioedema, bronchospasm.

    From the central nervous system: insomnia.

    From the side of 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 digestive tract, hypocoagulation, bleeding (including in the digestive tract), visual impairment, reduced 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.

    When such symptoms appear, it is recommended to stop taking the drug and immediately consult a doctor.
    Overdose:

    Symptoms of overdose caused by acetylsalicylic acid may occur after a single dose of a large dose or with prolonged use. If a single dose is less than 150 mg / kg, acute poisoning is considered mild, 150 - 3.02 mg / kg - moderate and when applied at doses greater than 300 mg / kg - heavy.

    Symptoms: With mild poisoning - salicylism syndrome (nausea, vomiting, tinnitus, visual impairment, dizziness, severe headache, general malaise, fever - a 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 developing chronic intoxication is observed in the elderly with more than 100 mg / kg / 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 charcoal and laxatives, alkalinization of urine (shown at a salicylate concentration above 40 mg%, is provided by intravenous infusion of sodium bicarbonate - 88 meq per 1 liter of 5% dextrose solution, at a rate of 10-15 ml / kg / h) , restoration of the volume of circulating blood and induction of diuresis (achieved by adding sodium bicarbonate solution in 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 more 300 mg / day (including the background abuse coffee - a cup natural coffee 4, 150 ml) can cause, anxiety, tremor, headache, pain, confusion, extrasystole. Treatment: Vomiting provocation, reception of activated coal.

    Interaction:

    Acetylsalicylic acid, enhances methotrexate toxicity, reducing its renal clearance, effects. narcotic .analgetikov, other NSAIDs, oral hypoglycemic drugs, heparin, anticoagulants,thrombolytics and antiplatelet agents; 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 mucosa 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 digestive tract, increases the excretion of Li + drugs in the urine, accelerates absorption and enhances the action of cardiac glycosides, and 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.

    Effect on the ability to drive transp. cf. and fur:Not described.
    Form release / dosage:

    Tablets 500 mg + 50 mg.

    Packaging:

    For 10 tablets in a contoured cell pack of a PVC film or PVC / PVDC and aluminum foil printed lacquered.

    1 the contoured cell pack together with the instruction for use is placed in a pack of cardboard.

    Storage conditions:

    In the original packaging at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 of the year.Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:Without recipe
    Registration number:LS-001378
    Date of registration:30.03.2011 / 21.08.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp27.09.2017
    Illustrated instructions
      Instructions
      Up