Acetylsalicylic acid + Ascorbic acid (Acidum acetylsalicylicum + Acidum ascorbinicum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

NSAIDs - Salicylic acid derivatives

Included in the formulation
  • Aspinate® C
    pills inwards 
    VALENTA PHARM, PAO     Russia
  • Aspirin®-C
    pills inwards 
    Bayer Konsyumer Kare AG     Switzerland
  • Asprovit C
    pills inwards 
    "Vitale-HD" LLP     Estonia
    • АТХ:

    N.02.B.A.51   Acetylsalicylic acid in combination with other drugs, excluding psycholeptics

    Pharmacodynamics:

    Combined drug, the effect of which is determined by the components that make up its composition. Acetylsalicylic acid indiscriminately inhibits cyclooxygenase-1 and cyclooxygenase-2, disrupting the metabolism of arachidonic acid, reducing the synthesis of prostaglandins. Has a strong analgesic, antipyretic and anti-inflammatory effect; reduces the synthesis of thromboxane and inhibits the aggregation of platelets, lowering the coagulation status of the blood.

    Ascorbic acid participates in the regulation of oxidation-reduction processes, carbohydrate metabolism, blood coagulability, tissue regeneration, in the synthesis of steroid hormones; increases the body's resistance to infections, reduces vascular permeability, reduces the need for vitamins AT1, AT2, A, E, folic acid, pantothenic acid.Satisfies the increased needs of the body in vitamin C for diseases accompanied by fever.

    Pharmacokinetics:

    Acetylsalicylic acid

    Absorption is complete, fast. During absorption, it undergoes presystemic elimination in the intestinal wall and in the liver (deacetylated). PElimination half-life (half-life) of the drug - 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. Cmax 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 hydrogen index of urine (with alkalinization of urine ionization of salicylates increases, their reabsorption worsens and excretion increases significantly).

    Ascorbic acid

    When applied orally, it is rapidly absorbed, a sufficient concentration in the blood is observed after 30 minutes, the maximum concentration in 2 hours. Part of the drug is absorbed in the stomach, most in the small intestine.With an increase in the dose up to 200 mg, up to 140 mg (70%) is absorbed; with a further increase in the dose, the absorption decreases (50-20%). Connection with plasma proteins - 25%.
    The concentration of ascorbic acid in plasma is normally around 10-20 μg / ml, the body stores about 1.5 g when taking daily recommended doses and 2.5 g when taken at 200 mg per day. TCmax after oral administration - 4 hours.

    Easily penetrates into leukocytes, platelets, and then into all tissues; the greatest concentration is achieved in glandular organs, leukocytes, liver and lens of the eye; deposited in the posterior lobe of the pituitary gland, adrenal cortex, ocular epithelium, interstitial cells of the seminal glands, ovaries, liver, spleen, pancreas, lungs, kidneys, intestinal wall, heart, muscles, thyroid gland; penetrates the placenta.

    Metabolised mainly in the liver in desoxyascorbic and then in oxaloacetic and diketogulonovoy acid.

    It is excreted by the kidneys, through the intestines, with sweat, breast milk in the form of unchanged ascorbate and metabolites.

    At the appointment of high doses, the rate of excretion increases sharply. Smoking and the use of ethanol accelerate the destruction of ascorbic acid (conversion into inactive metabolites), sharply reducing the reserves in the body.

    It is in hemodialysis.

    Absorbed in the duodenum, in part - in the ileum (absorption decreases with increasing dose). F - 20-50% (when taking a dose exceeding 200 mg). Stocks in the body are about 1.5 g. Depot: leukocytes, platelets, endocrine glands, liver, ocular epithelium, lungs, kidneys, intestinal wall, heart, muscles. Connection with plasma proteins - 25%. Biotransformation in the liver. Elimination by the kidneys (in the form of metabolites).

    Indications:

    Feverish syndrome with infectious and inflammatory diseases; pain syndrome (of various origins) in adults: headache (including those associated with alcohol withdrawal syndrome), migraine, toothache, neuralgia, myalgia, arthralgia, algodismenorea.

    ICD-10

    VI.G40-G47.G43   Migraine

    X.J00-J06.J06   Acute upper respiratory tract infections of multiple and unspecified sites

    XIII.M70-M79.M79.1   Myalgia

    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, erosive-ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation), gastrointestinal bleeding, aspirin asthma, hemophilia, hemorrhagic vasculitis, hypoprothrombinemia,portal hypertension; avitaminosis K, renal failure, severe liver function disorder; pregnancy (I and III trimester), breast-feeding; G-6-FD deficiency, children's age (up to 15 years - the risk of developing Reye's syndrome in children with hyperthermia on the background of viral diseases).

    Carefully:

    Caution should be given to the drug with concomitant therapy with anticoagulants, gout, peptic ulcer and / or duodenal ulcer (in the anamnesis), erosive gastritis, susceptibility to gastrointestinal bleeding, hypoprothrombinemia, hypovitaminosis K, anemia, conditions predisposing to fluid retention in the body (including violations of heart function, arterial hypertension), thyrotoxicosis, gout, liver diseases.

    Pregnancy and lactation:

    Recommendations Food and Drug Administration (US Food and Drug Administration) - Category D.

    In the second trimester of pregnancy, one-time administration of the drug at recommended doses is possible only if the expected benefit for the mother will exceed the potential risk to the fetus.

    The drug is contraindicated in pregnancy (I and III trimesters) and during breastfeeding.

    If you need to use the drug during lactation, breastfeeding should be discontinued.

    Dosing and Administration:

    Inside. The average single dose for adults and children over 15 years is 1-2 tablets (depending on the content of acetylsalicylic acid and indications) 2-3 times a day, the highest daily dose - 8-10 tablets; the frequency of reception is 2-4 times a day with an interval of at least 4 hours.

    In the form of granules, adults and adolescents are prescribed in a single dose containing 0.5 g of acetylsalicylic acid; daily dose of 2.5 g. Directly before use, the granulate is dissolved in 200 ml of water.

    The duration of treatment (without consulting a doctor) should not exceed 7 days with an appointment as an analgesic and more than 3 days - as an antipyretic.

    Side effects:

    From the digestive system: abdominal pain, nausea, vomiting, obvious (black stools, bloody vomiting) or hidden signs of gastrointestinal bleeding, which can lead to iron deficiency anemia, erosive and ulcerative lesions (including perforations) gastrointestinal - intestinal tract; rarely - violations of the liver (increased liver transaminases).

    From the side of the central nervous system: dizziness, noise in the ears (usually are signs of an overdose).

    From the hemopoietic system: hemorrhagic syndrome, thrombocytopenia.

    From the side of the urinary system: when used in high doses - hyperoxaluria and the formation of urinary stones from calcium oxalate, damage to the glomerular apparatus of the kidneys.

    Allergic reactions: skin rash, anaphylactic reactions, bronchospasm, Quincke's edema.

    With long-term use - headache, visual impairment, tinnitus, reduced platelet aggregation, hypocoagulation, bleeding; kidney damage with papillary necrosis; deafness; malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), Reye's syndrome in children (hyperpyrexia, metabolic acidosis, disorders of the nervous system and psyche, vomiting, liver dysfunction).

    Overdose:

    Symptoms: with light intoxication - nausea, vomiting, gastralgia, dizziness, ringing in the ears. After a severe overdose - inhibition, drowsiness, collapse, convulsions, shortness of breath, anuria, bleeding.Initially, the central hyperventilation leads to respiratory alkalosis (shortness of breath, dyspnea, cyanosis, perspiration). As the intoxication progressive paralysis and respiratory uncoupling of oxidative phosphorylation causes respiratory acidosis.

    Prolonged use of high doses (above 1 g) - headache, increased excitability of the central nervous system, insomnia, nausea, vomiting, diarrhea, gastritis with acidity, ulceration of the mucosa of the gastrointestinal tract, inhibition of pancreatic function, the deposition of calcium oxalate kidney damage, kidney damage, frequent urination (when taking a dose of more than 600 mg per day). Deterioration of trophism of tissues, increase of arterial pressure. With intravenous administration in high doses - the threat of abortion, the destruction of red blood cells.

    Treatment: continuous monitoring of the acid-base state and electrolyte balance; depending on the state of metabolism - the introduction of sodium bicarbonate, sodium citrate or sodium lactate. Increased reserve alkalinity increases the excretion of acetylsalicylic acid due to the alkalinity of urine.

    Interaction:

    Acetylsalicylic acid enhances the action of heparin, oral anticoagulants, reserpine, steroid hormones and hypoglycemic drugs.

    Non-steroidal anti-inflammatory drugs, methotrexate increase the risk of side effects.

    Increases the toxicity of methotrexate, the effects of narcotic analgesics, other non-steroidal anti-inflammatory drugs, oral hypoglycemic drugs, heparin, indirect anticoagulants, thrombolytic agents and platelet aggregation inhibitors, sulfonamides (including co-trimoxazole), triiodothyronine, reserpine; reduces the effects of uricosuric drugs (benzbromarone, sulfinpyrazone), antihypertensive drugs and diuretics (spironolactone, furosemide).

    Increases the concentration of digoxin, barbiturates and lithium preparations in blood plasma.

    Glucocorticosteroids, alcohol and alcohol-containing drugs increase the damaging effect on the mucous membrane of the gastrointestinal tract, increase the risk of developing gastrointestinal bleeding.

    Antatsida, containing magnesium and / or aluminum hydroxide, slow down and worsen the absorption of acetylsalicylic acid.

    Ascorbic acid improves the absorption of iron and aluminum preparations in the intestine. May decrease the effectiveness of warfarin. With alcohol abuse, the need for ascorbic acid increases.

    Special instructions:

    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.

    Because the acetylsalicylic acid slows the clotting of the blood, the patient, if he is to undergo surgery, must warn the doctor in advance about taking the drug.

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

    Acetylsalicylic acid in low doses reduces the excretion of uric acid.In patients with a corresponding predisposition, this can in some cases provoke a gout attack.

    During treatment should be abandoned the use of ethanol (increased risk of gastrointestinal bleeding).

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