Acetylsalicylic acid + (Citric acid + Sodium bicarbonate) (Acidum acetylsalicylicum + [Acidum citricum + Natrii hydrocarbonas])

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
  • Alka-Seltzer®
    pills inwards 
    Bayer Konsyumer Kare AG     Switzerland
  • Zorex Morning®
    pills inwards 
    VALENTA PHARM, PAO     Russia
    • АТХ:

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

    Pharmacodynamics:

    Acetylsalicylic acid inhibits cyclooxygenase (COX-1 and COX-2) and irreversibly inhibits the cyclooxygenase pathway of arachidonic acid metabolism, blocks the synthesis of prostaglandins (PGA2, PGD2, PGF2αulf, PGE1, PGE2, etc.) and thromboxane. Reduces flushing, exudation, permeability of capillaries, activity of hyaluronidase, limits the energy supply of the inflammatory process by inhibiting the production of adenosine triphosphate. Affects the subcortical centers of thermoregulation and pain sensitivity. Reduction of the content of prostaglandins (mainly PGE1) 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.

    Sodium bicarbonate neutralizes free hydrochloric acid in the stomach, which reduces the risk of erosion and ulceration as a result of the actionacetylsalicylic acid. Citric acid promotes faster absorption of the drug

    Pharmacokinetics:

    After ingestion sufficiently sucked. In the presence of an enteric-soluble coat (resistant to the action of gastric juice and does not allow the absorption of acetylsalicylic acid in the stomach), it is absorbed in the upper part of the small intestine. During absorption, it undergoes presystemic elimination in the intestinal wall and in the liver (deacetylated). The absorbed part is very quickly hydrolyzed by special esterases, therefore half-elimination period (half-life) acetylsalicylic acid is not 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 of substance in blood plasma (serum) 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).

    Indications:

    Feverish syndrome with infectious and inflammatory diseases, pain syndrome of mild and moderate severity: headache (including associated with alcohol withdrawal syndrome), migraine, toothache, neuralgia, myalgia, arthralgia, algodismenorea.

    ICD-10

    V.F10-F19.F10.3   Mental and behavioral disorders caused by alcohol use - withdrawal symptoms

    VI.G40-G47.G43   Migraine

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

    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   Fever of unknown origin

    XVIII.R50-R69.R51   Headache

    Contraindications:

    Hypersensitivity, erosive-ulcerative lesions of the gastrointestinal tract (in the exacerbation phase), gastrointestinal bleeding, aspirin asthma, hemophilia, hemorrhagic diathesis, hypoprothrombinemia, portal hypertension, avitaminosis K, renal and / or hepatic insufficiency, glucose-6 deficiency -phosphate dehydrogenase, children's age (under 15 years - the risk of developing Reye syndrome in children with hyperthermia in the background of viral diseases).

    Carefully:

    With caution: with concomitant therapy with anticoagulants, gout, peptic ulcer and / or duodenal ulcer (history), including chronic or recurrent peptic ulcer disease, or episodes of gastrointestinal bleeding; renal and / or hepatic insufficiency, deficiency of glucose-6-phosphate dehydrogenase, hyperuricemia, heart failure.

    Pregnancy and lactation:

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

    The use of large doses of salicylates in the first trimester of pregnancy is associated with an increased frequency of fetal development defects (cleft palate, heart defects). In the II trimester of pregnancy, salicylates can only be prescribed taking into account the risk and benefit assessment. The appointment of salicylates in the III trimester of pregnancy is contraindicated.

    Salicylates and their metabolites penetrate into breast milk in small amounts. The accidental intake of salicylates during lactation is not accompanied by the development of adverse reactions in the child and does not require the cessation of breastfeeding. However, with prolonged use or administration in high doses, breast-feeding should be discontinued.

    Dosing and Administration:

    Inside, previously effervescent tablets are dissolved in 1 glass of water. Adults: single dose - 1-3 tablets with a maximum daily dose - 8 tablets (interval between doses should be 4-8 hours). Children over 15 years: single dose - 1 tablet, the maximum daily dose - 4 tablets.

    Side effects:

    Nausea, loss of appetite, gastralgia, diarrhea, erosive and ulcerative lesions of the gastrointestinal tract, bleeding from the gastrointestinal tract, allergic reactions (rash, angioedema, bronchoconstriction), elevated liver enzymes, liver and / or renal failure, blood (thrombocytopenia, aplastic anemia, agranulocytosis, pancytopenia), "Aspirin" asthma (including recurrent nasal polyposis mucosa and the paranasal sinuses); with prolonged use - dizziness, headache (when used in high doses), impaired vision, tinnitus, emesis, platelet aggregation reduction, hypocoagulation, bleeding, prerenal azotemia, hypercreatininemia, hypercalcemia, renal failure with papillary necrosis, nephrotic syndrome, Deafness ,malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell syndrome), Reye syndrome in children, aseptic meningitis, aggravation of chronic heart failure.

    Overdose:

    Symptoms: with mild intoxication - nausea, vomiting, gastralgia, dizziness, ringing in the ears. With a severe overdose - inhibition, drowsiness, collapse, convulsions, difficulty breathing, anuria, bleeding, hyperthermia, coma. Initially, central hyperventilation of the lungs leads to respiratory alkalosis (dyspnea, suffocation, cyanosis, sweating), as the intoxication intensifies, progressive respiratory paralysis and dissociation of oxidative phosphorylation cause respiratory acidosis. In chronic overdose, the concentration of the drug in the plasma does not correlate well with the severity of intoxication.

    Treatment: with acute overdose, induction of vomiting, the appointment of activated carbon, laxative drugs, monitoring of acid-base state and electrolyte balance; depending on the state of metabolism - the introduction of sodium bicarbonate, sodium citrate or sodium lactate.The increase in reserve alkalinity increases the excretion of acetylsalicylic acid by alkalinizing urine.

    Interaction:

    Strengthens the action of others non-steroidal anti-inflammatory drugs, oral anticoagulants, glucocorticoids, narcotic analgesics. Hanti-inflammatory drugs, methotrexate, antihistamines increase the risk of side effects. Reduces the effectiveness of spironolactone, furosemide, hypotensive, uricosuric medicines. Glucocorticoids and ethanol increase the adverse effect on the mucous membrane of the gastrointestinal tract, increase the risk of developing gastrointestinal bleeding. Antatsida, containing magnesium and aluminum hydroxide, slow down and worsen the absorption of acetylsalicylic acid.

    During treatment, alcohol is contraindicated, as it increases the risk of developing gastrointestinal bleeding.

    Joint application:

    - with methotrexate at a dose of 15 mg per week or more: the hemolytic cytotoxicity of methotrexate is increased (the renal clearance of methotrexate and methotrexate is replaced by salicylates in association with blood plasma proteins);

    - with anticoagulants, for example heparin: increased risk of bleeding due to inhibition of platelet function, damage to the mucosa of the gastrointestinal tract, displacement of anticoagulants (oral) from communication with plasma proteins;

    - with others non-steroidal anti-inflammatory agents, as well as with high doses of salicylates (3 g per day or more): as a result of synergistic interaction, the risk of ulceration and bleeding increases;

    - with uricosurates, for example benzbromarone: reduces the uricosuric effect;

    - with digoxin: the concentration of digoxin is increased due to decreased renal excretion;

    - with antidiabetic drugs, for example insulin: the hypoglycemic effect of antidiabetic drugs increases due to hypoglycemic action of acetylsalicylic acid;

    - with preparations of thrombolytics group: the risk of bleeding increases;

    - with diuretics at a dose of 3 mg per day or more: glomerular filtration decreases due to reduced synthesis of prostaglandins;

    - with systemic glucocorticosteroids, excluding hydrocortisone, used as a substitute therapy for Addison's disease: with the use of glucocorticosteroids, the level of salicylates in the blood decreases by increasing the excretion of the latter;

    - with inhibitors angiotensin-converting enzyme: a dose of 3 g per day and more reduced glomerular filtration by inhibiting prostaglandins and, as a consequence, the antihypertensive effect decreases;

    - with valproic acid: the toxicity of valproic acid is increased.

    Special instructions:

    It should be taken into account that drugs containing acetylsalicylic acid increase the risk of Reye's syndrome in the presence of a viral infection (symptoms of Reye syndrome: prolonged vomiting, acute encephalopathy, enlargement of the liver).

    With prolonged use of the drug, control of peripheral blood and the functional state of the liver, as well as examination of feces for latent blood, is necessary. Because the acetylsalicylic acid slows the clotting of the blood, then in the case of the forthcoming surgical intervention, it is necessary to stop taking the drug for 5-7 days before the operation.

    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).

    Instructions
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