Acetylsalicylic acid + Glycine (Acidum acsetylsalicylicum + Glycinum)

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-Prim®
    pills inwards 
    Pharmaceutical factory "POLFARMA" JSC     Poland
    • АТХ:

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

    Pharmacodynamics:

    Acetylsalicylic acid is an ester of salicylic acid, belongs to the group of non-steroidal anti-inflammatory drugs. The mechanism of action is based on the irreversible inactivation of the enzyme cyclooxygenase (COX-1), which blocks the synthesis of PG, prostacyclin and thromboxane. Reduces aggregation, platelet adhesion and thrombogenesis by irreversible suppression of thromboxane A2 synthesis in platelets. Increases fibrinolytic activity of plasma and reduces the concentration of vitamin K-dependent coagulation factors (II, VII, IX, X). The antiaggregation effect is most pronounced in platelets, because they are not able to re-synthesize cyclooxygenase. Anti-aggregation effect develops after the application of small doses of the drug and remains for 7 days after a single dose. These properties of acetylsalicylic acid are used in the prevention and treatment of myocardial infarction, ischemic heart disease, complications of varicose veins.

    Being in the composition of the drug glycine increases the solubility of acetylsalicylic acid, which provides rapid bioavailability of acetylsalicylic acid and less irritating effect on the mucosa of the gastrointestinal tract; simultaneously glycine buffers the acidic properties of acetylsalicylic acid, reducing the risk of side effects.

    Pharmacokinetics:

    Acetylsalicylic acid

    Ingestion acetylsalicylic acid absorbed quickly and completely from the gastrointestinal tract. Acetylsalicylic acid partially metabolized during adsorption. During and after suction acetylsalicylic acid turns into a major metabolite, salicylic acid, which is metabolized mainly in the liver under the influence of liver enzymes to form metabolites such as phenyl salicylate, glucuronide salicylate and salicyluric acid, found in many tissues and in urine. In women, the metabolic process is slower (less enzyme activity in the blood serum).

    Acetylsalicylic acid and salicylic acid are highly associated with blood plasma proteins (66 to 98% depending on the dose) and are rapidly distributed in the body. Salicylic acid penetrates the placenta and is excreted in breast milk.

    Half-Elimination (half-life) acetylsalicylic acid from the blood plasma is about 15-20 minutes. Unlike other salicylates, with repeated administration of the drug, unhydrolyzed acetylsalicylic acid does not accumulate in the blood serum. Only 1% of the ingested acetylsalicylic acid is excreted by the kidneys in the form of unhydrolyzed acetylsalicylic acid, the rest is excreted as salicylates and their metabolites. In patients with normal kidney function, 80-100% of a single dose of the drug is excreted by the kidneys within 24-72 hours.

    After intake quickly absorbed from the gastrointestinal tract. Excreted by the kidneys (80-100%) for 24-72 hours.

    Glycine

    Glycine easily penetrates into most biological fluids and body tissues, incl. in the brain; It is metabolized to water and carbon dioxide and does not accumulate in tissues.

    Indications:

    Pain syndrome of mild and moderate intensity (including headache,myalgia, arthralgia), hyperthermia (including catarrhal diseases, viral infections), dyspepsia (including heartburn, gastralgia, including those caused by overeating or abusing ethanol).

    ICD-10

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

    VI.G40-G47.G45.9   Transitory cerebral ischemic attack, unspecified

    VI.G40-G47.G43   Migraine

    IX.I20-I25.I21.9   Acute myocardial infarction, unspecified

    XVIII.R50-R69.R50   Fever of unknown origin

    XVIII.R50-R69.R51   Headache

    IX.I60-I69.I64   Stroke not specified as a hemorrhage or infarction

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

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

    XIII.M70-M79.M79.1   Myalgia

    XXI.Z80-Z99.Z95.1   Aortocoronary shunt transplant

    Contraindications:

    Hypersensitivity to non-steroidal anti-inflammatory drugs (including history), erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation), blood clotting disorders (hemophilia, thrombocytopenia), G-6-FD deficiency, bronchial asthma, nose polyps, lactation, children's age (up to 12 years), pregnancy (I and III trimester) and lactation period,concomitant use with methotrexate at a dose of 15 mg per week or more, severe renal failure (Cl creatinine <30 mL per minute), severe hepatic insufficiency (grade B and higher on the Child-Pugh scale), chronic heart failure III-IV functional class the NYHA classification.

    Carefully:

    Caution should be given to the drug for gout, hyperuricemia, peptic ulcer and duodenal ulcer or gastrointestinal hemorrhage (history), renal failure (Cl creatinine ≥ 30 mL per minute), liver failure (below grade B on the Child-Pugh scale) , bronchial asthma, chronic respiratory diseases, hay fever, nasal polyposis, drug allergies, incl. on the drugs of the group non-steroidal anti-inflammatory drugs (analgesics, anti-inflammatory, antirheumatic drugs); pregnancy (II trimester), with the proposed surgical intervention (including minor, including extraction of the tooth); with simultaneous administration with the following medicines: methotrexate in a dose of less than 15 mg per week; with anticoagulants, thrombolytic or antiplatelet agents; non-steroidal anti-inflammatory agents and derivatives of salicylic acid in large doses; with digoxin; hypoglycemic agents for oral administration (derivatives of sulfonylureas) and insulin; valproic acid; alcohol (alcoholic beverages in particular); selective serotonin reuptake inhibitors; ibuprofen; in old age.

    Pregnancy and lactation:

    The category of FDA recommendations is not defined. Qualitative and well-controlled studies on humans and animals have not been conducted.

    The use of large doses of salicylates in the first trimester of pregnancy is associated with an increased incidence of fetal developmental defects (split upper skies, heart defects). The appointment of salicylates in the first trimester of pregnancy is contraindicated.

    In the last trimester of pregnancy, salicylates in high doses (more than 300 mg / day) cause inhibition of labor, premature closure of the arterial duct in the fetus, increased bleeding in the mother and fetus, and the appointment immediately before childbirth can cause intracranial hemorrhages, especially in premature infants. The appointment of salicylates in the last trimester of pregnancy is contraindicated.

    In the second trimester of pregnancy, salicylates can only be given taking into account a strict risk assessment and benefit for the mother and fetus, preferably at doses not exceeding 150 mg / day and for a short time.

    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 of the drug or its administration in a high dose, breast-feeding should be stopped immediately.

    Dosing and Administration:

    Inside, during meals, pre-dissolved in 3/4 cups of boiled (not hot) water, 1-2 tablets 3-4 times a day.

    The drug is intended for long-term use. The duration of therapy is determined by the doctor.

    Side effects:

    Allergic reactions: skin rash, bronchospasm, angioedema. Formation on the basis of the hapten mechanism of the "aspirin triad" (combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid and preparations of pyrazolone series).

    From the gastrointestinal tract: nausea, vomiting, pain in the epigastric region, diarrhea.

    On the part of the hemopoietic system: thrombocytopenia, anemia, leukopenia, hemorrhagic syndrome (epistaxis, bleeding gums), prolongation of clotting time.

    With prolonged use in large doses, erosive and ulcerative lesions of the gastrointestinal tract, bleeding, black tar stool, general weakness, interstitial nephritis, prerenal azotemia with increased level of blood creatinine and hyperkalemia, bronchospasm, papillary necrosis, acute renal failure, nephrotic syndrome , aseptic meningitis, increased symptoms of chronic heart failure, edema, increased activity of hepatic transaminases.

    Overdose:

    Symptoms: with an overdose of moderate severity, dizziness, hearing and vision impairment, nausea, vomiting, confusion occur after withdrawal. Severe symptoms of intoxication were observed when taking in excess of 200 mg / kg: fever, hyperventilation, ketoacidosis, respiratory alkalosis, metabolic acidosis,depression of consciousness down to coma, cardiogenic shock, respiratory failure, severe hypoglycemia.

    Treatment: should be conducted in a specialized department. Vomiting or rinsing of the stomach should be prescribed, Activated carbon. It is recommended to monitor acid-base balance, alkalinize urine in order to obtain a urine pH of 7.5-8 (forced alkalinization of urine is considered achieved if the concentration of salicylic acid in the blood plasma is more than 500 mg / l (3.6 mmol / l) in adults or 300 mg / l (2.2 mmol / l) in children), hemodialysis, fluid loss compensation, symptomatic therapy.

    Interaction:

    Acetylsalicylic acid enhances the effect of oral anticoagulants and hypoglycemic drugs, insulin, methotrexate, other non-steroidal anti-inflammatory drugs, glucocorticosteroids, valproic acid, digoxin, ethanol.

    Acetylsalicylic acid weakens the effect of sulfinpyrazone, diflunizal, fenoprofen, ibuprofen, indomethacin, piroxicam, naproxen, sulindac, as well as drugs,which block tubular secretion.

    Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

    Special instructions:

    Acetylsalicylic acid can provoke bronchospasm, as well as cause attacks of bronchial asthma and other reactions of hypersensitivity. Risk factors are the availability of a history of asthma, hay fever, nasal polyposis, chronic diseases of the respiratory system as well as of allergic reactions to other drugs (e.g., skin reactions, pruritus, urticaria).

    The inhibitory effect of acetylsalicylic acid on platelet aggregation persists for several days after ingestion, which may increase the risk of bleeding during surgery or in the postoperative period. If absolute elimination of bleeding is necessary in the course of surgical intervention, it is necessary to completely abandon the use of acetylsalicylic acid in the preoperative period.

    It is not recommended combination of acetylsalicylic acid with ibuprofen in patients with an increased risk of cardiovascular disease,because the latter reduces the positive effect of acetylsalicylic acid on life expectancy (reduces the cardioprotective effect of acetylsalicylic acid).

    Excess dose of acetylsalicylic acid is associated with a risk of gastrointestinal bleeding.

    When combined with acetylsalicylic acid and ethanol (alcoholic beverages), the risk of damage to the mucous membrane of the gastrointestinal tract and prolongation of bleeding time are increased.

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