Acetylsalicylic acid + Caffeine + Paracetamol + Ascorbic acid (Acidum acetylsalicylicum + Coffeinum + Paracetamolum + Acidum ascorbinicum)

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

Other non-narcotic analgesics, including non-steroidal and other anti-inflammatory drugs

NSAIDs - Salicylic acid derivatives

Included in the formulation
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    PHARMSTANDART-UFIM VITAMIN FACTORY, OJSC     Russia
    • АТХ:

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

    Pharmacodynamics:The drug inhibits the activity of cyclooxygenase in peripheral tissues and the central nervous system; inhibits the biosynthesis of prostaglandins (acetylsalicylic acid, paracetamol). Increases working capacity, reduces drowsiness and fatigue, has a positive inotropic and chronotropic effect, increases blood pressure in hypotension, increases the permeability of histohematological barriers (caffeine). It has an antioxidant effect and increases the resistance of the body (ascorbic acid).
    Pharmacokinetics:

    Acetylsalicylic acid

    Absorption is complete, fast. During absorption, it undergoes presystemic elimination in the intestinal wall and in the liver (deacetylated). The connection with plasma proteins is high. PThe half-elimination period (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. 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).

    Caffeine

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

    Paracetamol

    Paracetamol is quickly and almost completely absorbed from the gastrointestinal tract (maximum concentration 5-20 μg / ml, time to reach a maximum concentration of 0.5-2 hours). It binds to plasma proteins by 15%. Paracetamol penetrates the blood-brain barrier. The therapeutically effective concentration of paracetamol in plasma is achieved when it is administered at a dose of 10-15 mg / kg body weight. The half-life is 1-4 hours. Paracetamol is metabolized in the liver and excreted in the urine, mainly in the form of glucuronides and sulfonated conjugates, less than 5% is excreted unchanged in urine.

    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 about 10-20 μg / ml, the reserves in the body are about 1.5 g when taking daily recommended doses and 2.5 g when taking 200 mg per day. Time to reach the maximum concentration after ingestion - 4 hours.

    Easily penetrates into leukocytes, platelets, and then into all tissues; the highest 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 oxalic-acetic 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. It is in hemodialysis.

    Indications:

    Pain syndrome (moderately or mildly, of various origins): headache and toothache, myalgia, arthralgia, neuralgia, algodismenorea, migraine, febrile syndrome for colds and acute respiratory viral infections.

    ICD-10

    VI.G40-G47.G43   Migraine

    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

    XVIII.R50-R69.R52   Pain, not elsewhere classified

    XVIII.R50-R69.R52.2   Another constant pain

    Contraindications:

    Hypersensitivity, erosive-ulcerative lesions of the gastrointestinal tract in the exacerbation phase, gastrointestinal hemorrhages in the anamnesis, violations of the liver and kidney function, organic diseases of the cardiovascular system (including pronounced atherosclerosis, hypertension), glucose-6 deficiency -phosphate dehydrogenase, blood system diseases, glaucoma, surgical interventions accompanied by bleeding, aspirin asthma pregnancy (I and III trimesters), lactation period (breastfeeding), children's age (up to 15 le - the risk of Reye's syndrome in children with hyperthermia on a background of viral diseases), irritability, sleep disturbances, the simultaneous use of other non-steroidal anti-inflammatory drugs or non-narcotic analgesics.

    Carefully:

    With caution apply in the elderly, with gout or arthritis, liver diseases. Do not prescribe to children and adolescents if symptoms of chicken pox or influenza occur because of the possibility of Reye's syndrome. It is not recommended to combine with barbiturates, anticonvulsants, zidovudine, rifampicin, alcohol.With continued use, control of peripheral blood and the functional state of the liver is necessary.

    Pregnancy and lactation:

    Recommendations Food and Drug Administration (US Food and Drug Administration) - category D (for acetylsalicylic acid), C (for caffeine), there is no single category.

    Contraindicated in pregnancy (I and III trimesters), during lactation.

    Acetylsalicylic acid has a teratogenic effect; when applied in the first trimester of pregnancy leads to malformations - the cleavage of the upper palate; in the third trimester - to inhibition of labor (inhibition of the synthesis of prostaglandins), to the closure of the arterial duct in the fetus, which causes hyperplasia of the pulmonary vessels and hypertension in the vessels of the small circle of blood circulation.

    Isolated with breast milk, which increases the risk of bleeding in the child due to impaired platelet function.

    Dosing and Administration:

    Inside, after eating, washed down with water or milk. Children over 6 years - 1/2 tablet (1 tablet contains acetylsalicylic acid 240 mg, paracetamol 180 mg, caffeine 30 mg, ascorbic acid 50 mg) 2-3 times a day; children over 12 years and adults - 1 tablet 2-3 times a day with a break between meals for at least 4 hours.The maximum daily dose is 4 tablets. Duration of intake should not exceed: as an anesthetic - 5 days, antipyretic - 3 days.

    Side effects:

    Temporary increase in blood pressure, tachycardia, sleep disorders, dizziness, tinnitus, heartburn, nausea, a feeling of heaviness in the epigastrium, impaired bone marrow function (hematopoiesis), kidneys, liver, allergic reactions (including Stevens-Johnson syndrome, Lyell) , bronchospasm.

    With prolonged use - headache, visual impairment, tinnitus, reduced platelet aggregation, hypocoagulation, hemorrhagic syndrome (epistaxis, bleeding gums, purpura, etc.), kidney damage with papillary necrosis; deafness; Reye's syndrome in children (hyperpyrexia, metabolic acidosis, disorders of the nervous system and psyche, vomiting, liver dysfunction).

    Overdose:

    Symptoms (due to acetylsalicylic acid): with light intoxication - nausea, vomiting, gastralgia, dizziness, ringing in the ears; severe intoxication - retardation, drowsiness, collapse, convulsions, bronchospasm, 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.

    Treatment: constant monitoring of acid-base balance 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:

    The drug enhances the effect of anticoagulants, corticosteroids, narcotic analgesics and non-steroidal anti-inflammatory drugs, sulfonylurea derivatives.

    Simultaneous appointment with others non-steroidal anti-inflammatory agents, methotrexate increases the risk of side effects.

    Reduces the effectiveness of spironolactone, furosemide, antihypertensive drugs, as well as anti-arthritis drugs that promote the excretion of uric acid.

    Barbiturates, rifampicin, salicylamide, antiepileptic drugs and other stimulants of microsomal oxidation contribute to the formation of toxic metabolites of paracetamol that affect liver function.

    Metoclopramide accelerates the absorption of paracetamol.

    Under the influence of paracetamol half-elimination period (half-life) Chloramphenicol increased by 5 times. At repeated reception paracetamol can enhance the effect of anticoagulants (derivatives of dicumarin).

    Simultaneous reception of paracetamol and ethanol increases the risk of hepatotoxic effects.

    Smoking and the use of ethanol accelerate the destruction of ascorbic acid (conversion into inactive metabolites), sharply reducing the reserves in the body.

    Caffeine accelerates the absorption of ergotamine.

    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 emergency care settings).

    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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