Acetylsalicylic acid + Caffeine + Ascorbic acid (Acidum acetylsalicylicum + Coffeinum + 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
АТХ:

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. 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 B1, B2, A, E, folic acid, pantothenic acid. Satisfies the increased needs of the body in vitamin C for diseases accompanied by fever.

Caffeine exerts a direct stimulating effect on the central nervous system: it regulates and intensifies the processes of excitation in the cerebral cortex, the respiratory and vasomotor center, activates positive conditioned reflexes and motor activity.Stimulates mental activity, increases mental and physical performance, shortens the reaction time. After the reception, cheerfulness appears, temporarily eliminated or reduced fatigue and drowsiness. It causes an increase and deepening of the breathing, especially against the background of the oppression of the respiratory center. Affects the cardiovascular system: increases the strength and heart rate (especially in large doses), increases blood pressure when hypotension (does not change the normal). Expands the bronchi, bile ducts, blood vessels of skeletal muscles, heart, kidneys, narrows - abdominal organs (especially with their dilatation). Reduces the aggregation of platelets. Has a moderate diuretic effect, mainly due to a decrease in the reabsorption of electrolytes in the renal tubules. Stimulates the secretion of the glands of the stomach. Increases basal metabolism, increases glycogenolysis, causing hyperglycemia.

Pharmacokinetics:

Acetylsalicylic acid

Absorption is complete, fast. During absorption, it undergoes presystemic elimination in the intestinal wall and in the liver (deacetylated). 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.

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. Maximum concentration of substance in blood plasma (serum) 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 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.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.

Indications:

Feverish syndrome, rheumatic diseases, pain syndrome of mild and moderate intensity of various genesis.

ICD-10

XIII.M70-M79.M79.0   Rheumatism, unspecified

XVIII.R50-R69.R50   Fever of unknown origin

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

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 insufficiency; 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 (incl.impaired heart function, arterial hypertension), thyrotoxicosis, gout, liver disease, glaucoma, increased excitability, epilepsy and a tendency to convulsive seizures, pregnancy, breast-feeding.

Pregnancy and lactation:

Recommendations Food and Drug Administration (US Food and Drug Administration) - category D (for acetylsalicylic acid), C (for caffeine)

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.

Penetrates into breast milk (1% of its concentration in the blood plasma of the mother). If a nursing mother consumes 6-8 cups of caffeine-containing drinks per day, the child may develop hyperactivity and insomnia. If you need to use the drug during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Inside - 1 bag of powder, previously dissolved in a glass of hot water (1 packet contains 350 mg of acetylsalicylic acid, 30 mg of caffeine and 300 mg of ascorbic acid). The maximum daily dose is 4 sachets.Duration of intake should not exceed: as an anesthetic - 5 days, antipyretic - 3 days.

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.

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.

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

Strengthens the action of heparin, oral anticoagulants, reserpine, steroid hormones and hypoglycemic drugs.

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

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

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.

Caffeine

Caffeine-containing drinks (coffee, tea, soft drinks), or other caffeine-containing drugs, or other means that stimulate the central nervous system - stimulation of the central nervous system, with nervousness, irritability, insomnia, convulsions, cardiac arrhythmias.

Ascorbic acid

Ascorbic acid improves the absorption of iron and aluminum. 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.

A sudden cessation of caffeine intake can lead to increased inhibition of the central nervous system (drowsiness, depression).

The effect of caffeine on the central nervous system depends on the type of nervous system and can be manifested as excitation or inhibition of higher nervous activity.

Due to the fact that the effect of caffeine on blood pressure is made up of the vascular and cardiac components, as a result, both the effect of heart stimulation and the oppression (weak) of its activity can develop.

Instructions
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