Composition:
1 tablet contains:
active substances: acetylsalicylic acid - 0.24 g
paracetamol - 0.18 g caffeine (in terms of caffeine monohydrate) - 0.03 g
excipients:
cocoa beans powder - 0.0225 g citric acid monohydrate - 0.0050 g potato starch - 0.0615 g
talc - 0.0055 g
calcium stearate - 0,0055 g
Pharmacodynamics:
Combined drug. Acetylsalicylic acid (ASA) has antipyretic and anti-inflammatory effects, alleviates pain, improves microcirculation in the focus of inflammation. Paracetamol has analgesic, antipyretic and extremely weak anti-inflammatory action. Caffeine reduces drowsiness, fatigue, increases mental and physical performance; raises the vascular tone of the brain.
Indications:
Pain syndrome of weak and moderate severity (of various genesis):
• headache;
• migraine;
• toothache;
• neuralgia;
• myalgia;
• arthralgia;
• algomenorrhea.
Febrile syndrome:
• in case of acute respiratory diseases (ARI), including influenza.
Pharmacokinetics:
ASC: when ingested absorption is complete. During absorption, it is subjected to presystemic elimination in the intestinal wall and systemic in the liver (deacetylated).
The resorbed part is rapidly hydrolyzed by cholinesterase and albumin esterase, therefore the half-life is no more than 15-20 minutes. It circulates in the body (75-90% due to albumin) and is distributed in the tissues as the salicylic acid anion. The time to reach maximum concentration is 2 hours.
Metabolized mainly in the liver to form 4 metabolites found in many tissues and urine. Excreted by active secretion in the tubules of the kidneys in the form of salicylate (60%) and its metabolites. The excretion of unchanged salicylate depends on the urine pH (when alkalinization of urine increases, the ionization of salicylates increases, their reabsorption worsens and excretion increases significantly). The rate of excretion depends on the dose: when small doses are taken, the half-life is 2-3 hours, with an increase in dose it can increase up to 15-30 hours. In newborns, the elimination of salicylates is much slower than in adults.
Paracetamol: adsorption is high, the maximum concentration is reached in 0.5-2 hours and is 5-20 μg / ml. Communication with plasma proteins - 15%. It penetrates the blood-brain barrier. Less than 1% of the paracetamol dose taken by the nursing mother passes into breast milk. A therapeutically effective concentration of paracetamol in plasma is achieved when taken in a dose of 10-15 mg / kg. Metabolized in the liver (90-95%): 80% reacts conjugation with glucuronic acid and sulfates with the formation of inactive metabolites; 17% undergoes hydroxylation with the formation of 8 active metabolites, which are conjugated with glutathione with the formation of already inactive metabolites. With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. CYP2E1 isoenzyme is also involved in the metabolism. The half-life is 1-4 hours.
Excreted by the kidneys as metabolites, mainly conjugates, only 3% unchanged. In elderly patients, the clearance of the drug decreases and the half-life increases. Caffeine: when ingested, good absorption occurs throughout the intestine. Absorption occurs mainly due to lipophilicity, but not water solubility.
The maximum concentration is reached in 50-75 minutes and is 1.58-1.76 mg / l. It is rapidly distributed in all organs and tissues of the body; easily penetrates the blood-brain barrier and the placenta. The volume of distribution in adults is 0.4-0.6 l / kg, in newborns it is 0.78-0.92 l / kg.
Communication with blood proteins (albumin) - 25-36%. More than 90% of children undergo metabolism in the liver, up to 10-15% in children of the first years of life.
In adults, about 80% of the dose of caffeine is metabolized to paraxanthin, about 10% to theobromine and about 4% to theophylline, which are subsequently demethylated to monomethylxanthines and then to methylated uric acids.
The elimination half-life in adults is 3.9-5.3 h (sometimes up to 10 h), in newborns it is 65-130 h (by 4-7 months of life it decreases to the value in adults). The excretion of caffeine and its metabolites is carried out by the kidneys (1-2% is excreted unchanged in adults, up to 85% in newborns).
Side effects:
Allergic reactions (including Stevens-Johnson syndrome, Lyell syndrome), bronchospasm. On the part of the digestive tract: gastralgia, nausea, vomiting, hepatotoxicity, erosive and ulcerative lesions of the gastrointestinal tract. On the part of the hemopoietic system: with prolonged use - a reduction in platelet aggregation, hypocoagulation, hemorrhagic syndrome (nosebleeds, bleeding gums, purpura, etc.).
Since the cardiovascular system: increased blood pressure, tachycardia. On the part of the central nervous system: with prolonged use - dizziness, headache, blurred vision, tinnitus, deafness. On the part of the urinary system: nephrotoxicity, with prolonged use - kidney damage with papillary necrosis.
Perhaps the development of Reye's syndrome in children (hyperpyrexia, metabolic acidosis, disorders of the nervous system and psyche, vomiting, liver dysfunction). Sales features
Without prescription:
Special conditions:
With prolonged use of the drug requires monitoring of peripheral blood and the functional state of the liver.
Since ASA slows down blood clotting, the patient, if he is to undergo surgery, must notify the doctor in advance about taking the drug. ASC in low doses reduces the excretion of uric acid.
In patients with a corresponding predisposition, this can in some cases provoke an attack of gout. During treatment, you should stop using ethanol (increased risk of gastrointestinal bleeding). Ability to influence the speed of reactions when driving vehicles or working with other mechanisms One should refrain from driving and working with other mechanisms, since caffeine, which is part of the drug, can cause impaired concentration of attention and speed of reactions.
Indications:
Pain syndrome of weak and moderate severity (of various genesis):
• headache;
• migraine;
• toothache;
• neuralgia;
• myalgia;
• arthralgia;
• algomenorrhea.
Febrile syndrome:
• in case of acute respiratory diseases (ARI), including influenza.
Contraindications:
Hypersensitivity; erosive and ulcerative lesions of the gastrointestinal tract (in the acute phase); gastrointestinal bleeding; complete and incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to ASA or other nonsteroidal anti-inflammatory drugs (including in history);
hemophilia,
hemorrhagic diathesis,
hypoprothrombinemia;
portal hypertension; avitaminosis K;
renal failure; pregnancy, lactation; deficiency of glucose-6-phosphate dehydrogenase; arterial hypertension of III degree; severe ischemic heart disease; glaucoma; hyperexcitability; sleep disorders; surgical procedures involving bleeding;
children's age (up to 15 years - the risk of Reye's syndrome in children with hyperthermia on the background of viral diseases). Carefully
Gout, hyperuricemia; peptic ulcer and 12 duodenal ulcers, gastrointestinal bleeding (in history); renal or hepatic failure, chronic obstructive pulmonary disease, hay fever, nasal polyposis, drug allergy; simultaneous use of methotrexate in a dose of less than 15 mg / week; concomitant anticoagulant therapy; elderly age.
Use during pregnancy and during breastfeeding
Use during pregnancy and lactation is contraindicated.
Drug Interactions:
ASA: enhances the action of heparin, indirect anticoagulants, reserpine, steroid hormones, hypoglycemic agents. Simultaneous use with methotrexate and nonsteroidal anti-inflammatory drugs increases the risk of side effects. Reduces the effectiveness of spironolactone, furosemide, antihypertensive drugs, anti-gout agents.
Paracetamol: simultaneous use with barbiturates, rifampicin, salicylamide, antiepileptic drugs, other inducers of liver microsomal enzymes promotes the formation of toxic paracetamol metabolites that affect liver function.
Simultaneous use with ethanol increases the risk of hepatotoxic effects. Metoclopramide accelerates the absorption of paracetamol. Under the influence of paracetamol, the half-life of chloramphenicol is increased 5 times. With repeated use of paracetamol can enhance the effect of anticoagulants (coumarin derivatives). Caffeine: accelerates the absorption of ergotamine, reduces the absorption of calcium preparations, reduces the effect of narcotic and hypnotic drugs. With simultaneous use with β2-adrenergic at high doses (salbutamol, fenoterol) increases the risk of hypokalemia, with methylxanthines, their concentration in plasma increases and the risk of toxic action increases.
Dosage:
Inside (during or after meals). Adults and children over 15 years 1-2 tablets 2-3 times a day. The break between taking the drug should be at least 4 hours. The average daily dose is 3-4 tablets, the maximum daily dose is 8 tablets. The course of treatment is not more than 7-10 days.
The drug should not be taken more than 5 days as an analgesic drug and more than 3 days - antipyretic (without prescription and observation of a doctor). Other doses and regimens are prescribed by a doctor.
Overdose:
Symptoms caused by ASA: for mild intoxication - nausea, vomiting, gastralgia, dizziness, tinnitus; with severe intoxication - lethargy, drowsiness, collapse, convulsions, bronchospasm, difficulty breathing, anuria, bleeding, encephalopathy, coma. Initially, central hyperventilation of the lungs leads to respiratory alkalosis (shortness of breath, asphyxiation, cyanosis, perspiration); with increasing intoxication, progressive respiratory paralysis and dissociation of oxidative phosphorylation cause respiratory acidosis. After 1-2 days, signs of liver damage are identified (liver failure).
Symptoms caused by paracetamol: during the first 24 hours after administration - pallor of the skin, nausea, vomiting, anorexia, pain in the abdominal region; metabolic acidosis. After 12-48 hours - symptoms of abnormal liver function. In severe overdose - liver failure with progressive encephalopathy, coma, death; acute renal failure with tubular necrosis; arrhythmia; pancreatitis. Hepatotoxic effect in adults appears when taking 10 g or more. Treatment: gastric lavage, the appointment of adsorbents (activated carbon).
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 (increasing reserve alkalinity increases the excretion of ASA due to alkalization of urine). In case of liver lesions caused by paracetamol, administration of acetylcysteine specific antidote as early as possible (within 8 hours after overdose).
