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Active ingredients
Acetylsalicylic acid + Caffeine + Paracetamol
Release form
Pills
Composition
1 tablet contains active substances: paracetamol 250 mg acetylsalicylic acid 250 mg Caffeine 65 mg adjuvants: Hyprolosis - 5 mg; MCC - 100 mg; stearic acid - 2.5 mg film shell: carnauba wax - 0.08 mg; white film material (hypromellose, titanium dioxide, propylene glycol, povidone, sorbitan laurate, polysorbate 20, mineral oil, benzoic acid, simethicone emulsion, brilliant blue dye) - 4.48 mg
Pharmacological effect
Excedrine is a combined preparation containing paracetamol, acetylsalicylic acid and caffeine. Paracetamol has analgesic, antipyretic and extremely weak anti-inflammatory effect, due to its effect on the thermoregulation center in the hypothalamus and the weakly expressed ability to inhibit GH synthesis in peripheral tissues. Acetylsalicylic acid has analgesic, antipyretic and anti-inflammatory effects. Quickly relieves pain, especially caused by the inflammatory process, and also moderately inhibits platelet aggregation and slows the thrombosis process, improving microcirculation in the inflammation. kidney, reduces platelet aggregation. Reduces drowsiness, fatigue, increases mental and physical performance. In this combination, a small dose of caffeine practically does not have a stimulating effect on the central nervous system, but it contributes to the normalization of the vascular tone of the brain and the acceleration of blood flow in it.
Pharmacokinetics
Paracetamol is easily absorbed in the gastrointestinal tract, Tmax in blood plasma - in the interval from 30 minutes to 2 hours after administration. Paracetamol is metabolized in the liver and excreted by the kidneys, mainly in the form of glucuronides and sulphate conjugates. Less than 5% paracetamol is excreted unchanged. The duration of T1 / 2 varies from 1 to 4 hours. The association with plasma proteins is insignificant at usual therapeutic doses, but increases with increasing dose. The hydroxylated metabolite,formed in small quantities in the liver under the influence of mixed oxidases and usually neutralized by binding to glutathione, can accumulate during paracetamol overdose and cause liver damage. Acetylsalicylic acid is rapidly and completely absorbed, undergoes rapid hydrolysis in the gastrointestinal tract, liver and blood before the formation of salicylates, which are subjected to further metabolism, mainly in the liver. Caffeine is completely and rapidly absorbed. Tmax in blood plasma - in the interval from 5 to 90 minutes after administration on an empty stomach. In adults, excretion is almost entirely through hepatic metabolism. There is a pronounced variability of individual values of elimination in adults. The mean T1 / 2 from plasma is 4.9 hours (in the range 1.9–12.2 hours). Caffeine is distributed in all body fluids. The relationship of caffeine with plasma proteins is 35%. Caffeine is almost completely metabolized by oxidation, demethylation and acetylation and excreted by the kidneys. The main metabolites are 1-methylxanthine, 7-methylxanthine, 1,7-dimethylxanthine.
Indications
Pain syndrome of medium and light intensity of different origin: headache, migraine, toothache, neuralgia, arthralgia and myalgia (pain in muscles and joints), algomenorrhea (pain during menstruation).
Contraindications
hypersensitivity to any of the components of the drug; erosive and ulcerative lesions of the gastrointestinal tract in the acute phase; gastrointestinal bleeding; a complete or incomplete combination of bronchial asthma, recurrent nasal polypnosis and acetylsalicylic acid or other NSAIDs (including history); surgery, accompanied by bleeding; hemophilia; hemorrhagic diathesis; hypoprothrombinemia; severe arterial hypertension; portal hypertension; severe ischemic heart disease; glaucoma; ittamosis K; renal failure; simultaneous use of other drugs containing paracetamol, acetylsalicylic acid or other NSAIDs; glucose-6-phosphate dehydrogenase deficiency; irritability; sleep disturbances; pregnancy; lactation; children under 15 years of age (risk of developing Reye’s syndrome in children with hyperthermia on the background of viral diseases).
Precautionary measures
With care: gout or arthritis; liver disease; headaches associated with head trauma; taking anticoagulants, hypoglycemic agents, as well as the simultaneous use of drugs containing acetylsalicylic acid or other painkillers and antipyretic components.
Use during pregnancy and lactation
Despite the fact that acetylsalicylic acid can be used in the second trimester of pregnancy, the safety of this combination in pregnant and lactating women has not been studied, so the drug is contraindicated for pregnant women (in all trimesters) and lactating.
Dosage and administration
Inside, during or after a meal. Adults and adolescents from 15 years: 1 tab. every 4–6 hours. At the first signs of migraine, table 2 is taken. The average daily dose is 3-4 tables. per day, the maximum daily dose - 6 pills. per day. After taking 2 tab. relief of headache and other types of pain usually comes quickly - after 15 minutes, with migraine, relief usually comes after 30 minutes. In pain syndrome, the drug should not be taken for more than 5 days without consulting a doctor; with migraine, the drug should not be taken for more than 3 days without consulting a doctor.
Side effects
Gastralgia, nausea, vomiting, hepatotoxicity, nephrotoxicity, erosive and ulcerative lesions of the gastrointestinal tract, allergic reactions, tachycardia, increased blood pressure, bronchospasm. With prolonged use - dizziness, headache, visual disturbances, tinnitus, reduction of platelet aggregation, hypocoagulation, hemorrhagic syndrome (nasal bleeding, bleeding gums, purpura), kidney damage with papillary necrosis, deafness, malignant exudative erythema, syndromy, syndromy. ), toxic epidermal necrolysis (Lyell's syndrome), Reye's syndrome in children (hyperpyrexia, metabolic acidosis, disorders of the nervous system and the psyche, vomiting, abnormal liver function).
Overdose
Symptoms due to the presence of paracetamol (when taken in doses of more than 10–15 g / day): for the first 24 hours, pallor of the skin, nausea, vomiting, anorexia, abdominal pain, impaired glucose metabolism, metabolic acidosis. Symptoms of abnormal liver function may appear 12–48 h after overdose. In severe overdose, liver failure with progressive encephalopathy, coma, death; acute renal failure with tubular necrosis (including in the absence of severe damage to the liver); arrhythmia, pancreatitis.Hepatotoxic effect in adults manifests when taking 10 g or more. Symptoms caused by the presence of acetylsalicylic acid (when taken in doses of more than 150 mg / kg): for mild intoxications - nausea, vomiting, tinnitus, blurred vision, dizziness, severe headache . In severe poisoning, hyperventilation of the central lung (dyspnea, asphyxiation, cyanosis, cold sticky sweat, respiratory paralysis), respiratory acidosis. The greatest risk of chronic intoxication is observed in children and the elderly when taking for several days more than 100 mg / kg / day. In case of moderate and severe poisoning, hospitalization is required. Symptoms due to caffeine (when taken in doses of more than 300 mg / day): gastralgia, agitation, anxiety, agitation, anxiety, confusion, delirium, dehydration, tachycardia, arrhythmia, hyperthermia, frequent urination, headache, increased tactile or pain sensitivity, tremor, or muscle twitching; nausea and vomiting, sometimes with blood; tinnitus, epileptic seizures (in acute overdose - tonic-clonic). Treatment: control 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 alkalinity increases the excretion of acetylsalicylic acid due to alkalization of urine. Gastric lavage in the first 4 hours, induction of vomiting, the appointment of activated carbon, laxative drugs, the introduction of donators of SH-groups and precursors of the synthesis of glutathione - methionine for 8–9 hours after overdose and acetylcysteine - for 8 hours
Interaction with other drugs
The drug can increase the effects of heparin, indirect coagulants, reserpine, steroid hormones and hypoglycemic LS.Odnovremennoe use with other NSAIDs, methotrexate increases the risk of side effektov.Umenshaet efficiency spironolactone, furosemide, antihypertensive drugs, as well as protivopodagricakih drugs that promote excretion of uric kisloty.Barbituraty , rifampicin, salicylamide, antiepileptic drugs and other inducers of microsomal liver enzymes promote the formation of toxic meta Olita paracetamol, affecting pecheni.Metoklopramid function speeds up the absorption of paracetamol.Under the influence of paracetamol T1 / 2 chloramphenicol is increased 5 times. When repeated, paracetamol can increase the effect of anticoagulants (coumarin derivatives). Simultaneous reception of paracetamol, acetylsalicylic acid and alcoholic beverages increases the risk of hepatotoxic effects. Caffeine accelerates the absorption of ergotamine.
special instructions
If after taking the drug the symptoms persist, worsening or new symptoms occur, you should immediately consult a doctor. When taking the drug in the recommended dose, the body receives as much caffeine as is contained in one cup of coffee, therefore, the consumption of caffeine-containing products should be reduced during treatment with this drug in order to avoid the development of nervous excitement, irritability, insomnia and heart palpitations due to caffeine overdose. If you suspect an overdose, you should immediately seek medical help, even if the symptoms are absent. You should refrain from using alcohol while taking the drug due to the increased risk of liver damage and gastrointestinal bleeding. Since acetylsalicylic acid slows down blood clotting, the patient who has to undergo surgery intervention, must warn the doctor in advance about taking the drug. Acetylsalicylic acid in low doses reduces the excretion of uric acid, and therefore in patients with predisposition the drug can provoke an attack of gout. With prolonged use of the drug requires monitoring of peripheral blood and the functional state of the liver. The effect on the ability to drive vehicles and work with mechanisms. Not reported on the effect of the drug on the ability to drive and work with mechanisms.