Excedrine - instructions for use, dose, side effects, contraindications

Excipients: giprolose 5.0 mg, cellulose microcrystalline 100.0 mg, stearic acid 2.5 mg, film coat: carnauba wax 0.08 mg, white film material 4.48 mg (hypromellose, titanium dioxide, propylene glycol, povidone, sorbitan laurate, polysorbate-20, mineral oil, benzoic acid, simethicone emulsion, brilliant blue dye).

Description:

tablets of oblong form of white color, covered with a film shell, with engraving "E" on one side. A cross-sectional view is the core of a white or almost white color.

Pharmacotherapeutic group:analgesic combined (NSAIDs + analgesic non-narcotic remedy + psychostimulant).

ATX: & nbsp

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

Pharmacodynamics:

Excedrine®-combined preparation containing paracetamol, acetylsalicylic acid and caffeine.

Paracetamol has an analgesic, antipyretic and extremely weak anti-inflammatory effect, which is associated with its influence on the thermoregulatory center in the hypothalamus and a weak ability to inhibit the synthesis of prostaglandins in peripheral tissues. Acetylsalicylic acid has an analgesic, antipyretic and anti-inflammatory effect. Rapidly relieves pain, especially caused by the inflammatory process, and also moderately inhibits platelet aggregation and slows the process of thrombosis, improving microcirculation in the focus of inflammation.

Caffeine increases the reflex excitability of the spinal cord, excites the respiratory and vasomotor centers, dilates the blood vessels of skeletal muscles, brain, heart, kidneys, reduces platelet aggregation. Reduces drowsiness, fatigue, increases mental and physical performance. In this combination caffeine in a small dose 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 it is easily absorbed in the gastrointestinal tract, maximum concentrations in the blood plasma are detected in the interval from 30 minutes to 2 hours after administration. Paracetamol metabolized in the liver and excreted by the kidneys, mainly in the form of glucuronides and sulfate conjugates. Less than 5% of paracetamol is excreted unchanged. The duration of the half-life period varies from 1 to 4 hours. The connection with plasma proteins is negligible at usual therapeutic doses, however, it increases with increasing dose. Hydroxylated metabolite, formed in small amounts in the liver under the influence of mixed oxidases and usually rendered harmless by binding to glutathione, can accumulate at overdose of paracetamol and cause liver damage.

Acetylsalicylic acid quickly and completely absorbed, subjected to rapid hydrolysis in the gastrointestinal tract, liver and blood to the formation of salicylates, which undergo further metabolism, mainly in the liver.

Caffeine completely and quickly absorbed.The maximum concentrations are observed in the interval from 5 to 90 minutes after administration on an empty stomach. In adults, excretion occurs almost entirely through hepatic metabolism. There is a pronounced variability in the individual values of elimination in adults. The mean half-life of plasma is 4.9 hours in the range 1.9-12.2 hours. Caffeine is distributed in all liquid media of the body. Communication of caffeine with plasma proteins is 35%. Caffeine 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 various origins: headache, migraine, toothache, neuralgia, arthralgia and myalgia (pain in muscles and joints), algodismenorea (pain in menstruation).

Contraindications:

Hypersensitivity to any of the components in the preparation, erosive and ulcerative lesions of the gastrointestinal tract in the exacerbation phase, gastrointestinal bleeding, complete or incomplete combination of bronchial asthma, recurrent polypnosis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs (incl. h.in history), surgical interventions accompanied by hemorrhage, hemophilia, hemorrhagic diathesis, hypoprothrombinemia, severe arterial hypertension, portal hypertension, severe course of ischemic heart disease, glaucoma, avitaminosis K, renal failure, simultaneous use of other drugs containing paracetamol, acetylsalicylic acid or other non-steroidal anti-inflammatory agent, deficiency of glucose-6-phosphate dehydrogenase, pregnancy, lactation, increased excitability, sleep disorders, children under 15 years of age (risk of developing Reye syndrome in children with hyperthermia in the presence of viral diseases).

Carefully:Gout, liver disease, headaches associated with head trauma, taking anticoagulants, hypoglycemic drugs, gout or arthritis, and concurrent administration of drugs containing acetylsalicylic acid or other analgesic and antipyretic components.

Pregnancy and lactation:

In spite of the fact that it is possible to use acetylsalicylic acid in the second trimester of pregnancy, the safety of this combination in pregnant and breast-feeding patients has not been studied, therefore the drug is contraindicated in pregnant women (in all trimesters) and breast-feeding.

Dosing and Administration:

The drug is taken orally during or after a meal.

Adults and adolescents with 15 years of age: 1 tablet every 4-6 hours.

At the first signs of migraine, 2 tablets are taken.

The average daily dose is 3-4 tablets a day, the maximum daily dose is 6 tablets per day.

After taking 2 tablets, relief of headache and other types of pain usually comes quickly - after 15 minutes, with migraine, relief usually comes after 30 minutes.

With pain syndrome, the drug should not be taken for more than 5 days without consulting a doctor. When migraine, the drug should not be taken more than 3 days without consulting a doctor.

Side effects:

Gastralgia, nausea, vomiting, hepatotoxicity, nephrotoxicity, erosive-ulcerative lesions of the gastrointestinal tract, allergic reactions, tachycardia, increased blood pressure, bronchospasm.

With prolonged use - dizziness, headache, visual disturbances, tinnitus, decreased platelet aggregation, hypocoagulation, hemorrhagic syndrome (nosebleeds, bleeding gums, purpura, etc.), kidney damage with papillary necrosis, deafness, malignant exudative erythema (syndrome Stevens-Johnson),toxic epidermal necrolysis (Lyell's syndrome), Reye's syndrome in children (hyperpyrexia, metabolic acidosis, disorders of the nervous system and psyche, vomiting, liver dysfunction).

Overdose:

Symptoms caused by the presence of paracetamol (when taken in doses of more than 10-15 g / day): during the first 24 hours, pale skin, nausea, vomiting, anorexia, abdominal pain, glucose metabolism disorder, metabolic acidosis. Symptoms of liver dysfunction may appear 12-48 hours after an overdose. In severe overdose - liver failure with progressive encephalopathy, coma, death; acute renal failure with tubular necrosis (including in the absence of severe liver damage); arrhythmia, pancreatitis. Hepatotoxic effect in adults is manifested when taking 10 g or more. Symptoms caused by the presence of acetylsalicylic acid (when taken in doses of more than 150 mg / kg): with light intoxication - nausea, vomiting, tinnitus, visual impairment, dizziness, severe headache. In severe poisoning - hyperventilation of the lungs of the central genesis (dyspnea, choking, cyanosis, cold sticky sweat, respiratory paralysis), respiratory acidosis.The greatest risk of developing chronic intoxication is noted in children and the elderly with more than 100 mg / kg / day for several days. With moderate and severe poisoning, hospitalization is necessary.

Symptoms caused by the presence of caffeine (when taken in doses of more than 300 mg / day): gastralgia, agitation, anxiety, agitation, motor 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; ringing in the ears, epileptic seizures (with acute overdose - tonic-clonic).

Treatment: control of 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 alkalinization of urine. Gastric lavage in the first 4 hours, provocation of vomiting, intake of activated charcoal, laxatives, introduction of donators SH-rpynn and the precursors of the synthesis of glutathione methionine for 8-9 hours after an overdose and acetylcysteine - for 8 hours.

Interaction:

The drug can enhance the action of heparin, indirect coagulants, reserpine, steroid hormones and hypoglycemic) drugs.

Simultaneous use with other non-steroidal anti-inflammatory drugs, methotrexate increases the risk of side effects. Reduces the effectiveness of spironolactone, furosemide, antihypertensive drugs, as well as anti-gouty drugs that promote the excretion of uric acid. Barbiturates, rifampicin, salicylamide, antiepileptic drugs and other inducers of microsomal liver enzymes contribute to the formation of toxic metabolites of paracetamol that affect liver function. Metoclopramide accelerates the absorption of paracetamol. Under the influence of paracetamol, the half-life of chloramphenicol increases five-fold. With repeated admission, paracetamol can enhance the effect of anticoagulants (coumarin derivatives).

Simultaneous reception of paracetamol,Acetylsalicylic acid and alcoholic beverages increase the risk of hepatotoxic effects. Caffeine accelerates the absorption of ergotamine.

Special instructions:

If symptoms persist after taking the drug, worsening or new symptoms occur, immediately consult a doctor. When taking the drug at the recommended dose, the same amount of caffeine is fed into the body as it is contained in one cup of coffee, so you should reduce the consumption of caffeine-containing products when treated with this drug in order to avoid the development of nervous excitement, irritability, insomnia and rapid heartbeat against caffeine overdose.

If you suspect an overdose, you should immediately seek medical help, even if you have no symptoms.

It should be refrained from drinking alcohol when taking the drug in connection with an increased risk of liver damage and gastrointestinal bleeding. Because the acetylsalicylic acid slows the clotting of blood, the patient, who is to undergo surgery, 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 a predisposition the drug can trigger a gout attack. With continued use of the drug, control of peripheral blood and the functional state of the liver is necessary.

Effect on the ability to drive transp. cf. and fur:

It was not reported on the effect of the drug on the ability to drive and work with machinery.

Form release / dosage:

Film-coated tablets.

Packaging:

2 tablets in a multilayer bag made of aluminum foil and polymer laminate. The bag together with the instruction for use is placed in a cardboard box.

For 10 tablets in a blister of PVC / PCTFE / PVC film and aluminum foil. For 1, 2 or 3 blisters together with instructions for use are placed in a cardboard box.

For 24 or 50 tablets in a vial of PVP, sealed with a white polypropylene lid, equipped with a moisture-absorbing material and a protective film to control the first opening. The bottle together with the instruction for use is placed in a cardboard box.

Storage conditions:

At a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

2 years.Do not use after the expiry date indicated on the package.

Terms of leave from pharmacies:Without recipe

Registration number:P N009980

Date of registration:08.02.2011

The owner of the registration certificate:Новартис Консьюмер Хелс САНовартис Консьюмер Хелс СА Switzerland

Manufacturer: & nbsp

NOVARTIS CONSUMER HEALTH, S.A. Switzerland

Representation: & nbspNOVARTIS CONSUMER HELS S.A. (part of Novartis groups) NOVARTIS CONSUMER HELS S.A. (part of Novartis groups) Switzerland

Information update date: & nbsp08.02.2011

Illustrated instructions

Instructions

Excedrine® (Exedrin®)