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Excedrin
Last reviewed: 03.07.2025
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Excedrin is a combination drug that has analgesic, anti-inflammatory and antipyretic properties. In addition, it helps improve blood circulation in the brain.
Indications Excedrin
It is indicated for the relief of pain (mild or moderate severity) of various origins: migraines and headaches, toothaches, as well as menstrual pain, myalgia, neuralgia, and in addition arthralgia.
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Release form
Available in tablet form. Contained in sachets of 2 tablets each. One pack contains 1 sachet.
Also available in blisters - 10 tablets per blister. The package contains 1, 2 or 3 blister strips.
In addition, it is available in vials closed with a cap made of moisture-absorbing material, with a protective film (1st opening control). 1 vial contains 24 or 50 tablets. One package contains 1 vial with tablets.
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Pharmacodynamics
Excedrin contains substances such as caffeine with paracetamol and aspirin.
The properties of paracetamol are antipyretic and analgesic; it also has a weak anti-inflammatory effect (due to the effect on the thermoregulatory center located in the hypothalamus, as well as a weak ability to suppress the synthesis of PG in peripheral tissues).
Aspirin has all three of the above effects. It allows you to quickly reduce pain (especially caused by inflammation), and in addition, it moderately suppresses the process of platelet aggregation and slows down the formation of blood clots. It allows you to speed up microcirculation in the area of inflammation.
Caffeine increases reflex spinal excitability, and at the same time activates the centers of respiration and vascular movement, dilates blood vessels located in the brain with kidneys, and in addition to this, in the heart and skeletal muscles, and weakens the adhesion of platelets. Relieves fatigue and drowsiness, improves physical, and at the same time mental performance. Caffeine, with such a combination of elements in a small dosage, almost does not stimulate the central nervous system, but helps to normalize vascular tone in the brain and accelerate blood circulation in it.
Pharmacokinetics
Paracetamol is rapidly absorbed from the gastrointestinal tract, reaching peak plasma concentrations approximately 0.5-2 hours after ingestion. Metabolism occurs in the liver and excretion occurs through the kidneys (mainly in the form of sulfate conjugates and glucuronides). Less than 5% of the substance is excreted unchanged. The half-life ranges from 1-4 hours. Synthesis with plasma protein is insignificant at recommended medicinal doses, but it also increases as the dose increases.
The hydroxylated breakdown product, which is formed in small quantities in the liver (under the influence of mixed oxidases) and, as a rule, is neutralized through synthesis with the substance glutathione, can accumulate in the case of an overdose of paracetamol, and subsequently provoke liver damage.
Aspirin is completely and fairly quickly absorbed, and then undergoes rapid hydrolysis in the gastrointestinal tract, as well as in the blood and liver. As a result of this process, salicylates are formed, which enter the liver and are metabolized there.
Caffeine is absorbed completely and very quickly, reaching a maximum plasma concentration in the period of 5-90 minutes after taking the drug on an empty stomach. The excretion process in adults is almost entirely carried out by metabolism in the liver. Significant variability in individual elimination rates is noticeable. On average, the half-life from blood plasma lasts 4.9 hours (range 1.9-12.2 hours). The substance is distributed throughout all body fluids. With plasma protein, 35% is synthesized. Caffeine is almost completely metabolized by oxidation, and in addition, acetylation with demethylation. Excretion is through the kidneys. The main decay products are 1- and 7-methylxanthine, and in addition 1,7-dimethylxanthine.
Dosing and administration
Take orally, with or after food. For children over 15 years of age and adults, the dosage is 1 tablet every 4-6 hours.
At the first signs of a migraine, take 2 Excedrin tablets.
The average daily dosage is 3-4 tablets, the maximum you can take per day is 6 tablets.
After taking the medicine in the amount of 2 tablets, headaches and other types of pain syndromes usually pass quickly - after 15 minutes. During migraines, the weakening of symptoms usually begins after half an hour.
Without a doctor's prescription, the medicine cannot be used for various pains for more than 5 days. For migraines, the same period is a maximum of 3 days.
Use Excedrin during pregnancy
Although aspirin is permitted to be taken in the 2nd trimester, the effect of a specific combination of active ingredients on lactating and pregnant women has not been studied, as a result of which the drug is contraindicated for the entire period of lactation and pregnancy.
Contraindications
Among the contraindications of the drug:
- intolerance to any of the active ingredients of the drug;
- aggravated ulcers or erosions in the gastrointestinal tract;
- gastrointestinal bleeding;
- classic aspirin triad (also in history);
- operations that are accompanied by bleeding;
- the presence of hemorrhagic diathesis, and in addition hemophilia or hypoprothrombinemia;
- a sharp increase in blood pressure;
- portal hypertension;
- Severe coronary heart disease;
- presence of glaucoma;
- avitaminosis type K;
- renal failure;
- combined use with other medications containing aspirin, paracetamol or other NSAIDs;
- G6PD deficiency in the body;
- strong excitability;
- sleep disorders;
- children under 15 years of age (children with hyperthermia may develop white liver disease - against the background of viral pathologies).
Caution is necessary if the patient has arthritis or gout, liver pathologies and headaches due to head injury, as well as when using antidiabetic drugs, anticoagulants and other drugs that contain aspirin or other antipyretic and analgesic substances.
Side effects Excedrin
The use of drugs can provoke the following side effects: nausea with vomiting, allergies, bronchial spasms, gastralgia, nephro- and hepatotoxicity, tachycardia, as well as an increase in blood pressure and the appearance of ulcers and erosions in the gastrointestinal tract.
As a result of prolonged use, headaches with dizziness, tinnitus, visual disturbances, deterioration of platelet aggregation processes, and hypocoagulation may develop. In addition, hemorrhagic syndrome (purpura, bleeding from the nose and gums), deafness, Lyell's or Stevens-Johnson syndromes, kidney disorders with necrotic papillitis, and acute hepatic encephalopathy in children (symptoms: excessive fever, metabolic acidosis, liver and nervous system disorders, and vomiting) may develop.
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Overdose
Manifestations caused by paracetamol (in case of daily consumption of the drug in the amount of more than 10-15 g): in the first 24 hours there is nausea together with vomiting, paleness of the skin, abdominal pain, development of anorexia and metabolic acidosis, as well as disorder of the glucose metabolism process. Signs of disorder in liver function may appear 12-48 hours after consumption of an excessive dose of the drug.
In case of severe overdose, liver failure develops, accompanied by encephalopathy, which progresses rapidly, and then a comatose state and death are possible. In addition, acute renal failure with tubular necrosis (also without a severe stage of liver pathology) may develop. Pancreatitis and arrhythmia are also observed. In adults, hepatotoxicity develops after consuming 10+ g of the drug.
Manifestations caused by aspirin (when using the drug in doses exceeding 150 mg/kg): in case of mild poisoning - nausea with vomiting, vision problems, the appearance of noise in the ears, and along with this, sharp headaches with dizziness. In case of severe intoxication - the appearance of central pulmonary hyperventilation (suffocation, dyspnea, respiratory paralysis, the appearance of sticky cold sweat, as well as the development of cyanosis), and in addition to this, respiratory acidosis. Chronic poisoning is most likely to occur in the elderly or children (when using the drug for several days in a dose of more than 100 mg/kg). In case of moderate or severe intoxication, the patient must be hospitalized.
Symptoms caused by caffeine (when consumed in daily doses exceeding 300 mg): a feeling of anxiety, as well as confusion or strong excitement, in addition to this, the development of agitation, gastralgia, arrhythmia, tachycardia and hyperthermia. Also the development of delirium and headaches, the occurrence of motor restlessness, increased frequency of urination and dehydration. Increased pain or tactile sensitivity, the appearance of muscle twitching or tremor, and also nausea with vomiting (sometimes with blood) are possible. Epileptic seizures may occur (in case of overdose - in tonic-clonic form) and ringing in the ears.
To eliminate these symptoms, it is necessary to stabilize the electrolyte balance and control the acid-base balance. Taking into account the state of metabolism, administer sodium citrate/hydrocarbonate/lactate. Increasing alkalinity accelerates the excretion of aspirin due to alkalization of urine. Also, during the first 4 hours after taking the drug, gastric lavage should be done, vomiting should be induced, and the patient should be given a laxative and activated carbon. In addition, SH-category donors and elements preceding the process of glutathione binding should be administered - methionine (for 8-9 hours after the appearance of overdose signs), as well as acetylcysteine - for 8 hours.
Interactions with other drugs
The drug increases the effect on the body of direct acting coagulants, heparin, antidiabetic agents, and in addition reserpine with steroid hormones.
When combined with methotrexate and other NSAIDs, the likelihood of side effects increases.
Excedrin weakens the effect of antihypertensive drugs, furosemide with spironolactone, and also anti-gout drugs that accelerate the excretion of uric acid.
Barbiturates, anticonvulsants, salicylamide with rifampicin, as well as other inducers of microsomal liver enzymes cause the formation of toxic paracetamol breakdown products that negatively affect liver function.
Metoclopramide enhances the absorption of paracetamol. And paracetamol increases the half-life of chloramphenicol by 5 times.
In case of repeated use, paracetamol can enhance the properties of anticoagulants (coumarin derivatives).
The combination of aspirin and paracetamol with alcohol increases the likelihood of hepatotoxicity. Caffeine increases the absorption of ergotamine.
Shelf life
Excedrin is good for use for 3 years from the date of manufacture.
Attention!
To simplify the perception of information, this instruction for use of the drug "Excedrin" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.