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Excedrine
Last reviewed: 23.04.2024
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Excedrine is a combination medicine with analgesic, anti-inflammatory and antipyretic properties. In addition, it helps to improve the circulatory processes in the brain.
Indications Excedrine
It is indicated for the elimination of pains (light or medium severity) of a different nature: migraines and headaches, dental, and menstrual pains, myalgia, neuralgia, and in addition to this arthralgia.
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Release form
Produced in tablet form. Contained in bags of 2 tablets per each. In one packet - 1 sachet.
Also available in blisters - 10 tablets per one. The package contains 1, 2 or 3 blister plates.
In addition, it is available in vials closed with a lid of moisture-absorbing material, with a protective film (control of the first autopsy). In the 1st bottle 24 or 50 tablets. One package contains 1 bottle of pills.
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Pharmacodynamics
Excerdine contains substances such as caffeine with paracetamol, and aspirin.
Properties of paracetamol - antipyretic and analgesic; 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 within the peripheral tissues).
Aspirin has all three of the above actions. It allows you to quickly reduce pain (in particular, caused by inflammation), and besides this, it moderately suppresses the process of gluing of platelets and inhibits the formation of thrombi. Allows to accelerate microcirculation at the site of inflammation.
Caffeine enhances reflex spinal excitability, and at the same time activates the centers of respiration and movement of blood vessels, expands the ones located in the brain with the kidneys, and besides it in the heart and muscles of the skeleton blood vessels 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 it helps to normalize the vascular tone in the brain and accelerate the circulation in it.
Pharmacokinetics
Paracetamol is rapidly absorbed from the digestive tract, reaching a peak plasma concentration approximately 0.5-2 hours after use. Metabolism is carried out in the liver, and excretion is through the kidneys (mainly in the form of sulfate conjugates, as well as glucuronides). Less than 5% of the substance is excreted unchanged. The duration of the half-life varies between 1-4 hours. Synthesis with plasma protein in recommended dosages is insignificant, but as the dose is increased, it also increases.
The hydroxylated decay product, which is formed in the liver in a small amount (under the action of mixed oxidases) and, as a rule, is rendered harmless by synthesis with the substance glutathione, is able to be cumulated in case of an overdose with paracetamol, and subsequently provoke liver damage.
Aspirin is absorbed completely and quickly enough, and then there is rapid hydrolysis inside the gastrointestinal tract, as well as blood and liver. As a result of this process, salicylates are formed that enter the liver and are metabolized there.
Caffeine is absorbed fully and very quickly, reaching a maximum of plasma concentration in the 5-90 minute period after fasting drug use. The process of excretion in adults is almost completely performed by metabolism inside the liver. Noticeable significant variability in individual elimination indicators. On average, the half-life of blood plasma lasts 4.9 hours (range 1.9-12.2 hours). The distribution of the substance occurs over all body fluids. With plasma protein is synthesized by 35%. The metabolism of caffeine is almost complete, carried out by oxidation, and besides this acetylation with demethylation. Excretion through the kidneys. The main decay products are 1- and 7-methylxanthine, and in addition 1,7-dimethylxanthine.
Dosing and administration
Eat orally, with or after food. For children from 15 years of age and adults, the dosage is 1 tablet after every 4-6 hours.
If you experience the first signs of migraine, you should drink 2 tablets of Excerdin.
The average daily dosage is 3-4 tablets, maximum of a day can be consumed no more than 6 pieces.
After taking medication in the amount of 2 tablets, the headache and other types of pain syndromes usually pass quickly - after 15 minutes. During migraines, the easing of symptoms mostly begins after half an hour.
Without the doctor's prescription, the medicine can not be used for various pain for more than 5 days. With migraine, the same period is a maximum of 3 days.
Use Excedrine during pregnancy
Although aspirin is allowed to be taken in the 2nd trimester, the effects of a specific combination of active ingredients on lactating and pregnant women have not been studied, as a result of which the drug is contraindicated for the entire lactation and pregnancy period.
Contraindications
Among the contraindications of drugs:
- intolerance to any of the active elements of the drug;
- exacerbated ulcers or erosion in the gastrointestinal tract;
- bleeding in the gastrointestinal tract;
- classical aspirin triad (also in history);
- operations that are accompanied by bleeding;
- presence of hemorrhagic diathesis, and besides this hemophilia or hypoprothrombinemia;
- a strong increase in blood pressure;
- portal form of hypertension;
- CHD in a severe degree;
- the presence of glaucoma;
- avitaminosis of type K;
- kidney failure;
- combined use with other medicines that contain aspirin, paracetamol or another drug NSAIDs;
- deficiency in the body G6FD;
- 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 injuries, and besides using antidiabetic drugs, anticoagulants and other drugs that have aspirin or other antipyretic and analgesic substances.
Side effects Excedrine
The use of drugs can provoke such side effects: nausea along 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 digestive tract.
As a result of prolonged use, headaches with dizziness, tinnitus, visual disturbances, worsening of platelet adhesion, and hypocoagulation can develop. In addition, the development of hemorrhagic syndrome (purpura, nosebleeds and gums), deafness, Lyell or Stevens-Johnson syndromes, kidney disorders with necrotic papillitis, and also acute hepatic encephalopathy in children (symptoms: excessive fever, metabolic acidosis, disorders in work of the liver and HC, as well as vomiting).
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Overdose
Manifestations caused by paracetamol (in the case of daily use of drugs in the amount of more than 10-15 grams): in the first 24 hours, nausea along with vomiting, skin blanching, abdominal pain, development of anorexia and metabolic acidosis, as well as glucose metabolism disorder . Signs of the disorder in the liver can occur 12-48 hours after the use of the excess dose of drugs.
In case of a severe overdose, hepatic failure develops, supplemented with encephalopathy, which progresses rapidly, and then a coma and death are possible. In addition, it is possible to develop an acute form of renal failure with a tubular form of necrosis (also without a severe stage of hepatic pathology). Pancreatitis and arrhythmia are also observed. In adults, after 10 + g of the drug develops hepatotoxicity.
Manifestations caused by aspirin (when using drugs in doses exceeding 150 mg / kg): in case of mild poisoning - nausea with vomiting, eye problems, tinnitus, and with it sharp headaches with dizziness. In case of severe intoxication, the emergence of a centralized pulmonary hyperventilation (choking, dyspnoea, respiratory paralysis, the appearance of sticky cold sweat, and the development of cyanosis), and in addition to respiratory acidosis. Chronic poisoning is most likely to occur in the elderly or in children (if used for several days, drugs at a dosage greater 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, and besides confusion or strong arousal, in addition to the development of agitation, gastralgia, arrhythmia, tachycardia and hyperthermia. Also the development of delirium and headaches, the emergence of motor anxiety, increased frequency of urination and dehydration of the body. Perhaps increased pain or tactile sensitivity, the appearance of muscle twitching or tremor, and in addition nausea along with vomiting (sometimes with blood). Epileptic seizures may occur (in the case of an overdose, in tonic-clonic form) and ring in the ears.
To eliminate these signs, it is required to stabilize the electrolyte balance and to control the acid-base equilibrium. Given the state of metabolism, administer citrate / hydrogen carbonate / sodium lactate. Increasing alkalinity accelerates aspirin excretion due to alkalinization of urine. Also for the first 4 hours after taking drugs, you should do gastric lavage, induce vomiting and give the patient a laxative and activated charcoal. In addition, SH-category donors and elements that precede the glutathione-methionine binding process (within 8-9 hours after the onset of overdose symptoms), as well as acetylcysteine, should be administered for 8 hours.
Interactions with other drugs
The drug increases the effect on the body of coagulants direct action, heparin, antidiabetics, and in addition to this reserpine with steroid hormones.
When combined with methotrexate and other NSAIDs, the likelihood of adverse reactions increases.
Excerdine weakens the effect of antihypertensive drugs, furosemide with spironolactone, and in addition to anti-arthritis drugs that accelerate the excretion of uric acid.
Barbiturates, anticonvulsants, salicylamide with rifampicin, and other inducers of microsomal hepatic enzymes cause the formation of toxic products of paracetamol disintegration, which negatively affect the functioning of the liver.
Metoclopramide enhances the absorption of paracetamol. And paracetamol increases the half-life of chloramphenicol 5 times.
In case of repeated use, paracetamol is able to enhance the properties of anticoagulants (coumarin derivatives).
The combination of aspirin and paracetamol with alcohol increases the likelihood of developing hepatotoxicity. Caffeine increases the absorption of ergotamine.
Shelf life
Excerdine is suitable for use within 3 years from the date of its release.
Attention!
To simplify the perception of information, this instruction for use of the drug "Excedrine" 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.