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

Excipients: citric acid anhydrous 1114.00 mg, sodium hydrogen carbonate 942.00 mg, sodium carbonate anhydrous 332.00 mg, sorbitol 300.00 mg, sodium saccharinate 7.00 mg, sodium docusate 0.227 mg, povidone 1.287 mg, sodium benzoate 60.606 mg.

Description:

Round, flat with bevelled edges and a risk on one side of white tablets. When dissolved in water, intensive emission of gas bubbles is observed.

Pharmacotherapeutic group:analgesic non-narcotic remedy

ATX: & nbsp

N.02.B.E Anilides

N.02.B.E.01 Paracetamol

Pharmacodynamics:Paracetamol (para-aminophenol derivative) has analgesic, antipyretic and mild anti-inflammatory effects.

The exact mechanism of analgesic and antipyretic effects of paracetamol is not established. Apparently, it includes the central and peripheral components. The drug blocks cyclooxygenase I and II mainly in the central nervous system, affecting the centers of pain and thermoregulation. In inflamed tissues cellular peroxidase neutralize the effect of paracetamol on the cyclo-oxygenase, which explains the almost complete absence of his anti-inflammatory effect. The drug does not have a negative effect on water-salt metabolism (sodium and water retention) and gastrointestinal mucosa due to the lack of influence on the synthesis of prostaglandins in peripheral tissues.

Pharmacokinetics:

Absorption

Ingestion paracetamol absorbed quickly and completely. C max (the maximum concentration of paracetamol in plasma) is reached after 10 to 60 minutes after administration.

Distribution

Paracetamol quickly distributed in all tissues. Concentration in blood, saliva and plasma is the same. Binding to plasma proteins is negligible.

Metabolism

Paracetamol is mainly metabolized in the liver. There are two main ways of metabolism with the formation of glucuronides and sulfates.The latter is mainly used if the accepted dose of paracetamol exceeds the therapeutic dose.

A small amount of paracetamol is metabolized by isoenzyme cytochrome P450 to form an intermediate N-acetylbenzoquinonimine, which under normal conditions undergoes rapid detoxification with glutathione and is excreted in the urine after binding to cysteine and mercaptopuric acid; However, with massive intoxication, the content of this toxic metabolite increases.

Excretion

It is carried out mainly with urine; 90% of the accepted dose of paracetamol is excreted by the kidneys within 24 hours, mainly in the form of glucuronide (60 to 80%) and sulfate (20 to 30%). Less than 5% is displayed unchanged. The half-life is about 2 hours.

Pharmacokinetics in special groups patients

With severe renal dysfunction (creatinine clearance less than 30 ml / min) excretion of paracetamol and its metabolites is delayed.

Indications:

- Moderate or mild pain syndrome (headache, toothache, migraine pain, neuralgia, muscle pain, back pain, pain in injuries and burns, sore throat, painful menstruation);

- Elevated body temperature for colds and other infectious and inflammatory diseases.

Contraindications:

- Hypersensitivity to paracetamol, propacetamol hydrochloride (paracetamol prodrug) or any other component of the drug.

- Severe hepatic insufficiency or decompensated liver disease in the acute stage.

- Deficiency of sugar / isomaltase, intolerance to fructose, glucose-galactose malabsorption.

- Pregnancy (I and III trimester) and lactation.

- Children under 12 years.

Carefully:Severe renal insufficiency (clearance, creatinine <30 ml / min), liver failure, chronic alcoholism, malnutrition, anorexia, bulimia, cachexia, hypovolemia, dehydration, glucose-6-phosphate dehydrogenase deficiency, congenital hyperbilirubinemia (Gilbert syndrome, Dubinin-Johnson syndrome and Rotor), viral hepatitis, elderly age.

Dosing and Administration:Inside. Dissolve the tablet in a glass of water (200 ml). Do not chew or swallow tablets. Usually used for 1 - 2 tablets 2-3 times per day with intervals of at least 4 hours. The maximum single dose is 2 tablets (1 g), the maximum daily - 8 tablets (4 g), which corresponds to a single dose of 10-15 mg / kg of body weight, for maximum daily - 75 mg / kg of body weight.

As a rule, there is no need to exceed the recommended daily dose of paracetamol equal to 3 g. The daily dose can be increased to a maximum (4 g) only in case of severe pain.

If the renal function is temporary Creatinine less than 10 ml / min, not less than 6 hours - with the clearance of creatinine 10-50 ml / min.

In patients with chronic or compensated active liver diseases, especially accompanied by hepatic deficiency in patients with chronic alcoholism, chronic insufficiency nutrition (insufficient supply of glutathione in liver), dehydration or body weight less than 50 kg daily dose should not exceed 3 g, i.e. 6 tablets.

The drug should be used with caution in children and patients with weight body less than 50 kg to eliminate risk exceeding the recommended dose.

Dosage regimen in children older than 12 years and a body weight of more than 43 kg is the same as in adults, with the interval should preferably be 6 hours (strictly no less than 4 hours).

Duration reception without consultation from the doctor is not more than 5 days old. appointment to as an anesthetic and 3 days as an antipyretic agent.

Side effects:When the drug was used, The following side effects installed):

Allergic reactions: reactions Hypersensitivity, itchy skin, rash on skin and mucous membranes (erythema or urticaria), Quincke's edema, multiforme exudative erythema (including Stephen-Johnson syndrome), toxic epidermal necrolysis (Lyell's Syndrome), anaphylactic shock, acute generalized exanthematous pustulosis.

From the central and peripheral nervous system: (when taking high doses) dizziness, psychomotor agitation and disruption of orientation in space and in time.

On the part of the digestive system: nausea, Diarrhea, epigastric pain, increased activity of "liver" enzymes, as rule, without the development of jaundice, hepatonecrosis (dose-dependent effect).

From the endocrine system: hypoglycemia, up to hypoglycemic coma.

From the hematopoiesis: anemia (cyanosis), sulfogemaglobinemia, methemoglobinemia (dyspnea, pain in the heart), hemolytic anemia (especially in patients with deficiency of glucose-6-phosphate dehydrogenase),thrombocytopenia, neutropenia, and leukopenia.

Other: decrease in blood pressure (as a symptom of anaphylaxis), change prothrombin time and international normalized relationship (INR).

Overdose:

Overdose may lead to intoxication, especially in children, patients with liver diseases (caused by chronic alcoholism), in patients with eating disorders, as well as in patients taking enzyme inducers, at which fulminant hepatitis, hepatic insufficiency, cholestatic hepatitis, cytolytic hepatitis, in the cases indicated above - sometimes with a fatal outcome.

The clinical picture of acute overdose develops within 24 hours after taking paracetamol.

Symptoms: gastrointestinal disorders (nausea, vomiting, decreased appetite, discomfort in the abdomen and / or abdominal pain), pale skin, sweating, malaise. With the simultaneous administration of 7.5 grams or more to adults or children over 140 mg / kg, cytolysis of hepatocytes occurs with complete and irreversible necrosis of the liver, development of hepatic insufficiency, metabolic acidosis and encephalopathy, which can lead to coma and death. Across 12-48 hours after the introduction of paracetamol, there is an increase in activity "hepatic" transaminases, lactate dehydrogenase, concentration of bilirubin and decrease in the concentration of prothrombin. Clinical symptoms of liver damage occur 1-2 days after drug overdose and reach a maximum of 3-4 days.

Treatment:

- Immediate hospitalization;

- Determination of the quantitative content of paracetamolbut in the blood plasma before treatment at the earliest possible time after an overdose;

- Rinsing the stomach;

- Introduction donators SHgroups and precursors of the synthesis of glutathione - methionine and acetylcysteine within 8 hours after an overdose. The need for additional therapeutic measures (further introduction of methionine, in / in introduction of acetylcysteine) is determined depending on the concentration of paracetamol in blood, as well as from the time that has passed since its introduction;

- Symptomatic treatment;

- Hepatic tests should be performedOdy at the beginning of treatment and then every 24 hours. AT In most cases, the activity of hepatic transaminAs it normalizes within 1-2 weeks. In very serious cases, liver transplantation may be required.

Interaction:

Phenytoin decreases the effectiveness paracetamol and increases the risk of hepatotoxicity. Patients receiving phenytoin, frequent use of paracetamol should be avoided, especially at high doses.

Probenecid almost halves the clearance of paracetamol, inhibiting the process of its conjugation with glucuronic acid. With a simultaneous appointment, consideration should be given to reducing the dose of paracetamol.

Caution should be exercised while using paracetamol and inducers of microsomal liver enzymes (for example, ethanol, barbiturates, isoniazid, rifampicin, carbamazepine, anticoagulants, zidovudine, amoxicillin + clavulanic acid, phenylbutazone, tricyclic antidepressants).

Long-term simultaneous use of barbiturates decreases the effectiveness paracetamol.

Salicylamide can increase the time half-life of paracetamol.

Monitoring of INRs during and after the concurrent use of paracetamol (especially in high doses and / or for a long time) and coumarins (eg, warfarin), since paracetamol when taken at a dose of 4 g / day for at least 4 days may increase the effect of indirect anticoagulants and increase the risk of bleeding. If necessary, correct the dose of anticoagulants.

Special instructions:To avoid an overdose account for the content of paracetamol in other preparations that the patient receives simultaneously with Efferalgan®.

Paracetamol intake in doses exceeding recommended, can cause severe lesions of the liver.

With continued febrile syndrome against paracetamol more than 3 days, and pain syndrome - more than 5 days, consultation of the doctor is required.

The use of Efferalgan® can distort indicators of laboratory quantify the content glucose and uric acid in plasma.

To avoid toxic damage to the liver paracetamol should not be combined with the reception of alcoholic beverages, but also to people prone to chronic alcohol consumption.

The risk of liver damage increases in patients with alcoholic hepatosis.

When the drug is used for a long time, it is necessary to monitor the pattern of peripheral blood and the functional state of the liver. Paracetamol can cause serious skin reactions, such as Stephen-Johnson syndrome, toxic epidermal necrolysis, acute generalized exanthematous pustulosis, which can be lethal. At the first manifestation of rash or other hyper-responsiveness reactions, the drug should be discontinued.

Also, the use of paracetamol should be discontinued if a patient has acute viral hepatitis.

Efferalgan® contains 412.4 mg sodium per tablet, which should be taken into account by patients on a strict low-salt diet.

Because the drug contains sorbitol, it should not be used with a deficiency of sugar / isomaltase, intolerance fructose, glucose-galactose malabsorption.

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

The impact on the ability to drive and work with machinery has not been studied.

If the patient experiences dizziness, psychomotor agitation and disorientation in space and time, he is not recommended to drive and other mechanisms during treatment with the drug.

Form release / dosage:

Tablets effervescent 500 mg.

Packaging:

For 4 tablets in a strip (aluminum foil / polyethylene). 4 strips together with instructions for use in a cardboard box.

Storage conditions:

Store in a dry place at a temperature of 15-30 ° C.

Keep out of the reach of children!

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:П N011549 / 01

Date of registration:09.07.2010

The owner of the registration certificate:Bristol-Myers SquibbBristol-Myers Squibb France

Manufacturer: & nbsp

BRISTOL-MYERS SQUIBB France

Representation: & nbspBRISTOL-Majers SKVIBB, LLCBRISTOL-Majers SKVIBB, LLCRussia

Information update date: & nbsp04.10.2015

Illustrated instructions

Instructions

Efferalgan® (Efferalgan®)