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

Excipients: Macrogol-6000 - 20,000 g; sugar syrup (sucrose, water) - 50,000 g; sodium saccharinate - 0.150 g; potassium sorbate - 0.400 g; citric acid - 0.107 g; aroma caramel-vanilla * - 0.200 g; purified water - up to 100 ml.

* Composition of caramel-vanilla flavoring: Butanedione, acetylmethyl carbinol, benzaldehyde, propylene glycol, gamma-heptalactone, benzyl alcohol, triacetin, piperronal, amylcinnamate, vanillin, acetyl vanillin.

Description:Slightly viscous brown solution with a caramel-vanilla scent.

Pharmacotherapeutic group:analgesic non-narcotic remedy

ATX: & nbsp

N.02.B.E Anilides

N.02.B.E.01 Paracetamol

Pharmacodynamics:

Paracetamol has an analgesic, antipyretic and weak anti-inflammatory effect. The exact mechanism of analgesic and antipyretic effects of paracetamol is not established. Apparently, it includes the central and peripheral components. Paracetamol blocks cyclooxygenase 1 (COX) and COX2 mainly in the central nervous system, affecting the centers of pain and thermoregulation. In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on COX, which explains the almost complete absence of anti-inflammatory effect. The absence of a blocking effect on the synthesis of prostaglandins in peripheral tissues causes the absence of a negative effect on the water-salt metabolism (delay Na + and water) and the mucous membrane of the gastrointestinal tract.

Pharmacokinetics:

Absorption of paracetamol after ingestion is complete and rapid. The maximum concentration in plasma is reached in 30-60 minutes after administration. The distribution of paracetamol in tissues is rapid. The volume of distribution in children is 0.7-1.01 l / kg.

Appropriate concentrations of paracetamol in blood, saliva and plasma are achieved. The connection with plasma proteins is low, 10-25%. Penetrates through the blood-brain barrier.

Paracetamol is metabolized mainly in the liver with the formation of glucuronides and sulfates. A small part (4%) of paracetamol is metabolized by cytochrome P450 to form an active intermediate metabolite (N-acetylbenzoquinonimine), which under normal conditions is quickly rendered harmless by reduced glutathione and is excreted in the urine after binding to cysteine and mercapturic acid. However, with massive intoxication, the amount of this toxic metabolite increases. The half-life in adults is 2.7 hours, in children 1.5-2 hours, in newborns 3.5 hours, and the total clearance is 18 liters per hour. Paracetamol is excreted mainly in the urine; 90% of the accepted dose is excreted by the kidneys within 24 hours, mainly in the form of glucuronide (60-80%) and sulfate (20-30%).

Less than 5% is displayed unchanged. In severe renal failure (creatinine clearance below 10-30 ml / min) excretion of paracetamol somewhat slows down. The rate of excretion of glucuronide and sulfate in patients with severe renal failure is less than in healthy patients.

Children under 10 years paracetamol more deduced in the form of sulphate, and not glucuronide, which is typical for adult patients. The total excretion of paracetamol and its metabolites in patients of all age groups is the same.

Indications:

Efferalgan is used in children from 1 month to 12 years old (with a body weight of 4 to 32 kg) as an antipyretic agent for acute respiratory infections, influenza, childhood infections, post-vaccination reactions and other conditions accompanied by fever.

The drug is also used as an anesthetic for pain syndrome of mild or moderate intensity, including: headache and toothache, muscle pain, neuralgia, pain in injuries and burns.

Contraindications:

Do not use if your child has:

- hypersensitivity to paracetamol, propacetamol hydrochloride (paracetamol prodrug) or other components of the drug;

- severe liver dysfunction or decompensated liver disease in the active stage;

- age up to 1 month;

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

Carefully:

Severe renal insufficiency (creatinine clearance <30 ml / min), hepatic insufficiency, chronic alcoholism, anorexia, bulimia, cachexia, hypovolemia, dehydration, deficiency of glucose-6-phosphate dehydrogenase.

Dosing and Administration:

The average single dose of the drug depends on the weight of the child and is 10-15 mg / kg of body weight.

The maximum daily dose should not exceed 60 mg / kg of body weight. The minimum interval between doses of the drug should be 4 hours. Follow regular intervals between taking the drug. For convenience and accuracy of dosing, use a measuring spoon.

On the measuring spoon, there are divisions indicating the child's body weight: 4, 6, 8, 10, 12, 14 or 16 kg.

Undetected divisions correspond to the intermediate body weight: 5, 7, 9, 11, 13 or 15 kg.

Children with body weight from 4 to 16 kg: fill the measuring spoon up to the mark corresponding to the mass of the child's body, or to the mark closest to the body weight of the child. For example, if the weight of your child is from 4 to 5 kg, fill the measuring spoon up to the mark corresponding to 4 kg. If necessary, the drug should be taken every 4-6 hours.

Children with body weight from 16 to 32 kg: fill the measuring spoon up to the mark corresponding to 10 kg, then refill the measuring spoon until the label so as to obtain the weight of the child's body in total. For example, if your child's weight is between 18 and 19 kg, fill the measuring spoon up to a mark corresponding to 10 kg, then refill the measuring spoon up to a mark of 8 kg. If necessary, the drug should be taken every 4-6 hours.

The drug can be given to a child both without dilution, and after dilution (water, milk or juice).

Duration of treatment:

3 days as an antipyretic and up to 5 days as an analgesic. If you need to continue taking the drug, you need to have a doctor's consultation.

In case of severe impairment of renal function, the time interval between doses should be at least 8 hours with creatinine clearance less than 10 ml / min, at least 6 hours - with creatinine clearance of 10-50 ml / min.

In case of violations of the liver function and in patients with chronic alcoholism, malnutrition (low stock of liver glutathione) or dehydration, the daily dose should not exceed 3 g.

Side effects:

Possible diarrhea, abdominal pain, nausea, vomiting, tenesmus, a decrease or increase in the prothrombin index and of international normalized relations (INR), decline arterial pressure (as a symptom of anaphylaxis), thrombocytopenia, leukopenia, neutropenia, allergic reactions of the skin and subcutaneous tissue (skin rash, pruritus, urticaria, angioneurotic edema, anaphylactic shock, acute generalized exanthematous pustulosis, Stevens-Johnson syndrome, toxic epidermal necrolysis).

With prolonged use in large doses, hepatotoxic and nephrotoxic effects are possible.

When there are adverse reactions stop taking the drug and contact the doctor.

Overdose:

When possible overdose toxicity, especially in children, patients with liver disease (caused by chronic alcoholism) patients with eating disorders, as well as in patients receiving inductors liver microsomal enzymes, in which can develop fulminant hepatitis, hepatic insufficiency, cholestatic hepatitis, cytolytic hepatitis, in the above cases - 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, abdominal discomfort and / or abdominal pain), pale skin. With the simultaneous administration of 7.5 g or more to adults or children over 140 mg / kg, cytolysis of hepatocytes occurs with complete and irreversible necrosis of the liver, the development of hepatic insufficiency, metabolic acidosis and encephalopathy, which can lead to coma and fatal outcome. After 12-48 hours after the injection of paracetamol, an increase in the activity of "liver" transaminases, lactate dehydrogenase, bilirubin concentration and a decrease in the prothrombin content is noted.

Clinical symptoms of liver damage are manifested 1-2 days after drug overdose and reach a maximum of 3-4 days.

Treatment:

- Immediate hospitalization;

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

- Introduction donators SH-groups and precursors of the synthesis of glutathione-methionine and acetylcysteine within 10 hours after an overdose.The need for additional therapeutic measures (further introduction of methionine, intravenous injection of acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration;

- Symptomatic treatment;

- Hepatic tests should be performed at the beginning of treatment and then every 24 hours. In most cases, liver transaminases activity 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 developing hepatotoxicity.

Patients receiving phenytoin, frequent use should be avoided paracetamol, especially in high doses.

Probenecid almost halves clearance of paracetamol, inhibiting the process its conjugation with glucuronic acid.

With simultaneous appointment should consider lowering the dose paracetamol.

Care should be taken when simultaneous application of paracetamol and inducers of microsomal enzymes liver (for example, ethanol, barbiturates, isoniazid, rifampicin, carbamazepine, anticoagulants, zidovudine, amoxicillin+ clavulanic acid, phenylbutazone, tricyclic antidepressants).

Prolonged use of barbiturates reduces the effectiveness of paracetamol.

Salicylamide increases the half-life of paracetamol.

Monitoring of the INR in time and after the end of the simultaneous application of paracetamol (especially in high doses and / or for long time) and coumarins (for example, warfarin), since paracetamol when taken in a dose of 4 grams in for at least 4 days may strengthen the effect of indirect anticoagulants.

Special instructions:

The preparation contains paracetamol, so to avoid exceeding the maximum daily dose should not be used the drug at the same time as others medicines (prescription and over-the-counter) containing paracetamol.

When using the drug for more than 5-7 days need to monitor the picture peripheral blood and functional the state of the liver.

Paracetamol can cause serious skin reactions, such as acute generalized exanthematous pustulosis, Stevens-Johnson syndrome, toxic epidermal necrolysis, which can be fatal.At the first manifestation of a rash or other hypersensitivity reactions, the drug should be discontinued.

In case of taking the drug by patients with diabetes mellitus ora diet with a low sugar content, it should be borne in mind that in 1 ml of the drug contains 0.335 g of sugar (0.67 g of sugar per each calibration division by a dimensional spoons (indicated by labels in kg).

Paracetamol distorts results laboratory content research Glucose and uric acid in plasma blood.

In the absence of a therapeutic effect: continued fever for more than 3 days and pain syndrome for more than 5 days follows contact your doctor.

Form release / dosage:

Syrup [for children] 30 mg / ml.

Packaging:

For 90 ml in a plastic bottle (polyethylene terephthalate), capped with a cap "push and open" from low-density polyethylene. 1 bottle with a measuring spoon and instructions for use in a cardboard pack.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children!

Shelf life:

3 years.

Do not use the product after the expiry date indicated on the package.

Terms of leave from pharmacies:Without recipe

Registration number:П N011549 / 05

Date of registration:14.05.2009

The owner of the registration certificate:BRISTOL-MIYERS SQUIPB BRISTOL-MIYERS SQUIPB USA

Manufacturer: & nbsp

BRISTOL-MYERS SQUIBB France

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

Information update date: & nbsp07.10.2015

Illustrated instructions

Instructions

Efferalgan® (Efferalgan®)