Efferalgan oral solution 30mg / ml, 90ml

For children aged 1 month to 12 years (weighing from 4 to 32 kg):

- as an antipyretic agent for acute respiratory infections, influenza, childhood infections, post-vaccination reactions and other conditions accompanied by an increase in body temperature;

- as an anesthetic for pain syndrome of mild or moderate intensity, incl. headache and toothache, muscle pain, neuralgia, pain in trauma and burns.

The average single dose of the drug depends on the child's body weight and is 10-15 mg / kg of body weight. The maximum daily dose should not exceed 60 mg / kg body weight. The minimum interval between doses of the drug should be 4 hours. Regular time intervals between taking the drug should be adhered to. For convenience and accuracy of dosing, a measuring spoon should be used.

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

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

Children weighing from 4 to 16 kg Fill the measuring spoon to the mark corresponding to the child's body weight, or to the mark closest to the child's body weight. For example, if the child's body weight is between 4 and 5 kg, fill the measuring spoon up to the 4 kg mark.

If necessary, the drug should be taken every 4-6 hours. Children weighing from 16 to 32 kg Fill the measuring spoon to the mark corresponding to 10 kg, then refill the measuring spoon to the mark so that the total body weight of the child is obtained. For example, if your child weighs between 18 and 19 kg, fill the measuring spoon to the 10 kg mark, then refill the measuring spoon to the 8 kg mark.

If necessary, the drug should be taken every 4-6 hours. The drug can be given to the child either without dilution or after dilution (with water, milk or juice). The duration of treatment is 3 days as an antipyretic and up to 5 days as a pain reliever. If it is necessary to continue taking the drug, a doctor's consultation is required. For children aged 1 to 3 months, the drug can only be given as directed by a doctor. In severe renal dysfunction, the time interval between doses of the drug should be at least 8 hours with CC less than 10 ml / min, at least 6 hours - with CC 10-50 ml / min. In patients with chronic or compensated active liver diseases, especially accompanied by liver failure, in patients with chronic alcoholism,chronic malnutrition (insufficient supply of glutathione in the liver), Gilbert's syndrome, dehydration or body weight less than 50 kg, the dose of the drug should be reduced or the interval between doses should be increased. The daily dose should not exceed 2 g.

Oral solution (for children) brown, slightly viscous, with a caramel-vanilla smell.

100 ml

paracetamol 3 g

macrogol-6000 - 20 g,

sugar syrup (sucrose, water) - 50 g,

sodium saccharinate - 0.15 g,

potassium sorbate - 0.4 g,

caramel-vanilla flavor * - 0.2 g,

citric acid - 0.107 g,

purified water - up to 100 ml.

• 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 sucrase / isomaltase, fructose intolerance, glucose-galactose malabsorption.

• With care: severe renal failure (CC <30 ml / min), liver failure, chronic alcoholism, anorexia, bulimia, cachexia, hypovolemia, dehydration, glucose-6-phosphate dehydrogenase deficiency.

pharmachologic effect

Paracetamol has analgesic, antipyretic and mild anti-inflammatory effects. The exact mechanism of the analgesic and antipyretic effects of paracetamol has not been established. Apparently, it includes central and peripheral components. Paracetamol blocks cyclooxygenase (COX) -1 and COX-2 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 the anti-inflammatory effect. The absence of a blocking effect on the synthesis of prostaglandins in peripheral tissues determines the absence of a negative effect on water-salt metabolism (sodium and water retention) and the gastrointestinal mucosa.

Pharmacokinetics

Absorption and distribution

Absorption of paracetamol after oral administration is complete and fast. Cmax in plasma is reached within 30-60 minutes after administration. The distribution of paracetamol in tissues is rapid. The volume of distribution (Vd) in children is 0.7-1.01 l / kg. Comparable concentrations of the drug in blood, saliva and plasma are achieved. Plasma protein binding is low (10-25%). Penetrates the BBB.

Metabolism

Paracetamol is metabolized mainly in the liver to form glucuronides and sulfates. A small part (4%) of paracetamol is metabolized by cytochrome P450 to form an active intermediate metabolite (N-acetylbenzoquinone imine), which under normal conditions is quickly rendered harmless by reduced glutathione and excreted in the urine after binding with cysteine ??and mercapturic acid. However, with massive intoxication, the amount of this toxic metabolite increases.

Withdrawal

T1 / 2 in adults is 2.7 hours, in children - 1.5-2 hours, in newborns - 3.5 hours, total clearance - 18 l / h. Paracetamol is excreted mainly in the urine; 90% of the dose taken 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.

Pharmacokinetics in special patient groups

In severe renal failure (creatinine clearance (CC) below 10-30 ml / min), the excretion of paracetamol slows down somewhat. The rate of excretion of glucuronide and sulfate in patients with severe renal failure is lower than in healthy patients.

In children under 10 years of age, paracetamol is excreted to a greater extent in the form of sulfate, and not glucuronide, which is typical for adult patients. At the same time, the total excretion of paracetamol and its metabolites in patients of all age groups is the same.

Side effect

From the digestive system: possible - diarrhea, abdominal pain, nausea, vomiting, tenesmus; with prolonged use in high doses, a hepatotoxic effect is possible.

From the hematopoietic system: possible - thrombocytopenia, leukopenia, neutropenia.

Skin and subcutaneous tissue disorders: possible - skin rash, itching, acute generalized exanthematous pustulosis, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Allergic reactions: possible - urticaria, Quincke's edema, anaphylactic shock, lowering blood pressure (as a symptom of anaphylaxis).

Others: decrease or increase in prothrombin index and international normalized ratio (INR); with prolonged use in high doses, a nephrotoxic effect is possible.

If any adverse reactions occur, the patient should stop taking the drug and consult a doctor.

Application during pregnancy and lactation

The drug should be used during pregnancy only if the expected benefit to the mother outweighs the possible risk to the fetus, strictly adhering to the dosage regimen and timing of treatment.

Clinical experience with the use of paracetamol during pregnancy and during breastfeeding is limited. However, according to epidemiological data on the use of paracetamol in therapeutic doses, no undesirable effect on the course of pregnancy or the health of the fetus and newborn has been identified.

Reproductive toxicity studies in animals have not revealed teratogenic, embryotoxic, or fetotoxic potential.

After oral administration, paracetamol passes into breast milk in small amounts. In some cases, children whose mothers used paracetamol during breastfeeding have experienced a rash. Paracetamol is allowed to be used during breastfeeding in therapeutic doses.

Application for violations of liver function

The drug should be used with caution in case of mild and moderate hepatic dysfunction.

Application for impaired renal function

The drug should be used with caution in case of mild and moderate renal dysfunction.

Application in children

It can be used in children over the age of 1 month according to indications and in doses that take into account the age or body weight of the patient.

special instructions

The drug contains paracetamol, therefore, in order to avoid exceeding the maximum daily dose, the drug should not be used simultaneously with other drugs (prescription and over-the-counter) containing paracetamol.

When using the drug for more than 5-7 days, it is necessary to control the picture of peripheral blood and the functional 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 use of the drug should be discontinued.

For children from 1 to 3 months, the drug can only be given as directed by a doctor.

Patients with diabetes mellitus or on a diet with a low sugar content should take into account that 1 ml of the drug contains 0.335 g of sugar (0.67 g of sugar for each graduation division of a measuring spoon (indicated by marks in kg).

Paracetamol distorts the results of laboratory tests of the content of glucose and uric acid in the blood plasma.

In the absence of a therapeutic effect (continued fever for more than 3 days and pain syndrome for more than 5 days), you should consult your doctor.

Influence on the ability to drive vehicles and mechanisms

The effect on the ability to drive vehicles and work with mechanisms has not been studied. If the patient experiences dizziness, psychomotor agitation and disorientation in space and time, it is not recommended for him to drive a car and other mechanisms during treatment with the drug.

Overdose

In case of an overdose, intoxication is possible, especially in children, patients with liver diseases (caused by chronic alcoholism), in patients with nutritional disorders, as well as in patients taking inducers of microsomal liver enzymes, in which fulminant hepatitis, liver failure, cholestatic hepatitis, cytolytic hepatitis, in the above cases - sometimes fatal. The clinical picture of an acute overdose develops within 24 hours after taking paracetamol.

Symptoms: gastrointestinal upset (nausea, vomiting, loss of appetite, abdominal discomfort and / or abdominal pain), pallor of the skin. When administered simultaneously to adults 7.5 g and more or children more than 140 mg / kg, cytolysis of hepatocytes occurs with complete and irreversible liver necrosis, the development of liver failure, metabolic acidosis and encephalopathy, which can lead to coma and death. 12-48 hours after the introduction of paracetamol, there is an increase in the activity of hepatic transaminases, LDH, bilirubin concentration and a decrease in prothrombin content. Clinical symptoms of liver damage appear 1-2 days after drug overdose and reach a maximum on 3-4 days.

Treatment: immediate hospitalization; determination of the quantitative content of paracetamol in blood plasma before starting treatment as early as possible after an overdose; the introduction of donors of 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 administration of methionine, intravenous administration 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; liver tests should be performed at the beginning of treatment and then every 24 hours. In most cases, hepatic transaminase activity will return to normal within 1Ц2 weeks. In very severe cases, a liver transplant may be required.

Drug interactions

Phenytoin reduces the effectiveness of paracetamol and increases the risk of developing hepatotoxicity. Patients taking phenytoin should avoid frequent use of paracetamol, especially at high doses.

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

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

Long-term use of barbiturates reduces the effectiveness of paracetamol.

Salicylamide increases the T1 / 2 of paracetamol.

INR should be monitored during and after the end of the simultaneous use of paracetamol (especially in high doses and / or for a long time) and coumarins (for example, warfarin), because paracetamol, when taken in a dose of 4 g for at least 4 days, can enhance the effect of indirect anticoagulants.

Caution should be exercised with the simultaneous use of paracetamol and flucloxacillin, which is associated with an increased risk of metabolic acidosis with a high anionic difference, especially in patients with a risk factor for the development of glutathione deficiency (including patients with severe renal failure, sepsis, malnutrition and chronic alcoholism). Careful monitoring is recommended in order to detect signs of acid-base imbalance, namely metabolic acidosis with a high anion difference, including the determination of 5-oxoproline in urine.