Paracetamol EXTRA children - instructions for use, dose, side effects, contraindications

active substances: Paracetamol - 120 mg; Ascorbic acid-10 mg Excipients: citric acid, dextrin, flavoring (orange or cherry, or caramel), sucrose (sugar), aspartame, dye ("sunset sunset" or "azorubine" ("carmoazine"), or "quinoline yellow").

Description:

Granular powder of orange or crimson, or yellow color with a characteristic faint smell (orange, cherry, caramel).

An aqueous solution of the contents of one sachet in 100 ml of water with a temperature of 40-45 ° C is a slightly cloudy solution of orange or crimson or yellow pveta with the characteristicethirdsa smell (orange, cherry, carrota piece of chalkand).

Pharmacotherapeutic group:Analgesic combined (analgesic non-narcotic remedy + vitamin)

ATX: & nbsp

N.02.B.E Anilides

N.02.B.E.51 Paracetamol in combination with other drugs, excluding psycholeptics

Pharmacodynamics:Paracetamol has an analgesic and antipyretic effect. The drug blocks cyclooxygenase 1 and 2 mainly in the central nervous system (CNS), 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 render negative impact on water-salt metabolism (sodium and water retention) and the mucous membrane of the gastrointestinal tract (GIT), due to the lack of influence on the synthesis of prostaglandins in peripheral tissues. The preparation in the form of a warm drink is convenient for use in patients with inflammatory diseases of the oropharynx, as taking drugs in solid dosage forms is difficult.The possibility of methaemoglobin formation is unlikely.

Ascorbic acid (vitamin C) is not formed in the human body, it comes only with food.

Physiological functions: is an cofactor of some reactions gidrixylandthe transfer of electrons to enzymes, providing them with a reducing equivalentm. Participates in the reactions of hydroxyProlene and lysine residues of procollagen with formation of hydroxyproline and hydroxylizine (post-translational modification of collagen), oxidation of side chains of lysine in proteins with the formation of hydroxy(during the synthesis of kartonite), the oxidation of folic acid to folinic, the metabolism of drugs in liver microsomes, and the hydroxylation of dopamine with the formation of noradrenaline.

Increases activity amidating enzymes involved in the processing of oxytocin, antidiuretic hormone and holitsistokinina. Participates in steroidogenesis in the adrenal glands.

The main role at the tissue level is participation in the synthesis of collagen, proteoglycans and other organic components of the intercellular substance of the teeth, bones and endothelium of the capillaries.

Pharmacokinetics:

Paracetamol. Absorption is high. The time required to reach the maximum concentration (TC_mOh) - 0.5-2 hours; maximum concentration (Сmah) - 5-20 mcg / ml. Connection with plasma proteins - 15%. Penetrates through blood-brainephalicth barrier (BBB). ABOUTFailing distribution varietiesirrayt from 0,8_ to 1,36 l / kg of body weight. Less than 1% of the dose of paracetamol taken by the lactating mother penetrates into breast milk. The therapeutically effective concentration of paracetamol in plasma is achieved when it is administered at a dose of 10-15 mg / kg. Metabolised in the liver in three main ways: conjugation with glucuronides, conjugation with sulfates, oxidation with microsomal enzymes of the liver. In the latter case, Toxic intermediates are formed, which are subsequently conjugated to glutathione, followed by cysteine and mercapturic acid. The main isoenzymes of cytochrome P450 for this pathway of metabolism are isoenzyme T CYP2E1 (predominantly), CYP1A2 and CYP3A4 (a secondary role). With a deficiency of glutathione, these metabolites can cause damage and necrosis of hepatocytes.

Additional ways of metabolism are the hydroxylation of up to 3-hydroxyparathyetamol and methoxylation up to 3-methoxyparacetamol, which are subsequently conjugated to glucuronides or sulfates.

In adults glucuronation predominates, y. Newborns (including prematurity) and small children - sulfation. Conjugated metabolites of paracetamol (glucuronides, sulfates and conjugates with glutathione) have low pharmacological (including toxic) activity.

The half-life (T1 / 2) is 1-4 hours. It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% in unchanged form. In elderly patients the clearance of the drug decreases and T1 / 2 increases.

Ascorbic acid Connection with plasma proteins - 25%.

The concentration of ascorbic acid in the plasma is normally around 10-20 μg / ml. Easily penetrates into leukocytes, platelets, and then into all tissues; the greatest concentration is achieved in glandular organs, leukocytes, liver and lens of the eye; penetrates the placenta. The concentration of ascorbic acid in leukocytes and platelets is higher than in erythrocytes and in plasma. With deficient states, the concentration in leukocytes decreases later and more slowly and is considered as the best criterion for assessing the deficit than the concentration in the plasma.Metabolised mainly in the liver in desoxyascorbic and then in oxaloacetic and ascorbate-2-sulfate.

It is excreted by the kidneys, through the intestines, with sweat, breast milk in unchanged form and in the form of metabolites.

At the appointment of high doses, the rate of excretion increases sharply. Smoking and the use of ethanol accelerate the destruction of ascorbic acid (conversion into inactive metabolites), sharply reducing the reserves in the body. It is in hemodialysis.

Indications:

Paracetamol EXTRA childrenskI nRemenyayut as:

- antipyretic agents for infectious and inflammatory diseases (ARVI, including influenza);

- anesthetic for mild to moderate pain syndrome (headache, toothache) of non-inflammatory origin, with neuralgia, pain in muscles and joints.

Contraindications:

Severe diseases of the kidneys, liver, including renal and / or hepatic insufficiency; deficiency of glucose-6-phosphotehydrogenase; erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation), gastrointestinal bleeding; phenylketonuria; children under 2 years; intolerance to fructose, glucose-galactose malabsorption, sugarazo-isomaltous insufficiency.

Carefully:

Erosive-ulcerative lesions of the gastrointestinal tract (in the anamnesis), congenital hyperbilirubinemia (syndromes Gilbert, Dubin-Johnson, and Rotor).

Diseases of the blood (thrombocytopenia, leukopenia, agranulocytosis), sideroblastic anemia, thalassemia.

Deficiency of glucose-6-phosphate dehydrogenase, hemochromatosis, hyperoxaluria, urolithiasis.

Bronchial asthma. Diabetes.

Dosing and Administration:

Inside. To prepare the solution, the contents of the sachet are dissolved in a small amount of boiled water. Use in a warm form. Children aged 2-3 years are assigned the contents of 1 packet, diluted in 50 ml of liquid, 4-6 years - 2 bags in 100 ml, 7-10 years - 2-3 packets in 100-150 ml, 10-12 years - 3-4 packets in 150 ml. Multiplicity of reception 4 once a day at intervals of not less than 4 hours.

Duration of admission is not more than 5 days with the appointment as an anesthetic and 3 days - as an antipyretic agent.

Further treatment with the drug is possible only after consulting a doctor.

Do not exceed the indicated dose.

In case of an overdose, seek medical help immediately, because there is a risk of delayed signs of serious liver damage.

Side effects:

Paracetamol.

From the digestive sideaboutth system: rarely - tnausea, very rarely - vomiting, diarrhea, epigastric pain, jaundice, pancreatitis and increased activity of "liver" enzymes.

Allergic reactions: rarely - skin rash, skin itching, hives, angioedema, edema).

On the part of the organs of hematopoiesis and lymphatic system: very rarely - anemia, leukopenia.

Other: weakness.

Ascorbic acid.

Allergic reactions: skin rash, skin hyperemia.

Laboratory indicators: thrombocytosis, hyperprotrombinemia, erythropenia, neutrophilic leukocytosis, hypokalemia, glucosuria.

Overdose:Symptoms (due to paracetamol): during the first 24 hours after administration - pallor of the skin, nausea, vomiting; anorexia, abdominal pain; disturbance of glucose metabolism, metabolic acidosis. Symptoms of liver dysfunction may appear 12-48 hours after an overdose. In severe overdose - liver failure with progressive encephalopathy, coma, death; acute renal failure with turbulent necrosis (including in the absence of severe liver damage); arrhythmia, pancreatitis.Hepatotoxic effect in adults is manifested when taking 10 g or more. Rarely, liver failure develops at a lightning speed and can be complicated by renal insufficiency (tubular necrosis).

Treatment: introduction of donators SH-groups and precursors of the synthesis of glutathione-methionine-for 8-9 hours after an overdose and acetylcysteine-for 8 hours.

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 admission.

Symptoms (due to ascorbic acid): diarrhea, nausea,

irritation of the mucous membrane of the gastrointestinal tract, flatulence, abdominal pain of a spastic nature, frequent urination, nephrolithiasis, insomnia, irritability, hypoglycemia.

Treatment: symptomatic, forced diuresis.

Interaction:

When taking other medicines at the same time with Paracetamol EXTRA, a child should consult with a doctor.

Paracetamol reduces the effectiveness of uricosuric drugs.

For prolonged and regular use paracetamol potentiates the effects of warfarin and other coumarin derivatives and increases the risk of bleeding.

Simultaneous reception of colestyramine leads to a decrease in paracetamol absorption (and weakening of paracetamol effects).

Metoclopramide and domperidone increase the absorption of paracetamol. Simultaneous application. paracetamol. and non-steroidal anti-inflammatory drugs (metamizol sodium, acetylsalicylic acid, ibuprofen etc.) increases the risk of developing "analgesic" nephropathy and renal papillary necrosis, the terminal stage of renal failure.

Simultaneous use of paracetamol and chloramphenicol may be accompanied by an increase in T1 / 2 chloramphenicol up to 5 times.

Inductors of microsomal liver enzymes (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites, which causes the possibility of severe intoxication even with small overdoses.

Salicylamide increases T1 / 2 paracetamol, which leads to the accumulation of paracetamol and, accordingly, increased formation of its toxic metabolites.

Simultaneous use of paracetamol and ethanol can enhance hepatotoxicity of paracetamol, as well as promote the development of acute pancreatitis.

Diflunisal increases the plasma concentration of paracetamol by 50% - the risk of developing hepatotoxicity.

Do not use other medicines containing paracetamol, as well as other non-narcotic analgesics. Simultaneous use of other medicines should be agreed with the doctor.

Ascorbic acid increases the concentration in the blood of benzylpenicillin and tetracycline; in a dose of 1 g / day increases the bioavailability of ethinyl estradiol (also included in oral contraceptives); improves intestinal absorption of drugs Fe (converts trivalent iron into bivalent iron); can increase excretion of iron with simultaneous application with deferoxamine; reduces the effectiveness of heparin and indirect anticoagulants.

Acetylsalicylic acid, oral contraceptives, fresh juices and alkaline drink reduce the absorption and absorption of ascorbic acid.

With simultaneous use with acetylsalicylic acid, urinary excretion of ascorbic acid increases and the excretion of acetylsalicylic acid decreases.

Acetylsalicylic acid reduces the absorption of ascorbic acid by about 30%.

Ascorbic acid increases the risk of developing crystalluria in the treatment of salicylates and sulfonamides short-acting, slows the excretion of kidney acids, increases the excretion of drugs, having niChristmas tree reaction (including alcaloids), reduces the concentration of oral contraceptives in the blood.

Drugs of quinoline series, CaCl₂, salicylates, GCS with long-term use deplete the stores of ascorbic acid.

With simultaneous application ascorbic acid reduces the chronotropic effect of isoprenaline.

With prolonged use or use in high doses ascorbic acid can interfere with the interaction of disulfiram and ethanol; in high doses increases the excretion of mexiletine by the kidneys.

Barbiturates and primidon increase the excretion of ascorbic acid in the urine. Ascorbic acid reduces the therapeutic effect of antipsychotic drugs (neuroleptics) - phenothiazine derivatives, tubular reabsorption of amphetamine and tricyclic antidepressants.

Special instructions:

Do not exceed the recommended dose of the drug.

With hyperthermia, which lasts more than 3 days, and the painful syndrome over, 5 days require a doctor's consultation.

After 5 days of using Paracetamol EXTRA, children need control of the picture of peripheral blood and the functional state of the liver.

Paracetamol distorts the results of laboratory studies in quantifying the concentration of glucose and uric acid in the plasma. To avoid toxic damage to the liver paracetamol should not be combined with the reception of drinks containing alcohol, and also to persons who are prone to alcohol abuse.

There is evidence that frequent use of drugs containing paracetamol, leads to a weighting of the symptoms of bronchial asthma. Paracetamol EKSTRA children's preparation contains sucrose, so the drug is not recommended for patients with congenital fructose intolerance, glucose-galactose malabsorption syndrome or isomaltase deficiency.

The drug contains sugar. The contents of 1 packet Paracetamol EXTRA baby corresponds to 1.0 g of sugar. Do not prescribe to patients with diabetes.

Form release / dosage:

Powder for solution for oral administration (orange, cherry, caramel) 120 mg + 10 mg.

Packaging:

For 1.5 grams in bags heat-sealable from a film-combined material or from a combined multilayered or foil-wrapped packaging material.

For 5, 10, 20, 30, 40 or 50 bags with instructions for medical use are placed in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LSR-004801/10

Date of registration:27.05.2010

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Information update date: & nbsp27.09.2015

Illustrated instructions

Instructions

Paracetamol EXTRA for children (Paracetamol EXTRA kids)