Paracetamol Extra - instructions for use, dose, side effects, contraindications

active substances - Paracetamol - 0.5 g; Ascorbic acid 0.15 gExcipients: citric acid, Dextrin, flavor (orange or cherry, or caramel), sucrose (sugar), aspartame, dye ("sunset yellow sun" or "azorubin", 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 at a temperature of 40-45 ° C is a slightly cloudy solution of orange or crimson or yellow color with a characteristic slight odor (orange, cherry, caramel).

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 adversely affect the water-salt metabolism (sodium and water retention) and the mucous membrane of the gastrointestinal tract (HCS), 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, since the administration of drugs in solid dosage forms is difficult.The possibility of methaemoglobin formation is unlikely.

Ascorbic acidbut (vitamin C) is not formed in human body, comes tOnly with food.

Physiological functions: is a cofactor of some hydroxylation and amidation reactions - transfers electrons to enzymes, providing them with a replacement equivalent. Participates in reactions hydroxylation of proline and lysine residues procollagen to form hydroxyproline and hydroxylysine (postranslyatsionnaya collagen modification), the oxidation of the side chains of lysine in proteins to form gidroksitrimetillizina (during synthesis kartinita) oxidation of folic acid to folinic, drug metabolism in liver microsomes and hydroxylation dopamine with the formation of norepinephrine.

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 - participation in the synthesis of collagen, proteoglycants 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; the maximum concentration (Cmax) is 5-20 μg / ml. Connection with plasma proteins - 15%. Penetrates through the blood-brain barrier (BBB). The volume of distribution varies from 0.8 to 1.36 l / kg 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 administered in a dose 10-15 mg / kg. MetabolismThe liver is healed in three main ways: conjugation with glucuronides, conjugation with sulfates, oxidation^-microsomal enzymes of the liver. In the latter case, toxic intermediate metabolites are formed, which are subsequently conjugated to glutathione, and then to cysteine and mercapturic acid. The main isoenzymes of cytochrome P450 for this pathway of metabolism are isozyme 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 hydroxylation of up to 3-hydroxyparacetamol and methoxylation to 3-methoxyparacetamol, which are subsequently conjugated to glucuronides or sulfates.

In adults, glucuronation predominates, in newborns (including premature infants) and small children, sulfation. Conjugated metabolites of paracetamol (glucuronides, sulfates and conjugates with glutathione) possess 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 of predominantly 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 deoxy-ascorbic acid and then into oxaloacetic and ascorbate-2-sulfate.

It is excreted by the kidneys, through the intestines, with sweat, breast milk in unchanged form and in the Type 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 is used 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, bowhether in muscles and joints, algodismenorea.

Contraindications:

Severe diseases of the kidneys, liver, including renal and / or hepatic insufficiency; deficiency of glucose-6-phosphate dehydrogenase; erosive ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation), gastrointestinal bleeding; phenylketonuria; children's age till 6 years; intolerance to fructose, glucose-galactose malabsorption, sugarazo-isomaltous insufficiency; pregnancy (I-III trimesters), lactation period.

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. Alcoholism.

Pregnancy and lactation:

Data on the efficacy and safety studies of the combination of paracetamol and ascorbic acid in pregnant and lactating women are not available. Thus, it is not possible to assess the possible correlation of risk and benefit, and therefore the use of the drug in these categories of patients is not recommended.

Dosing and Administration:Inside. To make a solution, dissolve the contents of the sachet in the required amount of boiled water. Use in a warm form. Children from 6 to 12 years old for 1 packet, not more than 3 bags per day; over 12 years old (weighing more than 50 kg) per 1 sachet, not more than 4 sachets per day. Adults take 1 packet 3-4 times / day with an interval between doses 4-8 hours.

Side effects:

Paracetamol.

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

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

From the organs of hematopoiesis and lymphatic system: Very rarely - anemia, leukopenia.

Other: weakness.

Ascorbic acid.

Allergic reactions: skin rash, skin hyperemia.

LaboRatio indicators: thrombosistheng, hyperprothrombinemia, erythropenia, neutrophilic leukocytosis, hypokalemia, glucosuria.

Overdose:Symptoms (due to paracetamol): at 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 SHand the precursors of the synthesis of glutathione - methionine - within 8-9 hours after. 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 concomitantly taking other medicines with Paracetamol EXTRA, you should consult your doctor.

Paracetamol reduces the effectiveness of uricosuric drugs.

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

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

Metoclopramide and domceridone increase the absorption of paracetamol. Simultaneous use of 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.

The simultaneous use of paracetamol and chloramphenicol can accompanied by an increase in T1 / 2 chloramphyenicol up to 5 times.

Inductors of microslum enzymes liver (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% risk development of 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 of benzylpenicillin and tetracyclines in the blood; 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 that have an alkaline reaction (including alkaloids), 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 Paracetamol EXTRA for hyperthermia that lasts more than 3 days and pain syndrome for more than 5 days requires medical advice.

After 5 days of Paracetamol EXTRA, monitoring of the peripheral blood and the functional state of the liver is necessary. Paracetamol distorts the indicators of laboratory studies for r quantitative determination of the concentration of glucose and uric acid in 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. The drug Paracetamol EXTRA 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. corresponds to 3.9 g of sugar. Do not prescribe to patients with diabetes.

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

There is no data on the effect of Paracetamol EXTRA on the ability to drive vehicles and other technical means.

Form release / dosage:

Powder for solution for oral administration (orange, cherry, caramel) 500 mg + 150 mg.

Packaging:

For 5 grams in bags heat-sealable from a film-combined material or from a combined multi-layered or foil-laminated 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:

AT dry, protected from light at a temperature of not more than 25 FROM.

Keep out of the reach of children.

Shelf life:

2 years.

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

Terms of leave from pharmacies:Without recipe

Registration number:LSR-004844/10

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: & nbsp02.10.2015

Illustrated instructions

Instructions

Paracetamol Extra (Paracetamol Extra)