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

Excipients: malic acid 0.050 g, xanthan gum 0.600 g, maltitol 80,000 g, sorbitol noncrystallizing 70% -1.330 g, citric acid anhydrous 0.020 g, sodium nipasept (methyl parahydroxybenzoate sodium, ethyl parahydroxybenzoate sodium, sodium propyl parahydroxybenzoate) 0.150 g, strawberry flavoring - 0.100 g, azorubin dye 0.001 g, water up to 100 ml.

Description:ABOUTa pink suspension with a characteristic odor.

Pharmacotherapeutic group:Analgesic non-narcotic remedy

ATX: & nbsp

N.02.B.E Anilides

N.02.B.E.01 Paracetamol

Pharmacodynamics:

The drug has analgesic and antipyretic properties.It blocks cyclooxygenase in the central nervous system, affecting the centers of pain and thermoregulation. The anti-inflammatory effect is practically absent. Has no effect on the state of the mucosa of the gastrointestinal tract and water-electrolyte metabolism, since it has an extremely small effect on the synthesis of prostaglandins in peripheral tissues.

Pharmacokinetics:

Absorption is high, the drug is quickly and almost completely absorbed from the gastrointestinal tract. The connection with plasma proteins is about 10-25%. The peak concentration in plasma is achieved after 0.5-2 hours. The maximum plasma concentration is 5-20 μg / ml. Penetrates through the blood-brain barrier. Less than 1% of the mother's dose of paracetamol penetrates into breast milk. Distribution of the drug in body fluids is relatively even.

Metabolized mainly 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 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 are isozymes CYP2E1 (predominantly), CYP1A2, CYP3A4 (a secondary role). With a deficiency of glutathione, these metabolites can cause damage and necrosis of hepatocytes. Additional metabolic pathways include hydroxylation to 3-hydroxyparacetamol and methoxylation to 3-methoxyparacetamol, which are subsequently conjugated to glucuronides or sulfates.

In newborns and in children 3-10 years, the main metabolite of paracetamol is paracetamol sulfate, in children 12 years and older - conjugated glucuronide. Conjugated metabolites of paracetamol (glucuronides, sulfates and conjugates with glutathione) have low pharmacological (including toxic) activity.

The half-life of the therapeutic dose is 1-4 hours, in adults 2.7 hours, in children 15-2 hours, the total clearance is 18 liters / hour. When taking therapeutic doses, 90-100% of the dose taken is excreted in the urine within 24 hours. The main amount of the drug is released after conjugation in the liver, in the form of glucuronide (60-80%) and sulfate (20-30%). In the unchanged form, not more than 5% of the received dose of the drug is released.

In elderly patients Paracetamol clearance decreases and the elimination half-life increases (T_1/2).

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

Indications:

Applied in children from 3 months to 12 years as:

- antipyretics - to reduce high fever on the background of catarrhal diseases, influenza and childhood infectious diseases (chicken pox, mumps, measles, scarlet fever, etc.);

- anesthetic - with toothache, including when teething or removing teeth, headache, earache with otitis and with sore throat.

For children aged 2-3 months, one-time administration is possible to reduce the temperature after vaccination. If the temperature does not decrease, consult a doctor.

Contraindications:

- Hypersensitivity to paracetamol or any other ingredient in the drug;

- marked violations of the liver or kidneys;

- age younger than 2 months;

- intolerance to fructose.

Carefully:

Apply with caution in case of impaired liver function (incl.Gilbert syndrome), viral hepatitis, with impaired renal function (creatinine clearance less than 30 ml / min), genetic absence of glucose-6-phosphate dehydrogenase enzyme, severe blood diseases (severe anemia, leukopenia, thrombocytopenia), hypovolaemia, dehydration, anorexia, bulimia, chronic alcoholism, diabetes mellitus. In such cases, before taking the drug should consult with a doctor.

The drug should not be taken concurrently with other drugs containing paracetamol.

Pregnancy and lactation:

Paracetamol penetrates the placental barrier. To date, there has been no adverse effect of paracetamol on fetal development in humans. Paracetamol is excreted in breast milk: the content in milk is 0.04-0.23% of the dose taken by the mother. Nevertheless, when paracetamol is needed during pregnancy and lactation (breastfeeding), the expected benefit of therapy for the mother and possible potential risk to the fetus or the child should be carefully weighed. In experimental studies, embryotoxic, teratogenic and mutagenic effects of paracetamol have not been established.

There is no data on the effect on fertility.

Dosing and Administration:

The drug is taken orally. It is recommended to use with a lot of liquid 1-2 hours after eating. Before use, the contents of the vial should be shaken well. Measuring cup or spoon, embedded inside the package, allows you to correctly and rationally dose the drug. The dose of the drug depends on the age and body weight of the child. Children older than 3 months of the drug prescribed 10-15 mg / kg body weight 3-4 times a day, the maximum daily dose is not more than 60 mg / kg body weight. If necessary, you can take the drug every 4-6 hours in a single dose (15 mg / kg), but no more than 4 times for 24 hours.

Body weight (kg)	Age	Single dose, ml	Single dose, mg	Max, the whole day. dose, ml	Max, the whole day. dose, mg
4,5-6	2-3 months	Only by prescription. physician	Only by prescription. physician	Only by prescription. physician	Only by prescription. physician
6-8	3-6 months	4,0	96	16	384
8-10	6-12 months	5,0	120	20	480
10-13	1 -2 years	7,0	168	28	672
13-15	2-3 years	9,0	216	36	864
15-21	3-6 years old	10,0	240	40	960
21-29	6-9 years	14,0	336	56	1344
29-42	9-12 years old	20,0	480	80	1920

Do not exceed the recommended dose.

Duration of admission without consulting a doctor: to reduce the temperature and to reduce pain - no more than 3 days. In the future, as well as in the absence of therapeutic effect, it is necessary to consult a doctor.

Children aged 2 to 3 months a single dose of 10-15 mg / kg. Apply 1-2 times a day, with an interval of at least 4 hours. If the fever persists after taking a second dose of the drug, you should consult a doctor. Paracetamol in children in age 2-3 months for other indications - only according to the doctor's prescription.

In case of renal dysfunction, 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.

Side effects:

Adverse events are grouped according to frequency (according to post-registration observation): very often (≥ 1/10), often (≥ 1/100 to <1/10), infrequently (≥ 1/1000 to <1/100), rarely (≥ 1/10000 to <1/1000), very rarely (<1/10000), the frequency is not set.

On the part of the blood and lymphatic system:

Rarely: anemia, thrombocytopenia, leukopenia

From the respiratory system, organs of the chest and mediastinum:

Very rarely: bronchospasm in patients with hypersensitivity to acetylsalicylic acid and intolerance to other non-steroidal anti-inflammatory drugs.

From the immune system:

Very rarely: anaphylaxis, angioedema.

From the skin and subcutaneous tissues:

Very rarely: skin reactions of hypersensitivity, including skin rash, toxic epidermal necrolysis (Lyell's syndrome), Stevens-Johnson syndrome, acute generalized exanthematous pustulosis, skin itching, urticaria.

From the gastrointestinal tract:

Rarely: diarrhea, abdominal pain, nausea, vomiting.

From the liver and biliary tract:

Very rarely: a violation of the liver.

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

If any adverse reactions occur, stop taking the medication immediately and consult a doctor!

Overdose:

In case of overdose, intoxication is possible, especially in children, patients with liver diseases, in patients with eating disorders, in persons taking inductors of microsomal liver enzymes, with the appearance of fulminant hepatitis, hepatic insufficiencyoste, cholestatic hepatitis, cytolytic hepatitis, sometimes fatal.

Symptoms Acute paracetamol poisoning is nausea, vomiting, stomach pain, anorexia, a violation of glucose metabolism (dizziness, unconsciousness, sweating), pallor of the skin, metabolic acidosis.When 10 mg or more are administered to adults, and children over 125 mg / kg, hepatitis cytolysis occurs with complete and irreversible necrosis of the liver, development of hepatic insufficiency, metabolic acidosis, encephalopathy, which can lead to coma and fatal outcome. After 1-2 days, signs of liver damage are determined (tenderness in the liver, increased activity of liver enzymes, bilirubin concentrations and a decrease in prothrombin content). Clinical symptoms of liver damage peaked at 3-4 days. In severe cases of overdose, hepatic insufficiency develops, progressive encephalopathy, coma, death. Possible development of acute renal failure with tubular necrosis, characteristic signs of which are pain in the lumbar region, hematuria, proteinuria, with severe liver damage may be absent, as well as arrhythmia and pancreatitis. With prolonged use with excess of the recommended dose, hepatotoxic and nephrotoxic effects (renal colic, nonspecific bacteriuria, interstitial nephritis, papillary necrosis) can be observed.

Treatment: discontinue use and consult a doctor immediately.

Recommended gastric lavage and intake of enterosorbents (Activated carbon, polyphepan), symptomatic therapy. Before starting treatment as soon as possible after an overdose it is necessary to determine the quantitative content of paracetamol in the blood plasma. When poisoning with paracetamol, the introduction of 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, acetylcysteine, etc.) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed since its use. Hepatic tests should be performed at the beginning of treatment and then every 24 hours. In most cases, the normalization of liver enzymes occurs within 1-2 weeks. In severe cases, liver transplantation may be required.

If an accidental overdose occurs immediately seek medical help, even if the child feels well.

Treatment of children with severe impairment of liver function 24 hours after taking the drug should be conducted in conjunction with specialists from a toxicology center or a specialized department of hepatology.

Interaction:

When using the drug simultaneously with drugs that are inducers of microsomal liver enzymes (for example, barbiturates, ethanol, anticonvulsants, rifampicin, isoniazid, anticoagulants, zidovudine, amoxicillin + clavulanic acid, phenylbutazone, tricyclic antidepressants), caution should be exercised.

Flumecinol, butadione, preparations of St. John's wort perfume increase the production of hydroxylated active metabolites, causing the possibility of developing severe liver damage in case of an overdose of paracetamol (5 g and above).

With the combined use of paracetamol and chloramphenicol, the time of chloramphenicol elimination is increased by a factor of 5, which increases the risk of chloramphenicol poisoning.

Metoclopramide and domperidone increase, and colestramine reduces the rate of absorption of paracetamol.

Paracetamol reduces the effectiveness of uricosuric medicines.

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

MONOs should be monitored during and after the concurrent use of paracetamol (especially at high doses and / or for a long time) and indirect anticoagulants (eg, warfarin), as paracetamol when taken in a dose of 4 g for at least 4 days can enhance the effect of indirect anticoagulants. Irregular reception of paracetamol does not have a significant effect on the effects of anticoagulants.

Alcohol contributes to the development of acute pancreatitis.

Inhibitors of microsomal oxidation (including cimetidine) reduce the risk of hepatotoxic effects.

Long-term combined use of paracetamol and other non-steroidal anti-inflammatory drugs increases the risk of developing "analgesic" nephropathy and renal papillary necrosis, the onset of the terminal stage of renal failure.

Simultaneous long-term administration of paracetamol in high doses and salicylates increases the risk of developing kidney or bladder cancer.

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

Myelotoxic drugs enhance the manifestation of hematotoxicity of paracetamol.

Phenytoin reduces the effectiveness of paracetamol and increases the risk of hepatotoxicity.

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

Special instructions:

The preparation contains paracetamol, therefore, in order to avoid exceeding the maximum daily dose, the drug should not be used simultaneously with other drugs containing paracetamol.

Patients with glutathione deficiency are overdose, care must be taken.

Liver failure cases have also been reported in patients with low glutathione levels, particularly in severely malnourished patients with anorexia, persons with chronic alcoholism or patients with low body mass index.

The use of paracetamol in patients with low levels of glutathione, for example in sepsis, may increase the risk of metabolic acidosis.

Children from 2 to 3 months of the drug can be given only as prescribed by a doctor.

When analyzing the determination of uric acid and blood sugar, tell your doctor about Paracetamol. Paracetamol distorts the results of laboratory studies of glucose and uric acid.

If there is no therapeutic effect for more than 3 days, consult a doctor.

When taking the drug for more than 5 days, it is recommended to monitor the parameters of peripheral blood and the functional state of the liver.

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

The drug does not affect the ability to drive vehicles and engage in other, potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Suspension for oral administration, 120 mg / 5 ml.

Packaging:

For 100 ml of the suspension in a bottle of glass, orange glass or a vial or a bottle of polyethylene terephthalate for medicines,Sealed with a polymeric screw cap with a first opening control or a "push-turn" lid.

A label is attached to the vial on the basis of a self-adhesive film or a label of label paper.

One bottle, along with the instructions for use, as well as a measuring cup or measuring spoon, or without a measuring cup and a measuring spoon, is placed in a cardboard package (bundle).

Storage conditions:

In the dark place at a temperature of no higher than 25 ° 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:LP-004029

Date of registration:22.12.2016

Expiration Date:22.12.2021

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Representation: & nbspOZONE LLC OZONE LLC Russia

Information update date: & nbsp20.01.2017

Illustrated instructions

Instructions

Paracetamol for children (Paracetamol for kids)