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

Pharmacodynamics:Non-narcotic analgesic, blocks COX1 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.No blocking effect on synthesis Pg in peripheral tissues determines the absence of a negative effect on water-salt metabolism (delay Na + and water) and the mucous membrane of the gastrointestinal tract.

Pharmacokinetics:Absorption - high, TSmah - 0.5-2 hours; Cmax - 5-20 mcg / ml. Connection with plasma proteins - 15%. Penetrates through the BBB. Less than 1% of the dose of paracetamol taken by the lactating mother penetrates into breast milk. Metabolised in the liver in three main ways: conjugation with glucuronides, conjugation with sulfates, oxidation with microsomal enzymes of the liver. AT In the latter case, toxic intermediate metabolites are formed, which subsequently conjugated to glutathione, followed by cysteine and mercapturic acid. The main isoenzymes of cytochrome P450 for this pathway of metabolism are isoenzyme CYP2E1 (predominantly), CYP1A2 and 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 adults, glucuronation predominates, in newborns (including prematurity) and small children, sulfation. Conjugated metabolites of paracetamol (glucuronides, sulfates and conjugates with glutathione) have low pharmacological (including toxic) activity.

T1 / 2 1-4 h. It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% unchanged.

Indications:

Applied in children from 3 months to 12 years as:

- antipyretics for acute respiratory infections, influenza, children's infections, post-vaccination reactions and other conditions, accompanied by an increase in body temperature;

- painkiller with pain syndrome of mild and moderate intensity, including: headache and toothache, muscle pain, neuralgia, pain with injuries and burns.

Contraindications:Hypersensitivity, the period of newborns (up to 1 month.).

Carefully:

Renal and hepatic insufficiency, benign hyperbilirubinemia (including Gilbert's syndrome), viral hepatitis, blood diseases (leukopenia, thrombocytopenia), early infancy (up to 3 months).

Dosing and Administration:

Rectally.

Multiplicity of admission 2-4 times a day; interval - not less than 4 hours.

The dose depends on the age and body weight of the child. The average single dose is 10-12 mg / kg body weight. The maximum daily dose of paracetamol should not exceed 60 mg / kg of body weight.

Depending on age, the following single doses are recommended:

from 6 before 12 months - 0.5-1 suppository (50-100 mg);

from 1 year to 3 years - 1-1.5 suppository (100-150 mg);

from 3 to 5 years - 1,5-2 suppositories by (150-200 mg);

from 5 to 10 years - 2,5-3,5 suppository (250-350 mg);

from 10 to 12 years - 3,5-5 suppositories (350-500 mg).

Do not take the drug for more than 3 days as an antipyretic agent and 5 days as an anesthetic without prescribing a doctor! In children younger than 3 months can be used at an elevated temperature caused by vaccination (vaccination). For all other indications Paracetamol in children under 3 months of age, it is only administered as prescribed by the doctor.

Side effects:

Allergic reactions (including skin rash, itching, angioedema).

Rarely - violations of hematopoiesis (anemia, thrombocytopenia, methemoglobinemia).

Overdose:

Symptoms: During the first 24 hours after ingestion of gastrointestinal disorders, (diarrhea, loss of appetite, nausea, vomiting, cramps, stomach pain).Symptoms of liver dysfunction may appear 12-48 hours after an overdose (the severity of necrosis directly depends on the degree of overdose) - an increase in the activity of "liver" transaminases, an increase in prothrombin time; a detailed clinical picture of liver damage manifests itself after 1-6 days. In severe overdose - liver failure with progressive encephalopathy. Rarely, liver function abnormalities develop with lightning speed and can be complicated by renal failure (tubular necrosis).

Treatment: introduction of donators SH-groups and precursors of glutathione-methionine synthesis within 8-9 hours after an overdose and N-acetylcysteine - up to 12 hours. The need for additional therapeutic measures (further management of methionine, intravenous administration N - acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration.

Interaction:

Stimulants of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, flumecinol, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated activemetabolites, which makes it possible to develop a hepatotoxic effect with small overdoses. Inhibitors of microsomal oxidation (incl. cimetidine) reduce the risk of hepatotoxic effects. When taken together with salicylates, the nephrotoxic effect of paracetamol increases. The combination with chloramphenicol leads to an increase in the toxic properties of the latter. Strengthens the effect of anticoagulants of indirect action and reduces the effectiveness of uricosuric drugs.

Special instructions:

Paracetamol should not be used concomitantly with other paracetamol-containing drugs, as this can cause an overdose of paracetamol. When using the drug for more than 5-7 days, it is necessary to monitor the peripheral blood and the functional state of the liver. Paracetamol distorts the results of laboratory studies of glucose and uric acid in the blood plasma.

Form release / dosage:

Suppositories rectal for children 100 mg.

Packaging:

5 pieces in a planar cell package. Two contour packs together with the instruction for use are placed in a bundle.

Storage conditions:

In a dry, dark place at a temperature of no higher than 15 ° C.

Shelf life:

2 years.

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

Terms of leave from pharmacies:Without recipe

Registration number:LS-001147

Date of registration:28.04.2011

The owner of the registration certificate:ALTAYVITAMINS, CJSC ALTAYVITAMINS, CJSC Russia

Manufacturer: & nbsp

ALTAYVITAMINS, CJSC Russia

Information update date: & nbsp03.10.2015

Illustrated instructions

Instructions

Paracetamol (Paracetamol)