Composition, form of production and packaging
? Suppositories rectal for children from white to white with a creamy or white with a yellowish hue of color, torpedo-shaped.
1 supp.
paracetamol 100 mg
Excipients: solid fat base to obtain a suppository with a mass of 1.25 g.
5 pieces. - packings cellular planimetric (2) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
PHARMACHOLOGIC EFFECT
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. The absence of a blocking effect on the synthesis of Pg in peripheral tissues causes the absence of a negative effect on the water-salt metabolism (Na + and water retention) and the mucous membrane of the gastrointestinal tract.
PHARMACOKINETICS
Absorption - high, TC max - 0.5-2 h; C max is 5-20 μg / 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. 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 the 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.
T 1/2 - 1-4 hours. 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:
- antipyretic agents for acute respiratory infections, influenza, childhood infections, post-reaction reactions and other conditions accompanied by fever;
- painkiller with pain syndrome of mild and moderate intensity, including: headache and toothache, muscle pain, neuralgia, pain with injuries and burns.
DOSING MODE
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 to 12 months - 0.5-1 suppositories (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 less than 3 months of age is only used as directed by the doctor.
SIDE EFFECT
Allergic reactions (including skin rash, itching, angioedema).
Rarely - violations of hematopoiesis (anemia, thrombocytopenia, methemoglobinemia).
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).
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution: kidney failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution: hepatic insufficiency, benign hyperbilirubinemia (including Gilbert's syndrome), viral hepatitis.
APPLICATION FOR CHILDREN
Contraindicated in the period of newborns (up to 1 month).
With caution: early infancy (up to 3 months).
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.
OVERDOSE
Symptoms: during the first 24 hours after ingestion, 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 overdose) - increased 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: the introduction of donors of SH-groups and precursors of glutathione-methionine synthesis for 8-9 hours after overdose and N-acetylcysteine ​​- up to 12 hours. The need for additional therapeutic measures (continued methionine administration, intravenous administration of N-acetylcysteine) is determined in dependence from the concentration of paracetamol in the blood, as well as from the time elapsed after its administration.
DRUG INTERACTION
Stimulants of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, flumecinol, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites, which makes it possible to develop a hepatotoxic effect with small overdoses. Inhibitors of microsomal oxidation (including 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.
TERMS OF RELEASE FROM PHARMACY
The drug is approved for use as a means of OTC.
TERMS AND CONDITIONS OF STORAGE
In a dry, dark place at a temperature of no higher than 15 В° C.
Shelf life. 2 years. Do not use after the expiry date printed on the package.
