Efferalgan suppositories rectal 80 mg 12 pcs
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Active ingredients
Paracetamol
Release form
Suppositories
Composition
Paracetamol. Excipients: semi-synthetic glycerides (up to the mass of suppository 1 g);
Pharmacological effect
Efferalgan contains paracetamol, which blocks COX-1 and -2 mainly in the central nervous system, affecting the centers of pain and thermoregulation. In inflammatory tissues, cellular peroxidases neutralize the effect of paracetamol on COX, which explains the almost complete absence of an anti-inflammatory effect. The absence of a blocking effect on the synthesis of PG in peripheral tissues determines the absence of a negative effect on the water-salt metabolism (retention of Na + and water) and the gastrointestinal mucosa;
Pharmacokinetics
Absorption of paracetamol is complete and fast. The peak plasma concentration is reached in 30–60 min after administration. The distribution of paracetamol in the tissues occurs quickly. Achieved comparable concentrations of the drug in blood, saliva and plasma. Plasma protein binding is low, 10–25%. It penetrates the BBB.; Metabolism occurs in the liver, 80% reacts conjugation with glucuronic acid and sulfates with the formation of inactive metabolites; 17% undergoes hydroxylation with the formation of 8 active metabolites, which are conjugated with glutathione with the formation of already inactive metabolites. With a lack of glutathione, these metabolites can block the enzyme systems of the hepatocytes and cause their necrosis. CYP2E1 isoenzyme is also involved in the metabolism of the drug. T1 / 2 - 1-4 h. It is excreted by the kidneys as metabolites, mainly conjugates. Unchanged output is less than 5% .;
Indications
For children aged 3 months to 10 years; - acute respiratory infections, influenza, childhood infections, post-vaccination reactions, other infectious inflammatory diseases and conditions accompanied by fever; - moderately or mild pain, including headache, toothache, muscle pain, neuralgia, pain from injuries and burns;
Contraindications
Severe abnormal liver function; - Severe renal dysfunction; - blood diseases; - deficiency of glucose-6-phosphate dehydrogenase; - recent inflammation or bleeding in the rectum; - children's age up to 3 months; - hypersensitivity to paracetamol.; The drug should be used with caution in case of dysfunction of the liver or kidneys of mild and moderate degree, in case of Gilbert syndrome;
Dosage and administration
The drug is used rectally.After releasing the suppository from the package, insert the child into the anus (preferably after a cleansing enema or spontaneous emptying of the intestines); the average single dose of Efferalgana depends on the body weight of the child and is 10-15 mg / kg 3-4 times / day. The maximum daily dose is 60 mg / kg.; Children aged from 5 years to 10 years (with a body weight of 20 to 30 kg) are administered 1 rectal suppository (300 mg) 3-4 times / day with an interval of 4-6 hours You should not use more than 4 suppositories per day; Children aged from 6 months to 3 years (with a body weight of 10 to 14 kg) are administered 1 rectal suppository (150 mg) 3-4 times / day with an interval of 4-6 h. You should not use more than 4 suppositories per day.; Children aged 3 to 5 months (with a body weight of 6 to 8 kg) are administered 1 rectal suppository (80 mg) 3-4 times / day with an interval of 4-6 h. Should not be used Five more suppositories per day. The duration of treatment is 3 days when used as a febrifuge and up to 5 days as an analgesic;
Side effects
Allergic reactions: seldom - skin rash, itching, hives, angioedema; From the alimentary system: rarely - nausea, vomiting; long-term use in high doses may have a hepatotoxic effect, irritation of the mucous membrane of the rectum, tenesmus. From the hematopoietic system: extremely rare - anemia, thrombocytopenia, leukopenia.; Others: with long-term use in high doses, nephrotoxic action is possible. in the recommended doses.; With the development of adverse reactions, it is necessary to stop using the drug and consult a doctor;
Overdose
Symptoms: nausea, vomiting, stomach pain, sweating, pallor of the skin. After 1-2 days, there are signs of liver damage. In severe cases, liver failure, hepatonecrosis, encephalopathy and a comatose state develops. Treatment: cancel the drug, patients need to consult a doctor;
Interaction with other drugs
With simultaneous use of Efferalgan with barbiturates, anticonvulsants, rifampicin, the risk of a hepatotoxic effect is greatly increased. When used simultaneously with levomycetin (chloramphenicol), the toxicity of the latter increases.; Paracetamol enhances the effects of anticoagulants of indirect effect.; blood should be reported to the doctor about the use of Efferalgan;
special instructions
When using the drug for more than 7 days, it is necessary to control the picture of peripheral blood and the functional state of the liver. Paracetamol distorts the results of laboratory studies of glucose and uric acid in plasma;