Efferalgan (paracetamol) effervescent tablets №10

Description

Efferalgan №10 Composition
active substance: paracetamol;

1 rectal suppository contains 150 mg of paracetamol;

Efferalgan №10 excipients: solid fat.

Efferalgan №10 Dosage form
Rectal suppositories.

Basic physical and chemical properties: white, smooth and glossy suppositories.

Pharmacotherapeutic group
Analgesics and antipyretics. ATX code N02B E01.

Pharmacodynamics
It has analgesic, antipyretic and mild anti-inflammatory effects. The mechanism of action is due to the inhibition of the synthesis of prostaglandins and the predominant effect on the center of thermoregulation in the hypothalamus.

Pharmacokinetics
Absorption of paracetamol with rectal administration is slower than with oral administration, but it is more complete. The maximum concentration in blood plasma is reached within 2-3 hours after administration.

Paracetamol is rapidly distributed in all tissues. Concentrations in blood, saliva and plasma are comparable to each other. Plasma protein binding is weak.

Paracetamol is metabolized in the liver to form inactive compounds with glucuronic acid and sulfates.

The minimal metabolic pathway catalyzed by cytochrome P450 leads to the formation of an intermediate reagent (N-acetylbenzoquinone imine), which, under normal use, is rapidly detoxified by reduced glutathione and excreted in the urine after conjugation with cysteine ​​and mercaptopuric acid. However, with massive poisoning, the amount of this toxic metabolite increases.

It is excreted mainly in the urine. 90% of the taken dose of paracetamol is excreted by the kidneys within 24 hours, mainly in the form of conjugates with glucuronic acid (60 to 80%) and sulfate conjugates (20 to 30%).

Less than 5% of the substance is excreted unchanged.

The half-life is 4 to 5 hours.

In severe renal failure (creatinine clearance below 10 ml / min), the excretion of paracetamol and its metabolites slows down.

Indications
Symptomatic treatment of diseases accompanied by mild to moderate pain and / or fever.

Contraindications
Hypersensitivity to paracetamol or other components of the drug.

Age up to 1 month (child’s body weight up to 4 kg).

Severe renal and / or liver dysfunction, hepatocellular insufficiency, congenital hyperbilirubinemia, glucose-6-phosphate dehydrogenase deficiency, alcoholism, blood diseases, severe anemia, leukopenia.

Inflammation of the rectal mucosa and dysfunction of the anus, rectal bleeding.

Do not use for diarrhea.

Interaction with other medicinal products and other forms of interaction
When taking the maximum doses of paracetamol (4 g / day) for at least 4 days, there is a risk of an increase in the effect of an oral anticoagulant and an increased risk of bleeding. The INR (International Normalized Ratio) should be monitored at regular intervals. If necessary, the dose of anticoagulant administration should be adjusted during treatment with paracetamol.

The absorption rate of paracetamol can be increased by metoclopramide and domperidone and decreased by cholestyramine. Barbiturates reduce the antipyretic effect of paracetamol. Anticonvulsants (including phenytoin, barbiturates, carbamazepine), which stimulate the activity of liver microsomal enzymes, can increase the toxic effect of paracetamol on the liver due to an increase in the conversion of the drug to hepatotoxic metabolites. With the simultaneous use of paracetamol with hepatotoxic agents, the hepatotoxic effect of the drug on the liver increases. The simultaneous use of high doses of paracetamol with isoniazid, rifampicin increases the risk of developing hepatotoxic syndrome. Paracetamol reduces the effectiveness of diuretics. Do not use simultaneously with alcohol.

High concentrations of paracetamol can affect laboratory results for the determination of blood glucose by the oxidase-peroxidase method, uric acid when using the phosphotungstic acid method.

Application features
For children weighing less than 37 kg, the maximum daily dose of paracetamol should not exceed 80 mg / kg / day.

For children weighing from 38 kg to 50 kg, the maximum daily dose of paracetamol should not exceed 3 g / day.

For children weighing more than 50 kg, the maximum daily dose of paracetamol should not exceed 4 g / day.

When using suppositories, there is a risk of local toxicity, the frequency and intensity of toxicity increases with prolonged use, in the case of short intervals between doses and in the case of an increase in dose.