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

Active ingredient: paracetamol 80 mg, 150 mg or 300 mg respectively. Excipients: glycerides semi-synthetic (solid fat) 920 mg, 850 mg or 1000 mg respectively.

Description: Smooth glossy suppositories are white.

Pharmacotherapeutic group:analgesic non-narcotic remedy

ATX: & nbsp

N.02.B.E Anilides

N.02.B.E.01 Paracetamol

Pharmacodynamics:

Efferalgan suppositories contain paracetamol, which blocks cyclooxygenase (COX) 1 and COX2 mainly in the central nervous system, acting on pain centers 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 prostaglandins in peripheral tissues causes the absence of a negative effect on the water-salt metabolism (delay Na + and water) and the mucous membrane of the gastrointestinal tract.

Pharmacokinetics:

Absorption of paracetamol with rectal administration is slower than with oral administration. The peak concentration in plasma is achieved 2-3 hours after the injection. The distribution of paracetamol in tissues is rapid. There are comparable concentrations of the drug in the blood, saliva and plasma. The connection with plasma proteins is low, 10 - 25%. Penetrates through the blood-brain barrier. Metabolism occurs in the liver, 80% enters the conjugation reaction with glucuronic acid and sulfates with the formation of inactive metabolites; 17% undergoes hydroxylation with the formation of 8 active metabolites. With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. In the metabolism of the drug is also involved isoenzyme CYP2E1. T1 / 2 1-4 h. It is excreted by the kidneys in the form metabolites, mainly conjugates. In unchanged formless than 5%. Half-lead period4-5 hours.

Indications:

Efferalgan suppositories are used in children as an antipyretic agent for acute respiratory infections, influenza, childhood infections, post-vaccination reactions and other infectious and inflammatory diseases accompanied by fever.

The drug is also used as an anesthetic for pain syndrome of mild or moderate intensity, including: headache and toothache, muscle pain, neuralgia, pain in injuries and burns.

Suppositories of 80 mg are used in children with a body weight of 6 to 8 kg (aged 3 to 5 months), 150 mg suppositories are used in children with a body weight of 10 to 14 kg (aged 6 months to 3 years) , suppositories of 300 mg are used in children with a body weight of 20 to 30 kg (aged 5 to 10 years).

Contraindications:

Do not use if your child has:

- Hypersensitivity to paracetamol, propacetamol hydrochloride (paracetamol prodrug) or other components of the drug;

- Severe dysfunction of the liver, kidney or decompensated liver disease in the active stage;

- Diseases of the blood;

- Deficiency of the enzyme glucose-6-phosphate dehydrogenase;

- Early infancy (up to 3 months);

- Recent inflammation or bleeding in the rectum (contraindication associated with the route of administration).

Carefully:

The drug should be used with caution in the case of impaired liver function, Gilbert's syndrome, dehydration, hypovolemia, as well as anorexia, bulimia or cachexia (inadequate supply of glutathione in the liver).

Before taking the drug, you should consult your doctor.

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 greater than or equal to 10 ml / min.

Do not use if your child has diarrhea (diarrhea).

Dosing and Administration:

The drug is used rectally. After releasing the candle from the package, insert the child into the anus (preferably after cleansing enema or spontaneous bowel movement). The average single dose of Effergangan depends on the weight of the child and is 15 mg / kg of body weight 4 times a day (every 4-6 hours). The maximum daily dose should not exceed 60 mg / kg of body weight.

Children with a body weight of 6 to 8 kg (age from 3 before 5 months) 1 candle (80 mg) 4 times a day every 4-6 hours.

Children with a body weight of 10 to 14 kg (age from 6 months to 3 years) are administered 1 candle (150 mg) 4 times a day every 4-6 hours.

Children with a body weight of 20 to 30 kg (age from 5 to 10 years) are administered 1 candle (300 mg) 4 times a day every 4-6 hours.

Regular intervals between the use of suppositories should be observed - from 4 to 6 hours.

Do not use more than 4 candles per day.

Duration of treatment:

In view of a possible local toxic effect, the use of suppositories more than 4 times a day is not recommended, the duration of application should be as short as possible: 3 days as an antipyretic and up to 5 days as an analgesic.

If there is no therapeutic effect, discontinue treatment and consult your doctor.

In patients with chronic or compensated active liver diseaseneither, especially in patients with hepatitisocellular insufficiency, chronic alcoholism, chronic malnutrition (inadequate supply of glutathione in the liver) and dehydration, the daily dose should not exceed 3 g.

Side effects:

On the part of the digestive system: abdominal pain, diarrhea, nausea, vomiting, tenesmus.

From the liver and bile ducts: hepatic insufficiency, liver necrosis, hepatitis, increased activity of hepatic enzymes.

On the part of the organs of hematopoiesis: Thrombocytopenia, anemia, leukopenia, neutropenia.

From the cardiovascular system: decrease or increase prothrombin index, lowering of arterial pressure (as a symptom of anaphylaxis).

From the skin and subcutaneous tissue: allergic reactions (skin rash, itching, urticaria, Quincke's edema, acute generalized exanthematous pustules, Stevens-Johnson syndrome, toxic epidermal necrolysis).

From the immune system: anaphylactic shock

Local reactions: irritation of the rectal mucosa, irritation in the anal passage.

If any side effects occur, discontinue use and consult a doctor.

Overdose:

Signs of acute paracetamol poisoning are nausea, vomiting, anorexia, pain in the epigastric region, sweating, paleness of the skin, appearing in the first 24 hours after ingestion.Paracetamol administration in a dose of 140 mg / kg of body weight in children causes destruction of liver cells leading to complete and irreversible hepatonecrosis, liver failure, metabolic acidosis, encephalopathy, which in turn can lead to coma and death.

After 12-48 hours after admission, an increase in the level of liver transaminases (ALT, ACT), lactate dehydrogenase and bilirubin with a simultaneous decrease in the level of prothrombin. The clinical picture of liver damage usually occurs after one or two days and reaches a maximum through 3-4 day.

When symptoms of poisoning appear, discontinuation of the drug and immediate hospitalization are recommended. It is necessary to take blood samples for the initial determination of the level of paracetamol in the blood plasma. Gastric lavage is carried out in the case of oral administration of the drug, taking enterosorbents (Activated carbon, hydrolysis lignin), administration of the antidote of acetylcysteine (intravenously or orally) within up to 8 hours after taking the drug. Acetylcysteine can be effective even after 16 hours after an overdose.

Also carry out symptomatic treatment.

Hepatic tests should be performed at the beginning of treatment and then every 24 hours. In most cases, liver transaminases activity normalizes within 1-2 weeks. In very serious cases, liver transplantation may be required.

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

Interaction:

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. Patients should be monitored to exclude hepatotoxicity.

Probenecid almost halves the clearance of paracetamol, inhibiting the process of its conjugation with glucuronic acid. With simultaneous application, consideration should be given to reducing the dose of paracetamol.

Caution should be exercised while using paracetamol and inducers of microsomal liver enzymes (for example, ethanol, barbiturates, isoniazid, rifampicin, carbamazepine, anticoagulants, zidovudine, amoxicillin + clavulanic acid, phenylbutazone, tricyclic antidepressants).Long-term use of barbiturates reduces the effectiveness of paracetamol. Salicylamide increases the half-life of paracetamol.

Monitor the international normalized ratio (INR) during and after the concurrent use of paracetamol, (especially at high doses and / or for a long time) and coumarins (eg, warfarin), since paracetamol when taken in a dose of 4 g for at least 4 days can enhance the effect of indirect anticoagulants. It is necessary to inform the attending physician about the use of Efferalgan® in the analysis of uric acid and blood glucose.

Special instructions:

When using the drug for more than a week, control over the functional state of the liver and the picture of peripheral blood is necessary.

Paracetamol intake in doses exceeding the recommended levels can lead to serious liver damage.

There is a risk of overdose in patients suffering from liver disease, chronic alcoholism, chronic malnutrition (due to low levels of glutathione in hepatocytes)receiving inductors of microsomal liver enzymes. To avoid the risk of overdose, it is not recommended at the same timeEffergangan® and other drugs containing paracetamol. Paracetamol can cause serious skin reactions, such as acute generalized exanthematous pustulosis, Stevens-Johnson syndrome, toxic epidermal necrolysis, which can be legal. At the first manifestation of a rash or other hypersensitivity reactions, the drug should be discontinued.

Form release / dosage: Suppositories rectal 80 mg, 150 mg, 300 mg.

Packaging: 6 suppositories into a contoured cell pack of PVC / low density polyethylene. 2 contour squares with instructions for use in a pack of cardboard.

Storage conditions:

Store at a temperature not exceeding 30 ° C.

Keep out of the reach of children!

Shelf life:3 years.

Do not use the product after the expiry date indicated on the package.

Terms of leave from pharmacies:Without recipe

Registration number:П N011549 / 03

Date of registration:01.07.2008

The owner of the registration certificate:BRISTOL-MIYERS SQUIPB BRISTOL-MIYERS SQUIPB USA

Manufacturer: & nbsp

BRISTOL-MYERS SQUIBB France

Representation: & nbspBRISTOL-Majers SKVIBB, LLCBRISTOL-Majers SKVIBB, LLCRussia

Information update date: & nbsp08.10.2015

Illustrated instructions

Instructions

Efferalgan® (Efferalgan®)