Efferalgan (Paracetamol) for kids

Instructions for Efferalgan

pharmachologic effect Efferalgan:

Pharmacological action - analgesic, inhibiting COX.
Efferalgan

Pharmacodynamics Efferalgan:

Efferalgan suppositories contain paracetamol, which blocks COX-1 and -2 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 the anti-inflammatory effect.
The absence of a blocking effect on the synthesis of PG in peripheral tissues leads to the absence of a negative effect on water-salt metabolism (Na + and water retention) and the gastrointestinal mucosa.

Pharmacokinetics Efferalgan:

Absorption of paracetamol with rectal administration is slower than with oral administration. Cmax in plasma is achieved 2-3 hours after administration.
The distribution of paracetamol in tissues is rapid. Comparable concentrations of the drug in blood, saliva and plasma are achieved.
The connection with plasma proteins is low, 10–25%. Penetrates the BBB.
Metabolism occurs in the liver, 80% enters into conjugation reactions with glucuronic acid and sulfates to form inactive metabolites; 17% undergoes hydroxylation to form 8 active metabolites.
With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. The isoenzyme CYP2E1 is also involved in the metabolism of the drug. T1 / 2 - 1-4.
It is excreted by the kidneys in the form of metabolites, mainly conjugates. Less than 5% is displayed unchanged. T1 / 2 is 4–5.
Efferalgan

Indications for use Efferalgan:

Efferalgan suppositories are used in children as an antipyretic agent for the following diseases and conditions accompanied by an increase in body temperature:
Acute respiratory diseases;
Flu;
Childhood infections;
Post-vaccination reactions;
Infectious and inflammatory diseases.
As an anesthetic for pain syndrome of mild or moderate intensity, including:
Headache and toothache;
Muscle pain;
Neuralgia;
Pain in trauma and burns.
Suppositories of 80 mg are used in children weighing 6 to 8 kg (age from 3 to 5 months). Suppositories of 150 mg are used in children weighing 10 to 14 kg (age from 6 months to 3 years). Suppositories of 300 mg are used in children weighing from 20 to 30 kg (age from 5 to 10 years).

Contraindications Efferalgan:

Hypersensitivity to paracetamol, propacetamol hydrochloride (paracetamol prodrug) or any other component of the drug;
Severe liver or kidney dysfunction or active decompensated liver disease;
Blood diseases;
Deficiency of the enzyme glucose-6-phosphate dehydrogenase;
Recent inflammation or bleeding in the rectum (contraindication associated with the route of administration);
Early infancy (up to 3 months).
Carefully. Impaired renal function. Liver. Gilbert's syndrome. Dehydration. Hypovolemia. Anorexia. Bulimia. Cachexia. Chronic nutritional deficiencies (insufficient supply of glutathione in the liver). Diarrhea (diarrhea).
Before taking the drug, you should consult your doctor.
In case of impaired renal function (Cl creatinine <10 ml / min), the time interval between doses of the drug should be at least 8 hours; with Cl creatinine ≥10 ml / min - at least 6.

Side effects Efferalgan:

From the digestive system. Abdominal pain, diarrhea, nausea, vomiting, tenesmus.
From the liver and biliary tract. Liver failure, liver necrosis, hepatitis, increased activity of liver enzymes.
On the part of the hematopoietic organs. Thrombocytopenia, anemia, leukopenia, neutropenia.
From the CCC side. Decrease or increase in prothrombin index, decrease in blood pressure (as a symptom of anaphylaxis).
On the part of the skin and subcutaneous tissue. Allergic reactions (skin rash, itching, urticaria, Quincke's edema, acute generalized exanthematous pustulosis, Stevens-Johnson syndrome, toxic epidermal necrolysis).
From the immune system. Anaphylactic shock.
Local reactions. Irritation of the rectal mucosa, irritation in the anal canal.
If any adverse reactions occur, you should stop using the drug and consult a doctor.

Interaction

Phenytoin reduces the effectiveness of paracetamol and increases the risk of developing hepatotoxicity. In patients taking phenytoin, frequent use of paracetamol should be avoided, especially at high doses. Patients should be monitored to rule out hepatotoxicity.
Probenecid almost halves the clearance of paracetamol, inhibiting the process of its conjugation with glucuronic acid. With simultaneous use, consider reducing the dose of paracetamol.

Caution should be exercised with the simultaneous use of 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 T1 / 2 of paracetamol.
MHO should be monitored during and after the end of the simultaneous use of paracetamol (especially in high doses and / or for a long time) and coumarins (for example, warfarin), etc. paracetamol, when taken in a dose of 4 g for at least 4 days, can enhance the effect of indirect anticoagulants.
Caution should be exercised with the simultaneous use of paracetamol and flucloxacillin, which is associated with an increased risk of metabolic acidosis with a high anionic difference, especially in patients with a risk factor for glutathione deficiency (including patients with severe renal failure, sepsis, malnutrition and chronic alcoholism). Careful monitoring is recommended to detect signs of acid-base imbalance, namely metabolic acidosis with a high anion difference, including determination of 5-oxoproline in urine.
The attending physician should be informed about the use of Efferalgan when conducting tests to determine uric acid and blood glucose levels.

Method of administration and dosage Efferalgan:

Rectally, preferably after a cleansing enema or spontaneous bowel movement. Having released the candle from the packaging, insert the child into the anus.
The average single dose of Efferalgan depends on the child's body weight and is 15 mg / kg 4 times a day (every 4-6 hours). The maximum daily dose should not exceed 60 mg / kg.
Children weighing 6 to 8 kg (age from 3 to 5 months) are administered 1 supp. (80 mg) 4 times a day every 4-6 hours; 10-14 kg (age from 6 months to 3 years) - 1 supp. (150 mg) 4 times a day every 4-6 hours; 20-30 kg (age from 5 to 10 years) enter 1 supp. (300 mg) 4 times a day every 4-6.
Regular intervals between the use of suppositories should be observed - from 4 to 6 Suppositories should not be used more than 4. / day

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

In the absence of a therapeutic effect, stop treatment and contact your doctor.
In patients with chronic or compensated active liver diseases, especially accompanied by liver failure, patients with chronic alcoholism, chronic malnutrition (insufficient supply of glutathione in the liver), Gilbert's syndrome, dehydration, or weighing less than 50 kg, the dose of the drug should be reduced or the interval between receptions. The daily dose should not exceed 2 g.