Contraindications
- hypersensitivity to paracetamol or other components of the drug;
- age up to one month (child’s body weight up to 4 kg);
- severe renal and/or liver dysfunction, hepatocellular failure, 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.
Mode of application
The drug should be used under medical supervision, with extreme caution in children under one year of age. Apply rectally.
Suppositories cannot be divided to obtain the required dosage. If, when calculating the daily dose in accordance with the child’s body weight, a single dosage is required, less than the contents of one suppository, then after consultation with a doctor it is recommended to use other dosage forms of paracetamol (for example, oral solution).
When treating children, you should follow the dosage calculation regimen in accordance with the child’s body weight and, depending on this, choose an acceptable dosage form.
The approximate ages of children based on body weight are provided as a guideline only.
Rectal suppositories of 150 mg are intended for children weighing from 8 to 12 kg (aged approximately 6 months to 2 years). From 3 to 4 suppositories per day with an interval of 6 hours between doses, depending on the child’s body weight, at the rate of 60 mg/kg/day.
The recommended daily dose of paracetamol is about 60 mg/kg/day, which should be divided into 4 doses, i.e. 15 mg/kg body weight every 6 hours. In case of severe renal failure (creatinine clearance less than 10 ml/minute), the interval between doses should be at least 8 hours.
Application involves the rectal administration of one suppository, which is repeated if necessary at intervals of at least 6 hours, but not exceeding the daily dose and the number of 4 suppositories per day.
Due to the risk of local toxicity, the use of suppositories more than 4 times a day is not recommended, and the duration of use with the rectal route of administration should be shortest.
Efferalgan supp rect for children 300 mg No. 12
Compound
Active substance: paracetamol 300 mg.
Excipients: semi-synthetic glycerides (solid fat) - 1000 mg.
Pharmacokinetics
Suction and distribution
Absorption of paracetamol when administered rectally is slower than when administered orally. Cmax in plasma is achieved 2-3 hours after administration. The distribution of paracetamol in tissues occurs quickly. Comparable drug concentrations are achieved in blood, saliva and plasma. Plasma protein binding is low, 10-25%. Penetrates through the BBB.
Metabolism and excretion
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 CYP2E1 isoenzyme is also involved in the metabolism of the drug.
T1/2 - 1-4 hours. Excreted by the kidneys in the form of metabolites, mainly conjugates. Less than 5% is excreted unchanged.
Indications for use
- In children as an antipyretic for acute respiratory diseases, influenza, childhood infections, post-vaccination reactions and other infectious and inflammatory diseases accompanied by an increase in body temperature;
- as an analgesic for pain of mild or moderate intensity, incl. headache and toothache, muscle pain, neuralgia, pain from injuries and burns.
Contraindications
- Hypersensitivity to paracetamol, propacetamol hydrochloride (prodrug of paracetamol) or other components of the drug;
- severe liver dysfunction or decompensated liver disease in the active stage;
- severe renal dysfunction;
- blood diseases;
- deficiency of the enzyme glucose-6-phosphate dehydrogenase;
- early infancy (up to 3 months);
- recent inflammation or bleeding in the rectum (contraindication related to route of administration).
With caution: the drug should be used with caution in case of impaired renal function, liver function, Gilbert's syndrome, dehydration, hypovolemia, as well as anorexia, bulimia, cachexia or chronic nutritional deficiency (insufficient supply of glutathione in the liver).
Before taking the drug, you should consult your doctor.
If renal function is impaired, the time interval between doses of the drug should be at least 8 hours when the clearance is less than 10 ml/min, and at least 6 hours when the clearance is greater than or equal to 10 ml/min.
The drug should not be used if the child has diarrhea.
Directions for use and doses
The drug is administered rectally. Having freed the suppository from the package, insert it into the child's anus (preferably after a cleansing enema or spontaneous bowel movement).
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 from 6 to 8 kg (age from 3 to 5 months) are administered 1 suppository (80 mg) 4 times a day every 4-6 hours.
- Children weighing from 10 to 14 kg (age from 6 months to 3 years) are administered 1 suppository (150 mg) 4 times a day every 4-6 hours.
- Children weighing from 20 to 30 kg (age from 5 to 10 years) are administered 1 suppository (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.
You should not use more than 4 suppositories per day.
Duration of treatment
In view of the possible local toxic 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 an analgesic.
If there is no therapeutic effect, you should stop treatment and consult your doctor.
In patients with chronic or compensated active liver diseases, especially those accompanied by liver failure, in patients with chronic alcoholism, chronic malnutrition (insufficient supply of glutathione in the liver), Gilbert's syndrome, dehydration or body weight up to 50 kg, the dose of the drug should be reduced or the interval increased between doses. The daily dose should not exceed 2 g.
Storage conditions
The drug should be stored out of the reach of children at a temperature not exceeding 30°C.
Best before date
3 years. Do not use the drug after the expiration date indicated on the packaging.
special instructions
Before taking the drug, you should consult your doctor.
When using the drug for more than a week, monitoring the functional state of the liver and peripheral blood patterns is necessary.
Taking paracetamol in doses higher than recommended may cause 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 reserves in hepatocytes) and in patients receiving inducers of microsomal liver enzymes.
To avoid the risk of overdose, simultaneous use of Efferalgan® and other drugs containing paracetamol is not recommended.
Paracetamol can cause serious skin reactions such as acute generalized exanthematous pustulosis, Stevens-Johnson syndrome, toxic epidermal necrolysis, which can be fatal. At the first appearance of a rash or other hypersensitivity reactions, use of the drug should be discontinued.
Description
Analgesic non-narcotic drug.
Use in children
Use is contraindicated in early infancy (up to 3 months).
Pharmacodynamics
Efferalgan suppositories contain paracetamol, which blocks cyclooxygenase (COX)-1 and COX-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 anti-inflammatory effect.
The absence of a blocking effect on the synthesis of prostaglandins in peripheral tissues determines the absence of a negative effect on water-salt metabolism (sodium and water retention) and the gastrointestinal mucosa.
Side effects
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.
From the hematopoietic system: thrombocytopenia, anemia, leukopenia, neutropenia.
From the blood coagulation system: decrease or increase in prothrombin index.
From 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, decreased blood pressure (as a symptom of anaphylaxis).
Local reactions: irritation of the rectal mucosa, irritation in the anal area.
If adverse reactions occur, you should stop taking the drug and consult a doctor.
Interaction
Phenytoin reduces the effectiveness of paracetamol and increases the risk of hepatotoxicity. Patients taking phenytoin should avoid frequent use of paracetamol, especially in high doses. Patients should be monitored for hepatotoxicity.
Probenecid reduces the clearance of paracetamol by almost 2 times, inhibiting the process of its conjugation with glucuronic acid. If used concomitantly, consider reducing the dose of paracetamol.
Caution should be exercised during 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 T1/2 of paracetamol.
The international normalized ratio (INR) should be monitored during and after cessation of concomitant use of paracetamol (especially in high doses and/or for a long time) and coumarins (for example, warfarin), because 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 when using paracetamol and flucloxacillin simultaneously, which is associated with an increased risk of developing metabolic acidosis with a high anion gap, especially in patients with a risk factor for developing glutathione deficiency (including patients with severe renal failure, sepsis, malnutrition and chronic alcoholism). Careful monitoring is recommended to identify signs of acid-base imbalance, namely metabolic acidosis with a high anion gap, including the determination of 5-oxoproline in the urine.
You should inform your doctor about the use of Efferalgan® when performing tests to determine uric acid and blood glucose levels.
Overdose
Symptoms: signs of acute paracetamol poisoning are nausea, vomiting, anorexia, epigastric pain, sweating, pale skin, appearing in the first 24 hours after administration. Taking paracetamol at a dose of 140 mg/kg 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.
12-48 hours after administration, an increase in the level of liver transaminases (ALT, AST), LDH and bilirubin may be observed with a simultaneous decrease in the level of prothrombin. The clinical picture of liver damage is usually detected after 1 or 2 days and reaches a maximum after 3-4 days.
Treatment: if symptoms of poisoning appear, it is recommended to stop taking the drug and immediate hospitalization. Blood samples should be taken for an initial determination of plasma paracetamol levels. Gastric lavage is carried out in case of oral administration of the drug, intake of enterosorbents (activated carbon, hydrolytic lignin), administration of the antidote acetylcysteine (iv or orally) for up to 8 hours after taking the drug. Acetylcysteine can be effective even 16 hours after an overdose. Symptomatic treatment is also carried out.
Liver tests should be performed at the beginning of treatment and then every 24 hours. In most cases, the activity of liver transminases normalizes within 1-2 weeks. In very severe cases, a liver transplant may be required.
With long-term use in large doses, hepatotoxic and nephrotoxic effects are possible.
Side effects
Very rarely:
- allergic reactions: anaphylaxis, anaphylactic shock, Quincke's edema, erythema, urticaria, itching, rash on the skin and mucous membranes, exudative erythema multiforme, toxic epidermal necrolysis;
- from the hematopoietic organs: anemia, sulfhemoglobinemia and methemoglobinemia (cyanosis, shortness of breath, heart pain), hemolytic anemia, thrombocytopenia, leukopenia and neutropenia;
- from the respiratory system: bronchospasm in patients sensitive to aspirin and other NSAIDs;
- from the digestive system: nausea, epigastric pain, impaired liver function, increased activity of liver enzymes, usually without the development of jaundice, hepatonecrosis (dose-dependent effect);
- from the endocrine system: hypoglycemia, up to hypoglycemic coma.
Associated with the dosage form: irritation of the rectum and anus.
If any adverse reactions occur, you should stop using the drug and be sure to consult a doctor.
Efferalgan rectal suppositories. 150 mg package No. 10
Efferalgan, rectal suppositories, 150 mg International nonproprietary name Paracetamol Release form Rectal suppositories 80 mg, 150 mg, 300 mg. Composition of the drug 1 suppository contains the active substance: paracetamol 80 mg, 150 mg or 300 mg, respectively; excipient: solid fat.
Description Suppositories are white in color with a smooth and shiny surface.
Pharmacotherapeutic group Analgesics and antipyretics. ATX code: N02BE01.
Pharmacological properties Pharmacokinetics Absorption of paracetamol when administered rectally occurs more slowly, but more completely than when administered orally. Maximum plasma concentrations are achieved 2-3 hours after administration. Paracetamol is quickly distributed into all tissues. Concentrations in blood, saliva and plasma are comparable. Plasma protein binding is weak. Paracetamol is predominantly metabolized in the liver and excreted in the urine. 90% of the dose taken is excreted by the kidneys within 24 hours, mainly in the form of glucuronide conjugates (60-80%) and sulfate conjugates (20-30%). Less than 5% is excreted unchanged. The half-life is 4-5 hours. A small part of paracetamol, with the participation of cytochrome P450, is converted into a metabolite that combines with glutathione and is excreted in the urine. In case of overdose, the amount of this metabolite increases. In case of severe renal failure (creatinine clearance below 10 ml/min), the elimination of paracetamol and its metabolites is slowed down.
Pharmacodynamics Efferalgan suppositories have analgesic and antipyretic effects. The mechanism of action is associated with inhibition of prostaglandin synthesis, with a predominant effect on the thermoregulation center in the hypothalamus.
Indications for use: Symptomatic treatment of mild to moderate pain and/or febrile conditions.
Method of administration and dosage The drug is used rectally only in children from 3 months to 10 years. The recommended daily dose of paracetamol depends on the child's body weight at the rate of 60 mg/kg/day, divided into 4 doses. A single dose is 15 mg/kg every 6 hours, doses should be taken at equal intervals, including at night. In children, dosage should be observed in accordance with the child's body weight. Age and corresponding body weight are given approximately. Children weighing from 4 to 10 kg (from 3 to 6 months) are administered 1 suppository (80 mg) no more than 4 times a day every 6 hours, not exceeding 4 suppositories per day. Children weighing from 10 to 14 kg (from 6 months to 4 years) are administered 1 suppository (150 mg) no more than 4 times a day every 6 hours, not exceeding 4 suppositories per day. Children weighing from 14 to 24 kg (from 4 years to 10 years) are administered 1 suppository (300 mg) no more than 4 times a day every 6 hours, not exceeding 4 suppositories per day. In case of diarrhea, the use of a suppository is not recommended. You should not use more than 4 suppositories per day. In case of severe renal failure (creatinine clearance below 10 ml/min), the interval between two doses should be at least 8 hours. Due to the risk of local toxicity, rectal administration of paracetamol should be kept as short as possible. The duration of use should be as short as possible: up to 3 days as an antipyretic and up to 5 days as an analgesic. If there is no therapeutic effect, you should stop treatment and consult a doctor.
Side effects Very rare: Allergic reactions: - anaphylaxis, skin itching, rash on the skin and mucous membranes (usually a generalized rash, erythematous, urticaria), angioedema, exudative erythema multiforme (including Stevenson-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome). From the digestive system: - nausea, epigastric pain, increased activity of liver enzymes, usually without the development of jaundice. From the endocrine system: - hypoglycemia, up to hypoglycemic coma. From the hematopoietic organs: - anemia, thrombocytopenia, leukopenia, neutropenia, sulfhemoglobinemia and methemoglobinemia (cyanosis, shortness of breath, heart pain), hemolytic anemia. From the respiratory system: - bronchospasm in patients sensitive to acetylsalicylic acid and other NSAIDs. Local reactions: - irritation of the rectum and anus. If any adverse reactions occur, you should stop using the drug and be sure to consult a doctor.
Contraindications - hypersensitivity to paracetamol; - hepatocellular failure; - severe dysfunction of the liver and kidneys; - recent proctitis, anusitis or rectal bleeding; - blood diseases; - deficiency of the enzyme glucose-6-phosphate dehydrogenase; - children up to 3 months of age.
Interaction with other drugs Oral anticoagulants Paracetamol enhances the effect of oral anticoagulants and increases the risk of bleeding when taken in maximum doses (4 g/day) for at least 4 days, so regular monitoring of the prothrombin index is necessary. If necessary, the dosage regimen of anticoagulants should be adjusted during the use of paracetamol and after its discontinuation. Effect on laboratory test results At abnormally high concentrations, taking paracetamol may affect blood glucose results through the glucose oxidase-peroxidase reaction. The use of paracetamol may affect the results of determining blood urea by a method that uses phosphotungstic acid. Barbiturates reduce the antipyretic effect of paracetamol. Anticonvulsants (including phenytoin, barbiturates, carbamazepine), which stimulate the activity of microsomal liver enzymes, may increase the toxic effects of paracetamol on the liver due to an increase in the degree of conversion of the drug to hepatotoxic metabolites. With the simultaneous use of paracetamol with isoniazid, the risk of developing hepatotoxic syndrome increases. Paracetamol reduces the effectiveness of diuretics.
Precautions To avoid the risk of overdose, you should check that paracetamol is not included in other medicines. Maximum permissible doses: - in children weighing up to 37 kg, the maximum daily dose of paracetamol should not exceed 80 mg/kg/day; - in children weighing from 38 to 50 kg, the maximum daily dose of paracetamol should not exceed 3 g/day; - in adults and children weighing more than 50 kg, the maximum daily dose of paracetamol should not exceed 4 g/day. When treating children, the dosage regimen should be followed in accordance with the child’s body weight, and depending on this, the appropriate dosage form should be selected (see section Method of administration and dosage). If, when calculating the daily dose in accordance with the child’s body weight, the required single dosage is less than the contents of one suppository, then after consultation with a doctor it is recommended to use other dosage forms of paracetamol. In case of diarrhea, the use of suppositories is not recommended. There is a risk of local toxicity when using suppositories, especially with frequent and prolonged use. The drug should be used with caution in case of impaired liver function, Gilbert's syndrome, dehydration, hypovolemia. Before taking the drug, you should consult your doctor.
Pregnancy and lactation The drug is intended for use only in children from 3 months to 10 years of age. Paracetamol crosses the placental barrier and is excreted in breast milk. When using paracetamol during pregnancy and lactation, the expected benefits of therapy for the mother and the potential risk for the fetus and child should be carefully weighed.
The peculiarity of the drug’s influence on the ability to drive vehicles and dangerous mechanisms does not affect.
Overdose There is a risk of poisoning in older people and especially young children, which can be life-threatening. Symptoms: nausea, vomiting, anorexia, pallor, abdominal pain, usually appearing in the first day. A single dose of more than 10 g of paracetamol by an adult and a single dose of more than 150 mg/kg body weight by a child can cause necrosis of hepatocytes, leading to hepatocellular failure, metabolic acidosis, encephalopathy and death. 12-48 hours after an overdose, an increase in the level of liver transaminases, lactate dehydrogenase and bilirubin, as well as a decrease in the level of prothrombin, may be observed. Treatment: If symptoms of poisoning occur, consult a doctor immediately. A blood test to determine the level of paracetamol in plasma, gastric lavage (if taken orally), taking the antidote N-acetylcysteine intravenously or orally within 10 hours after taking the drug, and symptomatic treatment are recommended.
Packaging 5 suppositories in a blister pack. 2 blister packs along with instructions for use are placed in a cardboard box.
Storage conditions Store at a temperature not exceeding 30C. Keep out of the reach of children!
Shelf life: 3 years. Do not use after expiration date.
Dispensing conditions Without a prescription.
Manufacturer information UPSA SAS, 304 avenue du Doctor Jean Bru, 47000 Agen, France. Marketing authorization holder: UPSA SAS, 3 rue Joseph Monnier, 92500 Rueil-Malmaison, France.
Note!
Description of the drug Efferalgan supp. rectal 150 mg No. 10 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
