Efferalgan effervescent tablets 500 mg No. 16

A country

France
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Active substance

Paracetamol + Phenylephrine + Ascorbic acid

Compound

1 tablet contains: paracetamol 500 mg. Excipients: anhydrous citric acid - 1114.00 mg, sodium bicarbonate - 942.00 mg, anhydrous sodium carbonate - 332.00 mg, sorbitol - 300.00 mg, sodium saccharinate - 7.00 mg, sodium docusate - 0.227 mg, povidone - 1.287 mg, sodium benzoate - 60.606 mg. Effervescent tablets are white, round, flat, with beveled edges and a score line on one side. When dissolved in water, intense release of gas bubbles is observed.

pharmachologic effect

Analgesic-antipyretic. Has an analgesic and antipyretic effect. Inhibits 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 its anti-inflammatory effect. It does not have a negative effect on water-salt metabolism (sodium and water retention) and the gastrointestinal mucosa due to the lack of influence on the synthesis of prostaglandins in peripheral tissues. The possibility of methemoglobin formation is unlikely.

Indications for use

- pain syndrome of mild or moderate intensity: headache, toothache, migraine, neuralgia, muscle pain, lower back pain, pain from injuries and burns, sore throat, algodismenorrhea; - increased body temperature with colds and other infectious and inflammatory diseases .

Mode of application

The tablet should be dissolved in a glass of water (200 ml) and drunk. Prescribed orally 0.5-1 g (1-2 tablets) 2-3 times a day at intervals of at least 4 hours. The maximum single dose is 1 g (2 tablets), the daily dose is 4 g (8 tablets). patients with impaired liver or kidney function and elderly patients, the daily dose should be reduced, the interval between doses of the drug should be at least 8 hours. The duration of treatment (without consulting a doctor) is no more than 5 days when used as an analgesic and 3 days - as an antipyretic.

Interaction

Inducers of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites of paracetamol, which makes it possible to develop severe intoxication with a small overdose of the drug. Inhibitors of microsomal oxidation (including cimetidine) reduce the risk hepatotoxic effect of paracetamol. Paracetamol reduces the effectiveness of uricosuric drugs. When used simultaneously with paracetamol, ethanol promotes the development of acute pancreatitis.

Side effect

Allergic reactions: sometimes - skin rash, itching, Quincke's edema. From the hematopoietic system: rarely - anemia, thrombocytopenia, methemoglobinemia. Others: with long-term use in doses significantly higher than recommended, the likelihood of impaired liver and kidney function increases (monitoring of the peripheral picture is necessary blood). The drug is well tolerated in recommended doses.

Contraindications

- chronic alcoholism; - deficiency of glucose-6-phosphate dehydrogenase; - I and III trimesters of pregnancy; - lactation period (breastfeeding); - children under 15 years of age (body weight less than 50 kg); - hypersensitivity to the components of the drug. With caution the drug should be used for renal and/or liver failure, congenital hyperbilirubinemia (Gilbert, Dubin-Johnson and Rotor syndromes), viral hepatitis, alcoholic liver damage, and in elderly patients.

Overdose

Symptoms: — pallor of the skin, anorexia, nausea, vomiting; — hepatonecrosis (the severity of necrosis due to intoxication directly depends on the degree of overdose). Toxic effects in adults are possible after taking paracetamol in a dose of more than 10-15 g: increased activity of liver transaminases, increased prothrombin time (12-48 hours after administration); - a detailed clinical picture of liver damage appears after 1-6 days. Rarely - fulminant development of liver failure, which can be complicated by renal failure (tubular necrosis). Treatment: in the first 6 hours after an overdose - gastric lavage, administration of SH-group donors and precursors for the synthesis of glutathione - methionine 8-9 hours after the overdose and N- acetylcysteine after 12 hours. The need for additional therapeutic measures (further administration of methionine, intravenous administration of N-acetylcysteine) is determined by the concentration of paracetamol in the blood, as well as the time elapsed after its administration.

special instructions

If the febrile syndrome continues during the use of paracetamol for more than 3 days, and pain syndrome for more than 5 days, a doctor’s consultation is required. Distorts laboratory test results when quantifying the content of uric acid in plasma. To avoid toxic damage to the liver, paracetamol should not be combined with alcoholic beverages , and also taken by people prone to chronic alcohol consumption. The risk of developing liver damage increases in patients with alcoholic hepatosis. With prolonged use of the drug, monitoring of the peripheral blood picture and the functional state of the liver is necessary. Efferalgan contains 412.4 mg of sodium in 1 tablet, which should be taken into account by patients on a strict low-salt diet. The tablets contain sorbitol, so the drug should not be used in case of fructose intolerance, low absorption of glucose and galactose, or isomaltase deficiency.

Storage conditions

Room temperature

Efferalgan®

- Inducers of liver microsomal enzymes or potentially hepatotoxic substances (for example, alcohol, rifampicin, isoniazid, hypnotics and antiepileptic drugs, including phenobarbital, phenytoin and carbamazepine) increase the toxicity of paracetamol and can lead to liver damage even at non-toxic doses of paracetamol, so liver function should be monitored .

- Phenytoin reduces the effectiveness of paracetamol and increases the risk of hepatotoxicity; therefore, patients taking phenytoin should avoid frequent use of paracetamol, especially in high doses. Reduces the effectiveness of uricosuric drugs. Paracetamol may increase the risk of increased chloramphenicol concentrations and, as a result, may increase the risk of developing neutropenia, and therefore hematological parameters should be monitored. The simultaneous use of these two drugs is possible only after consulting a doctor. Probenecid almost halves the clearance of paracetamol, which requires a reduction in the dose of paracetamol. Repeated use of paracetamol for more than 4 days increases the anticoagulant effect. The international normalized ratio (INR) should be monitored during and after the cessation of concomitant use of paracetamol (especially in high doses and/or for a long time) and coumarin derivatives. If necessary, adjust the dose of anticoagulants.

— Irregular use of paracetamol does not have a significant effect on the effect of anticoagulants. Propantheline and other drugs that slow down gastric emptying reduce the rate of absorption of paracetamol, which may delay or reduce the onset of the effect.

— Metoclopramide and domperidone increase the rate of absorption of paracetamol and, accordingly, the onset of analgesic and antipyretic effects. Long-term use of barbiturates reduces the effectiveness of paracetamol. Ethanol contributes to the development of acute pancreatitis. Long-term combined use of paracetamol and other NSAIDs increases the risk of developing “analgesic” nephropathy and renal failure. Simultaneous long-term administration of paracetamol in high doses and salicylates increases the risk of developing cancer of the bladder or bladder. Diflunisal increases the plasma concentration of paracetamol by 50% - the risk of developing hepatotoxicity. Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.

- Salicylamide may increase the half-life of paracetamol.

- 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). Close 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.

Efferalgan tablets spike 500 mg No. 16

Compound

1 effervescent tablet contains:
Active substance:

paracetamol 500 mg.

Excipients:

anhydrous citric acid 1114.00 mg, sodium bicarbonate 942.00 mg, anhydrous sodium carbonate 332.00 mg, sorbitol 300.00 mg, sodium saccharinate 7.00 mg, sodium docusate 0.227 mg, povidone 1.287 mg, sodium benzoate 60.606 mg.

Pharmacokinetics

Absorption

When taken orally, paracetamol is absorbed quickly and completely. Cmax (maximum concentration of paracetamol in plasma) is reached 10 to 60 minutes after administration.

Distribution

Paracetamol is quickly distributed in all tissues. The concentration in blood, saliva and plasma is the same. Plasma protein binding is negligible.

Metabolism

Paracetamol is mainly metabolized in the liver. There are two main metabolic pathways producing glucuronides and sulfates. The latter is mainly used if the dose of paracetamol exceeds the therapeutic dose.

A small amount of paracetamol is metabolized by the cytochrome P450 isoenzyme to form the intermediate compound N-acetylbenzoquinoneimine, which under normal conditions is rapidly detoxified by glutathione and excreted in the urine after binding to cysteine and mercaptopuric acid. However, with massive intoxication, the content of this toxic metabolite increases.

Removal

Carried out mainly in the urine, 90% of the taken dose of paracetamol is excreted by the kidneys within 24 hours, mainly in the form of glucuronide (60 to 80%) and sulfate (20 to 30%). Less than 5% is excreted unchanged. The half-life is approximately 2 hours.

Pharmacokinetics in special groups of patients

In case of severe renal dysfunction (creatinine clearance less than 30 ml/min), the elimination of paracetamol and its metabolites is delayed.

Indications for use

— Moderate or mild pain syndrome (headache, toothache, migraine pain, neuralgia, muscle pain, lower back pain, pain from injuries and burns, sore throat, painful menstruation),

— Increased body temperature during colds and other infectious and inflammatory diseases.

Contraindications

In case of overdose, intoxication is possible, especially in children, patients with liver diseases (caused by chronic alcoholism), in patients with nutritional disorders, as well as in patients taking enzyme inducers, which can develop fulminant hepatitis, liver failure, cholestatic hepatitis, cytolytic hepatitis, in the above cases - sometimes with death.

The clinical picture of acute overdose develops within 24 hours after taking paracetamol.

Symptoms:

gastrointestinal disorders (nausea, vomiting, loss of appetite, abdominal discomfort and/or abdominal pain), pale skin, sweating, malaise. When administered simultaneously to adults of 7.5 g or more or to children of more than 140 mg/kg, cytolysis of hepatocytes occurs with complete and irreversible liver necrosis, the development of liver failure, metabolic acidosis and encephalopathy, which can lead to coma and death. 12-48 hours after the administration of paracetamol, there is an increase in the activity of liver transaminases, lactate dehydrogenase, bilirubin concentration and a decrease in prothrombin concentration. Clinical symptoms of liver damage appear 1-2 days after an overdose of the drug and reach a maximum on days 3-4.

Treatment:

— Immediate hospitalization,

— Determination of the quantitative content of paracetamol in the blood plasma before starting treatment as early as possible after an overdose,

- Gastric lavage

- Administration of SH-group donors and precursors for glutathione synthesis - methionine and acetylcysteine - within 8 hours after an overdose. The need for additional therapeutic measures (further administration of methionine, intravenous administration of acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration,

- Symptomatic treatment,

- Liver tests should be performed at the beginning of treatment and then every 24 hours. In most cases, liver transaminase activity returns to normal within 1-2 weeks. In very severe cases, a liver transplant may be required.

Directions for use and doses

Inside. Dissolve the tablet in a glass of water (200 ml). Do not chew or swallow the tablets. Usually take 1 - 2 tablets 2-3 times a day at intervals of at least 4 hours. The maximum single dose is 2 tablets (1 g), the maximum daily dose is 8 tablets (4 g), which corresponds to 10-15 mg/kg body weight for a single dose, and 75 mg/kg body weight for a maximum daily dose.

As a rule, there is no need to exceed the recommended daily dose of paracetamol of 3 g. The daily dose can be increased to the maximum (4 g) only in case of severe pain.

If renal function is impaired, temporary creatinine is less than 10 ml/min, for at least 6 hours - with creatinine clearance 10-50 ml/min.

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), dehydration or body weight less than 50 kg, the daily dose should not exceed 3 g, i.e. . 6 tablets.

The drug should be used with caution in children and patients weighing less than 50 kg to avoid the risk of exceeding the recommended dose.

The dosage regimen for children over 12 years of age and weighing more than 43 kg is the same as for adults, and the interval should preferably be 6 hours (strictly at least 4 hours).

The duration of use without consulting a doctor is no more than 5 days when prescribed as an analgesic and 3 days as an antipyretic.

Storage conditions

Store in a dry place at a temperature of 15-30 C.

Keep out of the reach of children!

Best before date

3 years.

Do not use after the expiration date.

special instructions

To avoid overdose, the content of paracetamol in other drugs that the patient takes simultaneously with Efferalgan should be taken into account.

Taking paracetamol in doses higher than recommended can cause severe liver damage.

If fever continues during the use of paracetamol for more than 3 days, and pain continues for more than 5 days, a doctor’s consultation is required.

Taking Efferalgan may distort laboratory test results when quantifying the content of glucose and uric acid in plasma.

To avoid toxic liver damage, paracetamol should not be combined with alcoholic beverages, or taken by persons prone to chronic alcohol consumption.

The risk of developing liver damage increases in patients with alcoholic hepatosis.

With prolonged use of the drug, monitoring of the peripheral blood picture and the functional state of the liver is necessary. Paracetamol can cause serious skin reactions such as Steven-Johnson syndrome, toxic epidermal necrolysis, acute generalized exanthematous pustulosis, which can be fatal. At the first appearance of a rash or other hypersensitivity reactions, use of the drug should be discontinued.

Also, the use of paracetamol should be discontinued if acute viral hepatitis is detected in the patient.

Efferalgan contains 412.4 mg of sodium per tablet, which should be taken into account by patients on a strict low-salt diet.

Since the drug contains sorbitol, it should not be used in cases of sucrase/isomaltase deficiency, fructose intolerance, or glucose-galactose malabsorption.

Description

Round, flat, white tablets with beveled edges and a score on one side. When dissolved in water, intense release of gas bubbles is observed.

Conditions for dispensing from pharmacies

Over the counter

Dosage form

effervescent tablets

Pharmacodynamics

Paracetamol (paraaminophenol derivative) has analgesic, antipyretic and weak anti-inflammatory effects.

The exact mechanism of the analgesic and antipyretic effect of paracetamol has not been established. Apparently, it includes central and peripheral components. The drug blocks cyclooxygenase I and II mainly in the central nervous system, affecting the centers of pain and thermoregulation. In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on cyclooxygenase, which explains its almost complete lack of anti-inflammatory effect. The drug does not have a negative effect on water-salt metabolism (sodium and water retention) and the gastrointestinal mucosa due to the lack of influence on the synthesis of prostaglandins in peripheral tissues.

Side effects

When using the drug, the following side effects were observed (frequency not established):

Allergic reactions:

hypersensitivity reactions, skin itching, rash on the skin and mucous membranes (erythema or urticaria), Quincke's edema, exudative erythema multiforme (including Steven-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), anaphylactic shock, acute generalized exanthematous pustulosis .

From the central and peripheral
nervous system :
(when taking high doses) dizziness, psychomotor agitation and disturbance of orientation in space and time.

From the digestive organs:

nausea, diarrhea, epigastric pain, increased activity of liver enzymes, usually without the development of jaundice, hepatonecrosis (dose-dependent effect).

From the endocrine system:

hypoglycemia, up to hypoglycemic coma.

From the hematopoietic organs:

anemia (cyanosis), sulfohemaglobinemia, methemoglobinemia (shortness of breath, heart pain), hemolytic anemia (especially in patients with glucose-6-phosphate dehydrogenase deficiency), thrombocytopenia, neutropenia, leukopenia.

Other:

decreased blood pressure (as a symptom of anaphylaxis), changes in prothrombin time and international normalized ratio (INR).

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.

Probenecid almost halves the clearance of paracetamol, inhibiting the process of its conjugation with glucuronic acid. If administered 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 simultaneous use of barbiturates reduces the effectiveness of paracetamol.

Salicylamide may increase the half-life of paracetamol.

INR monitoring should be carried out during and after the cessation of simultaneous use of paracetamol (especially in high doses and/or for a long time) and coumarins (for example, warfarin), since paracetamol when taken at a dose of 4 g / day for at least 4- x days may enhance the effect of indirect anticoagulants and increase the risk of bleeding. If necessary, adjust the dose of anticoagulants.