Paracetamol soluble

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT PARACETAMOL SOLUBLE

Composition:

Active ingredient: paracetamol;

1 tablet contains 500 mg of paracetamol;

Excipients: sodium hydrogen carbonate, sodium carbonate, citric acid, sorbitol (E 420), sodium saccharin, povidone, sodium lauryl sulfate, dimethicone.

Pharmaceutical form. Effervescent tablets.

Main physicochemical properties: white, round, flat tablets with bevelled edges and a score line on one side. Effervescence (gas bubble release) is observed when dissolved in water.

Pharmacotherapeutic group. Analgesics and antipyretics. Paracetamol.

ATC code N02B E01.

Pharmacological properties.

Pharmacodynamics.

The drug contains paracetamol, an analgesic and antipyretic (pain-relieving and fever-reducing agent). The effect is based on inhibition of prostaglandin synthesis in the central nervous system.

Pharmacokinetics.

Paracetamol is rapidly and almost completely absorbed in the gastrointestinal tract and distributed into most body tissues. Protein binding of paracetamol to plasma proteins is minimal when administered at therapeutic doses.

Clinical studies have shown that maximum plasma concentration of paracetamol is reached within 20 minutes after administration of the drug, which is significantly faster than that observed with conventional paracetamol-containing tablets.

Paracetamol is primarily metabolized in the liver and excreted in urine as metabolites. The average elimination half-life in plasma after oral administration is approximately 2.3 hours.

Clinical characteristics.

Indications.

Treatment of pain and fever, including headache, such as migraine and tension headache, back pain, rheumatic pain, pain due to osteoarthritis, muscle pain, sore throat, menstrual pain in women, neuralgia, toothache, pain following tooth extraction or dental procedures, fever and pain after vaccination, symptoms of cold and flu, such as fever, malaise, and body aches.

Contraindications.

Hypersensitivity to the components of the drug, severe impairment of liver and/or kidney function, congenital hyperbilirubinemia, glucose-6-phosphate dehydrogenase deficiency, alcoholism, blood disorders, Gilbert's syndrome, pronounced anemia, leukopenia. Pediatric use under 6 years of age.

Interaction with other medicinal products and other types of interactions.

The absorption rate of paracetamol may be increased when used concomitantly with metoclopramide and domperidone, and decreased with cholestyramine. The anticoagulant effect of warfarin and other coumarins, with an increased risk of bleeding, may be enhanced during long-term concomitant use of paracetamol. Occasional use does not have a significant effect. Barbiturates reduce the antipyretic effect of paracetamol.

Anticonvulsant drugs (including phenytoin, barbiturates, carbamazepine), which stimulate hepatic microsomal enzyme activity, may enhance the hepatotoxic effect of paracetamol due to increased formation of hepatotoxic metabolites. Concomitant use of paracetamol with hepatotoxic agents increases the hepatotoxic effects of the drugs. Simultaneous use of high doses of paracetamol with isoniazid increases the risk of developing hepatotoxic syndrome. Caution is advised when using paracetamol concomitantly with flucloxacillin, as co-administration is associated with metabolic acidosis with a high anion gap, as a result of pyroglutamic acidosis, particularly in patients with risk factors (see section "Special precautions for use").

Paracetamol reduces the effectiveness of diuretics. Do not use concomitantly with alcohol.

Special precautions for use

The product contains paracetamol; therefore, it should not be used together with other medicinal products containing paracetamol, such as those used for fever reduction, pain relief, symptoms of influenza and colds, or insomnia. Concurrent use with other paracetamol-containing products may result in overdose. Paracetamol overdose may cause liver failure, which may require liver transplantation or may result in death.

In patients with liver or kidney disease, medical advice should be sought before using this product.

It should be noted that patients with liver disease have an increased risk of hepatotoxic effects of paracetamol. The product may affect laboratory test results for blood glucose and uric acid levels. Patients who take analgesics daily for mild forms of arthritis should consult a physician before use.

Cases of liver function impairment/liver failure have been reported in patients with reduced glutathione levels, such as in severe malnutrition, anorexia, low body mass index, or chronic alcoholism.

Cases of high anion gap metabolic acidosis (HAGMA) due to 5-oxoproline (pyroglutamic acid) accumulation have been reported in patients with severe underlying conditions such as severe renal impairment and sepsis, or in patients with poor nutrition and other causes of glutathione deficiency (e.g., chronic alcoholism), who were treated with paracetamol at therapeutic doses for prolonged periods or with a combination of paracetamol and flucloxacillin. If HAGMA due to pyroglutamic acidosis is suspected, immediate discontinuation of paracetamol is recommended, along with careful monitoring. Measurement of 5-oxoproline levels in urine may be useful in identifying pyroglutamic acidosis as the underlying cause of HAGMA in patients with multiple risk factors. Symptoms of metabolic acidosis include deep, rapid, or labored breathing, nausea, vomiting, and loss of appetite. Immediate medical attention should be sought if these symptoms occur.

If symptoms persist, medical advice should be sought.

One tablet contains 427 mg of sodium (854 mg sodium in two tablets), which should be considered by patients on a sodium-controlled diet. One tablet contains 59.9 mg of sorbitol (E 420). If a patient has been diagnosed with intolerance to certain sugars, medical advice should be sought before taking this medicinal product.

Keep the product out of the sight and reach of children.

Use during pregnancy or breastfeeding

Paracetamol crosses the placental barrier and is excreted in breast milk.

The use of this product during pregnancy or breastfeeding may be considered if the expected benefit to the mother outweighs the potential risk to the fetus or infant. Studies in humans and animals have not shown any risk to fetal development, the course of pregnancy, or breastfeeding. Extensive data from pregnant women do not indicate any teratogenic or fetal/neonatal toxicity. Epidemiological studies on neurodevelopment in children exposed to paracetamol in utero have not provided conclusive evidence. If clinically necessary, paracetamol may be used during pregnancy, but it should be administered at the lowest effective dose, for the shortest possible duration, and with the least possible frequency.

Effect on ability to drive or operate machinery

No effect.

Method of Administration and Dosage

The product is intended for oral administration.

Do not exceed the recommended dose. The lowest effective dose required to achieve therapeutic effect should be used.

Adults and children aged 12 years and older: Dissolve 1–2 tablets in half a glass of water and take every 4–6 hours as needed. The interval between doses should be at least 4 hours. Maximum daily dose – no more than 8 tablets within 24 hours.

The interval between doses should be at least 4 hours.

Do not take more than 8 tablets (4000 mg) within 24 hours.

Children (aged 6–11 years): Dissolve ½–1 tablet in half a glass of water. Take every 4–6 hours as needed.

The single dose of paracetamol is 10–15 mg/kg body weight; the maximum daily dose is 60 mg/kg body weight.

The maximum duration of use in children without medical consultation is 3 days.

Do not take more than 4 doses within 24 hours.

The interval between doses should be at least 4 hours.

Children.

Use in children under 6 years of age is not recommended.

Overdose.

Paracetamol overdose can cause liver failure, which may lead to liver transplantation or death. Liver damage may occur in adults who have ingested 10 g or more of paracetamol, and in children who have ingested more than 150 mg/kg body weight. In patients with risk factors (long-term treatment with carbamazepine, phenobarbital, phenytoin, primidone, rifampicin, St. John’s wort, or other drugs that induce liver enzymes; chronic excessive alcohol consumption; glutathione deficiency (malnutrition, cystic fibrosis, HIV infection, fasting, cachexia)), ingestion of 5 g or more of paracetamol may result in liver damage.

In case of overdose, prompt medical intervention is required. Treatment must be initiated immediately. The patient should be taken to hospital even if early symptoms of overdose are absent.

Symptoms within the first 24 hours: pallor, nausea, vomiting, loss of appetite, and abdominal pain. Liver damage may become apparent 12–48 hours after overdose. Glucose metabolism disturbances and metabolic acidosis may occur. In severe poisoning, liver failure may progress to encephalopathy, hemorrhage, hypoglycemia, coma, and may be fatal. Acute renal failure with acute tubular necrosis may present with severe flank pain, hematuria, proteinuria, and may develop even in the absence of severe liver damage. Cardiac arrhythmias and acute pancreatitis have also been reported, usually accompanied by liver function abnormalities and hepatotoxicity.

With prolonged use of the drug at high doses, hematological disorders such as aplastic anemia, pancytopenia, agranulocytosis, neutropenia, leukopenia, and thrombocytopenia may develop. High-dose intake may also lead to central nervous system effects such as dizziness, psychomotor agitation, and disorientation; urinary system effects may include nephrotoxicity (renal colic, interstitial nephritis, capillary necrosis).

Symptoms may be limited to nausea and vomiting or may not reflect the severity of overdose or risk of organ damage. Consider treatment with activated charcoal if an excessive dose of paracetamol was ingested within the past hour. Plasma paracetamol concentration should be measured at least 4 hours after ingestion (earlier concentrations are unreliable). Treatment with N-acetylcysteine may be administered within 24 hours of paracetamol ingestion, but maximum protective effect is achieved when administered within 8 hours of ingestion. The efficacy of the antidote decreases significantly after this time. If required, N-acetylcysteine should be administered intravenously according to current guidelines. In the absence of vomiting, oral methionine may be used as an appropriate alternative in remote areas outside hospital settings.

High doses of sodium bicarbonate may cause gastrointestinal symptoms such as belching and nausea. Furthermore, high doses of sodium bicarbonate may lead to hypernatremia; therefore, electrolyte levels should be monitored and appropriate supportive measures implemented.

Side effects

Blood and lymphatic system disorders: Rare (< 1/10000) – thrombocytopenia.

Immune system disorders: Rare – anaphylaxis, skin hypersensitivity reactions including skin rash, angioedema, Stevens-Johnson syndrome, and toxic epidermal necrolysis.

Respiratory, thoracic and mediastinal disorders: Rare – bronchospasm in patients sensitive to acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs.

Hepatobiliary disorders: Rare – liver function abnormalities.

Metabolism and nutrition disorders: Not known (cannot be estimated from available data) – metabolic acidosis with high anion gap.

Cases of metabolic acidosis with high anion gap, resulting from pyroglutamic acidosis, have been reported with the use of paracetamol in patients with risk factors (see section "Special precautions for use"). Pyroglutamic acidosis may occur due to low glutathione levels in these patients.

Other adverse reactions observed after administration of paracetamol-containing medicinal products include: pruritus; erythema multiforme; nausea; epigastric pain; hypoglycemia, up to hypoglycemic coma; agranulocytosis; anemia; sulfhemoglobinemia and methemoglobinemia (cyanosis, dyspnea, chest pain); hemolytic anemia; bruising or bleeding; increased liver enzyme activity, usually without development of jaundice.

Reporting of side effects

Reporting of suspected adverse reactions after medicinal product authorization is important. It allows ongoing monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals and patients, as well as their legal representatives, should report any suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.

Shelf life. 2 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach and sight of children.

Packaging.

Effervescent tablets № 12 (2x6) in a strip in a box.

Prescription status.

Over-the-counter.

Manufacturer.

CORPORATION "ZDOROV'YA" LIMITED LIABILITY COMPANY.

Manufacturer's address and place of business.

22, Shevchenka Street, Kharkiv, Kharkiv Oblast, 61013, Ukraine.