Paracetamol, 100 ml

Pharmacological group: analgesic non-narcotic drug

Paracetamol has antipyretic and analgesic effects. Non narcotic analgesic, it blocks cyclooxygenase (COX) 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 COX, which explains the almost complete lack of anti-inflammatory effect. Since paracetamol has extremely little effect on the synthesis of prostaglandins in peripheral tissues, it does not change water-electrolyte metabolism and does not cause damage to the mucosa of the gastrointestinal tract.

Hence, paracetamol is particularly suitable for patients with a history of gastrointestinal disease (such as in patients with a history of gastrointestinal bleeding or in elderly patients) or in patients taking concomitant medications where inhibition of peripheral prostaglandins may be undesirable.

Indications

Used in children from 3 months to 12 years as:

If the temperature does not decrease, a doctor’s consultation is necessary.

Active ingredient

Composition

For 1 ml of oral solution:

the active ingredient:

paracetamol 25.0 mg;

excipients:

sucrose 300.0 mg;

propylene glycol 400.0 mg;

methylparahydroxybenzoate 0.8 mg;

citric acid 0.1 mg;

vanillin 1.0 mg;

purified water to 1.0 ml.

How to take, the dosage

For oral administration only, with plenty of fluid 1-2 hours after a meal.

Do not exceed the indicated dose.

The lowest dose necessary to achieve an effect should be taken. The interval between doses should be at least 4 hours.

The drug should not be taken at the same time as other paracetamol-containing medications.

In children aged from 2 months to 3 months. For symptomatic relief of postvaccination reactions, the single dose is 10-15 mg/kg. Use 1-2 times a day with an interval of at least 4 hours. If fever persists after the second dose of the drug, consult a physician. For all other indications use the drug in patients of this age category only on the doctor’s recommendation!

Children aged 3 months to 12 years. The maximum daily dose is 60 mg/kg divided into several doses of 10-15 mg/kg. A single daily dose should be taken 3-4 times a day with an interval of at least 4 hours. Take no more than four single doses in 24 hours. Do not exceed the indicated dose. Maximum duration of using the drug without consulting a physician is 3 days. If it is necessary to continue taking the drug for more than 3 days, a physician’s consultation is required.

Do not exceed the recommended dose! If there is no therapeutic effect, it is necessary to consult a physician.

Patients with impaired renal function

Patients with impaired renal function should consult a physician before taking paracetamol. The limitations associated with the use of paracetamol-containing medications in patients with impaired renal function are primarily related to the paracetamol content of the medication.

Patients with impaired liver function

Patients with impaired liver function should consult a physician before taking paracetamol. The limitations associated with the use of paracetamol-containing medications in patients with impaired liver function are primarily related to the paracetamol content of the medication.

Interaction

If you or your child are already taking other medicines, you should consult your doctor before starting to take paracetamol.

The inducers of microsomal liver enzymes or potentially hepatotoxic substances (e.g., alcohol, rifampicin, isoniazid, hypnotics and antiepileptics including phenobarbital, phenytoin and carbamazepine) increase the toxicity of paracetamol and can lead to liver damage even with non-toxic doses of paracetamol, so liver function should be monitored.

Phenytoin reduces the effectiveness of paracetamol; therefore, patients taking phenytoin should avoid frequent use of paracetamol, especially in high doses.

Decreases the effectiveness of uricosuric drugs.

Chloramphenicol. Paracetamol may increase the risk of elevated concentrations of chloramphenicol.

Zidovudine. Paracetamol may increase the risk of neutropenia; therefore, hematologic parameters should be monitored. Simultaneous use is possible only after consultation with a physician.

Probenecid. Probenecid almost halves the clearance of paracetamol, which requires reducing the dose of paracetamol.

Indirect anticoagulants

Multiple administration of paracetamol for more than 4 days increases the anticoagulant effect. The international normalized ratio (INR) should be monitored during and after concomitant use of paracetamol (especially in high doses and/or for prolonged periods of time) and coumarin derivatives. Irregular administration of paracetamol has no significant effect. Propantelin and other drugs that slow down the evacuation from the stomach decrease the rate of absorption of paracetamol, which may delay or reduce the onset of effect.

Methoclopramide and domperidone increase the rate of absorption of paracetamol and therefore the onset of analgesic and antipyretic effects.

Long-term use of barbiturates reduces the effectiveness of paracetamol. Ethanol promotes the development of acute pancreatitis.

Long-term concomitant use of paracetamol and other NSAIDs increases the risk of “analgesia”. NSAIDs increases the risk of developing “analgesic” nephropathy and renal papillary necrosis, the onset of terminal renal failure.

The simultaneous long-term prescription of paracetamol in high doses and salicylates increases the risk of developing kidney or bladder cancer. Diflunisal increases the plasma concentration of paracetamol by 50% – risk of hepatotoxicity.

Myelotoxic drugs increase the hematotoxicity of the drug.

Special Instructions

In case of continued febrile syndrome on the background of using paracetamol for more than 3 days and pain syndrome for more than 5 days, medical consultation is required.
The risk of liver damage increases in patients with alcoholic hepatosis. It distorts laboratory indices in quantitative determination of glucose and uric acid in plasma.

During long-term treatment it is necessary to monitor the picture of peripheral blood and functional state of the liver.

Children and adults who have chronic diseases.

The effect on the ability to drive and operate vehicles

There are no data on the effect of paracetamol on the ability to drive or operate other mechanisms. However, given the possible adverse reactions, caution is recommended when taking paracetamol to drive vehicles or operate other mechanisms.

Contraindications

Hypersensitivity to paracetamol or any other component of the drug in the history of:

– age less than 2 months;

– severe hepatic and renal impairment.

With caution:

Renal and hepatic insufficiency of mild to moderate severity, benign hyperbilirubinemia (including. Gilbert’s syndrome), enzyme deficiency of glucose-6-phosphate dehydrogenase, dehydration, hypovolemia, anorexia, bulimia and cachexia (insufficient glutathione reserve in the liver), viral hepatitis, alcoholic liver damage, alcoholism, pregnancy, breast-feeding, advanced age, young breast-feeding age (less than 3 months).

Before starting to take paracetamol, a doctor should be consulted.

Side effects

Blood and lymphatic system disorders

Heart and vascular disorders: Very rare: hypotension, decreased or increased prothrombin index.

Respiratory system, chest and mediastinum disorders: Very rare: bronchospasm (in patients with hypersensitivity to acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs).

Gastrointestinal disorders: Rare: abdominal pain, diarrhea, dyspepsia, bloating.

Liver and biliary tract disorders

Hepatotoxic and nephrotoxic effects are possible with prolonged use in high doses.

If any of the above side effects occur, discontinue the drug and see a physician immediately.

Overdose

Symptoms

The clinical picture of acute overdose develops within 24 hours after taking paracetamol. Gastrointestinal disorders (nausea, vomiting, decreased appetite, feeling of discomfort in the abdomen and (or) abdominal pain), pale skin. When administered to adults 7.5 g or more or children more than 140 mg/kg at a time, 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.

Ingestion of 5 g or more of paracetamol may lead to liver damage in the presence of risk factors (long-term treatment with carbamazepine, phenobarbital, phenytoin, primidone, rifampicin, St. John’s wort or other drugs that are inducers of microsomal liver enzymes; ethanol abuse, glutathione deficiency, digestive disorders, cystic fibrosis, HIV infection, starvation, cachexia). In 12-48 hours after paracetamol administration, increased activity of microsomal liver enzymes, lactate dehydrogenase, bilirubin concentration and decreased prothrombin content are noted. Clinical symptoms of liver damage appear 2 days after overdose of the drug and reach their maximum on the 4th-6th day.

In overdose intoxication is possible, especially in elderly patients, children, patients with liver diseases (caused by chronic alcoholism), in patients with nutritional disorders, as well as in patients taking inducers of microsomal liver enzymes, with lightning hepatitis, liver failure, cholestatic hepatitis, cytolytic hepatitis may develop, sometimes with fatal outcome. In severe cases of overdose as a result of liver failure may develop encephalopathy (brain dysfunction), cerebral edema, bleeding, hypoglycemia, up to death. Acute renal failure with acute tubular necrosis may develop, characterized by pain in the lumbar region, hematuria (blood or red blood cells in the urine), proteinuria (high protein content in the urine), while severe liver damage may be absent. There have been cases of abnormal heart rhythm and pancreatitis.

Treatment

Hospitalization immediately. If overdose is suspected, even if the first symptoms are not pronounced, the use of paracetamol should be stopped and medical attention should be sought immediately. Paracetamol plasma levels should be determined, but not earlier than 4 hours after overdose (earlier results are unreliable). Laboratory tests of microsomal liver enzyme activity should be performed at the beginning of treatment and then every 24 hours. Administration of SH-group donators and precursors of glutathione synthesis – methionine and acetylcysteine – is most effective in the first 8 hours.

Symptomatic treatment

In 1 hour after overdose it is recommended to wash the stomach and take enterosorbents (activated charcoal, etc.). In most cases, the activity of microsomal liver enzymes is normalized within 1-2 weeks. Liver transplantation may be needed in very severe cases. Administration of acetylcysteine within 24 hours of overdose. Maximum protective effect is provided during the first 8 hours after overdose, with time the effectiveness of the antidote decreases sharply.

If necessary, acetylcysteine is administered intravenously. In the absence of vomiting before the patient is admitted to the hospital, methionine may be used.

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 since its administration. Treatment of patients with severe liver dysfunction 24 hours after paracetamol ingestion should be done in conjunction with specialists from a toxicology center or a specialized department of liver disease.

Pregnancy use

There have been no animal or human studies that have shown any risk of using the drug in pregnant women or any harmful effects of the drug on the development of the embryo and fetus. Paracetamol can be used during pregnancy, but it is advisable to use the minimum effective dose and the shortest possible course.

Breast-feeding period

It penetrates into breast milk in small amounts. Studies have not found harmful effects of paracetamol on the baby during breastfeeding, however, it is necessary to use with caution.

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