INSTRUCTION

for medical use of the drug

PARACETAMOL

 

Storage:

active substance: paracetamol;

1 tablet contains paracetamol 200 mg;

Excipients: potato starch, calcium stearate, colloidal anhydrous silica, hydroxypropylmethylcellulose.

Dosage form. Tablets.

Basic physical and chemical properties: solid regular, round cylinders, the upper and lower surfaces of which are flat, the edges of the surfaces are beveled, with a dash for separation, white or white with a creamy tinge.

Pharmacotherapeutic group.

Analgesics and antipyretics. Paracetamol. ATX code N02B E01.

Pharmacological properties.

Pharmacodynamics.

Paracetamol is a 4-hydroxyacetanilide, a non-narcotic, non-salicylate analgesic and antipyretic whose analgesic activity is associated with central and peripheral action. Increases the threshold of pain sensitivity, has a weak anti-inflammatory effect as a result of inhibition of prostaglandin synthesis and blocks impulses at bradykinin-sensitive receptors.

Pharmacokinetics.

The drug is rapidly and completely absorbed after oral administration. The maximum concentrations in blood plasma are registered in 15-60 minutes after its reception. Therapeutically effective concentration of paracetamol in blood plasma is reached at its appointment in a dose of 10-15 mg / kg. Paracetamol is metabolized in the liver mainly by conjugation reactions with sulfuric and glucuronic acids, with the formation of glucuronide and paracetamol sulfate. Paracetamol is excreted by the kidneys, less than 5% is excreted unchanged. The half-life after oral administration is approximately 1-4 hours. In severe renal insufficiency (creatinine clearance below 10 ml / min) excretion of paracetamol and its metabolites is slower.

Clinical characteristics.

Indication.

Headache, including migraine and tension headache; neuralgia; toothache; relief of cold and flu symptoms such as fever, aches, pain.

 

Contraindication.

Hypersensitivity to the components of the drug. Severe hepatic and / or renal impairment, congenital hyperbilirubinemia, glucose-6-phosphate dehydrogenase deficiency, alcoholism, blood diseases, severe anemia, leukopenia.

Interaction with other medicinal products and other forms of interaction.

At simultaneous appointment of barbiturates, anticonvulsants (antiepileptic) means, rifampicin, alcohol use the risk of hepatotoxic action considerably increases.

Paracetamol increases the effect of indirect anticoagulants (coumarin derivatives). Metoclopramide and domperidone increase, and cholestyramine - reduces the rate of absorption. Paracetamol should be used 1 hour before or 4-6 hours after taking cholestyramine. Barbiturates reduce antipyretic activity.

The anticoagulant effect of warfarin and other coumarins may be enhanced by concomitant long-term daily use of paracetamol, with an increased risk of bleeding. Periodic intake has no significant effect.

Anticonvulsants (including phenytoin, barbiturates, carbamazepine), which stimulate the activity of liver microsomal enzymes, may increase the toxic effects of paracetamol on the liver by increasing the rate of conversion of the drug to hepatotoxic metabolites. Concomitant use of paracetamol with hepatotoxic drugs increases the toxic effects of drugs on the liver.

Concomitant use of high doses of paracetamol with isoniazid increases the risk of hepatotoxic syndrome. Paracetamol reduces the effectiveness of diuretics.

Probenecid halves the clearance of paracetamol by blocking its binding to glucuronic acid, so the dose of paracetamol should be reduced when combined with probenecid.

Paracetamol should be used with caution with chloramphenicol due to the prolongation of the half-life and increase of the toxic effect of the latter.

 Features of application.

It is necessary to consult a doctor about the possibility of using the drug:

- patients with impaired renal and hepatic function;

- patients taking warfarin or similar drugs that have an anticoagulant effect;

- patients taking analgesics for mild arthritis;

- In patients with severe infections, such as sepsis, which are accompanied by a decrease in glutathione levels, paracetamol increases the risk of metabolic acidosis. Symptoms of metabolic acidosis are deep, rapid or difficult breathing, nausea, vomiting, loss of appetite. You should see a doctor immediately if you experience these symptoms;

- if the headache becomes permanent.

Keep in mind that patients with alcoholic liver disease increase the risk of hepatotoxic effects of paracetamol; the drug may affect the results of laboratory tests for blood glucose and uric acid.

If symptoms persist, consult a physician.

Use during pregnancy or breastfeeding.

The drug can be prescribed during pregnancy only if the expected benefit to the mother outweighs the potential risk to the fetus or child.

Paracetamol passes into breast milk, but in clinically insignificant amounts. Available published data do not contain contraindications to breastfeeding.

 

Ability to influence the speed of reaction when driving a car or other machinery.

Does not affect.

 

Method of application and dosage.

The drug is intended for oral administration.

Adults and children over 12 years of age: 2 tablets (400 mg) 3-4 times a day, with an interval between doses of at least 4 hours. Not more than 4000 mg in 24 hours.

Children (6-12 years): 1-2 tablets (200-400 mg) every 4-6 hours.

Do not take more than 20 tablets (4000 mg) in 24 hours.

Children aged 3-6 years: ½-1 tablet (100-200 mg) up to 4 times a day.

The interval between receptions makes not less than 4 hours.

The duration of treatment is determined by the doctor.

The maximum period of use without consulting a doctor - 3 days.

Do not exceed the recommended dose.

Do not take with other medicines containing paracetamol.

 

Children.

Not recommended for children under 3 years.

 

Overdose.

Liver damage is possible in adults who have taken 10 g or more of paracetamol and in children who have taken more than 150 mg / kg body weight. In patients with risk factors (long-term treatment with carbamazepine, phenobarbitone, phenytoin, primidone, rifampicin, St. John's wort or other drugs that induce liver enzymes; regular intake of excessive amounts of ethanol; glutathione cachexia (indigestion, infection, mucus, ) taking 5 g or more of paracetamol may cause liver damage.

Symptoms of overdose in the first 24 hours: paleness, nausea, vomiting, anorexia and abdominal pain. Liver damage may become apparent 12-48 hours after an overdose. Glucose metabolism disorders and metabolic acidosis may occur. With severe poisoning, liver failure can progress to encephalopathy, hemorrhage, hypoglycemia, coma, and death. Acute renal failure with acute tubular necrosis can be manifested by severe lumbar pain, hematuria, proteinuria and develop even in the absence of severe liver damage. Cardiac arrhythmia and pancreatitis were also noted.

 

With long-term use of the drug in large doses by hematopoietic organs may develop aplastic anemia, pancytopenia, agranulocytosis, neutropenia, leukopenia, thrombocytopenia. At reception of large doses from the central nervous system - dizziness, psychomotor excitement and disturbance of orientation; from the urinary system - nephrotoxicity (renal colic, interstitial nephritis, capillary necrosis).

In case of overdose, emergency medical care is required. The patient should be taken to a hospital immediately, even if there are no early symptoms of overdose. Symptoms may be limited to nausea and vomiting, or may not reflect the severity of the overdose or the risk of organ damage. Activated charcoal treatment should be considered if an overdose of paracetamol has been taken within 1 hour. Plasma concentrations of paracetamol should be measured 4 hours or later after ingestion (earlier concentrations are inaccurate). N-acetylcysteine ​​treatment can be used within 24 hours after taking paracetamol, but the maximum protective effect is obtained when using it within 8 hours after taking.

The effectiveness of the antidote decreases sharply after this time. If necessary, the patient is intravenously administered N-acetylcysteine ​​according to the established list of doses. In the absence of vomiting, methionine can be used orally as a suitable alternative in remote areas outside the hospital.

 

Adverse reactions.

Discontinue use of the drug and consult a doctor immediately in case of adverse reactions.

Adverse reactions to paracetamol are very rare (<1 10="" 000="" :="" p="">

- allergic reactions: anaphylaxis, itchy skin, rashes on the skin and mucous membranes (usually generalized rash, erythematous urticaria), angioneurotic edema, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic Lacrimal necrosis );

- from the digestive tract: 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 blood and lymphatic system: thrombocytopenia, agranulocytosis, anemia, sulfhemoglobinemia and methemoglobinemia (cyanosis, shortness of breath, heart pain), hemolytic anemia, bruising or bleeding;

 - Respiratory disorders: bronchospasm in patients sensitive to acetylsalicylic acid (aspirin) and other nonsteroidal anti-inflammatory drugs.

Expiration date.

3 years.

Storage conditions.

Store in the original package at a temperature not exceeding 25 ºC.

Keep out of reach of children.

Packaging.

Tablets № 10 in blisters.

Vacation category. No prescription.

Producer.

JSC "Lubnipharm".

Location of the manufacturer and address of the place of its activity.

Ukraine, 37500, Poltava region, Lubny, street Barvinkova, 16.