Paracetamol - instructions for use, dose, side effects, contraindications

Excipients: potato starch, croscarmellose sodium (croscarmellose sodium), povidone (polyvinylpyrrolidone low molecular weight medical), stearic acid, talc.

Description:

Tablets white or white with a creamy shade of color,

flat cylindrical with risk

Pharmacotherapeutic group:analgesic non-narcotic remedy

ATX: & nbsp

N.02.B.E Anilides

N.02.B.E.01 Paracetamol

Pharmacodynamics:

Paracetamol has an analgesic and antipyretic effect.

The drug blocks cyclooxygenase 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 the absence of a significant anti-inflammatory effect. The drug does not adversely affect the water-salt metabolism and mucosa of the gastrointestinal tract.

Pharmacokinetics:

Absorption - high, maximum concentration (С_mOh) is 5-20 μg / ml, the time to reach the maximum concentration (T_max) - 0.5-2 hours; communication with plasma proteins - 15%. The therapeutically effective concentration of paracetamol in plasma is achieved when it is administered at a dose of 10-15 mg / kg.

Penetrates through the blood-brain barrier. 1-2% of the dose of the medication taken by the mother penetrates into the breast milk.

Metabolised in the liver: 80% enters the conjugation reaction with glucuronic acid and sulfates with the formation of inactive metabolites, 17% undergoes hydroxylation with the formation of 8 active metabolites, which are conjugated with glutathione and form inactive metabolites. With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. The half-life (T1 / 2) is 1-4 hours.Primarily excreted by the kidneys in the form of metabolites - glucuronides and sulfates, 3% - unchanged.

In elderly patients there is a decrease in clearance of the drug and an increase in T1 / 2.

Indications:

Pain syndrome of mild and moderate intensity (arthralgia, myalgia, neuralgia, migraine, dental and headache, algodismenorea), fever in infectious and inflammatory diseases (including viral infections).

Contraindications:

- individual hypersensitivity to the components of the drug;

- Children under 6 years of age (for this dosage form).

Carefully:

Renal and hepatic insufficiency, viral hepatitis, alcoholic liver damage, alcoholism, benign hyperbilirubinemia (Gilbert syndrome, Dubin-Johnson syndrome and Rotor syndrome), glycose-6-phosphate dehydrogenase deficiency, elderly age, pregnancy, lactation.

Pregnancy and lactation:

Paracetamol penetrates the placenta, when taken in therapeutic doses, the drug is safe for the fetus, so it is necessary to strictly follow the dosing regimen.

When breastfeeding, the concentration in the mother's milk is low (1-2% of the maternal dose).Adverse effects on infants are not documented. Application is possible with strict adherence to the dosing regimen.

Dosing and Administration:

Inside, before meals or 1-2 hours after eating, squeezed large amounts of liquid.

Adults and teenagers over 12 years of age (body weight more than 40 kg) single dose - 500 mg; the maximum single dose is 1 g. The maximum daily dose is 4 g.

Children the dose of paracetamol is calculated depending on the age and body weight.

Children aged 6-9 years (weight up to 30 kg): single dose - 250 mg (1/2 tablet); the maximum daily dose is 1 g; at the age of 9-12 years (weight from 30 to 40 kg): a single dose of 250-500 mg (1/2 tablet - 1 tablet), the maximum daily dose - 2 g (4 tablets).

Multiplicity of reception no more than 4 times a day with an interval of at least 4 hours.

In patients with impaired liver and kidney function, with benign hyperbilirubinemia and in the elderly, the daily dose should be reduced and the interval between doses should be increased.

Duration of treatment is no more than 3 days as an antipyretic agent and not more than 5 days as an anesthetic. Continuation of treatment with the drug is possible only after consulting a doctor!

Do not exceed the prescribed dose! Overdose of paracetamol can cause hepatic insufficiency.

Side effects:

Nausea, vomiting, abdominal pain.

Allergic reactions (skin rash, itching, urticaria, angioedema).

Rarely - leukopenia, agranulocytosis, thrombocytopenia.

With prolonged use in large doses - hepatotoxic and nephrotoxic (interstitial nephritis and papillary necrosis) action; hemolytic anemia, aplastic anemia, methemoglobinemia, pancytopenia.

Overdose:

Symptoms: pallor of the skin, nausea, vomiting, anorexia, abdominal pain; disturbance of glucose metabolism, metabolic acidosis. Symptoms of liver dysfunction may appear 12-48 hours after an overdose. In severe overdose - liver failure with progressive encephalopathy, coma, death; acute renal failure with tubular necrosis; arrhythmia, pancreatitis. Hepatotoxic effect in adults is manifested when taking 10 g or more.

Treatment: gastric lavage no later than 4 hours after poisoning, intake of adsorbents (Activated carbon). The introduction of methionine is important for 8-9 hours, acetylcysteine - for 8 hours. The need for additional therapeutic measures is determined independing on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration.

Interaction:

Inductors of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, flumecinol, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites, which makes it possible to develop severe intoxication with small overdoses.

Long-term use of barbiturates reduces the effectiveness of paracetamol. Simultaneous use with ethanol increases the risk of acute pancreatitis.

Inhibitors of microsomal oxidation (incl. cimetidine) reduce the risk of hepatotoxic effects.

When taken together with non-steroidal anti-inflammatory drugs, including salicylates, the nephrotoxic effect of paracetamol increases.

Diflunisal increases the plasma concentration of paracetamol by 50%, which increases the risk of hepatotoxicity.

Paracetamol increases the effect of anticoagulants of indirect action and reduces the effectiveness of uricosuric drugs.

Special instructions:

Paracetamol should not be used concomitantly with other paracetamol-containing drugs, as this can cause an overdose of paracetamol.

When using the drug for more than 5 days should monitor the peripheral blood and the functional state of the liver.

Paracetamol distorts the results of laboratory studies of glucose and uric acid in the blood plasma.

Form release / dosage:

Tablets 500 mg.

Packaging:

For 10 tablets in a contiguous cell-free or contiguous cell package.

1, 2, 3, 4 5 or contour of cellular packages with instructions for use in a pack of

cardboard.

Permissible metering contour and contour Valium packaging with an equal amount of instructions for use are placed in multipacks.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LS-001364

Date of registration:06.08.2010

The owner of the registration certificate:PHARMSTANDART-FORESTRY, OJSC PHARMSTANDART-FORESTRY, OJSC Russia

Manufacturer: & nbsp

PHARMSTANDART-FORESTRY, OJSC Russia

Information update date: & nbsp03.10.2015

Illustrated instructions

Instructions

Paracetamol (Paracetamol)