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

Paracetamol has an analgesic and antipyretic effect. The drug blocks cyclooxygenase I and II mainly in the central nervous system, affecting the centers of pain and thermoregulation. In inflammatory tissues, cellular peroxidases neutralize the effect of paracetamol on cyclooxygenase,which explains the almost complete absence of anti-inflammatory effect. The drug has no adverse effect on water-salt metabolism (sodium and water retention) and gastrointestinal mucosa due to the lack of influence on the synthesis of prostaglandins in peripheral tissues.

Pharmacokinetics:

Absorption is high; The time required to reach the maximum concentration is reached after 0.5-2 h; the maximum concentration is 5-20 μg / ml. Connection with plasma proteins - 15%. Penetrates through the blood-brain barrier. Less than 1% of the dose of paracetamol taken by the lactating mother penetrates into breast milk. The therapeutically effective concentration of paracetamol in plasma is achieved when it is administered at a dose of 10-15 mg / kg. Metabolised in the liver (90-95%); 80% enters the conjugation reaction with glucuronic acid and sulfates with the formation of inactive metabolites; 17% is subjected to hydroxylation with the formation of 8 active metabolites, which are conjugated with glutathione with the formation of already inactive metabolites. With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis.In the metabolism of the drug is also involved isoenzyme CYP2E1. Half-life is 1-4 hours. It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% in unchanged form. In elderly patients paracetamol clearance decreases and the half-life period increases.

Indications:

Feverish syndrome on the background of infectious diseases; pain syndrome (mild and moderate): arthralgia, myalgia, neuralgia, migraine, dental and headache, algodismenorea.

Contraindications:Hypersensitivity, children under 6 years.

Carefully:

Renal and hepatic insufficiency, benign hyperbilirubinemia (including Gilbert's syndrome), viral hepatitis, alcoholic liver damage, alcoholism, pregnancy, lactation period, elderly age.

Pregnancy and lactation:

Penetrates through the placental barrier. To date, there has been no adverse effect of paracetamol on the fetus in humans. It is excreted in breast milk: the content in milk is 0.04-0.23 % dose, taken by the mother. If paracetamol is needed during pregnancy and lactation (breastfeeding), the expected benefit of therapy for the mother and the potential risk to the fetus or child should be carefully weighed.

Dosing and Administration:

Inside, with a lot of fluid, 1 to 2 hours after eating (reception immediately after eating leads to a delay in the onset of action).

Adults and adolescents older than 12 years (body weight over 40 kg) single dose - 500 mg; the maximum single dose is 1 g. The multiplicity of the destination is up to 4 times a day. The maximum daily dose is 4 g.

Children: the maximum daily dose for children 6-9 years (up to 30 kg) - 1.5 g, 9-12 years (up to 40 kg) - 2 g.

The maximum duration of treatment without consulting a doctor is 3 days (when taken as an antipyretic drug) and 5 days (as analgesic).

Side effects:Possible nausea, epigastric pain, allergic reactions in the form of skin rash, itching, urticaria, Quincke edema, anemia, thrombocytopenia, methemoglobinemia. With prolonged use in high doses, hepatotoxic and nephrotoxic effects are possible.

Overdose:Symptoms: during the first 24 hours after admission - 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 nekrose (including in the absence of severe liver damage); arrhythmia, pancreatitis. Hepatotoxic effect in adults is manifested when taking 10 g or more.

Treatment: introduction of donators SH- groups and precursors of the synthesis of glutathione - methionine after 8-9 h after an overdose and N-acetylcysteine for 8 hours. The need for additional therapeutic measures (further introduction of methionine, intravenous administration N-acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration.

Interaction:

Reduces the effectiveness of uricosuric medicines. The concomitant use of paracetamol in high doses increases the effect of anticoagulant drugs (a decrease in the synthesis of procoagulant factors in the liver).

Inductors of microsomal liver enzymes (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants), ethanol and hepatotoxic drugs increase the production of hydroxylated active metabolites, which makes it possible to develop severe intoxication even with a slight overdose.

Long-term use of barbiturates reduces the effectiveness of paracetamol.

Ethanol promotes the development of acute pancreatitis.

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

Long-term combined use of paracetamol and other non-steroidal anti-inflammatory drugs increases the risk of developing "analgesic" nephropathy and renal papillary necrosis, the onset of the terminal stage of renal failure. Simultaneous long-term use 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% - the risk of developing hepatotoxicity.

Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

Special instructions:

With continued febrile syndrome in the presence of paracetamol for more than 3 days and pain syndrome for more than 5 days, a doctor's consultation is required. The risk of liver damage increases in patients with alcoholic liver disease.

Distorts the indicators of laboratory studies in the quantitative determination of glucose and uric acid in plasma.

During long-term treatment, monitoring of the peripheral blood pattern and the functional state of the liver is necessary. Simultaneous reception with ethanol is not recommended.

Effect on the ability to drive transp. cf. and fur:

Studies have not been conducted.

Form release / dosage:Tablets of 0.5 g.

Packaging:10 tablets per contour cell packaging. 1 or 2 contour cellsPacking with instructions for usein a cardboard box.

10 tablets per contour non-jam packedforging. 500 contour non-jammed packages withthe same number of instructions for use in a group package (for a hospital).

Storage conditions:

Store in a dark place at a temperature not exceeding 30 ⁰ FROM.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LS-001990

Date of registration:23.01.2012

The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia

Manufacturer: & nbsp

ORGANICS, JSC Russia

Information update date: & nbsp02.10.2015

Illustrated instructions

Instructions

Paracetamol (Paracetamol)