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

Non-narcotic analgesic, has antipyretic and analgesic effect, blocking cyclooxygenases 1 and 2 (COX1 and COX2) mainly in the central nervous system. In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on COX, which explains the almost complete absence of anti-inflammatory effect.Does not have a negative effect on the mucosa of the gastrointestinal tract (GIT) and water-salt metabolism (delay Na + and water), since it does not affect the synthesis of prostaglandins in peripheral tissues.

Pharmacokinetics:

The drug is quickly and almost completely absorbed from the digestive tract. The maximum concentration in plasma (TCmax) is reached after 30-120 minutes. Connection with plasma proteins - 15%. Penetrates through the placental and blood-brain barrier (BBB). 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% undergoes 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. The half-life (T1 / 2) is 1-4 hours.It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% unchanged. In elderly patients, the clearance of the drug decreases and T1 / 2 increases.

Indications:

Applied in children from 3 months in quality:

antipyretic - with acute respiratory infections, influenza and children's infectious diseases (chicken pox, mumps, mumps, rubella, scarlet fever, etc.), accompanied by an increase in body temperature,

anesthetic for pain of mild to moderate severity - with headache and toothache, pain in the ears, including with teething, myalgia, neuralgia, migraine.

Contraindications:

Hypersensitivity, the period of newborns (up to 1 month).

Carefully:

Renal and hepatic insufficiency, benign Hyperbilirubinemia (including Gilbert's syndrome), viral hepatitis, alcoholic liver damage, pregnancy, lactation, elderly age, early infancy (1-3 months), diabetes mellitus.

Dosing and Administration:

Inside, with a lot of liquid, 1-2 hours after eating (taking immediately after a meal leads to a delay in the onset of action).

1 measuring spoon or 1 measuring cup contains 5 ml of syrup.

The dose of the drug depends on the age and body weight of the child.

The maximum daily dose for children 1-6 months (up to 7 kg) is 350 mg (14 ml), from 6 months to 1 year (up to 10 kg) - 500 mg (20 ml), 1-3 years (up to 15 kg) - 750 mg (30 ml), 3-6 years (up to 22 kg) - 1 g (40 ml), 6-9 years (up to 30 kg) -1.5 g (60 ml), 9-12 years (up to 40 kg ) - 2 g (80 ml). The dose for children between the ages of 1 and 3 months is determined individually. Multiplicity of destination - 4 times a day; the interval between each reception is not less than 4 hours.

Adults and adolescents over 12 years of age receive a single dose of 500 mg; the maximum single dose -1 g. The multiplicity of the appointment - up to 4 times a day. The maximum daily dose is 4 g; the maximum duration of treatment is 5-7 days.

The maximum duration of treatment without consulting a doctor is 3 days as an antipyretic and 5 days as an analgesic. In the absence of therapeutic effect, a doctor's consultation is mandatory.

Side effects:

Allergic reactions (including skin rash).

Overdose:

Symptoms: During the first 24 hours after taking - nausea, vomiting, stomach pain, pale skin, sweating, anorexia, a violation of glucose metabolism, metabolic acidosis. 12-48 hours after an overdose, there are signs of liver damage - soreness in the liver, increased activity of hepatic enzymes in the blood, increased prothrombin time.With prolonged use with excess of the recommended dose, liver failure, hepatonecrosis, encephalopathy can develop. Hepatotoxic effect in adults is manifested when taking 10 g or more.

Treatment: If symptoms of poisoning appear, stop using the drug and consult a doctor immediately. It is recommended the introduction of donators SH-groups and precursors of glutathione-methionine synthesis 8-9 h after overdose and acetylcysteine after 12 h. The need for additional therapeutic measures (further introduction of methionine, iv injection of acetylcysteine) is determined depending on the concentration of paracetamol in the blood, and from the time that has elapsed since it was received.

Interaction:

Reduces the effectiveness of uricosuric medicines.

The concomitant use of paracetamol in high doses increases the effect of anticoagulant drugs.

In patients taking barbiturates, tricyclic antidepressants, alcohol, anticonvulsant drugs, rifampicin, much increases risk development of hepatotoxic effects of paracetamol.

Inhibitors of microsomal oxidation (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 the nephrotoxic effect of the drug increases.

Simultaneous long-term administration 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 agents 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 hepatosis.

Distorts the indicators of laboratory research in quantifying 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.

Form release / dosage:

Syrup 125 mg / 5 ml.

Packaging:

Syrup for oral intake of 50 ml or 100 ml in bottles of dark color from polyethylene terephthalate or glass. Each bottle is placed along with the instructions for use, a measuring spoon for 5 ml or a measuring cup of 5 ml into individual cardboard packs.

Storage conditions:

Store in a dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

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

Terms of leave from pharmacies:Without recipe

Registration number:LSR-009401/09

Date of registration:23.11.2009

The owner of the registration certificate:ROSFARM, LLC ROSFARM, LLC Russia

Manufacturer: & nbsp

ROSFARM, LLC Russia

Information update date: & nbsp04.10.2015

Illustrated instructions

Instructions

Paracetamol (Paracetamol)