Paracetamol

General characteristics. Structure:

Active agent: paracetamol - 2,4 g. Excipients: methylparahydroxybenzoate (нипагин or methylparaben), sorbitol liquid, глицерол (the glycerin distilled), gum xanthane, dye an azoruby (acid red 2C), fragrance strawberry (fragrance food "Strawberry"), sucrose (refined sugar), the water purified - to 100 ml.

Pharmacological properties:

Non-narcotic analgesic, blocks (TsOG) 1 and TsOG 2 cyclooxygenase preferential in the central nervous system, influencing the centers of pain and thermal control. In the inflamed fabrics cellular peroxidases neutralize influence of paracetamol on TsOG that explains almost total absence of antiinflammatory effect. Lack of the blocking influence on synthesis of prostaglandins in peripheral fabrics causes absence at it negative influence on a water salt metabolism (a delay of sodium and water) and a mucous membrane of digestive tract. 

Pharmacokinetics. Absorption - high, time of achievement of the maximum concentration (TCmax) - 0.5-2 h; the maximum concentration (Cmax) - 5-20 mkg/ml. Communication with proteins of plasma - 15%. Gets through a blood-brain barrier. Therapeutic effective concentration of paracetamol in plasma is reached at its appointment in a dose of 10-15 mg/kg. It is metabolized in a liver (90-95%): 80% enter conjugation tests with glucuronic acid and sulfates with formation of inactive metabolites; 17% are exposed to a hydroxylation with formation of 8 active metabolites which conjugate with glutathione with formation of already inactive metabolites. At a lack of glutathione these metabolites can block fermental systems of hepatocytes and cause their necrosis. CYP2E1 isoenzyme also participates in drug metabolism. An elimination half-life (T1/2) - 1-4 h. Only 3% in not changed look are removed by kidneys in the form of metabolites, preferential conjugates.

Indications to use:

Apply at children of 1 month (at children of 1-3 months use according to all indications is possible only to destination the pediatrician) in quality:
- an antipyretic - at acute respiratory diseases, flu and children's infectious diseases (chicken pox, epidemic parotitis (mumps), measles, a rubella, scarlet fever);
- the anesthetizing (analgeziruyushchy) means - at a pain syndrome of weak and moderate intensity, including: head and a dentagra, a mialgiya, an arthralgia, an ear-ache at otitis, at a pharyngalgia, neuralgia, pain at injuries and burns.

Route of administration and doses:

Inside, to food in not divorced look, washing down with water, 3-4 times a day with an interval of 4-6 h. Before the use contents of a bottle should be shaken up well. For convenience and the accuracy of dosing we recommend to use a bilateral spoon: the big spoon contains 5 ml (120 mg of paracetamol), small - 2,5 ml (60 mg of paracetamol), or the spoon having two tags: lower corresponds to 2,5 ml (60 mg of paracetamol) and upper - 5 ml (120 mg of paracetamol). The dose of drug depends on age and the body weight of the child. The single dose of drug makes 10-15 mg/kg of body weight. The maximum daily dose - no more than 60 mg/kg of body weight of the child. Depending on age drug is appointed in the following single doses: from 1 to 3 month - about 2 ml of suspension (about 50 mg of paracetamol), from 3 months to 1 year - 2,5-5 ml of suspension (60-120 mg of paracetamol), from 1 year to 6 years - 5-10 ml of suspension (120-240 mg of paracetamol), from 6 to 14 years - 10-20 ml of suspension (240-480 mg of paracetamol).
The maximum duration of treatment without consultation of the doctor no more than 3 days as an antipyretic and no more than 5 days - as anesthetic.

Treatment continuation by drug after consultation with the doctor.

Features of use:

It is necessary to avoid simultaneous use of paracetamol with others paracetamol - the containing drugs as it can cause paracetamol overdose.
At the proceeding feverish syndrome against the background of paracetamol use more than 3 days and a pain syndrome more than 5 days, consultation of the doctor is required.
Distorts indicators of laboratory researches at quantitative definition of glucose and uric acid in plasma.
During prolonged treatment control of a picture of peripheral blood and a functional condition of a liver is necessary.
The risk of development of injuries of a liver increases at patients with an alcoholic liver disease. The concomitant use with ethanol is not recommended.
Suspension contains 0,04 XE sucrose in 1 ml that should be considered at treatment of patients with a diabetes mellitus.

Side effects:

Allergic reactions (including skin rash).

Interaction with other medicines:

Reduces efficiency of uricosuric medicines.
The accompanying use of paracetamol in high doses increases effect of anticoagulating medicines (decrease in synthesis of procoagulant factors in a liver).
Inductors of a microsomal oxidation in a liver (Phenytoinum, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants), ethanol and hepatotoxic medicines increase products of hydroxylated active metabolites that causes a possibility of development of heavy intoxications even at small overdose.
Ethanol promotes development of acute pancreatitis.
Inhibitors of a microsomal oxidation (including Cimetidinum) reduce risk of a hepatotoxic action.
Simultaneous long purpose of paracetamol in high doses and salicylates increases risk of development of cancer of kidney or bladder.
Long use of barbiturates reduces efficiency of paracetamol.
Long sharing of paracetamol and other nonsteroid antiinflammatory drugs increases risk of development of an "analgetic" nephropathy and renal papillary necrosis, approach of an end-stage of a renal failure.
Diflunisal increases plasma concentration of paracetamol for 50% - risk of development of a hepatotoxic.
Myelotoxic medicines strengthen manifestations of a gematotoksichnost of drug.

Contraindications:

- hypersensitivity to paracetamol or other components of drug;
- the expressed disturbances of functions of a liver and kidneys;
- diseases of system of blood;
- genetic absence glyukozo-6-fosfatdegidrogenazy;
- the neonatality period (up to 1 month).

Overdose:

Symptoms: during the first 24 h after reception - pallor of integuments, nausea, vomiting, anorexia, abdominal pain; glucose metabolism disturbance, metabolic acidosis. Symptoms of an abnormal liver function can appear in 12-48 h after overdose. At heavy overdose - a liver failure from a progression-ruyushchey encephalopathy, a coma, death; an acute renal failure with a tubular necrosis (including in the absence of severe damage of a liver); arrhythmia, pancreatitis.
Treatment: a gastric lavage no later than in 4 h after poisoning, reception of adsorbents (absorbent carbon, Polyphepanum (a lignin hydrolytic)). Introduction of donators of SH-group and predecessors of synthesis of glutathione - methionine in 8-9 h after overdose and Acetylcysteinum - in 12 h. Need for holding additional therapeutic actions (further administration of methionine, intravenous administration of Acetylcysteinum) is defined depending on concentration of paracetamol in blood, and also from time which passed after its reception.

Storage conditions:

In the place protected from light at a temperature not above 25 °C. Not to freeze. To store in the places unavailable to children. 
Period of validity 2 years. Not to use after expiry date.

Issue conditions:

Without recipe

Packaging:

Suspension children's 120/mg/5ml 100 g фл.