Paracetamol

General characteristics. Structure:

Active ingredient: 500 mg of paracetamol.

Excipients: potato starch, stearic acid, povidone low-molecular, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Paracetamol possesses anesthetic and febrifugal action. Paracetamol blocks cyclooxygenase I and II only in TsNS, influencing the centers of pain and thermal control (in the inflamed fabrics cellular peroxidases neutralize influence of paracetamol on cyclooxygenase) that explains almost total absence of antiinflammatory effect.

Lack of 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 mucous a GIT. The possibility of formation of a methemoglobin – is improbable.

Indications to use:

Moderately or poorly expressed pain syndrome (head, tooth, migrenozny pain, neuralgia, a mialgiya).

The increased body temperature at catarrhal and other infectious and inflammatory diseases.

Route of administration and doses:

Apply inside with a large amount of liquid 0,5 g-1 of 2-3 times in bucketed days not less than 4 hours. The maximum single dose for adults and teenagers is more senior than 12 years (body weight more than 40 kg) makes 1 g, daily – 4 g.

At patients with abnormal liver functions or kidneys, with Gilbert's syndrome and at elderly patients the interval between administrations of drug has to make not less than 8 hours and the daily dose has to be reduced.

To children appoint at the rate of 10-15 mg/kg of body weight 3-4 times a day. The maximum daily dose for children from 8 to 9 years (body weight is up to 30 kg) – 1,5 g, up to 12 years (body weight is up to 40 kg) – 2 g.

Duration of reception is no more than 5 days at appointment as anesthetic and 3 days as an antipyretic.

Features of use:

Distorts indicators of laboratory researches at quantitative determination of content of uric acid in plasma.

In order to avoid toxic damage of a liver paracetamol should not be combined with reception of alcoholic beverages, and also to accept to the persons inclined to chronic consumption of alcohol.

The risk of development of injuries of a liver increases at patients with an alcoholic hepatosis.

At long use of drug control of a picture of peripheral blood and a functional condition of a liver is necessary.

Side effects:

- Nausea, vomiting, pain in epigastriums, allergic reactions (skin rash, an itch, a small tortoiseshell, a Quincke's edema).
- Seldom – anemia, a leukopenia, thrombocytopenia, an agranulocytosis.

Interaction with other medicines:

Stimulators of a microsomal oxidation in a liver (Phenytoinum, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants), ethanol and hepatotoxic medicines increase products of hydroxylated active metabolites that causes a possibility of development of heavy intoxications at small overdoses. Long use of barbiturates reduces efficiency of paracetamol.

Ethanol promotes development of acute pancreatitis. Inhibitors of a microsomal oxidation (including Cimetidinum) reduce risk of a hepatotoxic action. Long sharing of paracetamol, etc. NPVP increases risk of development of an "analgetic" nephropathy and renal papillary necrosis, approach of an end-stage of a renal failure.

Simultaneous long purpose of paracetamol in high doses and salicylates increases risk of development of cancer of kidney or bladder. The accompanying use of paracetamol in high doses increases effect of anticoagulants (decrease in synthesis of procoagulant factors in a liver).

Diflunisal increases concentration in a paracetamol blood plasma for 50% – the risk of development of a hepatotoxic increases.

Reduces efficiency of uricosuric drugs.

Contraindications:

• Hypersensitivity to paracetamol.
• Children's age up to 8 years.

With care – a renal and liver failure, high-quality hyperbilirubinemias (including Gilbert's syndrome), a viral hepatitis, alcoholic damage of a liver), alcoholism, pregnancy, the lactation period, advanced age, deficit glyukozo-6-fosfatdegidrogenazy.

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 with the progressing encephalopathy, a coma, death; an acute renal failure with a tubular necrosis (including in the absence of severe damage of a liver); arrhythmia, pancreatitis. The hepatotoxic effect at adults is shown at reception of 10 g and more.

Treatment: introduction of donators of SH-group and predecessors of synthesis of glutathione – methionine in 8-9 h after overdose and N-Acetylcysteinum – in 12 h. Need for holding additional therapeutic actions (further administration of methionine, in/in introduction of N-Acetylcysteinum) is defined depending on concentration of paracetamol in blood, and also from time which passed after its reception.

Storage conditions:

Period of validity - 3 years. Not to use drug after expiry date. To store in the dry, protected from light place, at a temperature not above 25 °C. To store in the place unavailable to children!

Issue conditions:

Without recipe

Packaging:

Tablets on 500 mg. 10 tablets in a planimetric bezjyacheykovy or strip packaging; on 30 tablets in glass jars of the BS-T or BTS type or banks polymeric. Each can or 1, 2, 3 blister strip packagings together with the application instruction in a pack. On 450 planimetric bezjyacheykovy packagings with the equal number of application instructions in group packaging.