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

Paracetamol refers to analgesic non-narcotic drugs. It has analgesic, antipyretic and insignificant anti-inflammatory effect. The mechanism of action of the drug is associated with inhibition of the synthesis of prostaglandins, a predominant effect on the center of thermoregulation in the hypothalamus.

Pharmacokinetics:

After oral administration, it is rapidly absorbed from the gastrointestinal tract, reaching a maximum concentration after 20 - 60 minutes. The maximum concentration is 5-20 μg / ml. Connection with plasma proteins - 15%. Penetrates through blood-brain barrier, placental barriers, is found in breast milk (less than 1% of the dose of paracetamol taken by the mother feeding the mother). Therapeutically effective concentration; paracetamol in plasma is achieved with its administration in a dose of 10-15 mg / kg.

Metabolized by microsomal enzymes of the liver (90-95%). 80% enters the conjugation reaction with glucuronic acid and sulfates with the formation of inactive metabolites; 17% is subjected to hydroxylirobaia 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. It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% unchanged; the elimination half-life is 1-4 hours. In elderly patients, the clearance of the drug decreases and increases Tl / 2.

Indications:

Paracetamol is used for:

- removal of a moderately or mildly expressed pain syndrome (headache, dental, migraine pain, sore throat, neuralgia, myalgia);

- decrease in elevated body temperature for colds and other infectious and inflammatory diseases.

Paracetamol is intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected.

Contraindications:

- hypersensitivity to paracetamol;

- marked violations of the liver and kidneys;

- genetic absence of glucose-6-phosphate dehydrogenase;

- blood diseases;

- pregnancy and the period of breastfeeding;

- children under 3 years;

- bronhoobstruktsiya, rhinitis, urticaria, provoked by the use of acetylsalicylic acid or other NSAIDs (including in the anamnesis);

- condition after aorto-coronary bypass surgery;

- confirmed hyperkalemia;

- erosive and ulcerative changes in the mucous membrane of the stomach and duodenum;

- active gastrointestinal bleeding;

- inflammatory bowel disease.

Carefully:

- Gilbert's syndrome (constitutional hyperbilirubinemia);

- impaired liver and kidney function;

- cardiac ischemia;

- chronic heart failure;

- cerebrovascular diseases;

- dyslipidemia / hyperlipidemia;

- diabetes;

- diseases of peripheral arteries;

- smoking;

- creatinine clearance less than 60 ml / min;

- anamnestic data on the development of ulcerative lesions of the gastrointestinal tract;

- presence of infection H. Pylori;

- elderly age;

- long-term use of NSAIDs;

- frequent use of alcohol;

- severe physical illness;

- simultaneous administration of oral glucocorticosteroids (incl. prednisolone), anticoagulants (incl. warfarin), antiplatelet agents (incl. acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (incl. citalopram, fluoxetine, paroxetine, sertralia).

Dosing and Administration:

Paracetamol should be administered orally 0.2 or 0.5 g up to 4 times a day.

The maximum single dose for adults - 1 g, daily dose - 4 g. Duration of admission: as an antipyretic agent - no more than 3 days; as an analgesic - no more than 5 days. An increase in the daily dose of the drug or the duration of treatment is possible only under the supervision of a physician.

For children, 10-15 mg / kg body weight every 6 hours. The maximum daily dose for children under 6 years (up to 22 kg) - 1 g; up to 9 years (up to 30 kg) - 1.5 g; up to 12 years (up to 40 kg) - 2 g.

It is recommended that children use pediatric medicinal forms.

Side effects:

In therapeutic doses, the drug is usually well tolerated.

From the side of the digestive tract: with prolonged admission in high doses, hepatotoxic effect is possible.

On the part of the hematopoiesis system: in rare cases - thrombocytopenia, leukopenia, agranulocytosis.

From the excretory system: with prolonged admission in high doses, nephrotoxic effect is possible.

There may be allergic reactions from the skin or systemic.

Overdose:

Symptoms acute poisoning: nausea, vomiting, pain in the stomach, after a day - two determine signs of liver damage. Treatment: cancellation of the drug.

Symptoms of a severe overdose: hepatic insufficiency, encephalopathy, coma. Treatment: The sufferer should do a gastric lavage, prescribe adsorbents (Activated carbon) and see a doctor.

Interaction:

With the simultaneous use of the drug with inducers of microsomal liver enzymes (barbiturates, diphenin, carbamazepine, rifampicin, zidovudine and etc.) increases risk of hepatotoxic action

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

With simultaneous application of the drug reduces eEffectiveness of uricosuric LS.

With the simultaneous use in high doses of the drug strengthens effect of anticoagulant drugs (decreased synthesis of procoagulant factors in the liver).

Ethanol promotes the development of acute pancreatitis.

Long-term combined use of paracetamol and other NSAIDs enhances risk of developing "analgesic" nephropathy and renal papillary necrosis, the onset of the terminal stage of renal failure.

With simultaneous long-term use in high doses of the drug with salicylates increases risk of developing kidney or bladder cancer.

With the simultaneous use of diflunisal enhances plasma concentration of paracetamol by 50%, increasing the risk of hepatotoxicity.

With the simultaneous use of myelotoxic drugs reinforce manifestations of hematotoxicity of the drug.

Special instructions:

To avoid toxic damage to the liver paracetamol should not be combined with the reception of alcoholic beverages, but also to people prone to chronic alcohol consumption. 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.

Form release / dosage:Tablets of 0.2 g or 0.5 g.

Packaging:

10 tablets per contour cell pack.

For 10 tablets in a contour non-jawed package.

1,2,5,10 contour packs together with instructions for use are placed in a pack of cardboard.

Allowed contour packings together with an equal number of instructions for use put in a group package.

Storage conditions:

List B. In a dry, the 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 the product after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:P N002018 / 01

Date of registration:25.11.2008

The owner of the registration certificate:MEDISORB, CJSC MEDISORB, CJSC Russia

Manufacturer: & nbsp

MEDISORB, CJSC Russia

Information update date: & nbsp07.10.2015

Illustrated instructions

Instructions

Paracetamol MS (Paracetamol MS)