PANADOL PILLS 500MG

Mechanism of action

Analgesic antipyretic. It has an analgesic and antipyretic effect. Blocks COX-1 and COX-2 mainly in the central nervous system, affecting the centers of pain and thermoregulation.

Anti-inflammatory effect is practically absent. Does not cause irritation of the mucous membrane of the stomach and intestines. It does not affect the water-salt metabolism, since it does not affect the synthesis of prostaglandins in peripheral tissues.

Suction and distribution

Absorption - high, Cmax is achieved in 0.5-2 hours and amounts to 5-20 μg / ml.

Communication with plasma proteins - 15%. Penetrates the BBB. Less than 1% of the Paracetamol dose taken by the nursing mother passes into breast milk. A therapeutically effective concentration of paracetamol in plasma is achieved when it is administered at a dose of 10-15 mg / kg.

Metabolism and excretion

Metabolized in the liver (90-95%): 80% reacts conjugation 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 the hepatocytes and cause their necrosis. CYP 2E1 isoenzyme is also involved in the metabolism of the drug.

T1/2 - 1-4 hours. Excreted by the kidneys as metabolites, mainly conjugates, only 3% unchanged.

Pharmacokinetics in special clinical situations

In elderly patients, the clearance of the drug decreases and T increases.1/2.

Indications and usage

Symptomatic therapy:

- pain syndrome: headache, migraine, toothache, sore throat, back pain, muscle pain, painful menstruation;

- febrile syndrome (as a febrifuge): increased body temperature against the background of colds and flu.

The drug is designed to reduce pain at the time of use and does not affect the progression of the disease.

Adults (including the elderly) the drug is prescribed in 500 mg-1 g (1-2 tab.) up to 4 times / day, if necessary. The interval between doses - at least 4 hours, a single dose (2 tablets) can be taken no more than 4 times (8 tablets) within 24 hours.

Children aged 6-9 years appoint 1/2 tab. 3-4 times / day if necessary. The interval between doses - at least 4 hours. The maximum single dose for children 6-9 years old - 1/2 tab. (250 mg), the maximum daily - 2 tab. (1 g).

Children aged 9-12 years appoint 1 tab. up to 4 times / day, if necessary. The interval between doses - at least 4 hours, a single dose (1 tab.) Can be taken no more than 4 times (4 tab.) Within 24 hours.

The drug is not recommended to be used for more than 5 days as an anesthetic and more than 3 days of an antipyretic without prescription and observation by a doctor. Increasing the daily dose of the drug or the duration of treatment is possible only under medical supervision.

Adverse reactions

In recommended doses, the drug is usually well tolerated.

Allergic reactions: sometimes - a rash on the skin, itching, angioedema.

Hemic and lymphatic: rarely - anemia, thrombocytopenia, methemoglobinemia.

Urogenital: with prolonged use in high doses - renal colic, nonspecific bacteriuria, interstitial nephritis, papillary necrosis.

- children's age up to 6 years;

- hypersensitivity to the drug.

WITH caution the drug should be used for kidney and liver failure, benign hyperbilirubinemia (including Gilbert syndrome), viral hepatitis, glucose-6-phosphate dehydrogenase deficiency, alcoholic liver damage, alcoholism, old age, during pregnancy and lactation.

Pregnancy and Breastfeeding

With caution and only under the supervision of a physician should use the drug during pregnancy and lactation.

WITH caution should use the drug for liver failure.

WITH caution should use the drug for renal failure.

Use in children

Contraindications: children up to 6 years.

WITH caution should use the drug in old age.

Special notes

With long-term use in high doses, control of the blood picture is necessary.

With caution and only under the supervision of a physician should use the drug for diseases of the liver or kidneys, while taking antiemetic drugs (metoclopramide, domperidone), as well as drugs that lower cholesterol in the blood (colestiramine).

In the case of the daily need for taking analgesics while taking anticoagulants, paracetamol can be taken occasionally.

When conducting tests for the determination of uric acid and the level of glucose in the blood should warn the doctor about taking Panadol.

In order to avoid toxic damage to the liver, paracetamol should not be combined with the intake of alcoholic beverages, as well as be taken by persons prone to chronic alcohol consumption.

Overdosage

The drug should be taken only in recommended doses. If you exceed the recommended dose, you should immediately seek medical help, even with good health, as there is a risk of delayed serious damage to the liver.

Liver damage in adults is possible when taking ≥ 10 g of paracetamol. Taking ≥ 5 g of paracetamol may result in liver damage in patients who have the following risk factors:

- long-term treatment with Carbamazepine, phenobarbital, phenytoin, primidone, rifampicin, preparations of Hypericum perforatum or other drugs that stimulate liver enzymes;

- regular use of alcohol in excess;

- possibly having glutathione deficiency (in case of malnutrition, cystic fibrosis, HIV infection, fasting and starvation).

Symptoms acute paracetamol poisoning are nausea, vomiting, stomach pain, sweating, pallor of the skin. After 1-2 days, signs of liver damage are determined (pain in the liver area, increased activity of liver enzymes). In severe cases of overdose, liver failure develops, acute renal failure with tubular necrosis (including in the absence of severe liver damage), arrhythmia, pancreatitis, encephalopathy, and comatose state may develop. Hepatotoxic effect in adults appears when taking ≥ 10 g of paracetamol.

Treatment: stop using the drug and immediately consult a doctor. It is recommended gastric lavage and reception of enterosorbents (activated carbon, polyphepan); the introduction of SH-group donators and precursors of the synthesis of glutathione - methionine after 8-9 hours after overdose and N-acetylcysteine ​​- after 12 hours. The need for additional therapeutic measures (further introduction of methionine, IV the concentration of paracetamol in the blood, as well as the time elapsed after taking it. Treatment of patients with severe liver dysfunction 24 hours after taking paracetamol should be carried out in conjunction with experts from a poison control center or a specialized department of liver diseases.

Drug Interactions

Prolonged use of paracetamol and other NSAIDs increases the risk of developing "analgesic" nephropathy and renal papillary necrosis, the onset of end-stage renal failure.

The 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%, which increases the risk of developing hepatotoxicity.

Myelotoxic drugs increase the hematotoxicity of the drug.

The drug, when taken for a long time, enhances the effect of indirect anticoagulants (warfarin and other coumarins), which increases the risk of bleeding.

The inducers of microsomal oxidation enzymes in the liver (barbiturates, phenytoin, carbamazepine, rifampicin, zidovudine, phenytoin, ethanol, flumecinol, phenylbutazone, and tricyclic antidepressants) increase the risk of hepatotoxic action in overdose.

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

Metoclopramide and Domperidone increase, and Kolestiramin reduces the rate of absorption of paracetamol.

Ethanol with simultaneous use with paracetamol contributes to the development of acute pancreatitis.

The drug can reduce the activity of uricosuric drugs.

The drug should be stored out of the reach of children at a temperature not higher than 25 ° C.