Composition, form of production and packaging
? The tablets, covered with a film shell of white color, capsular form with a flat edge, on one side of the tablet by the method of stamping are marked with a triangular sign, on the other side - with a risk.
paracetamol 500 mg
Excipients: corn starch - 21.4 mg, pregelatinized starch - 50 mg, potassium sorbate - 0.6 mg, povidone - 2 mg, talc - 15 mg, stearic acid - 5 mg, triacetin - 0.83 mg, hypromellose - 4.17 mg.
6 pcs. - blisters (2) - packs of cardboard.
12 pcs. - blisters (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
Analgetic-antipyretic. Has analgesic and antipyretic effect. It blocks COX-1 and COX-2 mainly in the central nervous system, affecting the centers of pain and thermoregulation.
The anti-inflammatory effect is practically absent. Does not cause irritation of the stomach and intestinal mucosa. Has no effect on water-salt metabolism, since it does not affect the synthesis of prostaglandins in peripheral tissues.
Suction and distribution
Absorption is high, C max is achieved in 0.5-2 hours and is 5-20 Ојg / ml.
Connection with plasma proteins - 15%. Penetrates through the 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.
Metabolism and excretion
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. The isozyme CYP 2E1 also participates in the metabolism of the drug.
T 1/2 - 1-4 hours. It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% unchanged.
Pharmacokinetics in special clinical cases
In elderly patients the clearance of the drug decreases and T 1/2 increases.
- Pain syndrome: headache, migraine, toothache, sore throat, back pain, muscle pain, painful menstruation;
- febrile syndrome (as an antipyretic agent): increased body temperature against the background of colds and flu.
The drug is designed to reduce pain at the time of use and the progression of the disease is not affected.
Adults (including the elderly) the drug prescribed 500 mg-1 g (1-2 tab.) Up to 4 times / day, if necessary. The interval between doses is not less than 4 hours, a single dose (2 tablets) can be taken no more often than 4 times (8 tab.) Within 24 hours.
Children aged 6-9 years are prescribed 1/2 tablet. 3-4 times / day, if necessary. The interval between doses is at least 4 hours. The maximum single dose for children 6-9 years is 1/2 table. (250 mg), the maximum daily - 2 tab. (1 g).
Children aged 9-12 years are prescribed 1 tab. up to 4 times / day, if necessary. The interval between doses is not less than 4 hours, a single dose (1 tab.) Can be taken no more often than 4 times (4 tab.) Within 24 hours.
The drug is not recommended for more than 5 days as an anesthetic and for more than 3 days of an antipyretic agent without prescribing and monitoring the doctor.An increase in the daily dose of the drug or the duration of treatment is possible only under the supervision of a physician.
In recommended doses, the drug is usually well tolerated.
Allergic reactions: sometimes - rashes on the skin, itching, swelling of Quincke.
From the hemopoietic system: rarely - anemia, thrombocytopenia, methemoglobinemia.
On the part of the urinary system: with prolonged use in high doses - renal colic, nonspecific bacteriuria, interstitial nephritis, papillary necrosis.
- children's age till 6 years;
- Hypersensitivity to the components of the drug.
With caution should be used in patients with renal and hepatic insufficiency, benign hyperbilirubinemia (including Gilbert's syndrome), viral hepatitis, glucose-6-phosphate dehydrogenase deficiency, alcoholic liver damage, alcoholism, in old age, during pregnancy and lactation.
PREGNANCY AND LACTATION
With caution and only under the supervision of a doctor, the drug should be used during pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Caution should be used in cases of kidney failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution , use the drug for liver failure.
APPLICATION FOR CHILDREN
Contraindication: children under 6 years.
APPLICATION IN ELDERLY PATIENTS
Caution should be applied to the drug in the elderly.
With prolonged use in high doses, blood control is necessary.
With caution and only under the supervision of a doctor, the drug should be used for liver or kidney disease, while taking antiemetics (metoclopramide, domperidone), as well as drugs that lower blood cholesterol (colestyramine).
In the case of a daily need for taking analgesics while taking anticoagulants, paracetamol can be taken occasionally.
When performing tests for determining uric acid and blood glucose levels, a doctor should be warned about taking Panadol.
To avoid toxic damage to the liver, paracetamol should not be combined with the intake of alcoholic beverages, and should also be taken to persons prone to chronic alcohol consumption.
The drug should be taken only at recommended doses. If the recommended dose is exceeded, you should immediately seek medical help, even if you are feeling well, since there is a risk of delayed serious liver damage.
Is liver damage in adults possible with admission? 10 g of paracetamol. Reception? 5 g of paracetamol can lead to liver damage in patients who have the following risk factors:
- long-term treatment with carbamazepine, phenobarbital, phenytoin, primidone, rifampicin, preparations of St. John's wort perfumed or other drugs that stimulate liver enzymes;
- regular consumption of alcohol in excess quantities;
- possibly having glutathione deficiency (for eating disorders, cystic fibrosis, HIV infection, fasting and starvation).
Symptoms of acute paracetamol poisoning are nausea, vomiting, stomach pain, sweating, pale skin. After 1-2 days, signs of liver damage are determined (tenderness in the liver, 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 coma can develop. Hepatotoxic effect in adults manifested during admission? 10 g of paracetamol.
Treatment: discontinue use and consult a doctor immediately. It is recommended to wash the stomach and receive enterosorbents (activated charcoal, polyphepan);introduction of donors of SH-groups and precursors of glutathione-methionine synthesis 8-9 hours after overdose and N-acetylcysteine вЂ‹вЂ‹after 12 hours. The need for additional therapeutic measures (further introduction of methionine, iv administration of N-acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as the time elapsed after its administration. Treatment of patients with severe impairment of liver function 24 hours after taking paracetamol should be done in conjunction with specialists from the toxicology center or specialized department of liver diseases.
Prolonged sharing of paracetamol and other NSAIDs increases the risk of developing "analgesic" nephropathy and renal papillary necrosis, the onset of the terminal stage of renal failure.
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 hepatotoxicity.
Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.
The drug, when taken for a long time, increases the effect of indirect anticoagulants (warfarin and other coumarins), which increases the risk of bleeding.
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 effects in overdoses.
Inhibitors of microsomal oxidation (cimetidine) reduce the risk of hepatotoxic effects.
Metoclopramide and domperidone are increased, and colestramine reduces the rate of absorption of paracetamol.
Ethanol with simultaneous application with paracetamol promotes the development of acute pancreatitis.
The drug may reduce the activity of uricosuric drugs.
TERMS OF RELEASE FROM PHARMACY
The drug is approved for use as a means of OTC.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 5 years.