Instructions for Paracetamol-Darnitsa tablets 500 mg No. 10
Composition
active ingredient: paracetamol;
1 tablet contains paracetamol 500 mg;
Excipients: pregelatinized starch, povidone, microcrystalline cellulose, croscarmellose sodium, calcium stearate.
Dosage form
Pills.
Main physicochemical properties: tablets of white or almost white color, flat-cylindrical shape, with a bevel and a score. A grayish tint is allowed.
Pharmacotherapeutic group
Analgesics and antipyretics. Anilides. Paracetamol. ATX code N02B E01.
Pharmacological properties
Pharmacodynamics
Non-narcotic analgesic. Non-selectively inhibits cyclooxygenase (COX), affecting the centers of pain and thermoregulation. In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on COX, which explains the insignificant anti-inflammatory effect. There is no effect on the synthesis of prostaglandins in peripheral tissues, which means that paracetamol does not have a negative effect on water-salt metabolism (sodium and water retention) and the mucous membrane of the gastrointestinal tract. The possibility of the formation of methemoglobin and sulfhemoglobin is unlikely.
Pharmacokinetics
Absorption is high, almost 100%. In the systemic bloodstream, 15% of the absorbed drug binds to plasma proteins. The time to reach maximum concentration in the blood (TCmax) is 20−30 minutes. Therapeutically effective concentration of paracetamol in blood plasma is achieved when administered at a dose of 10−15 mg/kg. Penetrates through the blood-brain barrier and into breast milk. The amount of the drug in breast milk is less than 1% of the dose of paracetamol taken by the nursing mother. Metabolized in the liver: 80% enters into conjugation reactions with glucuronic acid and sulfates with the formation of inactive metabolites. 17% of the drug undergoes hydroxylation with the formation of active metabolites, which conjugate with glutathione and form inactive metabolites. In case of glutathione deficiency, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. The half-life (T1/2) of paracetamol is 2−3 hours. In elderly patients, the clearance of the drug decreases and T1/2 increases. Excreted by the kidneys - 3% in unchanged form.
Indication
Headache, including migraine and tension headaches, toothache, backache, rheumatic pain, muscle pain, period pain in women, moderate arthritis pain; relief of fever and pain symptoms of colds and flu.
Contraindication
Hypersensitivity to the components of the drug, severe liver and/or kidney dysfunction, congenital hyperbilirubinemia, glucose-6-phosphate dehydrogenase deficiency, alcoholism, blood diseases, Gilbert's syndrome, severe anemia, leukopenia.
Interaction with other medicinal products and other types of interactions
The rate of absorption of paracetamol may be increased by metoclopramide and domperidone and decreased by cholestyramine.
Paracetamol should be taken 1 hour before or 4-6 hours after taking cholestyramine.
The anticoagulant effect of warfarin and other coumarins with an increased risk of bleeding may be enhanced by concomitant long-term use of paracetamol. Intermittent use has no significant effect.
Barbiturates reduce the antipyretic effect of paracetamol.
Anticonvulsants (including phenytoin, barbiturates, carbamazepine), which stimulate the activity of liver microsomal enzymes, may enhance the toxic effect of paracetamol on the liver due to an increase in the degree of conversion of the drug to hepatotoxic metabolites. With the simultaneous use of paracetamol with hepatotoxic drugs, the toxic effect of the drugs on the liver increases. The simultaneous use of large doses of paracetamol with isoniazid increases the risk of developing hepatotoxic syndrome.
Probenecid halves the clearance of paracetamol by blocking its binding to glucuronic acid, therefore, in case of combination therapy with probenecid, the dose of paracetamol should be reduced.
Paracetamol should be used with caution with chloramphenicol due to the prolongation of the half-life and increased toxicity of the latter.
Caution should be exercised when using paracetamol with flucloxacillin, as concomitant administration has been associated with high anion gap metabolic acidosis, especially in patients with risk factors.
Paracetamol reduces the effectiveness of diuretics.
Do not use simultaneously with alcohol.
Application features
Do not exceed the indicated doses. Do not take the drug with other products containing paracetamol - this may lead to overdose. Paracetamol overdose can cause liver failure, which may require a liver transplant or be fatal.
Cases of liver dysfunction/liver failure have been reported in patients with reduced glutathione levels, such as those with severe wasting, anorexia, low body mass index, chronic alcoholism, or sepsis.
It is necessary to consult a doctor regarding the possibility of using the drug:
– patients with impaired kidney and liver function;
– patients taking warfarin or similar drugs that have an anticoagulant effect;
– patients who use analgesics for mild arthritis;
− if the headache becomes permanent.
Patients with severe infections such as sepsis, which are accompanied by a decrease in glutathione levels, are at increased risk of metabolic acidosis when taking paracetamol. Symptoms of metabolic acidosis include deep, rapid or difficult breathing, nausea, vomiting, loss of appetite. If these symptoms occur, you should consult a doctor immediately.
Caution should be exercised when using paracetamol with flucloxacillin due to the increased risk of high anion gap metabolic acidosis, especially in patients with severe renal insufficiency, sepsis, malnutrition and other sources of glutathione deficiency (e.g. chronic alcoholism), as well as those taking maximum daily doses of paracetamol. Close monitoring, including measurement of urinary 5-oxoproline, is recommended.
The drug may affect the results of laboratory tests for blood glucose and uric acid.
During treatment with paracetamol, you should not drink alcoholic beverages.
If symptoms persist, you should consult a doctor.
Use during pregnancy or breastfeeding
Pregnancy. The drug can be prescribed during these periods only if the expected benefit to the mother outweighs the potential risk to the fetus or child.
As with all medicines, consult your doctor before taking paracetamol during pregnancy. A large amount of data on pregnant women indicate neither malformative nor feto/neonatal toxicity. Epidemiological studies on the development of the nervous system in children exposed to paracetamol in utero have not yielded conclusive results. If clinically necessary, paracetamol can be used during pregnancy, but it should be used at the lowest effective dose for the shortest duration and with the least possible frequency.
Breastfeeding: Paracetamol is excreted in breast milk, but in clinically insignificant amounts. Available published data do not indicate a contraindication to breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
Does not affect.
Method of administration and doses
The medicine is intended for oral administration.
Adults and children over 12 years of age: 1-2 tablets 4 times daily as needed. Do not take more than 8 tablets (4000 mg) in 24 hours.
Children (6-12 years): ½-1 tablet 3-4 times a day if necessary.
A single dose of paracetamol is 10-15 mg/kg body weight, the maximum daily dose is 60 mg/kg body weight. Do not take more than 4 doses within 24 hours.
The maximum period of use for children without consulting a doctor is 3 days.
The interval between doses is at least 4 hours.
Do not exceed the recommended dose.
Do not take with other medicines containing paracetamol.
Children
Do not use in children under 6 years of age.
Overdose
Paracetamol overdose can cause liver failure, which can lead to the need for liver transplantation or death. Clinical signs of liver damage after paracetamol overdose usually appear 24–48 hours after the overdose and reach a maximum after 4–6 days.
There is an increased risk of paracetamol poisoning, particularly in elderly patients, children, patients with liver disease, chronic alcoholism, and chronic malnutrition.
Liver damage is possible in adults who have taken 10 g or more of paracetamol, and in children who have taken more than 150 mg/kg of body weight. In patients with risk factors (long-term use of carbamazepine, phenobarbitone, phenytoin, primidone, rifampicin, St. John's wort or other drugs that induce liver enzymes; alcohol abuse; insufficiency of the glutathione system, for example: digestive disorders, cystic fibrosis, HIV infection, starvation, cachexia) taking 5 g or more of paracetamol can lead to liver damage.
Symptoms of overdose in the first 24 hours: pallor, nausea, vomiting, loss of appetite and abdominal pain, asymptomatic overdose is also possible.
Acute renal failure with acute tubular necrosis may present with severe back pain, hematuria, and proteinuria, and may occur even in the absence of severe liver damage. Cardiac arrhythmias and pancreatitis have also been reported.
With prolonged use of the drug in high doses, aplastic anemia, pancytopenia, agranulocytosis, neutropenia, leukopenia, thrombocytopenia may develop from the hematopoietic system. When taking large doses, dizziness, psychomotor agitation and disorientation are possible from the central nervous system; nephrotoxicity (renal colic, interstitial nephritis, capillary necrosis) is possible from the urinary system.
Treatment: In case of overdose, immediate medical attention is required. The patient should be taken to hospital immediately, even if there are no early symptoms of overdose, as liver damage may not develop immediately. Symptoms may be limited to nausea and vomiting and may not reflect the severity of the overdose or the risk of organ damage. Treatment with activated charcoal should be considered if an overdose of paracetamol has been taken within 1 hour. The concentration of paracetamol in the blood plasma should be measured 4 hours or later after ingestion (earlier concentrations are unreliable). Treatment with N-acetylcysteine can be used within 24 hours of paracetamol ingestion, but the maximum protective effect is obtained when it is used within 8 hours of ingestion. The effectiveness of the antidote decreases sharply after this time. If necessary, the patient should be given N-acetylcysteine intravenously according to current recommendations. In the absence of vomiting, oral methionine can be used as a suitable alternative in remote areas outside the hospital.
Symptomatic treatment is also necessary.
Adverse reactions
In case of adverse reactions, discontinue use of the drug and consult a doctor immediately.
Adverse reactions to paracetamol are rare (< 1/10,000):
Respiratory system: bronchospasm in patients sensitive to acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs.
Gastrointestinal: nausea, epigastric pain.
From the liver and biliary tract: impaired liver function, increased activity of liver enzymes, usually without the development of jaundice.
On the part of the endocrine system: hypoglycemia, up to hypoglycemic coma.
From the blood and lymphatic system: thrombocytopenia, agranulocytosis, anemia, sulfhemoglobinemia and methemoglobinemia (cyanosis, shortness of breath, heart pain), hemolytic anemia, bruising or bleeding.
On the part of the immune system: anaphylaxis, hypersensitivity reactions, including skin itching, rash on the skin and mucous membranes (usually generalized rash, erythematous rash, urticaria), angioedema, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).
Reporting of suspected adverse reactions.
Reporting suspected adverse reactions after the marketing authorisation of a medicinal product is an important procedure. It allows for continued monitoring of the benefit-risk balance of the medicinal product in question. Healthcare professionals should report any suspected adverse reactions via the national reporting system.
Expiration date
4 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
10 tablets in a blister pack; 1 blister pack in a pack; 10 tablets in blister packs.
Vacation category
Without a prescription - tablets No. 10.
Producer
PrJSC "Pharmaceutical Company "Darnitsa".
Location of the manufacturer and address of its place of business
Ukraine, 02093, Kyiv, Boryspilska St., 13.
