Paracetamol tablets 200mg №10×2

Name:
Paracetamol tab.
Description:
Pills of white or white color with a creamy tinge, flat-cylindrical, with a notch and a facet. Pharmacotherapeutic group Analgesics. Other analgesics-antipyretics. Anilides. Paracetamol ATC code N02BE01 Pharmacological properties Pharmacokinetics After oral administration, it is rapidly absorbed mainly in the small intestine, mainly by passive transport. After a single application at a dose of 500 mg, the maximum plasma concentration is reached after 0.5-2 hours and is about 16 μg / ml, after which it gradually decreases to a level of 11-12 μg / ml 6 hours after administration. With repeated administration of the drug, its pharmacokinetics do not change. Cumulation of the drug is not observed. In plasma, about 10-15% of the drug is in a protein-bound state. It penetrates well through histohematic barriers, evenly distributed over organs and tissues (with the exception of adipose tissue). Passes through the blood-brain barrier, the placenta, enters breast milk (less than 1% of the dose taken). The volume of distribution (Vd) is 0.95 l/kg. Metabolized in the liver in three independent ways: 1) conjugation with glucuronic acid (about 50%) with the formation of inactive metabolites; 2) conjugation with sulfates (about 30%) with the formation of inactive metabolites; 3) hydroxylation by the cytochrome P450 system with the formation of an active intermediate metabolite of N-acetyl-benzoiminoquinone (N-ABI about 17%). N-ABI further binds to glutathione and undergoes inactivation with the formation of paracetamol-mercaptopurate with the participation of mercaptopurine and cysteine. With a lack of glutathione, N-ABI can block the enzyme systems of hepatocytes and cause their necrosis. In premature infants, newborns and children under 10 years of age, the main metabolite of paracetamol is paracetamol sulfate, in children over 12 years of age, the main metabolite of paracetamol is glucuronide. The elimination half-life (T1 / 2) of paracetamol is 2-3 hours. In children, it is somewhat less, in newborns, the elderly and patients with impaired liver function, it is slightly longer. Excreted by the kidneys with urine, 30.5 – 58.5% as glucuronide, 17.5 – 33.9% – as sulfate, 4.5 – 6.1% – as paracetamol-mercaptopurate, 0.4 – 5 .9% – in the form of paracetamol-cysteine and 3.5 – 4.5% – unchanged. Excreted as metabolites in the urine. Pharmacodynamics Paracetamol has an analgesic and antipyretic effect. The mechanism of action is associated with inhibition of the activity of cyclooxygenase types I and II (COX-I and COX-II). As a result, the reactions of the arachidonic cascade of eicosanoid synthesis are blocked and the formation of prostaglandins PgE2, PgF2a, and their endoperoxides is disrupted. Paracetamol has an analgesic effect, increases the threshold of excitability of the pain centers of the thalamus. At the same time, it reduces the activity of the thermosetting center of the hypothalamus, the effect of endogenous pyrogens on it, and enhances heat transfer. It is effective for pain syndrome of low and moderate intensity, fever of infectious origin. It is used as an analgesic and antipyretic, primarily in people with contraindications to taking other non-steroidal anti-inflammatory drugs: patients with bronchial asthma, peptic ulcer, children with viral infections. The drug is devoid of anti-inflammatory action and does not have an antiplatelet effect. This is due to its inactivation in the focus of inflammation under the influence of oxygen peroxide and free radicals, which are formed in abundance in the focus of inflammation. Thus, in the area of inflammation, cyclooxygenase remains protected from the action of paracetamol and the anti-inflammatory effect does not develop. Paracetamol can be used in the treatment of pain in patients with disorders of the blood coagulation system (hemorrhagic diathesis, coagulopathy). Indications for use – moderate pain syndrome (including headache, migraine, neuralgia, toothache, sore throat, pain in osteoarthritis) – fever syndrome in acute infectious, infectious and inflammatory diseases. Method of application and doses For oral administration, 1-2 hours after a meal (taken immediately after a meal leads to a delay in the onset of action), drink plenty of liquid. This dosage form is not used in children under 6 years of age. Children 6-12 years: 200 – 400 mg (1 – 2 tablets) every 6 hours, the maximum daily dose is 1500 mg (weight up to 30 kg) or 2000 mg (weight up to 40 kg). Multiplicity of appointment – 3-4 times a day. The maximum duration of treatment when used as an analgesic and antipyretic is not more than 3 days. Do not exceed the indicated dose. In case of overdose, contact your doctor immediately, even if you feel well. Side effects – allergic reactions, skin rash, urticaria, angioedema, anaphylaxis, Stevens-Johnson syndrome – hepatotoxic effect with prolonged use – nausea, epigastric pain – hemolytic and aplastic anemia, thrombocytopenia, agranulocytosis, pancytopenia, methemoglobinemia – nephrotoxic effect in the form aseptic pyuria, interstitial nephritis, papillary necrosis – lowering blood pressure, hypoglycemia, dyspnea, vasculitis. Contraindications hypersensitivity to paracetamol or other components of the drug deficiency of glucose-6-phosphate dehydrogenase renal and hepatic insufficiency blood diseases pregnancy and lactation children under 6 years of age. Drug Interactions: With simultaneous use with cytochrome P450 inducers (phenytoin, alcohol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants, combined oral contraceptives), the production of hydroxylated toxic metabolite N-ABI and the risk of paracetamol hepatotoxicity increase. Alcohol also enhances the toxic effect of paracetamol on the pancreas and liver. With simultaneous use with inhibitors of cytochrome P450 (cimetidine, omeprazole, macrolide antibiotics), the risk of hepatotoxic action of paracetamol is reduced. When taken simultaneously with cholestyramine, cimetidine, omeprazole, the absorption rate of paracetamol decreases. Paracetamol can be used no earlier than one hour after the use of cholesterol, not earlier than two hours after the use of cimetidine, omeprazole. Paracetamol enhances the effect of agents that depress the central nervous system, potentiates the hematotoxic effect of chloramphenicol, weakens the effectiveness of uricosuric agents (sulfinpyrazone). With simultaneous use with myotropic antispasmodics (drotaverine, papaverine, pitophenone) and m-cholinergic blockers (fenpiverinium bromide, platifillin, atropine), there is a slowdown in the absorption of paracetamol, due to a slowdown in gastric emptying. With simultaneous use with prokinetic agents (metoclopramide), erythromycin, an acceleration of the absorption of paracetamol is observed, due to the acceleration of gastric emptying. Barbiturates weaken the antipyretic effect of paracetamol. The anticoagulant effect of warfarin and other coumarins may be increased with long-term regular use of paracetamol in patients with an increased risk of bleeding. Single doses do not have a significant anticoagulant effect. Simultaneous use with other drugs containing paracetamol is not recommended. Special instructions This dosage form is not intended for use in children under 6 years of age. Impact on laboratory parameters. During treatment with paracetamol, it is possible to increase the level of glucose in the blood plasma and distort the results of determining the glycemic profile. Pregnancy and lactation. The use of paracetamol during pregnancy and lactation is contraindicated. If it is necessary to use paracetamol during lactation, the child should be weaned from the breast for the entire period of treatment. The peculiarity of the effect of the drug on the ability to drive vehicles or potentially dangerous mechanisms Does not affect the ability to drive vehicles or potentially dangerous mechanisms. Overdose Occurs when paracetamol is taken at a dose of more than 10 g / day (or more than 140 mg / kg / day in children). In patients with alcoholism, hepatitis, the toxic effect of paracetamol can occur even when it is used at a dose of 2.5-4.0 g / day. Symptoms: there are 3 stages of development of intoxication. Stage 1 (12 – 24 hours) is characterized by dyspeptic symptoms, symptoms of irritation of the gastrointestinal tract, nausea, vomiting, sweating. Stage 2 (days 2–3) is characterized by nausea, vomiting, increased levels of transaminases, bilirubin, and an increase in the prothrombin index to 2.0–2.5. Stage 3 (3-5 days) is observed in 20% of persons with intoxication, characterized by deep progressive necrosis of hepatocytes, nausea, indomitable vomiting, jaundice, a sharp increase in transaminases, bilirubin, an increase in the prothrombin index of more than 2.5. There are signs of liver failure, hypoglycemia, encephalopathy, stupor, renal failure and myocardial dystrophy. Treatment: withdrawal of the drug, gastric lavage with activated charcoal, and the appointment of saline laxatives to prevent absorption of the drug in the stomach and intestines. Intravenously begin the introduction of glucose (5 – 10% solution of 200 – 400 ml). A specific antidote is introduced – N-acetylcysteine (restores glutathione reserves and eliminates its deficiency, while the toxic metabolite of paracetamol is neutralized). A 20% solution of N-acetylcysteine is used intravenously and orally: the first dose is 140 mg/kg (0.7 ml/kg), then 70 mg/kg (0.35 ml/kg). A total of 17 doses are administered. The most effective is the treatment started in the first 10 hours after the development of intoxication. If more than 36 hours have passed since intoxication, treatment is ineffective. With an increase in the prothrombin index of more than 1.5, vitamin K1 (phytomenadione) 1–10 mg is used; with an increase in the prothrombin index of more than 3.0, it is necessary to start intravenous administration of native plasma or a concentrate of coagulation factors (1–2 units). In the treatment of intoxication, forced diuresis and hemodialysis are contraindicated. It is unacceptable to use antihistamines and glucocorticosteroids. Release form and packaging 10 tablets in a contoured non-celled package made of a combined material on a paper and cardboard basis. Contour non-cell packs, together with the appropriate number of instructions for medical use in the state and Russian languages, in a group pack. Storage conditions Store in a dry, dark place at a temperature not exceeding 25 ° C. Keep out of the reach of children! Shelf life 3 years Do not use after the expiration date. Terms of dispensing from pharmacies Without a prescription Buy Paracetamol tablets 200mg No. 10×2 Price for Paracetamol tablets 200 mg No. 10×2