Pain of various origins of high intensity, fever, when the use of other drugs is contraindicated or ineffective.
Composition:
1 tabl contains 500 mg of sodium metamizol.
Action:
Metamizole sodium is a pyrazolone derivative with analgesic and antipyretic effect and weak spasmolytic activity. It inhibits the synthesis of prostaglandins by inhibiting the activity of the cyclooxygenase enzyme. Metamizole stimulates the release of beta-endorphin, lowers the level of endogenous pyrogens and has a direct impact on the thermoregulation center in the hypothalamus. Following oral administration, metamizole is rapidly hydrolyzed to the active metabolite 4-MAA and 4-aminoanthythmine (AA). AA is absorbed quickly and completely. The maximum concentration occurs after 1 to 2 h after administration. The MAA bioavailability is 90%. Metamizol metabolites bind to proteins at 50-60%, penetrate the blood-placenta barrier. Metamizole is extensively metabolised in the body. It is excreted in the urine mainly as metabolites. Only 3% of metamizol is excreted unchanged. Metamizol metabolites are also secreted into breast milk. Elimination of 4-MAA decreased by 22% after repeated administration of metamizol, and in elderly patients by 33%. In patients with kidney disease, clearance of 4-MAA remained unchanged, although the excretion of 4-FAA and 4-AcAA metabolites was clearly reduced. In cirrhotic patients, the excretion of all metabolites was lower. T0,5 active metabolite MAA in patients with hepatic impairment is about 3 times extended.
Contraindications:
Hypersensitivity to metamizol sodium or other pyrazolone derivatives, or to any of the excipients. Asthma triggered or exacerbated by NSAIDs. Hypersensitivity reactions to any NSAIDs or analgesics, in particular manifested by angioneurotic edema, urticaria, rhinitis. acute hepatic porphyria. Congenital deficiency of glucose-6-phosphate dehydrogenase. Severe hepatic and / or renal failure. Haematological diseases, including aplastic anemia, agranulocytosis and leukopenia. Pregnancy and lactation. Children and adolescents under 18 years of age.
Precautions:
Metamizole is only allowed in the short term and only if the benefit of this medicine outweighs the risk of side effects or other analgesics are ineffective or contraindicated. Discontinue treatment with agranulocytosis symptoms: fever, sore throat / larynx, swallowing pain, stomatitis, rhinitis, oral mucositis, inflammation of the genital and anal region; a blood count should be performed. In the case of long-term treatment, regular monitoring of blood counts is required, including changes in the number of white blood cells (increased risk of agranulocytosis). Special care should be taken in patients with bronchial asthma, in particular if accompanied by polypoid rhinitis and sinusitis, and with allergic diseases, hypersensitivity to other preparations and food (increased risk of hypersensitivity reactions and asthma attacks); with hypotension, dehydrated, in whom the volume of blood has decreased and in patients with heart failure (risk of hypotensive reaction); in patients with impaired renal or hepatic function and in peptic ulcer of the stomach and duodenum. If combined with alcohol, the risk of serious side effects increases. The drug contains wheat starch, which may contain gluten, but only in trace amounts, therefore it is believed that it can be used in people with celiac disease.
Pregnancy and lactation:
The use of the drug during pregnancy and during breast-feeding is contraindicated. The use of metamizol during pregnancy increases the incidence of Wilms' tumor in offspring and the risk of narrowing of the ductus arteriosus. If the drug is clearly indicated, breast-feeding should be discontinued for the duration of treatment.
Side effects:
Uncommon: drug eruption.Rare: leukopenia; maculopapular rash, anaphylactic reaction (pruritus, urticaria, general or local edema, erythema, angioneurotic edema, vasomotor disorders, bronchospasm, arrhythmia, drop in blood pressure sometimes preceded by its height) or anaphylactic shock (may occur especially after administration of large metamizole doses for patients with hypersensitivity or after parenteral administration). Very rare: agranulocytosis (risk of agranulocytosis is increased in patients taking the drug over a long time - over 1 week), thrombocytopenia, haemolytic anemia, aplastic anemia; asthma attack (in patients with Aspirin asthma syndrome), Stevens-Johnson syndrome, toxic epidermal necrolysis; proteinuria, oliguria, anuria, polyuria, interstitial nephritis. Frequency unknown: nausea, vomiting, abdominal pain, in large doses, bloody vomiting, blood in the stool (tarry stools).
Dosage:
Orally. Adults: 250 mg - 500 mg 2 to 3 times a day. The maximum single dose of 1 g. The maximum daily dose of 3 g. For patients with impaired liver function or mild and moderate renal impairment, it is recommended to use 1/2 dose for adults. Treatment can not last longer than 3 to 5 days. The drug should be used preferably after a meal.
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