Composition
Active ingredient: Metamizole sodium-0.5 g, Excipients: potato starch-0.0334 g, sucrose (sugar) – 0.0055 g, calcium stearate-0.0028 g, stearic acid-0.0028 g, talc – 0.0055 g
Pharmacological action
Pharmacotherapeutic group: Analgesic non-narcotic mediatx: N. 02. B. B. 02 Metamizole Natria Pharmacodynamics :
Metamizole sodium, a non-narcotic analgesic derived from pyrazolone, non-selectively blocks cyclooxygenase and reduces the formation of prostaglandins from arachidonic acid.
It interferes with pain extra-and proprioceptive impulses along the Gaulle and Burdach bundles, increases the excitability threshold of the thalamic centers of pain sensitivity, and increases heat transfer.
A distinctive feature is the insignificant severity of the anti-inflammatory effect, which causes a weak effect on water-salt metabolism (retention of sodium and water ions) and the mucous membrane of the gastrointestinal tract. It has analgesic, antipyretic and some antispasmodic (in relation to the smooth muscles of the urinary and biliary tract) effect. The effect develops in 20-40 minutes after taking the drug and reaches a maximum in 2 hours.
Pharmacokinetics: The maximum plasma concentration is reached 1-1.5 hours after oral use. In the intestinal wall, it is hydrolyzed to form an active metabolite. Unchanged metamizole sodium is absent in the blood. The binding of the active metabolite to proteins is 50-60%. Excretion of metabolites passes through the kidneys. In addition, metabolites are excreted in breast milk.
Indications
Febrile syndrome in infectious and inflammatory diseases, insect bites, post-transfusion complications.
Pain syndrome (mild to moderate): including neuralgia, myalgia, biliary colic, renal colic, postoperative pain syndrome, headache, toothache, algodismenorrhea.
Use during pregnancy and lactation
Contraindicated.
Contraindications
Hypersensitivity to the components of the drug, inhibition of hematopoiesis (agranulocytosis, cytostatic or infectious neutropenia), hepatic and/or renal failure, hereditary hemolytic anemia associated with glucose-6-phosphate dehydrogenase deficiency, sucrose/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption, bronchial asthma induced by taking the drug acetylsalicylic acid, salicylates or other nonsteroidal anti-inflammatory drugs, anemia, leukopenia, pregnancy, lactation, age up to 8 years.
With caution:
Kidney diseases (pyelonephritis, glomerulonephritis, including in the anamnesis), alcoholism, predisposition to the development of arterial hypotension.
Side effects
From the urinary system: impaired renal function, oliguria, anuria, proteinuria, interstitial nephritis, urine staining in red.
Allergic reactions: urticaria (including on the conjunctiva and nasopharyngeal mucosa), angioedema, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), bronchospastic syndrome, anaphylactic shock.
Hematopoietic disorders: agranulocytosis, leukopenia, thrombocytopenia.
Other: lowering blood pressure.
Interaction
Radiopaque drugs, colloidal blood substitutes and penicillin should not be used during treatment with metamizole sodium. With simultaneous use of cyclosporine, the concentration of the latter in the blood decreases.
Metamizole sodium displaces oral hypoglycemic drugs, indirect anticoagulants, glucocorticosteroids and Indometacin from plasma protein binding and increases their activity.
Phenylbutazone, barbiturates and other inducers of microsomal liver enzymes with simultaneous use reduce the effectiveness of metamizole sodium.
Concomitant use with other non-narcotic analgesics, tricyclic antidepressants, contraceptive hormone medications, and allopurinol may lead to increased toxicity.
Metamizole sodium enhances the effects of ethanol; concomitant use with chlorpromazine or phenothiazine may lead to severe hyperthermia.
Sedative and anxiolytic drugs (tranquilizers) enhance the analgesic effect of metamizole sodium
Thiamazole and cytostatics increase the risk of leukopenia.
The effect is enhanced by codeine, H2-histamine receptor blockers and propranolol (slows down inactivation).
Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.
How to take, course of use and dosage
Inside.
The maximum single dose is 1 g, the daily dose is 3 g.
For children from 8 years to 14 years, the recommended dose is 250 mg, for children from 15 years and adults – 250-500 mg, the frequency of use is 2-3 times a day.
The duration of admission without consulting a doctor is not more than 5 days.
Overdose
Symptoms: Â nausea, vomiting, epigastric pain, oliguria, hypothermia, decreased blood pressure, tachycardia, shortness of breath, tinnitus, drowsiness, delirium, impaired consciousness, acute agranulocytosis, hemorrhagic syndrome, acute renal and/or liver failure, convulsions, paralysis of the respiratory muscles.
Treatment: gastric lavage, saline laxatives, activated charcoal; forced diuresis, hemodialysis, with the development of convulsive syndrome – intravenous use of diazepam and fast-acting barbiturates.
Special instructions
In the treatment of patients receiving cytostatic drugs, metamizole sodium should be administered only under the supervision of a doctor.
Patients with atopic bronchial asthma and hay fever have an increased risk of developing allergic reactions.
While taking metamizole sodium, agranulocytosis may develop, and therefore, if an unmotivated fever, chills, sore throat, difficulty swallowing, stomatitis is detected, as well as with the development of vaginitis or proctitis, the drug should be immediately discontinued.
With prolonged use, it is necessary to monitor the picture of peripheral blood.
It should not be used to relieve acute abdominal pain (until the cause is determined).
Form of production
Tablets,500 mg.
Storage conditions
Keep out of the reach of children in a dark place, at a temperature not exceeding 25 °C.
Shelf
life is 5 years.
Do not use after the expiration date.
Active ingredient
Metamizole sodium
Dosage form
Tablets
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