Analgin (tablets 0,5 g)

Tabulettae Analgini 0,5

International nonproprietary name

Metamizole sodium.antifebrile

Metamizole Sodium.

Pharmacotherapeutic group

Not narcotic analgesics, including NSAID.

Composition of the preparation

1 tablet contains 500 mg of Analgin

Pharmacological action

Pharmacodynamics

Analgin has anti-inflammatory, analgesic, antifebrile action. Inhibits the activity of cyclooxygenase, reduces formation of endoperoxides, bradykinins, some of prostaglandins, free radicals, inhibits peroxidation oxidation of lipids. Prevents from conduction of painful extra-and proprioceptive impulses through Gaulle’s fascicles and Burdach's columns, increases excitability threshold of the thalamic centers of painful sensitivity, increasesemission of heat. Action develops in 20-40 mines and reaches its maximum in 2 h.

Pharmakokinetics

At intake the preparation is quickly and fully absorbed. It is hydrolyzed in intestine wall with formation of active metabolite - not changed Metamizol is absent in blood. The active metabolite - 4-methyl-amino-antipyrine is in turn metabolized in 4-formyl-amino-antipyrin and other metabolites. The level of active metabolite binding with proteins is 50-60 %. Metabolites are eliminated with urine, and also with breast milk.

Indications 

Preparation is indicated at arthralgia, rheumatism, chorea , pains: head, dental, menstrual, neuralgia, ischialgia, myalgia, at colics (renal, hepatic, intestinal), pulmonary infarction, myocardial infarction, aortadissecting aneurysm, thrombosis of main vessels, inflammatory processes (pleuritis, pneumonia, lumbago, myocarditis), traumas, burns, decompression   sickness, shingles, tumors, orchitis, pancreatitis, peritonitis, perforation of esophagus, pheumothorax, posttransfusion complications, priapism. It is administrated also at feverish syndrome at acute infectious, purulent and urological diseases (prostatitis), insect stings (mosquitoes, bees, gadflies, etc.).

Dosage and method of administration 

It should be administrated per orally, after meal per 250-500 mg 2-3 times a day. The maximal single dose is 1 g, daily dose is 3 g. For children should be administrated in a single dose of 5-10 mg/kg. A usual dose for children of 2-3 years old is 50-100 mg, 4-5 years is 100-200 mg, 6-7 years is 200 mg, 8-14 years is 250-300 mg 2-3 times a day.

Special indications

It should be administrated to children in the age under 3 with extra care.

It is necessary to control a peripheric blood picture at long administration.

At administration of Analgin red color of urine is possible due to elimination of the metabolite.

Side effects

Granulocytopenia, agranulocytosis, thrombocytopenia, hemorrhages, hypotension, interstitial nephritis, allergic reactions (including Stevens-Johnson's and Layell’s syndromes,  bronchospasm, anaphylactic shock).

Contraindications

Hypersensitivity (including to pyrazolone derivatives), depression of hemopoiesis (agranulocytosis, cytostatic or infectious neutropenia), serious failures of liver or kidneys function, prostaglandin bronchial asthma, hereditary hemolytic anemia associated with glucose 6-phosphate dehydrogenase deficiency, pregnancy, breast feeding (for the period of treatment should be withdrawn).

Safety measures

Intake of the preparation is necessary to carry out under the control of the doctor. Regular long-term intake is not recommended owing to myelotoxicity. It is excluded for use for relief of acute abdominal pains (before reasonclarification). At administration to patients with acute cardiovascular pathology the careful control over hemodynamics is necessary. With care should be administrated in patients with ABP level BP below 100 mm Hg, with anamnestic indications on kidneys diseases (pyelonephritis, glomerulonephritis) and at long-term alcoholic anamnesis.

Interactions with other medicinal preparations

The effect of Analgin is increased by barbiturates, Codeine, histaminic Н2-blockers, Propranolol (slows down an inactivation). The Sarcolysine and Mercazolil  increase probability of leukopenia development. Hypoglycemic activity of peroral antidiabetic preparations is raised (released from binding with blood proteins), increase sedative activity of alcohol, reduces concentration of cyclosporine in plasma. Simultaneous administration of the preparation with other analgetics - antipyretics, NSAID can lead to mutual intensifying of toxic effects. Tricyclic  antidepressants, peroral contraceptives, Allopyrinol disturb metabolism and increase toxicity of the preparation. Sedatives and tranquilizers strengthenanalgesic action of Analgin. Caffeine strengthens action of the preparation.

Overdosage

Signs:hypothermia, expressed hypotension, palpitation, breathlessness, tinnitus, nausea, vomiting, fatigue, sleepiness, delirium, impairment of consciousness, convulsive syndrome; development of acute agranulocytosis, hemorrhagic syndrome, acute renal and hepatic failure is possible.

Treatment:induction of vomiting, pump gastric lavage, administration of saline laxatives, activated coal and artificial diuresis carrying out, blood alkalescence, symptomatic therapy directed on the vital functions maintenance.

The form of release

500 mg tablets. 10 tablets in a blister; 20 tablets in a vial.