Metamizole sodium

Package leaflet (information for patients)

Tradename
Metamizole sodium

Dosage form
Injection 500mg / ml.

Description
Transparent liquid of light yellow color with a weak odor.

Structure
1 ml of solution contains:
Active ingredient: Metamizole sodium 500mg
Auxiliary components: ethyl oleate.

Pharmacotherapeutic group
Analgesic non-narcotic drug

Pharmacological properties
Analgesic antipyretic. Derived from pyrazolone. It has analgesic, antipyretic and anti-inflammatory effects, the mechanism of which is associated with inhibition of prostaglandin synthesis.
Pharmacokinetics
After oral administration, metamizole sodium is rapidly hydrolyzed in gastric juice with the formation of an active metabolite of 4-methyl-amino-antipyrine, which, after absorption, is metabolized to 4-formyl-amino- antipyrine and other metabolites.
After intravenous administration, metamizole sodium quickly becomes unavailable for determination.
Metamizole sodium metabolites do not bind to plasma proteins. Most of the dose is excreted in the urine in the form of metabolites. Metabolites are excreted in breast milk.

Indications for use
Arthralgia, rheumatism, chorea, pain: headache, dental, menstrual, neuralgia, sciatica, myalgia, with colic (renal, hepatic, intestinal), pulmonary infarction, myocardial infarction, dissecting aortic aneurysm, thrombosis of major pneumatic vessels, inflammatory processes (pleurisy, lumbago, myocarditis), trauma, burns, decompression sickness, shingles, tumors, orchitis, pancreatitis, peritonitis, esophageal perforation, pneumothorax, post-transfusion complications, priapism ; febrile syndrome in acute infectious, purulent and urological diseases (prostatitis), insect bites (including mosquitoes, bees, gadflies).

Method of administration and dosage
In / m, in / in, rectally. V / m or / in (with severe pain) - 1-2 ml of 50% or 25% solution 2-3 times / day, maximum daily dose 2 g; children are injected with 0.1-0.5 ml. Inside, after meals, or rectally, 250-500 mg 2-3 times / day, the maximum single dose is 1 g, the daily dose is 3 g. The usual dose for children 2-3 years old is 50-100 mg, 4-5 years old - 100-200 mg, 6-7 years old - 200 mg, 8-14 years old - 250-300 mg 2-3 times / day.

Side effects
From the urinary system: impaired renal function, oliguria, anuria, proteinuria, interstitial nephritis, urine staining red.
Allergic reactions: urticaria (including on the conjunctiva and mucous membranes of the nasopharynx), angioedema, in rare cases - malignant exudative erythema (Stevens- Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), bronchospastic shock, anaphylactic syndrome.
From the side of hematopoiesis: agranulocytosis, leukopenia, thrombocytopenia.
Others: decrease in blood pressure.
Local reactions: with intramuscular injection, infiltrates at the injection site are possible.
Overdose. Symptoms: nausea, vomiting, gastralgia, 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; carrying out forced diuresis, hemodialysis, with the development of convulsive syndrome - intravenous administration of diazepam and fast-acting barbiturates.

Contraindication
Hypersensitivity, inhibition of hematopoiesis (agranulocytosis, cytostatic or infectious neutropenia), hepatic and / or renal failure, hereditary hemolytic anemia associated with a deficiency of glucose-6-phosphate dehydrogenase, bronchial asthma induced by the intake of ASA, salicylates, anemia, or other NSAIDs. pregnancy (especially in the first trimester and in the last 6 weeks), lactation.
Carefully. Infants up to 3 months of age, kidney disease (pyelonephritis, glomerulonephritis - including a history), long-term ethanol abuse. Intravenous administration to patients with systolic blood pressure below 100 mm Hg. or with circulatory instability (for example, against the background of myocardial infarction, multiple trauma, incipient shock).

Overdose
Symptoms: hypothermia, severe hypotension, palpitations, shortness of breath, tinnitus, nausea, vomiting, weakness, drowsiness, delirium, impaired consciousness, convulsive syndrome; development of acute agranulocytosis, hemorrhagic syndrome, acute renal and hepatic failure is possible.
Treatment: induction of vomiting, gavage gastric lavage, prescription of saline laxatives, activated charcoal and forced diuresis, blood alkalization, symptomatic therapy aimed at maintaining vital functions.

Precautions
Medical supervision is required (high frequency of allergic reactions, including fatal ones, especially with parenteral administration). Regular long-term use is not recommended due to myelotoxicity. Use for the relief of acute abdominal pain is excluded (until the cause is clarified). When prescribing to patients with acute cardiovascular pathology, careful monitoring of hemodynamics is required. Use with caution in patients with systolic blood pressure below 100 mm Hg. Art., with anamnestic indications of kidney disease (pyelonephritis, glomerulonephritis) and with a long history of alcohol.

Interaction with other medicinal products
The effect is enhanced by barbiturates, codeine, caffeine, H2-antihistamines, propranolol (slows down inactivation). Sarkolizin and methimazole increase the likelihood of the development of leukopenia. Sedatives and tranquilizers enhance the analgesic effect of metamizole sodium. Tricyclic antidepressants, oral contraceptives, allopurinol disrupt metabolism and increase toxicity. Simultaneous use with other analgesics-antipyretics, NSAIDs can lead to mutual enhancement of toxic effects, with chlorpromazine or other phenothiazine derivatives - to the development of severe hyperthermia. Myelotoxic drugs enhance the manifestation of hematotoxicity of sodium metamizole. Phenylbutazone and other inducers of microsomal farm ntov impaired liver effect.
Metamizole sodium, displacing from the connection with blood proteins, increases the activity of oral hypoglycemic drugs, indirect anticoagulants, HA, indomethacin. Enhances the sedative effect of alcohol. Reduces the concentration of cyclosporine in plasma. Radiopaque contrast agents, colloidal blood substitutes and penicillin should not be used during treatment with metamizole sodium. Due to the high likelihood of pharmaceutical incompatibility, one must not mix with other drugs in the same syringe.

Special instructions
When treating children under 5 years of age and patients receiving cytostatic drugs, taking metamizole sodium should be carried out only under the supervision of a physician.
Intolerance is very rare, but the threat of anaphylactic shock after intravenous administration of the drug is relatively higher than after taking the drug inside. Patients with atopic bronchial asthma and pollinosis have an increased risk of developing allergic reactions.
Against the background of taking metamizole sodium, agranulocytosis may develop, and therefore, if an unmotivated rise in temperature, chills, sore throat, difficulty swallowing, stomatitis is detected, as well as with the development of vaginitis or proctitis, an immediate withdrawal of the drug is necessary. With prolonged use, it is necessary to control the peripheral blood picture.
It is unacceptable to use for the relief of acute abdominal pain (until the cause is clarified).
For intramuscular injection, a long needle must be used. It is possible that urine is stained red due to the release of a metabolite (does not matter).

Pregnancy and elbowing
Contraindicated for oral administration during pregnancy. Contraindicated for parenteral use in the I and III trimesters of pregnancy. Use parenteral with caution in the II trimester of pregnancy.
Use during lactation (breastfeeding) is contraindicated.

Influence on the ability to drive vehicles and work with mechanisms
Does not affect.

Storage conditions
Store in a dry, dark place at a temperature not exceeding 25 ° C, out of the reach of children.

Shelf life
3 years. Do not use after the expiration date printed on the package.

Vacation conditions
On prescription.

Packaging
The solution is in 2 ml glass ampoules. Each ampoule is fixed in a plastic clip for 5 ampoules. 5 ampoules are packed in a cardboard box in a fixer together with an enclosed leaflet.