Metamizole sodium Latin name. Metamizole sodium (Metamizole sodium)

Clinico-pharmacological group:  

Included in medications

ATH:

N.02.B.B.02 Metamizole sodium

Pharmacodynamics:

Non-selective blockade of cyclooxygenase and a decrease in the synthesis of prostaglandins and their precursors from arachidonic acid. It prevents the conduction of painful extra- and proprioceptive impulses along the Gaulle and Burdach bundles, increases the excitability threshold of the thalamic centers of pain sensitivity, enhances heat transfer. It has analgesic, antipyretic and anti-inflammatory effects.

Pharmacokinetics:

Well and quickly absorbed in the gastrointestinal tract. In the intestinal wall, it is hydrolyzed to form an active metabolite (4-methyl-amino-antipyrine); unchanged in the blood is absent (detected in plasma in small quantities only after intravenous administration). Penetrates into breast milk (in therapeutic doses). The connection of the active metabolite with plasma proteins is 50-60%. Biotransformation in the liver. It is excreted by the kidneys (in a small amount in the form of metabolites).

Indications:

· Arthralgia, rheumatism, chorea

· Headache, toothache, menstrual pain

· Neuralgia, sciatica, myalgia

· Renal, hepatic, intestinal colic.

· Pulmonary infarction, myocardial infarction, exfoliating aortic aneurysm, thrombosis of the main vessels.

· Inflammatory processes: pleurisy, pneumonia, lumbago, myocarditis.

· Trauma, burns, decompression sickness, shingles, swelling.

· Orchitis, pancreatitis, peritonitis, esophageal perforation, pneumothorax.

· Post-transfusion complications, priapism.

· Feverish syndrome in acute infectious, purulent and urological diseases, insect bites.

X.J00-J06 Acute upper respiratory infections

X.J10-J18.J11 Influenza, virus not identified

XVIII.R50-R69.R52.9 Pain, unspecified

XVIII.R50-R69.R52.0 Acute pain

XVIII.R50-R69.R52 Pain not elsewhere classified

XVIII.R50-R69.R51 Headache

XVIII.R00-R09.R07.2 Pain in the region of the heart

XIII.M20-M25.M25.5 Joint pain

XVIII.R50-R69.R50 Fever of unknown origin

XIII.M30-M36.M35.3 Rheumatic polymyalgia

XIII.M50-M54.M54.3 Sciatica

XIII.M70-M79.M79.1 Myalgia

XIII.M70-M79.M79.2 Neuralgia and neuritis, unspecified

XIV.N20-N23.N23 Renal colic, unspecified

VI.G20-G26.G25.5 Other types of chorea

Contraindications:

Individual intolerance.

Inhibition of hematopoiesis (agranulocytosis, cytostatic or infectious neutropenia).

Hereditary hemolytic anemia associated with deficiency of glucose-6-phosphate dehydrogenase.

Anemia, leukopenia, liver and / or kidney failure.

Aspirin form of bronchial asthma.

Pregnancy (especially the first trimester and the last 6 weeks), breastfeeding.

Carefully: No data. Pregnancy and lactation:The category of FDA recommendations has not been determined. Do not use during pregnancy and during breastfeeding. Dosage and administration:

Intramuscularor intravenously (with severe pain) - 1-2 ml of a 50% or 25% solution 2-3 times a day, the maximum daily dose is 2 g.

Inside, after meals, or rectally, 250-500 mg 2-3 times a day, the maximum single dose is 1 g, the daily dose is 3 g.

Side effects:

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 syndrome, anaphylactic shock.

Blood: agranulocytosis (not enough information to recommend the use of metamizole sodium for headache), leukopenia, thrombocytopenia.

Others: lowering blood pressure, nausea.

Local reactions: with intramuscular injection, the formation of infiltrates at the injection site is possible.

When administered intravenously - drowsiness, dry mouth.

Overdose:

In case of overdose, nausea, vomiting, gastralgia, oliguria, hypothermia, lowering blood pressure, tachycardia, shortness of breath, tinnitus, drowsiness, delirium, impaired consciousness, acute agranulocytosis, hemorrhagic syndrome, acute renal and / or liver failure, convulsions, respiratory paralysis muscles.

For treatment, gastric lavage, saline laxatives, enterosorbents, forced diuresis, hemodialysis are prescribed, with the development of a convulsive syndrome, intravenous administration of diazepam and high-speed barbiturates.

Interaction:

Allopurinol, non-narcotic analgesics, tricyclic antidepressants, hormonal contraceptives - increased toxicity.

Benzylpenicillin, colloidal blood substitutes and radiopaque agents - do not use during treatment with metamizole sodium.

Blockers of H 2 receptors, and (slows down inactivation) - increased efficiency.

Myelotoxic agents - increased hematotoxicity of the drug.

Hypoglycemic drugs for oral administration, indirect anticoagulants, glucocorticoids - an increase in their activity (displaces them from the connection with the protein).

Sedative and anxiolytic drugs (tranquilizers) - increased analgesic action of metamizole sodium.

Thiamazole and cytotoxic drugs - an increased risk of developing leukopenia.

Phenylbutazone, barbiturates and other hepatoinductors - while prescribing, reduce the effectiveness of metamizole sodium.

Chlorpromazine or other phenothiazine derivatives - the development of severe hyperthermia.

Cyclosporine - a decrease in its concentration in the blood.

Ethanol - enhancing the effect.

In the same syringe with other drugs, they are not administered due to the high likelihood of developing pharmaceutical incompatibility.

Special instructions:

An increased risk of developing hypersensitivity reactions is present in patients with bronchial asthma, especially with concomitant polyps in the sinus area; in patients with chronic urticaria; in patients with alcohol intolerance; in patients with intolerance to dyes (eg, tartrazine) or to preservatives (eg, benzoate).

With prolonged use, it is necessary to control the picture of peripheral blood. It is unacceptable to use the drug to relieve acute pain in the abdomen (until the cause is clarified).

Instructions

Metamizole sodium INN (tablets)

International name: Metamizole sodium

Dosage form: capsules, rectal suppositories [for children], tablets, tablets [for children]

Chemical Name:

Sodium salt [(2.3 - dihydro - 1.5 - dimethyl - 3 - oxo - 2 - phenyl - 1H - pyrazol - 4 - yl) methylamino] methanesulfonic acid (and as monohydrate)

Pharmachologic effect:

A non-narcotic analgesic agent, a pyrazolone derivative, non-selectively blocks COX and reduces the formation of Pg from arachidonic acid. It prevents the conduction of painful 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 slight severity of the anti-inflammatory effect, which causes a weak effect on the water-salt metabolism (retention of Na + and water) and the gastrointestinal mucosa. It has analgesic, antipyretic and some antispasmodic (in relation to the smooth muscles of the urinary and biliary tract) action. The action develops 20-40 minutes after ingestion and reaches a maximum after 2 hours.

Pharmacokinetics:

Well and quickly absorbed in the digestive tract. In the intestinal wall, it is hydrolyzed with the formation of an active metabolite - unchanged metamizole is absent in the blood (only after intravenous administration, its insignificant concentration is found in plasma). Communication of an active metabolite with proteins - 50-60%. Metabolized in the liver, excreted by the kidneys. In therapeutic doses, it passes into mother's milk.

Indications:

Feverish syndrome (infectious and inflammatory diseases, insect bites - mosquitoes, bees, gadflies, etc., post-transfusion complications); Pain syndrome (mild and moderate): incl. neuralgia, myalgia, arthralgia, biliary colic, intestinal colic, renal colic, injuries, burns, decompression sickness, herpes zoster, orchitis, sciatica, myositis, postoperative pain syndrome, headache, toothache, algomenorrhea.

Contraindications:

Hypersensitivity, oppression of hematopoiesis (agranulocytosis, cytostatic or infectious neutropenia), hepatic and / or renal failure, hereditary hemolytic anemia associated with deficiency of glucose-6-phosphate dehydrogenase, bronchial asthma induced by taking ASA, salicylates or other NSAIDs, anemia, leukopenia, pregnancy (especially in the first trimester and in the last 6 weeks), lactation. With caution. The neonatal period (up to 3 months), kidney disease (pyelonephritis, glomerulonephritis - including history), prolonged alcohol abuse. In / in the introduction of 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).

Dosing regimen:

Inside, 250-500 mg 2-3 times a day, the maximum single dose is 1 g, the daily dose is 3 g. Single doses for children 2-3 years old - 50-100 mg, 4-5 years old - 100-200 mg, 6-7 years - 200 mg, 8-14 years - 250-300 mg, frequency of administration - 2-3 times a day. Rectal use - for adults - 300, 650 and 1000 mg. The dose for children depends on the age of the child and the nature of the disease, while it is recommended to use children's suppositories of 200 mg: from 6 months to 1 year - 100 mg, from 1 year to 3 years - 200 mg, from 3 to 7 years - 200-400 mg, from 8 to 14 years - 200-600 mg. After the introduction of the suppository, the child should be in bed.

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 syndrome, anaphylactic shock. On the part of the hematopoietic organs: agranulocytosis, leukopenia, thrombocytopenia. Others: decrease in blood pressure. Local reactions: with i / m administration, infiltrates are possible at the injection site. 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 a convulsive syndrome - in / in the introduction of diazepam and high-speed barbiturates.

Special instructions:

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

Interaction:

Due to the high likelihood of developing pharmaceutical incompatibility, it cannot be mixed with other drugs in the same syringe. Enhances the effects of ethanol. Radiopaque drugs, colloidal blood substitutes and penicillin should not be used during treatment with metamizole. With the simultaneous appointment of cyclosporine, the concentration of the latter in the blood decreases. Metamizole, displacing oral hypoglycemic drugs, indirect anticoagulants, corticosteroids and indomethacin from the connection with the protein, increases their activity. Phenylbutazone, barbiturates, and other hepatoinducers, when administered simultaneously, reduce the effectiveness of metamizole. Simultaneous appointment with other non-narcotic analgesics, tricyclic antidepressants, contraceptive hormonal drugs and allopurinol can lead to increased toxicity. Sedative and anxiolytic drugs (tranquilizers) enhance the analgesic effect of metamizole. Thiamazole and cytostatics increase the risk of developing 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.

inside VRD-1.0 VSD-3.0

Formula: C13H16N3O4SNa, chemical name: [(2,3-dihydro-1,5-dimethyl-3-oxo-2-phenyl-1H-pyrazol-4-yl)methylamino]methanesulfonic acid sodium salt (and as monohydrate).
Pharmacological group: non-narcotic analgesics, including non-steroidal and other anti-inflammatory drugs / NSAIDs - Pyrazolones.
Pharmachologic effect: anti-inflammatory, analgesic, antipyretic.

Pharmacological properties

Metamizole sodium inhibits cyclooxygenase, reduces the formation of bradykinins, free radicals, endoperoxides, some prostaglandins, and inhibits lipid peroxidation. Metamizole sodium prevents the conduction of painful proprio- and extraceptive impulses through the Burdach and Gaulle bundles, increases heat transfer, and increases the excitability threshold of pain sensitivity centers in the thalamus. After oral administration, it is completely and rapidly absorbed. It is hydrolyzed in the intestinal wall with the formation of an active metabolite - there is no unchanged metamizol in the blood (only when administered intravenously, its insignificant concentrations are found in plasma). The active metabolite of metamizole sodium is 50-60% bound to plasma proteins. It is destroyed in the liver. It is excreted from the body by the kidneys. The action of metamizole sodium develops after 20-40 minutes and becomes maximum after 2 hours.

Indications

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

Method of application of metamizole sodium and doses

Metamizole sodium is taken orally, administered intramuscularly, intravenously, rectally. Intramuscularly or intravenously (with severe pain) - 2-3 times a day, 1-2 ml of a 25% or 50% solution, the maximum daily dose is 2 g; children are injected with 0.1 - 0.5 ml. Inside, after meals, or rectally 2-3 times a day, 250-500 mg, the maximum single dose is 1 g, daily - 3 g. For children 2-3 times a day, the usual dose of 2-3 years is 50-100 mg , 4 - 5 years - 100 - 200 mg, 6 - 7 years - 200 mg, 8 - 14 years - 250 - 300 mg.

When using metamizole sodium, it is possible to stain the urine red due to the release of the metabolite. You need a doctor's supervision when using metamizole sodium (since there is a high incidence of allergic reactions, including fatal ones, especially when administered parenterally). Regular long-term use is not recommended due to myelotoxicity. The use of metamizole sodium for the relief of acute abdominal pain is excluded (until their cause has been clarified). When prescribing to patients with pathology of the cardiovascular system, careful monitoring of hemodynamic parameters is necessary. Use with caution in patients with systolic blood pressure less than 100 mm Hg. Art., with indications of a history of kidney disease (glomerulonephritis, pyelonephritis), as well as with a long history of alcohol.

Contraindications for use

Hypersensitivity, severe violations of the functional state of the kidneys or liver, hematopoiesis suppression (infectious or cytostatic neutropenia, agranulocytosis), hemolytic hereditary anemia, which is associated with glucose-6-phosphate dehydrogenase deficiency, bronchial asthma (prostaglandin), breast-feeding, pregnancy.

Application restrictions

No data.

Use during pregnancy and lactation

The use of metamizole sodium is contraindicated in pregnancy. At the time of therapy with metamizole sodium, breastfeeding should be stopped.

Side effects of metamizole sodium

Granulocytopenia, thrombocytopenia, agranulocytosis, hemorrhages, interstitial nephritis, hypotension, allergic reactions (including bronchospasm, Lyell's syndrome, Stevens-Johnson syndrome, anaphylactic shock).

Interaction of metamizole sodium with other substances

The effect of metamizole sodium is enhanced by codeine, barbiturates, caffeine, propranolol, H2-antihistamines. Thiamazole and sarcolysin increase the risk of leukopenia when used together with metamizole sodium. Tranquilizers and sedatives enhance the analgesic effect of metamizole sodium. Oral contraceptives, tricyclic antidepressants, allopurinol increase the toxicity of metamizole sodium by disrupting its metabolism. The combined use of metamizole sodium with phenothiazine derivatives (including chlorpromazine) can cause a pronounced increase in body temperature, with other non-steroidal anti-inflammatory drugs, antipyretic analgesics - to a mutual increase in toxicity and related effects. Phenylbutazone and other inducers of microsomal liver enzymes weaken the effects of metamizole sodium. Myelotoxic drugs potentiate the hematotoxicity of metamizole sodium. Metamizole sodium potentiates the sedative effect of alcohol. Metamizole sodium, displacing from the connection with plasma proteins, increases the activity of indirect anticoagulants, oral hypoglycemic agents, indomethacin, glucocorticosteroids. Metamizole sodium reduces the plasma level of cyclosporine. Radiocontrast agents, penicillin and colloidal blood substitutes should not be used during therapy with metamizole sodium. Due to the high risk of pharmaceutical incompatibility, metamizole sodium should not be mixed in the same syringe with other drugs.

Overdose

With an overdose of metamizole sodium, hypothermia, palpitations, severe hypotension, shortness of breath, nausea, tinnitus, vomiting, drowsiness, weakness, delirium, convulsive syndrome, impaired consciousness develop; possible development of hemorrhagic syndrome, acute agranulocytosis, acute liver and kidney failure. It is necessary: ​​inducing vomiting, gastric lavage through a tube, the appointment of activated charcoal, saline laxatives and alkalization of the blood, forced diuresis, symptomatic treatment aimed at maintaining vital functions.

Trade names of drugs with the active substance metamizole sodium

In most economically developed countries, metamizole is banned due to side effects (Sweden (since 1972), USA (since 1977), Japan, Australia and a number of European Union countries), in particular because of the risk of agranulocytosis, or its use is significantly limited , which primarily concerns the use in children. In Russia, since 2009, metamizole sodium (analgin) has been excluded from the list of drugs for beneficiaries, but has been kept on the free market.

Metamizole sodium

Latin name

Metamizole sodium

chemical name

[(2,3-Dihydro-1,5-dimethyl-3-oxo-2-phenyl-1H-pyrazol-4-yl)methylamino]methanesulfonic acid sodium salt (and as monohydrate)

Gross formula

C 13 H 16 N 3 O 4 SNa

Pharmacological group

NSAIDs - Pyrazolones

Nosological classification (ICD-10)

CAS code

68-89-3

Characteristic

White or white with a barely noticeable yellowish tint crystalline powder, rapidly decomposes in the presence of moisture. Easily soluble in water (1:1.5), the aqueous solution has a pH of 6-7.5. Difficultly soluble in ethanol (1:60-1:80), practically insoluble in ether, chloroform, acetone.

Pharmacology

Pharmacological action - analgesic, anti-inflammatory, antipyretic.

It inhibits the activity of cyclooxygenase, reduces the formation of endoperoxides, bradykinins, some PGs, free radicals, and inhibits lipid peroxidation. It prevents the conduction of painful 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.

When taken orally, it is rapidly and completely absorbed. In the intestinal wall, it is hydrolyzed with the formation of an active metabolite - unchanged metamizole is absent in the blood (only after intravenous administration, its insignificant concentrations are found in plasma). The level of binding of the active metabolite to proteins is 50-60%. Destroyed in the liver. Excretion passes through the kidneys.

The action develops in 20-40 minutes and reaches a maximum after 2 hours.

Application

Arthralgia, rheumatism, chorea, pain: headache, dental, menstrual, neuralgia, sciatica, myalgia, colic (renal, hepatic, intestinal), pulmonary infarction, myocardial infarction, dissecting aortic aneurysm, thrombosis of the main vessels, inflammatory processes (pleurisy, pneumonia , lumbago, myocarditis), trauma, burns, decompression sickness, herpes zoster, 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).

Contraindications

Hypersensitivity, oppression of hematopoiesis (agranulocytosis, cytostatic or infectious neutropenia), severe violations of the liver or kidneys, prostaglandin bronchial asthma, hereditary hemolytic anemia associated with deficiency of glucose-6-phosphate dehydrogenase, pregnancy, lactation.

Side effects

Granulocytopenia, agranulocytosis, thrombocytopenia, hemorrhages, hypotension, interstitial nephritis, allergic reactions (including Stevens-Johnson, Lyell syndromes, bronchospasm, anaphylactic shock).

Interaction

The effect is enhanced by barbiturates, codeine, H 2 -antihistamines, propranolol (slows down inactivation). Sarcolysin and thiamazole increase the likelihood of developing leukopenia. Increases the hypoglycemic activity of oral antidiabetic drugs (releases from the connection with blood proteins), sedative - alcohol, reduces the concentration of cyclosporine in plasma.

Overdose

Symptoms: hypothermia, severe hypotension, palpitations, shortness of breath, tinnitus, nausea, vomiting, weakness, drowsiness, delirium, impaired consciousness, convulsive syndrome; possible development of acute agranulocytosis, hemorrhagic syndrome, acute renal and hepatic failure.

Treatment: induction of vomiting, gastric lavage, administration of saline laxatives, activated charcoal and forced diuresis, alkalization of the blood, symptomatic therapy aimed at maintaining vital functions.

Dosage and administration

V / m or / in (with severe pain) - 1-2 ml of a 50% or 25% solution 2-3 times / day, the maximum daily dose is 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 - 200 mg, 8-14 years - 250-300 mg 2-3 times / day.

Precautionary measures

Medical supervision is required (high frequency of allergic reactions, including fatal ones, especially when administered parenterally). Regular long-term use is not recommended due to myelotoxicity. Use for relieving acute pain in the abdomen is excluded (until the cause is clarified). When administered to patients with acute cardiovascular pathology, careful monitoring of hemodynamics is necessary. Use with caution in patients with SBP levels below 100 mm Hg. Art., with anamnestic indications of kidney disease (pyelonephritis, glomerulonephritis) and with a long history of alcohol.

special instructions

When using metamizole sodium, red staining of urine is possible due to the release of a metabolite.

Year of last adjustment

1999

Interactions with other active substances

Allopurinol*	Against the background of metamizole sodium, an increase in toxicity is possible.
Indomethacin*	Against the background of metamizole sodium, the effect is enhanced.
Codeine	Codeine enhances the effect.
Propranolol*	Propranolol slows down biotransformation and increases the effect.
Sarcolysin*	Sarcolysin increases (mutually) the likelihood of leukopenia.