Metamizole Sodium is a medicine antipyretic , analgesic , belongs to the group pyrazolones . The substance was synthesized back in 1920. Since the 70s, due to the risk of development, the medicine began to be excluded from sale in some European countries, Sweden, Australia, and Japan. At the moment, the product is sold strictly according to prescription. In the Russian Federation in 2009 it was removed from the list of vital and essential drugs. Metamizole sodium is commercially available. The substance was assigned a code OKPD 24.42.13.673.

According to its physical properties, the medicine is a white or white-yellow crystalline powder that quickly decomposes at high humidity. The product dissolves well in water, pH ready solution - from 6 to 7.5. Poorly soluble in alcohol, practically insoluble in acetone , on air And . Molecular weight of Metamizole = 311.4 grams per mole; Metamizole sodium – 333.3 grams per mole. The chemical compound is given in the form of tablets, suppositories, drops and injection solution.

pharmachologic effect

Antipyretic, analgesic, anti-inflammatory.

Pharmacodynamics and pharmacokinetics

According to the mechanism of action, Metamizole Sodium is similar to other NSAIDs. The product does not selectively inhibit the enzyme cyclooxygenase , inhibits the formation of inflammatory mediators from arachidonic acid . The substance makes it difficult to carry out proprio- and extrareceptive impulses By Burdach beams And Goll , increases the threshold of excitability of the pain sensitivity center in the thalamus, increases the degree of heat transfer.

The anti-inflammatory effect of taking the drug is slightly expressed, the substance has practically no effect on water-salt metabolism, does not retain water and sodium ions, and does not irritate the mucous membrane of the digestive tract. Metamizole Sodium has some antispasmodic effect on the biliary and urinary tract.

After oral administration of the medicine, the effect of it develops within 20-30 minutes, reaching its maximum after 4 hours. Metamizole lowers the temperature much faster than and, the drug has the most pronounced analgesic effect. In the gastrointestinal tract, the substance is absorbed quickly and almost completely. In the intestines (on the walls) the product undergoes reactions hydrolysis , where its active metabolite is formed. Pure Metamizole is absent in blood plasma after oral administration.

After intravenous administration, a small concentration of the unchanged compound is detected in the blood plasma. The degree of binding to plasma proteins ranges from 50 to 60%. The substance is also metabolized in the liver. Excreted via the kidneys.

Indications for use

The medicine is used:

at arthralgia , chorea , various types of pain;
for relief of dental, headache, menstrual pain;
at , myalgia , sciatica ;
in patients with renal, hepatic and intestinal colic;
in case of infarction of the lung, great vessels;
for treatment pleurisy , , pneumonia , myocarditis ;
to relieve pain from burns, various injuries, decompression sickness, tumors;
at orchitis , herpes zoster , peritonitis , ;
in patients with pneumothorax and perforation of the esophagus;
at priapism , post-transfusion complications;
as part of complex treatment of acute infections, urological and purulent diseases;
for bites from bees, mosquitoes, and gadflies.

Contraindications

if available on the active component;
patients with neutropenia ;
during lactation;
for liver and kidney diseases;
patients with hereditary hemolytic anemia associated with enzyme deficiency glucose-6-phosphate dehydrogenase ;
at anemia , leukopenia , aspirin asthma ;
women in the first trimester and in the last.

in newborns under 3 months of age;
for and other kidney diseases;
patients who abuse alcohol;
when administered intravenously to patients with low blood pressure;
with unstable blood circulation ( shock , multiple injuries).

Side effects

The following adverse reactions may occur:

oliguria , kidney dysfunction, nephritis ;
various allergic reactions;
thrombocytopenia , drop in blood pressure, leukopenia ;
Lyell's syndrome , malignant exudative erythema , bronchospastic syndrome (rarely);
, with intramuscular injections.

Metamizole, instructions for use (Method and dosage)

Tablets or rectal suppositories are prescribed in a dosage of 250 to 500 mg, 2 or 3 times a day. The maximum amount of Metamizole Sodium that can be taken per day is 3 grams, at a time – 1 gram.

For children, the dosage needs to be adjusted. Single dose = 50 or 100 mg for children 2-3 years of age; 100-200 mg – for children from 4 to 5 years old and 200-300 mg – up to 14 years old. The frequency of administration is the same as for adults.

The medicine is administered intravenously or intramuscularly at a dosage of 250-500 mg, 2-3 times a day. The maximum daily dosage is 2 grams. For children, injection doses of no more than 10 mg per kg of body weight at a time are recommended.

Overdose

When taking or administering large dosages of medication, the following are observed: severe decrease in blood pressure, palpitations, nausea, tinnitus, vomiting, and general weakness, loss of consciousness, convulsions . May develop: acute, acute hepatic and hemorrhagic syndrome .

It is recommended to rinse the victim’s stomach, prescribe saline laxatives, enterosorbents . Symptomatic therapy is also indicated, forced diuresis , alkalization of blood.

Interaction

Combination use of the drug with analgesics, antipyretics and non-steroidal anti-inflammatory drugs can lead to increased toxicity of the drugs.

When taken simultaneously with inducers of microsomal liver enzymes, the effectiveness of Metamizole may decrease.

Combined use with indirect anticoagulants, oral hypoglycemic agents, and glucocorticosteroids enhances the effectiveness of the latter.

Phenothiazine may provoke the development of severe hyperthermia .

When combining the drug with anxiolytics and sedatives, its analgesic effect is enhanced.

The simultaneous use of Metamizole Sodium and tricyclic antidepressants, oral contraceptives disrupts the processes of normal drug metabolism and increases the toxicity of Metamizole.

Caffeine enhances the effect of the drug.

Reduces plasma concentration of the drug.

The substance can be combined with pitofenone hydrochloride And fenpiverinium bromide . Farming is being strengthened. the effects of all drugs, relaxation of smooth muscles, normalization of body temperature, reduction in the severity of pain.

Metamizole sodium Latin name. Metamizole sodium

Clinical and pharmacological group:

Included in the preparations

ATX:

N.02.B.B.02 Metamizole sodium

Pharmacodynamics:

Non-selective blockade of cyclooxygenase and reduction 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 threshold of excitability of the thalamic centers of pain sensitivity, and 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 (found in plasma in small quantities only after intravenous administration). Passes into breast milk (in therapeutic doses). The connection of the active metabolite with plasma proteins is 50-60%. Biotransformation in the liver. Excreted by the kidneys (in small quantities in the form of metabolites).

Indications:

· Arthralgia, rheumatism, chorea

· Headache, toothache, menstrual pain

· Neuralgia, sciatica, myalgia

· Renal, hepatic, intestinal colic.

· Pulmonary infarction, myocardial infarction, dissecting aortic aneurysm, thrombosis of the great vessels.

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

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

· 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 respiratory infections of the upper respiratory tract

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

XVIII.R50-R69.R52.9 Unspecified pain

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 heart area

XIII.M20-M25.M25.5 Joint pain

XVIII.R50-R69.R50 Fever of unknown origin

XIII.M30-M36.M35.3 Polymyalgia rheumatica

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 FDA recommendation category has not been determined. Do not use during pregnancy and breastfeeding. Directions for use and dosage:

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

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

Side effects:

Urinary system: impaired renal function, oliguria, anuria, proteinuria, interstitial nephritis, red staining of urine.

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 (insufficient information to recommend the use of metamizole sodium for headaches), leukopenia, thrombocytopenia.

Others: decreased blood pressure, nausea.

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

With intravenous use - drowsiness, dry mouth.

Overdose:

In case of overdose, 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, respiratory paralysis are observed. muscles.

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

Interaction:

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

Benzylpenicillin, colloidal blood substitutes and radiocontrast agents should not be used during treatment with metamizole sodium.

H 2 receptor blockers, and (slows down inactivation) - increased effectiveness.

Myelotoxic drugs - increased hematotoxicity of the drug.

Sugar-lowering drugs for oral administration, indirect anticoagulants, glucocorticoids - increase their activity (displaces them from their connection with protein).

Sedative and anxiolytic drugs (tranquilizers) - enhance the analgesic effect of metamizole sodium.

Thiamazole and cytotoxic drugs increase the risk of developing leukopenia.

Phenylbutazone, barbiturates and other hepatoinducers - when administered simultaneously, reduce the effectiveness of metamizole sodium.

Chlorpromazine or other phenothiazine derivatives - development of severe hyperthermia.

Cyclosporine - a decrease in its concentration in the blood.

Ethanol - enhanced effect.

Do not administer in the same syringe with other drugs due to the high likelihood of developing pharmaceutical incompatibility.

Special instructions:

There is an increased risk of developing hypersensitivity reactions in patients with bronchial asthma, especially with concomitant polyps in the sinuses; in patients with chronic urticaria; in patients with alcohol intolerance; in patients with intolerance to dyes (for example, tartrazine) or to preservatives (for example, benzoate).

With long-term use, it is necessary to monitor the peripheral blood picture. It is unacceptable to use the drug to relieve acute abdominal pain (until the cause is determined).

Instructions

Metamizole sodium INN (tablets)

International name: Metamizole sodium

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

Chemical name:

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

Pharmachologic effect:

An analgesic non-narcotic drug, 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 threshold of excitability of the thalamic centers of pain sensitivity, and increases heat transfer. A distinctive feature is the insignificant anti-inflammatory effect, which causes a weak effect on water-salt metabolism (Na+ and water retention) and the gastrointestinal mucosa. It has an analgesic, antipyretic and some antispasmodic (in relation to the smooth muscles of the urinary and biliary tract) effect. The effect develops 20-40 minutes after oral administration and reaches a maximum after 2 hours.

Pharmacokinetics:

Well and quickly absorbed into the gastrointestinal tract. It is hydrolyzed in the intestinal wall to form an active metabolite - unchanged metamizole is absent in the blood (only after intravenous administration a small concentration is detected in the plasma). The connection of the active metabolite with proteins is 50-60%. Metabolized in the liver, excreted by the kidneys. In therapeutic doses it penetrates into mother's milk.

Indications:

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

Contraindications:

Hypersensitivity, inhibition of hematopoiesis (agranulocytosis, cytostatic or infectious neutropenia), liver 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 period. With caution. Neonatal period (up to 3 months), kidney disease (pyelonephritis, glomerulonephritis - including a history), long-term ethanol abuse. IV administration to patients with systolic blood pressure below 100 mm Hg. or in case of circulatory instability (for example, against the background of myocardial infarction, multiple trauma, incipient shock).

Dosage regimen:

Orally, 250-500 mg 2-3 times a day, maximum single dose - 1 g, daily - 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, and it is recommended to use 200 mg suppositories for children: 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 suppository is administered, the child should remain in bed.

Side effects:

From the urinary system: impaired renal function, oliguria, anuria, proteinuria, interstitial nephritis, red staining of urine. 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. From the hematopoietic organs: agranulocytosis, leukopenia, thrombocytopenia. Other: decreased 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 carbon; carrying out forced diuresis, hemodialysis, with the development of convulsive syndrome - intravenous administration of diazepam and fast-acting barbiturates.

Special instructions:

When treating children under 5 years of age and patients receiving cytostatic drugs, metamizole sodium should only be taken 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 taking the drug orally. 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 rise in temperature, chills, sore throat, difficulty swallowing, stomatitis is detected, as well as with the development of vaginitis or proctitis, immediate discontinuation of the drug is necessary. With long-term use, it is necessary to monitor the peripheral blood picture. It is not permissible to use it to relieve acute abdominal pain (until the cause is determined). For intramuscular administration it is necessary to use a long needle. It is possible that the urine may turn red due to the release of a metabolite (it does not matter).

Interaction:

Due to the high probability of developing pharmaceutical incompatibility, it should not 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 simultaneous administration of cyclosporine, the concentration of the latter in the blood decreases. Metamizole, displacing oral hypoglycemic drugs, indirect anticoagulants, corticosteroids and indomethacin from protein binding, increases their activity. Phenylbutazone, barbiturates and other hepatoinducers, when administered simultaneously, reduce the effectiveness of metamizole. Concomitant use with other non-narcotic analgesics, tricyclic antidepressants, contraceptive hormonal drugs and allopurinol may 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: Sodium salt of [(2,3-dihydro-1,5-dimethyl-3-oxo-2-phenyl-1H-pyrazol-4-yl)methylamino]methanesulfonic acid (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 transmission of painful proprio- and extraceptive impulses through the Burdach and Gaulle bundles, increases heat transfer, and increases the threshold of excitability of pain sensitivity centers in the thalamus. After oral administration, it is completely and quickly absorbed. It is hydrolyzed in the intestinal wall with the formation of an active metabolite - unchanged metamizole is absent in the blood (only when administered intravenously, minor concentrations are detected in the 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 effect of metamizole sodium develops after 20 - 40 minutes and becomes maximum after 2 hours.

Indications

Arthralgia, chorea, rheumatism; pain: dental, headache, menstrual, sciatica, neuralgia, myalgia, with pulmonary infarction, colic (hepatic, renal, intestinal), myocardial infarction, thrombosis of the great vessels, dissecting aortic aneurysm, inflammatory processes (pneumonia, pleurisy, myocarditis, lumbago), burns, injuries, 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 administration of metamizole sodium and dose

Metamizole sodium is taken orally, administered intramuscularly, intravenously, or rectally. Intramuscularly or intravenously (for 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 administered 0.1 - 0.5 ml. Orally, 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 is 2 - 3 years - 50 - 100 mg , 4 - 5 years - 100 - 200 mg, 6 - 7 years - 200 mg, 8 - 14 years - 250 - 300 mg.

When using metamizole sodium, urine may turn red due to the release of a metabolite. A doctor's supervision is required when using metamizole sodium (since there is a high incidence of allergic reactions, including fatal ones, especially with parenteral administration). Regular long-term use is not recommended due to myelotoxicity. The use of metamizole sodium for the relief of acute abdominal pain is excluded (their cause has not yet been clarified). When prescribed 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 in the anamnesis of kidney disease (glomerulonephritis, pyelonephritis), as well as with a long history of alcoholism.

Contraindications for use

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

Restrictions on use

No data.

Use during pregnancy and breastfeeding

The use of metamizole sodium is contraindicated during pregnancy. During therapy with metamizole sodium, you must stop breastfeeding.

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, and H2-antihistamines. Thiamazole and sarcolysine increase the risk of developing 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 due to disruption of its metabolism. The combined use of metamizole sodium with phenothiazine derivatives (including chlorpromazine) can cause the development of a pronounced increase in body temperature, with other non-steroidal anti-inflammatory drugs, analgesics and antipyretics - a mutual increase in toxicity and associated 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 its connection with plasma proteins, increases the activity of indirect anticoagulants, oral hypoglycemic agents, indomethacin, and glucocorticosteroids. Metamizole sodium reduces plasma levels 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 cannot be mixed in the same syringe with other drugs.

Overdose

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

Trade names of drugs with the active ingredient metamizole sodium

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

Metamizole sodium

Latin name

Metamizole sodium

Chemical name

Sodium salt of [(2,3-dihydro-1,5-dimethyl-3-oxo-2-phenyl-1H-pyrazol-4-yl)methylamino]methanesulfonic acid (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, quickly decomposes in the presence of moisture. Easily soluble in water (1:1.5), the aqueous solution has a pH of 6-7.5. Slightly soluble in ethanol (1:60-1:80), practically insoluble in ether, chloroform, acetone.

Pharmacology

Pharmacological action: analgesic, anti-inflammatory, antipyretic.

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 threshold of excitability of the thalamic centers of pain sensitivity, and increases heat transfer.

When taken orally, it is quickly and completely absorbed. It is hydrolyzed in the intestinal wall to form an active metabolite - unchanged metamizole is absent in the blood (only after intravenous administration, its insignificant concentrations are detected 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 after 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 great 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, inhibition of hematopoiesis (agranulocytosis, cytostatic or infectious neutropenia), severe impairment of liver or kidney function, prostaglandin bronchial asthma, hereditary hemolytic anemia associated with deficiency of glucose-6-phosphate dehydrogenase, pregnancy, breastfeeding.

Side effects

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

Interaction

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

Overdose

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

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

Directions for use and doses

IM or IV (for severe pain) - 1-2 ml of 50% or 25% solution 2-3 times a day, maximum daily dose 2 g; children are administered 0.1-0.5 ml. Orally after meals or rectally, 250-500 mg 2-3 times a day, maximum single dose - 1 g, daily dose - 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 a day.

Precautionary measures

Medical supervision is necessary (high frequency of allergic reactions, including deaths, especially with parenteral administration). Regular long-term use is not recommended due to myelotoxicity. Do not use it to relieve acute abdominal pain (until the cause is determined). When prescribed 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 alcoholism.

special instructions

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

Year of last adjustment

1999

Interactions with other active ingredients

Allopurinol*	Against the background of metamizole sodium, increased 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.