Analgin® [Metamizole sodium]

Pharmacological properties

NSAIDs, a derivative of pyrazolone. non-selectively blocks cog, reduces the formation of prostaglandins from arachidonic acid. prevents the conduct of painful extra- and proprioceptive impulses along the beams of the calf and burdock, increases the threshold of excitability of the thalamic centers of pain sensitivity, 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 (delay of na + and water) 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.

Pharmacokinetics With the / m introduction, it is rapidly and completely absorbed into the blood. In the liver, it undergoes oxidative deamination with the formation of an active metabolite. The relationship of the active metabolite with proteins is 50-60%. In children, deamination processes are slower than in adults. With frequent administration (usually 4 times a day) in children, cumulation of the drug and intoxication are possible. It is quickly and evenly distributed in tissues. C_max achieved 1–1.5 hours after i / m administration. T_½ is about 7 hours. Excreted in urine.

When used internally, it is rapidly absorbed in the digestive tract. In the intestinal wall is hydrolyzed with the formation of an active metabolite. Unchanged in the blood is absent. The active metabolite binds to plasma proteins by 50-60%. Time to reach C_max in blood plasma is 1-2 hours. T_½ - 2.5 hours. It is excreted mainly by the kidneys.

Indications

Pain syndrome of low and medium intensity of various origin and localization (headache, toothache, burns, pain in the postoperative period, dysmenorrhea, arthralgia, neuralgia, sciatica, myositis); hyperthermic syndrome, febrile conditions (with flu, acute respiratory and other infections); renal and hepatic colic (in combination with antispasmodics).

Application

Assign in oil, in / in stream and inside. the route of administration and dose depend on the severity of the disease and are determined individually. the analgesic effect with a / in the introduction is higher than with a / m.

The injected solution must have body temperature. To prevent a sharp decrease in blood pressure, IV administration should be carried out slowly (at a rate of not more than 1 ml / min), the patient should be in a supine position, blood pressure, heart rate and respiration should be monitored. The procedure requires the availability of antishock therapy. For iv administration, a long needle must be used.

Adults prescribe 0.5-1 ml (250-500 mg) 2-3 times a day. The maximum single dose for both routes of administration is 1 ml (500 mg), daily - 2 ml (1 g).

Children under 1 year of age should be prescribed at a dose of 0.01 ml / kg body weight. For children under 1 year of age, the drug is administered only in oil.

Duration of use - up to 3 days.

For children over the age of 1 year, administer 0.1 ml for 1 year of life 1-2 times a day. Duration of use - up to 3 days.

In tablet form, use in adults and children over the age of 14 years, 250–500 mg (½ – 1 tablet) 1-2 times a day. Take the tablets after meals, without chewing, without dissolving, with plenty of water.

The maximum daily dose is 1 g.

Children aged 12-14 years - 250 mg 1-2 times a day.

Analgin-Darnitsa is intended for symptomatic short-term use. The course of treatment is no more than 3 days.

If the symptoms of the disease do not disappear within 3 days, you should consult a doctor regarding the further use of the drug.

Contraindications

Hypersensitivity to the components of the drug. agranulocytosis, cytostatic or infectious neutropenia. hepatic and / or renal failure. hereditary hemolytic anemia associated with a deficiency of glucose-6-phosphate dehydrogenase. BA attacks caused by acetylsalicylic acid.anemia, leukopenia. abdominal pain of unknown genesis. kidney disease: pyelonephritis, glomerulonephritis, including a history of. can not be entered in / in patients with systolic hell 100 mm RT. Art. polytrauma. shock. porphyria.

Side effects

On the part of the liver and biliary tract: hepatitis.

From the side of the kidneys and urinary tract: oliguria, anuria, proteinuria, interstitial nephritis, urine staining in red.

From the cardiovascular system: lowering blood pressure, tachycardia.

On the part of the blood and lymphatic system: agranulocytosis, leukopenia, thrombocytopenia, anemia, granulocytopenia.

On the part of the immune system: hypersensitivity reactions, including rashes on the skin and mucous membranes, flushing of the skin, itching, urticaria, conjunctivitis, Quinckes edema; rarely - Stevens-Johnson syndrome, Lyell syndrome, bronchospastic syndrome, anaphylactoid reactions, anaphylactic shock.

General disorders and reactions at the injection site: infiltrates at the injection site (with i / m administration), hyperemia, edema, local rashes and itching of the skin at the injection site.

special instructions

With parenteral administration, medical supervision is necessary (high frequency of allergic reactions, including fatal outcomes) and the presence of conditions for anti-shock therapy.

Patients with atopic AD and hay fever have an increased risk of hypersensitivity reactions.

The use of an unknown genesis for the relief of acute abdominal pain is excluded (until the cause is clarified).

The drug should be used with caution in patients:

elderly - can lead to an increase in the frequency of adverse reactions, especially from the digestive system;

with inflammatory bowel disease, including ulcerative colitis and Crohn’s disease.

When prescribing to patients with acute cardiovascular pathology, careful monitoring of hemodynamics is necessary. Use with caution in patients with a blood pressure level of 100 mm Hg. Art., with myocardial infarction, multiple trauma, with anamnestic indications of liver and kidney diseases (pyelonephritis, glomerulonephritis), in the treatment of cytostatics, with chronic alcoholism, weighed down by an allergic history, with blood diseases.

Regular prolonged use of the drug is not recommended due to the myelotoxicity of metamizole sodium; it is necessary to control the picture of peripheral blood (leukocyte formula).

With the use of the drug, agranulocytosis may develop, and therefore, if an unexplained increase in body temperature, chills, sore throat, difficulty swallowing, stomatitis, as well as inflammation of the external genitalia and anus is necessary, immediate withdrawal of the drug is necessary.

SC administration of the drug should not be used due to possible tissue irritation.

During the treatment period, urine staining in red is possible (due to the release of the metabolite), which does not have clinical significance.

Rarely, sodium sulfite anhydrous (E221) can cause hypersensitivity reactions and bronchospasm.

The use of the drug must be stopped when rashes appear on the skin and mucous membranes.

The drug contains 1 mmol / dose of sodium, that is, it is practically free of sodium.

Use during pregnancy and lactation. Contraindicated during pregnancy, especially in the first trimester and in the last 6 weeks. During treatment, breast-feeding should be discontinued, as metamizole sodium passes into breast milk.

Children. For children under the age of 1 year, the drug is administered only in oil. In children, use under the supervision of a doctor for serious and vital indications. The drug in the form of tablets should not be used in children under the age of 12 years.

The ability to influence the speed of reactions when driving vehicles or working with other mechanisms. During the treatment period, it is not allowed to drive vehicles or engage in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Interactions

Due to the high likelihood of pharmaceutical incompatibility, it cannot be mixed with other drugs in the same syringe.

Ethanol - enhances the effect of ethanol.

Chlorpromazine or other phenothiazine derivatives - simultaneous use can lead to the development of severe hypothermia.

X-ray contrast agents, colloidal blood substitutes, and penicillin should not be used during treatment with metamizole sodium.

Cyclosporin - with simultaneous use, the concentration of cyclosporin in the blood decreases.

Oral hypoglycemic drugs, indirect anticoagulants, GCS, phenytoin, ibuprofen and indomethacin - metamizole sodium increase the activity of these drugs by displacing them from the protein.

Phenylbutazone, barbiturates and other hepatoinductors with simultaneous use reduce the effectiveness of metamizole sodium.

Non-narcotic analgesics, tricyclic antidepressants, hormonal contraceptives and allopurinol - the simultaneous use of metamizole sodium with these drugs can increase its toxicity.

Other NSAIDs - their analgesic and antipyretic effects are potentiated and the likelihood of additive unwanted side effects increases.

Sedatives and tranquilizers (sibazon, trioxazine, valocordin) enhance the analgesic effect of Analgin-Darnitsa.

Sarkolizin, merkazolil (tiamazole), drugs that suppress bone marrow activity, including gold preparations - the likelihood of hematotoxicity, including the development of leukopenia, increases.

Codeine, histamine H₂-blockers and propranolol enhance the effect of metamizole sodium.

Caution is necessary when using the drug with sulfonamide hypoglycemic drugs (the hypoglycemic effect is enhanced) and diuretics (furosemide).

Myelotoxic drugs cause increased hematotoxicity.

Methotrexate - metamizole in high doses can lead to an increase in the concentration of methotrexate in blood plasma and an increase in its toxic effects (on the digestive system and blood formation system).

Overdose

Symptoms: hypothermia, marked decrease in hell, palpitations, shortness of breath, tinnitus, nausea, vomiting, gastralgia, weakness, oliguria, anuria, drowsiness, delirium, impaired consciousness, tachycardia, convulsive syndrome; acute agranulocytosis, hemorrhagic syndrome, acute renal and hepatic failure, and respiratory muscle paralysis are possible.

Treatment: induction of vomiting, gastric lavage, administration of saline laxatives, activated charcoal. Conducting forced diuresis, hemodialysis, alkalization of blood, symptomatic therapy aimed at maintaining vital functions. With the development of convulsive syndrome, iv diazepam and high-speed barbiturates are administered.

Storage conditions

In the original packaging at a temperature not exceeding 25 ° C. rr do not freeze.