Analgin solution for intravenous and intramuscular administration 500mg/ml in ampoules 2ml №10

Name:
Analgin solution for IV and IV introduction.500mgml in amp.2ml in pack No. 10 CompositionOne ampoule (2 ml) contains: active substance – metamizole sodium – 1000 mg; excipient – water for injection.
Description:
Transparent yellowish liquid. Pharmacotherapeutic group Other analgesics and antipyretics. Pyrazolones. ATX code: N02BB02. Pharmacological properties Pharmacodynamics Analgin is a derivative of pyrazolone and has analgesic, antipyretic and mild antispasmodic effects. The mechanism of action is not fully understood. Some research results show that analgin and its main metabolite (4-N-methylaminoantipyrine) probably have both a central and a peripheral mechanism of action. Pharmacokinetics After intramuscular administration, it is rapidly absorbed into the blood. In the liver, it undergoes hydrolysis with the formation of the active metabolite 4-methylaminoantipyrine (4-MAA) and is demethylated to the second active metabolite – 4-aminoantipyrine (4-AA), and also biotransformed to inactive metabolites – 4-formylaminoantipyrine (4-FAA) and 4- acetylaminoantipyrine (4-AcAA). Unchanged analgin is found in the blood in small quantities only after intravenous administration. In the blood, it reversibly binds to plasma proteins (4-MAA by 58%, 4-AA by 48%). The effective concentration of the total metabolites of analgin is 10 μg / ml. The toxic effect is manifested at a concentration of metabolites over 20 μg / ml. With repeated administration of the drug, its pharmacokinetics do not change. Cumulation of the drug is not observed. The total systemic clearance of the active metabolites 4-MAA and 4-AA is (182.9 ± 15.1) ml/min and (55.2 ± 6.4) ml/min, respectively. Their half-life (T?) is 2.5-3.0 hours and 6-8 hours, respectively. Excreted as metabolites in the urine. In patients with impaired liver and kidney function, if the recommended dosing regimen is followed, no cumulation of the unchanged active substance is observed. Changes in pharmacokinetics in children over the age of 3 years, elderly people over the age of 70 years, as well as during pregnancy, have not been established. Indications for use acute pain after injury or surgery; renal and hepatic colic (in combination with antispasmodics); pain caused by a tumor; other acute and chronic intense pain when other therapeutic measures are not possible; fever, with the ineffectiveness of other measures. Parenteral administration of the drug used only in cases where enteral administration is not possible. Contraindications hypersensitivity to the active substance or other pyrazolone or pyrazolidine derivatives (including patients who developed agranulocytosis after using these drugs); in patients with a history of aspirin asthma or analgesic intolerance syndrome (urticaria, angioedema), i.e. in patients with bronchospasm or other forms of anaphylactoid reactions to salicylates, paracetamol or other non-narcotic analgesics such as diclofenac, ibuprofen, indomethacin or naproxen; bone marrow suppression (for example, after treatment with cytostatics) or diseases of the hematopoietic system; genetic deficiency of glucose-6-phosphate dehydrogenase ( hemolysis); acute intermittent hepatic porphyria (risk of developing an attack of porphyria); arterial hypotension and / or unstable hemodynamics; last trimester of pregnancy; breastfeeding period; newborns and children under 3 months of age or weighing less than 5 kg (no information instructions for use); children aged 3 months to 11 months for intravenous administration. With caution Prolonged alcohol abuse. Intravenous administration to patients with systolic blood pressure below 100 mm Hg. or with instability of blood circulation (for example, against the background of myocardial infarction, multiple trauma, incipient shock). Side effects The frequency of possible side effects listed below is defined as follows: very often (? 1/10), often (? 1/100 to < 1/10), infrequently (? 1/1000 to < 1/100), rarely ( ≥ 1/10,000 to < 1/1,000), very rare (< 1/10,000), unknown - cannot be estimated from the available data. Diseases of the blood and lymphatic system: rarely - leukopenia; very rarely - agranulocytosis, including fatal cases, thrombocytopenia; unknown - aplastic anemia, pancytopenia, including fatal cases. These reactions can also occur when taking anal-gin in previous cases without complications. There are several signs of an increased risk of developing agranulocytosis when taking analgin for more than a week. This reaction is dose-dependent and can develop at any time during treatment. It is manifested by high fever, chills, sore throat, difficulty swallowing, inflammation of the mouth, nose, throat, genital or anal area. In patients receiving antibiotics, these symptoms may be minimal. The erythrocyte sedimentation rate is significantly increased, the number of granulocytes is significantly reduced or completely disappear from the peripheral blood. The amount of hemoglobin, erythrocytes and platelets usually remains normal. It is necessary to immediately stop the administration of the drug, without waiting for the results of laboratory diagnostic tests in case of an unexpected deterioration in the general condition, the presence of persistent or recurrent fever, painful lesions of the mucous membrane, especially the mouth, nose and throat. With the development of pancytopenia, it is necessary to immediately stop treatment with analgin, followed by monitoring of a detailed blood test until it normalizes. Diseases of the immune system: rarely - anaphylactic or anaphylactoid reactions *; very rarely - "aspirin" asthma. Patients with intolerance to analgesics may develop asthma attacks. Frequency not known - anaphylactic shock *. * These reactions are more common with parenteral use, are serious and life-threatening, and can be fatal in some cases. They can also develop in cases where the previous use of analgin passed without complications. Such reactions can develop during the injection or immediately after taking the drug, as well as after a few hours. Preferably, these reactions develop within the first hour after administration. Milder reactions are manifested by reactions from the skin and mucous membranes (for example, itching, burning, redness, urticaria, swelling), shortness of breath and, rarely, symptoms from the gastrointestinal tract. Severe forms can be manifested by generalized urticaria, Quincke's edema (including the larynx), severe bronchospasm, cardiac arrhythmias, arterial hypotension (sometimes an increase in blood pressure may precede), vascular shock. If skin reactions occur, the use of analgin should be discontinued. From the side of the cardiovascular system: sometimes - hypotensive reactions during or after use, not associated with the use of other pharmacological agents or the development of anaphylactic / anaphylactoid reactions. Rapid intravenous administration increases the risk of developing a hypotensive reaction. In hyperthermia, the administration of the drug can lead to a critical dose-dependent decrease in blood pressure without any other symptoms of hypersensitivity reactions. Diseases of the skin and subcutaneous tissue: infrequently - fixed erythema; rarely - rash (for example, maculopapular rash); very rarely - Stevens-Johnson syndrome or toxic epidermal necrolysis (it is necessary to stop treatment, see section "Precautions"). Diseases of the kidneys and urinary tract: very rarely - a sharp deterioration in kidney function, which may be accompanied by proteinuria, oligo- or anuria, up to the development of acute renal failure, acute interstitial nephritis. General diseases and reactions at the injection site: red color of urine. Perhaps due to the presence in the urine in low concentrations of a harmless metabolite of dipyrone. PrecautionsThe painkiller contains a pyrazolone derivative - analgin, which can cause rare but life-threatening side effects in the form of shock and agranulocytosis. If the patient has an anaphylactoid reaction to analgin, it is impossible to exclude allergic reactions to other non-narcotic analgesics. In patients with anaphylactic or other immunologically mediated reactions (for example, agranulocytosis) to analgin in history, the development of cross-allergy to other pyrazolones and pyrazolidines is likely. Agranulocytosis If there are signs of agranulocytosis, thrombocytopenia, you must immediately stop taking the drug and conduct a blood test (including leukocyte formula). Treatment should be discontinued until laboratory results are available. Pancytopenia With the development of pancytopenia, treatment should be immediately discontinued, followed by a blood test until it normalizes. The patient should be informed of the need to see a doctor if signs and symptoms occur during treatment that indicate a pathological change in the blood (for example, malaise, infection, persistent fever, bruising, bleeding, pallor). Anaphylactic / anaphylactoid reactions When choosing the route of administration, it is important to remember that parenteral administration of painkillers is associated with a higher risk of anaphylactic or anaphylactoid reactions. The risk of potentially severe anaphylactoid reactions to analgin is significantly increased in patients with: asthma syndrome to analgesics or angioedema to non-narcotic analgesics; bronchial asthma, especially with concomitant rhinosinusitis and nasal polyps; chronic urticaria; intolerance to dyes (eg, tartrazine) and preservatives (eg , benzoates); alcohol intolerance. Such patients may react to alcoholic beverages, even in small quantities, with symptoms such as sneezing, watery eyes, and severe facial flushing. Such alcohol intolerance may be a sign of previously undiagnosed asthma on analgesics. Anaphylactic shock usually develops in predisposed patients. Therefore, special attention should be paid to patients with asthma or atopy. Severe skin reactions Life-threatening skin reactions such as Stevens-Johnson syndrome and toxic epidermal necrolysis have been reported with analgin. If symptoms or signs of Stevens-Johnson syndrome or toxic epidermal necrolysis appear (for example, a progressive skin rash, often with blisters or mucosal lesions), treatment with dipyrone should be stopped immediately. Patients should be aware of signs and symptoms and carefully monitor skin changes, especially during the first weeks of treatment. Isolated hypotensive reactions Analgin may lead to hypotensive reactions. These reactions may be dose dependent. Usually these reactions occur with parenteral administration, and not enteral. The risk of such reactions is also increased: with rapid intravenous injection; in patients with previous hypotension, dehydration or dehydration, unstable blood pressure, or incipient circulatory failure (for example, in patients with multiple injuries or a heart attack); in patients with high fever. Patients require careful examination and careful monitoring. Preventive measures (such as circulatory stabilization) may be necessary to reduce the risk of hypotensive reactions. In exceptional cases, analgin can be used in patients in whom a decrease in blood pressure should be avoided at all costs, for example, in severe coronary heart disease or corresponding stenosis of the cerebral arteries, only after careful monitoring of hemodynamic parameters. In patients with renal or hepatic insufficiency, the use of analgin is possible only after a thorough assessment of the benefit-risk ratio and the application of appropriate precautions (see section "Method of application and doses"). It is necessary to collect an anamnesis from the patient before the introduction of analgin. In patients with an increased risk of developing anaphylactic reactions, analgin can be used only after a thorough assessment of the benefits and risks. It is necessary to use analgin in this situation under close medical supervision and the possibility of providing emergency assistance. Prolonged use of analgin (more than 7 days). If it is necessary to regularly use analgin for more than 5 days, the picture of peripheral blood should be monitored weekly. Sharp pain in the abdomen. It is not recommended to use analgin for the relief of acute abdominal pain until its cause is clarified. Use in individuals with pathology of the cardiovascular system. Careful monitoring of hemodynamics is necessary, especially in patients with a systolic pressure level below 100 mm Hg, a history of kidney disease (pyelonephritis and glomerulonephritis), as well as in people with alcohol dependence. Pregnancy There are no adequate data on the use of analgesics during pregnancy. Metamizole crosses the placental barrier. In animal studies, analgin did not cause the development of teratogenic effects. Due to the lack of adequate studies in humans, analgin in the second and first trimester of pregnancy should be used only after a strict assessment of the benefits and risks. Despite the fact that analgin is a weak inhibitor of prostaglandin synthesis, there is a possibility of premature closure of the arterial duct and the development of perinatal complications due to a decrease in platelet aggregation in the child and mother. In this regard, analgin is contraindicated during the last trimester of pregnancy. Lactation period Analgin metabolites are excreted in breast milk, so breastfeeding should be discontinued within 48 hours after taking analgin. Use in pediatrics It is not recommended to use analgin in children in the first 3 months of life, due to the increased risk of developing impaired renal function. Influence on the ability to drive vehicles and control mechanisms The recommended dose range does not affect the concentration and reaction rate. As a precautionary measure, driving machines, vehicles, or other hazardous activities while taking high doses should be avoided. This applies in particular to the combination with alcohol. Urinary excretion of analgin biotransformation products can cause red staining of urine, which has no clinical significance and disappears after discontinuation of the drug. Interaction with other drugs Analgin may cause a decrease in the concentration of cyclosporine in the blood serum. It is necessary to monitor the concentration of cyclosporine while prescribing analgesics. With the simultaneous appointment of analgesics and chlorpromazine, severe hypothermia may develop. The appointment of metamizole while taking methotrexate may lead to an increase in hematological toxicity of methotrexate, especially in elderly patients. It is recommended that this combination be avoided. The possibility of interaction of pyrazolone derivatives with oral anticoagulants, captopril, lithium and triamterene, as well as the effect on the effectiveness of antihypertensive drugs and diuretics, has been established. The extent of the described interactions for analgin is not known. Due to potential incompatibility, it is not recommended to mix analgin injection with other drugs for injection or infusion (see also the section "Method of administration and doses"). OverdoseSymptoms: hypothermia, pronounced decrease in blood pressure, palpitations, shortness of breath, tinnitus, nausea, vomiting, gastralgia, weakness, oliguria, anuria, drowsiness, delirium, impaired consciousness, tachycardia, convulsive syndrome, possible development of acute agranulocytosis, hemorrhagic syndrome, acute renal and hepatic insufficiency, paralysis of the respiratory muscles. Treatment: forced diuresis, hemodialysis, blood alkalization, symptomatic therapy aimed at maintaining vital functions. With the development of a convulsive syndrome, intravenous administration of diazelam and high-speed barbiturates is carried out. UpakovkaPo 2 ml in glass ampoules. 10 ampoules, together with a leaflet for medical use, are placed in a cardboard box (No. 10). 10 ampoules, together with a knife for opening ampoules and a leaflet for medical use, are placed in a pack of cardboard (No. 10). Storage conditions In a place protected from light, at a temperature not exceeding 25 ° C. Keep out of the reach of children. Shelf life 3 years. Do not use the medicine after the expiration date. Terms of dispensing from pharmacies By prescription Analgin solution for intravenous and intramuscular administration 500mg/ml in ampoules 2ml №10