Baralgin M tablets 500mg, No. 20

• Severe acute or chronic pain syndrome in trauma and postoperative pain syndrome, in colic, in cancer and other conditions where other therapeutic measures are contraindicated.

• Fever resistant to other treatments.

A single dose for adults and adolescents over 15 years of age is 500 mg (1 tablet). The maximum single dose can reach 1000 mg (2 tablets). Unless otherwise prescribed, a single dose may be taken 2-3 times a day. The maximum daily dose is 2000 mg (4 tablets). Duration of admission - no more than 5 days when prescribed as an anesthetic and no more than 3 days as an antipyretic agent.

The tablets should be taken with a sufficient amount of water.

An increase in the daily dose of the drug or the duration of treatment is possible only under the supervision of a physician.

One tablet contains:

active substance: metamizole sodium - 500 mg;

Excipients:

macrogol 4000 - 47 mg, magnesium stearate - 3 mg.

- Hypersensitivity to metamizole sodium and other components of the drug, as well as other pyrazolones (phenazone, propiphenazone) or to pyrazolidines (phenylbutazone, oxyphenbutazone), including, for example, an indication of the history of the development of agranulocytosis when taking one of these drugs.

- Disorders of bone marrow hematopoiesis (for example, after treatment with cytostatics) or diseases of the hematopoietic system.

- Anamnesis indications for bronchospasm or other anaphylactic reactions (eg, urticaria, rhinitis, angioedema) while taking analgesics such as salicylates, paracetamol, diclofenac, ibuprofen, indomethacin, naproxen.

- Congenital deficiency of glucose-6-phosphate dehydrogenase (risk of hemolysis).

- Children's age (up to 15 years old).

- Pregnancy (first and third trimester).

- Lactation period.

- Acute intermittent hepatic porphyria (risk of developing porphyria attacks).

If you have any of these diseases or conditions, consult your doctor before taking this medicine.

Carefully:

- Hypotension (systolic blood pressure below 100 mm Hg), decreased circulating blood volume, hemodynamic instability (myocardial infarction, multiple trauma, incipient shock), incipient heart failure, high fever (increased risk of a sharp drop in blood pressure).

- Diseases in which a significant decrease in blood pressure may be of increased danger (patients with severe ischemic heart disease and stenosis of the arteries of the brain).

- Alcoholism.

- Bronchial asthma, especially in combination with concomitant polypous rhinosinusitis; chronic urticaria and other types of atopy (allergic diseases, in the development of which a hereditary predisposition to sensitization plays a significant role: hay fever, allergic rhinitis, etc.) (increased risk of developing anaphylactic / anaphylactoid reactions).

- Alcohol intolerance (reaction to even small amounts of certain alcoholic beverages with symptoms such as itching, watery eyes and severe facial flushing) (increased risk of anaphylactic / anaphylactoid reactions).

- Intolerance to dyes (eg tartrazine) or preservatives (eg benzoates) (increased risk of anaphylactic / anaphylactoid reactions).

- Severe impaired liver and kidney function (low doses are recommended due to the possibility of slowing down the excretion of metamizole sodium).

- Pregnancy (second trimester).

If you have any of these diseases or conditions, consult your doctor before taking this medicine.

Pharmacodynamics:

An analgesic non-narcotic agent, a pyrazolone derivative, non-selectively blocks cyclooxygenase and reduces the formation of prostaglandins from arachidonic acid.

It prevents the conduction of painful extra- and proprioceptive impulses along the Gaulle and Burkhard beams, increases the excitability threshold of thalamic centers of pain sensitivity, increases heat transfer.

A distinctive feature is the insignificant severity of the anti-inflammatory effect, which causes a weak effect on water-salt metabolism (retention of sodium and water ions) and the mucous membrane of the gastrointestinal tract. It has analgesic, antipyretic and some antispasmodic (in relation to the smooth muscles of the urinary and biliary tract) action.

Pharmacokinetics:

Metamizole sodium is well and quickly absorbed in the gastrointestinal tract. After oral administration, metamizole sodium is completely metabolized to form active 4-N-methylaminoantipyrine. The connection of the active metabolite with blood plasma proteins is 50-60%. Mainly excreted by the kidneys. After taking 1 g of metamizole sodium, the renal clearance for 4-N-methylaminoantipyrine was 5 + 2 ml / min. The half-life is 2.7 hours.

In therapeutic doses, it passes into breast milk.

In patients with liver cirrhosis, the half-life of 4-N-methylaminoantipyrine increased threefold and was about 10 hours.

Pregnancy and lactation:

Pregnancy

There is insufficient clinical data on the use of metamizole sodium in pregnant women, therefore, use during pregnancy is not recommended.

Breastfeeding period

Metamizole sodium metabolites penetrate into breast milk, therefore, when using the drug, as well as within 48 hours after taking / administering the last dose, it is necessary to stop breastfeeding.

Side effects:

Heart disorders

Frequency unknown: Kounis syndrome (allergic angina pectoris or allergic myocardial infarction).

Immune system disorders

Rarely: metamizole sodium can cause anaphylactic or anaphylactoid reactions that can be severe and life-threatening; in some cases, anaphylactic reactions can be fatal.

If anaphylactic / anaphylactoid reactions develop, it is necessary to immediately stop taking the drug, take measures to provide patients with emergency medical care, and conduct a detailed clinical blood test.

These reactions can occur even if the drug has been previously used many times without any complications. Such drug reactions can develop immediately or several hours after taking metamizole sodium, but they are usually observed within one hour.

Usually, milder anaphylactic or anaphylactoid reactions manifest as skin and mucosal symptoms (itching, burning, flushing, urticaria, edema), shortness of breath, or gastrointestinal complaints.

Mild reactions can progress to severe forms with generalized urticaria, severe angioedema (especially involving the larynx), severe bronchospasm, cardiac arrhythmias, a sharp decrease in blood pressure (sometimes preceded by an increase in blood pressure), and the development of circulatory shock.

Very rare: in patients with complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses, and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including a history), intolerance reactions usually manifest in the form of attacks of bronchial asthma.

Frequency unknown: anaphylactic shock.

Skin and subcutaneous tissue disorders

Uncommon: In addition to the manifestations of anaphylactic / anaphylactoid reactions on the skin and mucous membranes listed above, a fixed drug rash may occur infrequently.

Rare: rash may occur.

Very rare: Stevens-Johnson syndrome or Lyell's syndrome (toxic epidermal necrolysis) may develop.

Blood and lymphatic system disorders

Rarely: leukopenia.

Very rare: agranulocytosis (including fatal cases), thrombocygopenia.

Frequency unknown: aplastic anemia, pancytopenia, including fatal cases.

These reactions are immunological in nature. They can occur even if the drug has been previously taken many times without any complications.

Typical symptoms of agranulocytosis are lesions of the mucous membranes (mouth and pharynx, anorectal region and genitals), sore throat, fever. It should be borne in mind that if the patient receives antibiotic therapy, then the typical manifestations of agranulocytosis may be minimally pronounced. The erythrocyte sedimentation rate is significantly increased, while the enlargement of the lymph nodes is mild or absent.

Typical symptoms of thrombocytopenia are an increased tendency to bleeding and the appearance of petechiae on the skin and mucous membranes. In case of the development of the above disorders from the blood and lymphatic system, it is necessary to stop taking the drug and conduct a detailed clinical blood test (see the section 'Special instructions').

Overdose:

Symptoms

In case of an overdose, the following symptoms may appear: nausea, vomiting, abdominal pain, decreased renal function / acute renal failure with oliguria (for example, due to the development of interstitial nephritis), more rarely, symptoms from the central nervous system (dizziness, drowsiness, tinnitus, delirium, impaired consciousness, coma, convulsions) and a sharp decrease in blood pressure (sometimes progressing to shock), as well as heart rhythm disturbances (tachycardia), hypothermia, shortness of breath, acute agranulocytosis, hemorrhagic syndrome, acute liver failure, paralysis of the respiratory muscles. After taking high doses, excretion through the kidneys of a non-toxic metabolite (rubazonic acid) can cause red coloration of urine.

Treatment

If after taking the drug no more than 1-2 hours have passed, then you can induce vomiting, carry out a gastric lavage through a tube; give saline laxatives, activated charcoal. In case of overdose, forced diuresis is indicated. The main metabolite (4-N-methylaminoantipyrine) can be eliminated by hemodialysis, hemofiltration, hemoperfusion, or plasma filtration. With the development of convulsive syndrome - intravenous administration of diazepam and fast-acting barbiturates.

Interaction:

With cyclosporine

Metamizole sodium can reduce the concentration of cyclosporin in the blood serum, therefore, when they are used together, the concentration of cyclosporine should be monitored.

With other non-narcotic analgesics

The simultaneous use of metamizole sodium with other non-narcotic analgesics can lead to mutual enhancement of toxic effects.

With tricyclic antidepressants, oral contraceptives, allopurinol

Tricyclic antidepressants, oral contraceptives, allopurinol disrupt the metabolism of metamizole sodium in the liver and increase its toxicity.

With barbiturates, phenylbutazone and other inducers of liver microsomal enzymes

Barbiturates, phenylbutazone and other inducers of liver microsomal enzymes weaken the effect of sodium metamizole.

With sedatives and tranquilizers

Sedatives and tranquilizers enhance the analgesic effect of metamizole sodium. With the simultaneous use of metamizole sodium and chlorpromazine, severe hypothermia may develop.

With drugs that have a high protein binding (oral hypoglycemic agents, indirect anticoagulants, glucocorticosteroids and indomethacin)

Metamizole sodium, displacing oral hypoglycemic agents, indirect anticoagulants, glucocorticosteroid agents and indomethacin from the connection with plasma proteins, enhances their effect.

With myelotoxic drugs

Myelotoxic drugs increase the manifestation of hematotoxicity of metamizole sodium.

With methotrexate

The addition of metamizole sodium to methotrexate treatment may increase the hematotoxic effect of methotrexate, especially in elderly patients.

Therefore, this combination should be avoided.

With thiamazole and sarcolysin

Thiamazole and sarcolysin increase the risk of developing leukopenia.

With codeine, H2 blockers and propranolol

Codeine, histamine H2 receptor blockers and propranolol enhance the effects of metamizole sodium.

X-ray contrast agents, colloidal blood substitutes and penicillin should not be used during treatment with metamizole sodium (increased risk of anaphylactic / anaphylactoid reactions).

With acetylsalicylic acid

When used together, metamizole sodium can reduce the effect of acetylsalicylic acid on platelet aggregation. Therefore, this combination should be used with caution in the treatment of patients taking low doses of acetylsalicylic acid for cardioprotection (prevention of thrombus formation).

With bupropion

Metamizole sodium can reduce the concentration of bupropion in the blood, which should be taken into account with the simultaneous use of metamizole sodium and bupropion.

Special instructions:

When treating patients receiving cytostatic agents, metamizole sodium should be taken only under the supervision of a physician.

Anaphylactic / anaphylactoid reactions

The increased risk of developing hypersensitivity reactions to metamizole sodium is caused by the following conditions:

- complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including a history);

- chronic urticaria; alcohol intolerance (hypersensitivity to alcohol), against which, even when taking a small amount of some alcoholic beverages, patients experience sneezing, watery eyes and severe facial redness. Alcohol intolerance may indicate a previously unidentified aspirin asthma syndrome;

- intolerance or hypersensitivity to dyes (eg tartrazine) or preservatives (eg benzoates).

Before using metamizole sodium, it is necessary to carefully interview the patient. If the risk of developing an anaphylactoid reaction is identified, administration may be possible only after determining the risk / benefit ratio. In the case of using metamizole sodium in such patients, strict medical supervision of their condition is necessary and it is necessary to have funds to provide them with emergency assistance in the event of anaphylactic / anaphylactoid reactions.

Anaphylactic shock may occur in predisposed patients, therefore, metamizole sodium should be prescribed with caution in patients with asthma or atopy.

Severe skin reactions

With the use of metamizole sodium, life-threatening skin reactions have been described, such as Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN).

If symptoms of SJS or TEN appear (such as a progressive skin rash, often with blistering or mucosal lesions), treatment with metamizole sodium should be stopped immediately and should not be restarted.

Patients should be aware of the symptoms of these diseases. They should be closely monitored for skin reactions, especially during the first weeks of treatment.

Agranulocytosis

With prolonged use, it is necessary to control the peripheral blood picture.

Agranulocytosis may develop at any time during treatment with metamizole sodium.

ќн возникает очень редко, длитс¤ не менее недели, не зависит от дозы, может быть т¤желым, угрожать жизни и даже привести к летальному исходу.

¬ св¤зи с этим, при по¤влении симптомов возможно св¤занных с нейтропенией (лихорадки, озноба, болей в горле, затрудненного глотани¤, стоматита, эрозивно-¤звенных поражений ротовой полости, вагинита или проктита, снижени¤ количества нейтрофилов в периферической крови менее 1500/мм ), необходимо прекратить лечение препаратом и обратитьс¤ к врачу.

ѕанцитопени¤

¬ случае развити¤ панцитопении лечение следует немедленно прекратить, необходимо контролировать показатели развернутого анализа крови вплоть до их нормализации.

¬се пациенты должны быть осведомлены о том, что при по¤влении симптомов патологического изменени¤ крови (например, общего недомогани¤, инфекций, стойкой лихорадки, образовани¤ гематом, кровотечени¤, бледности) на фоне приема метамизола натри¤, следует немедленно обратитьс¤ за медицинской помощью. ќстра¤ боль в животе

Ќедопустимо использование препарата дл¤ сн¤ти¤ острых болей в животе (до вы¤снени¤ их причины).

Ќарушение функции печени и почек

” пациентов с нарушением функции печени и почек рекомендуетс¤ избегать приема метамизола натри¤ в высоких дозах из-за снижени¤ скорости выведени¤ препарата.

¬ли¤ние на способность управл¤ть трансп. ср. и мех.:

When taking the recommended doses, no undesirable effects on concentration and reactivity were noted. However, when using high doses, one should take into account the possible impairment of concentration and reactivity, which poses a risk when performing manipulations of particular importance (for example, driving a vehicle or machinery), especially after drinking alcohol.