Baralgin M - instructions for use, doses, side effects, contraindications

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

Prevents painful extra- and proprioceptive impulses by to the bundles of Gaull and Burkhard, raises the threshold of excitability of 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 water-salt metabolism (sodium and water retention) and the mucous membrane of the gastrointestinal tract. Has analgesic, antipyretic and some spasmolytic (with respect to the smooth muscles of the urinary and bile ducts) action.

Pharmacokinetics:

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

In therapeutic doses penetrates into breast milk.

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

Indications:

Severe acute or chronic pain syndrome with trauma and postoperative pain syndrome, when colic, with cancer diseases and other conditions, where contraindicated other therapeutic measures.

Fever resistant to other methods treatment.

Contraindications:

- Hypersensitivity to metamizol sodium and other components of the drug, as well as other pyrazolones (phenazone, propiphenazone) or to pyrazolidines (phenylbutazone, oxyphenbutazone), including, for example, indications of an anamnesis on the development of agranulocytosis with the administration of one of these drugs.

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

- Instructions for anamnesis on bronchospasm or other anaphylactic reactions (eg urticaria, rhinitis, angioedema) with analgesics such as salicylates, paracetamol, diclofenac, ibuprofen, indomethacin, naproxen.

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

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

- Pregnancy (first and third trimester).

- Lactation period.

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

If you have one of these diseases or conditions before taking the drug consult a doctor.

Carefully:

- Dhypotension (systolic blood pressure below 100 mm Hg), a decrease in the volume of circulating blood, unstable hemodynamics (myocardial infarction, multiple trauma, beginning shock), heart failure, high fever (increased risk of a sharp drop in blood pressure).

- Diseases in which a significant reduction in blood pressure may have an increased risk (patients with severe coronary heart disease and stenosis of the cerebral arteries).

- Alcoholism.

- Bronchial asthma, especially in combination with concomitant polyposis rhinosinusitis; chronic urticaria and other types of atopy (allergic diseases, in the development of whichsignificant role belongs to hereditary predisposition to sensitization: pollinosis, allergic rhinitis and etc.) (increased risk of developing anaphylactic / anaphylactoid reactions).

- Alcohol intolerance (reaction even to small amounts certain alcoholic beverages with symptoms such as itching, lacrimation and pronounced reddening of the face) (increased risk of anaphylactic / anaphylactoid reactions).

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

- Expressed violations of the liver and kidneys (recommended the use of low doses in connection with the possibility of slowing the excretion of metamizole sodium).

- Pregnancy (second trimester).

If you have any of these diseases or conditions before taking the drug, check with your doctor.

Pregnancy and lactation:

Pregnancy

There is insufficient clinical data for the use of metamizole sodium in pregnant women, so use in pregnancy is not recommended.

Breastfeeding period

Metabolites metamizol sodium penetrate into breast milk, so when using the drug, as well as within 48 hours after the administration / administration of the last dose should be abandoned breastfeeding.

Dosing and Administration:

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

Tablets should be washed down 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.

Side effects:

Side effects were classified according to the recommendations of the World Health Organization: very often (≥10%); often (≥1%, <10%); infrequently (≥0.1%, <1%); rarely (≥0.01%, <0.1%); very rarely (<0.01%); the frequency is unknown (according to available data it is impossible to estimate the incidence of side effects).

Heart Disease

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

Immune system disorders

Rarely: metamizol sodium can cause anaphylactic or anaphylactoid reactions that can be severe and life threatening; in some cases, anaphylactic reactions can lead to death.

In case of anaphylactic / anaphylactoid reactions, it is necessary to stop taking the medication immediately, to take measures to provide patients with emergency medical care, to conduct an extensive clinical analysis of the blood.

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

Usually softer anaphylactic or anaphylactoid reactions manifest themselves as skin symptoms and symptoms on the part of the mucous membranes (itching, burning, flushing, urticaria, edema), dyspnea or complaints from the gastrointestinal tract.

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

Rarely: in patients with complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including in anamnesis), the reactions of intolerance are usually manifested in the form of attacks of bronchial asthma.

Frequency unknown: anaphylactic shock.

Disturbances from the skin and subcutaneous tissues

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

Rarely: possibly the appearance of a rash.

Rarely: possibly the development of Stevens-Johnson syndrome or Lyell syndrome (toxic epidermal necrolysis).

Violations of the blood and lymphatic system

Rarely: leukopenia.

Rarely: agranulocytosis (including fatal cases), thrombocytopenia.

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

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

Typical symptoms of agranulocytosis are mucosal lesions (oral cavity and pharynx, anorectal area and genital organs), sore throat, fever. It should be borne in mind that if a patient receives antibiotic therapy, typical manifestations of agranulocytosis may be minimal. The rate of erythrocyte sedimentation increases significantly, while the increase in lymph nodes is weak or absent.

Typical symptoms of thrombocytopenia are increased tendency to bleeding and the appearance of petechias 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 analysis of the blood (see section "Special instructions").

Overdose:

Symptoms

Overdose may cause the following symptoms: nausea, vomiting, abdominal pain, decreased kidney 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, dyspnea, acute agranulocytosis, hemorrhagic syndrome, acute liver failure, respiratory muscle paralysis. After taking high doses, the excretion through the kidneys of a non-toxic metabolite (rubanzone acid) can cause red staining of urine.

Treatment

If after taking the drug did not take more than 1-2 hours, you can induce vomiting, conduct a gastric lavage through the probe; give salt laxatives, Activated carbon. Overdose shows forced diuresis. The main metabolite (4-N-methylaminoantipyrine) can be excreted by hemodialysis, haemofiltration, hemoperfusion or plasma filtration. With the development of convulsive syndrome - intravenous diazepam and high-speed barbiturates.

Interaction:

With cyclosporine

Metamizole sodium can reduce the concentration of cyclosporine in the blood serum, so when combined, the concentrations of cyclosporin should be monitored.

With other non-narcotic analgesics

The simultaneous use of metamizole sodium with other non-narcotic analgesics can lead to a 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 microsomal liver enzymes

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

With sedatives and tranquilizers

Sedatives and tranquilizers increase the analgesic effect of metamizole sodium. With the simultaneous use of metamizole sodium and chlorpromazine can develop severe hypothermia.

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

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

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-histamine receptor blockers and propranolol

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

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

With acetylsalicylic acid

When combined metamizol 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 thrombosis). With bupropion

Metamizole sodium can reduce the concentration of bupropion in the blood, which should be taken into account when concomitantly using metamizole sodium and bupropion.

Special instructions:

In the treatment of patients receiving cytostatic agents, reception metamizole should be conducted only for supervision of a doctor.

Anaphylactic /anaphylactoid reactions

Increased risk of reactions hypersensitivity to metamizole the following condition:

complete or incomplete combination bronchial asthma, recurrent nasal polyposis and

paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including in the anamnesis);

- chronic urticaria; alcohol intolerance (hypersensitivity to

alcohol), against which, even with a small amount of some alcoholic beverages drinks, patients are sneezing, lacrimation and pronounced face redness. Intolerance alcohol can indicate previously unidentified syndrome aspirin asthma;

- intolerance or increased sensitivity to dyes (for example, tartrazine) or preservatives (for example, benzoates).

Before using metamizole it is necessary to conduct sodium careful questioning of the patient. AT case of risk development anaphylactoid reaction, reception can be possible only after the relationship risk / benefit. In the case of metamizole sodium in these patients strictly medical monitoring their condition and It is necessary to have emergency care in case of development anaphylactic / anaphylactoid reactions.

In predisposed patients, anaphylactic shock can occur, so patients with asthma or atopy metamizol sodium should be administered with caution. Severe skin reactions

Against the background of metamizole sodium have been described as threatening life skin reactions, such as Stevens-Johnson syndrome (SDS) and toxic epidermal

necrolysis (TEN). When symptoms of SSD or TES (such as progressive skin rash, often with blisters or lesions mucous membrane) treatment metamizole immediately stop, it is not should start again.

Patients should be aware of about the symptoms of these diseases. Have they should be carefully to control skin reactions, especially during the first weeks treatment.

Agranulocytosis

With prolonged use need to monitor the picture

peripheral blood. At any time against metamizole treatment sodium possible development agranulocytosis. It is very rarely lasts at least a week, not depends on the dose, maybe severe, threatening life and even lead to a fatal outcome.

In this regard, when symptoms associated with neutropenia (fevers, chills, sore throat, difficult swallowing, stomatitis, erosive-ulcerative lesions of the oral cavity, vaginitis or proctitis,

decrease in the number of neutrophils in peripheral blood less than 1500 / mm), it is necessary to stop treatment with a drug and consult a doctor.

Pancytopenia

In the case of development of pancytopenia treatment should be immediately discontinue, it is necessary monitor indicators developed blood test up to before their normalization.

All patients must be Aware that when the appearance of symptoms pathological changes in blood (for example, general malaise, infections, persistent fever, formation of hematomas, bleeding, pallor) on the background of metamizole sodium, should immediately seek medical care. Acute abdominal pain

Inadmissible use preparation for the removal of acute pain in Belly (until finding out their cause). Impaired liver and kidney function

In patients with impaired function liver and kidney is recommended avoid taking metamizole sodium in high doses due to lowering the rate of excretion of the drug.

Effect on the ability to drive transp. cf. and fur:When taking the recommended doses, there was no undesirable effect on concentration of attention and reactivity. However, when using high doses, consideration should be given to the potential for impaired concentration and reactivity, which poses a risk when performing manipulations of particular importance (for example, driving a vehicle or machinery), especially after drinking alcohol.

Form release / dosage:

Tablets 500 mg.

Packaging:

For 10 tablets in a blister of PVC / aluminum foil.

For 1, 2, 5 or 10 blisters with instructions for use in a cardboard box.

Storage conditions:

Store in a dark place at a temperature of 8 ° C to 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011538 / 01

Date of registration:05.11.2008 / 06.05.2016

Expiration Date:Unlimited

The owner of the registration certificate:Aventis Pharma LimitedAventis Pharma Limited United Kingdom

Manufacturer: & nbsp

FarmSirma Soteks, ZAO Russia

Information update date: & nbsp28.08.2016

Illustrated instructions

Instructions

Baralgin® M (Baralgin® M)