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.

It prevents painful extra- and proprioceptive pulses along the Gaull and Burchard bundles, 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 (retention of sodium and water ions) 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:

After intravenous administration, the half-life for metamizole sodium is 14 minutes. Approximately 96% is excreted in the urine in the form of metabolites. The main metabolite (4- N-methylaminoantipyrine). When high doses are administered through the kidneys, a nontoxic metabolite (rubzanic acid) can be released that can color the urine red.

The association of the active metabolite with the blood plasma proteins is 50-60%. It is mainly excreted by the kidneys. In therapeutic doses penetrates into breast milk.

Indications:Severe acute or chronic pain syndrome with trauma and postoperative pain syndrome, with colic, with oncological diseases and other conditions, where other therapeutic measures are contraindicated.

Fever resistant to other methods of treatment.

Contraindications:

- Hypersensitivity to metamizol sodium and other components of the drug, as well as other pyrazolones (phenazone, propifenazone) 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).

- Pregnancy (first and third trimester).

- Lactation period

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

- Newborns under 3 months of age or with a body weight of less than 5 kg

- Breast children aged 3 to 12 months (contraindication only for intravenous administration).

- Arterial hypotension, instability of hemodynamics (contraindication only for intravenous administration).

Carefully:

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

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

- Alcoholism.

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

- Alcohol intolerance (reaction even to small amounts of 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 (eg 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).

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. Metamizol sodium penetrates the placenta.

During the first trimester pregnancy application metamizole sodium is contraindicated.

In the second trimester of pregnancy treatment with metamizole sodium should

be strictly medical indications if expected benefit for the mother exceeds the potential risk for the fetus. The use of metamizole sodium in the third trimester pregnancy also contraindicated: can not be excluded premature Closure of arterial (botallov) duct and perinatal complications due to influence on ability of platelets of mother and fetus to aggregation (since metamizole sodium is an inhibitor cyclooxygenase, although weak).

Breastfeeding period

Metabolites of metamizole sodium excreted in breast milk. AT the use of the drug in the period of breastfeeding, breastfeeding should be discontinued for at least 48 hours.

Dosing and Administration:

Parenteral administration of the preparation Baralgin® M is indicated only if it can not be ingested.

Before administration, the solution is recommended to be heated to body temperature.

Adults and adolescents 15 years and older: as a single dose, 1-2 ml of 50% (500 mg / ml) solution of Baralgin® M (IM or IV) is recommended, the maximum daily dose is 4 ml of the injection solution (not more than 2 g) divided by 2 -3 reception. The maximum single dose can be 1 g (2 ml of 50% solution).

Children and newborns: Baralgin® M for parenteral use can not be administered to newborns under 3 months of age or with a body weight of less than 5 kg. Children Baralgin® M is given in a dose of 50-100 mg per 10 kg of body weight (0.1 - 0.2 ml of 50% solution). A single dose can be prescribed 2-3 times a day.

For children aged 3-12 months, the introduction is only intramuscular (body weight of the child from 5 to 9 kg).

Intravenous administration should be slow: the rate of administration is not more than 1 ml (500 mg metamizol sodium) per minute, in the supine position, with control of arterial pressure, pulse and respiration rate, so that at the first signs of anaphylactic / anaphylactoid reaction stop the drug , as well as to minimize the risk of lowering blood pressure. Since a possible hypotensive effect is dose-dependent, Baralgin® M in high doses (more than 2 ml -1 g) should be administered with extreme caution.

With too rapid administration of the drug, a very sharp drop in blood pressure and shock can be observed.

Duration of treatment

In case of pain syndrome treatment duration is 1-5 days.

When used in a febrile syndrome, the duration of treatment is 1-3 days.

Side effects:

Side effects were classified according to the recommendations of the World Health Organization.

Health Organizations: 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 frequency of development of by-effects).

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

Disorders from the immune system systems

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

In case of development anaphylactic / anaphylactoid reactions are necessary immediately stop the injection, undertake activities to provide patients with emergency medical assistance, carry out a detailed clinical blood test.

These reactions can occur even if the drug was previously used many times without any complications.

Such drug reactions can develop during the injection of metamizole sodium or a few hours after its administration, but usually they are observed within one hour after the administration of the drug.

Usually softer anaphylactic and anaphylactoid reactions manifest themselves as skin symptoms and symptoms from 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 involvement of the larynx, severe bronchospasm, heart rhythm disturbances, abrupt lowering blood pressure

(which is sometimes preceded by increase in blood pressure) and the development of circulatory shock.

Rarely: in patients with 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), reactions intolerance is usually manifested in the form of asthma attacks.

Frequency unknown: anaphylactic shock.

Disturbances from the skin and under the skin tissues

Infrequently: except for manifestations anaphylactic / anaphylactoid reactions on the skin and mucous membranes shells listed above, infrequently may occur fixed drug rash.

Rarely: the emergence of rashes.

Rarely: possible development Stevens-Johnson syndrome or of Lyell's syndrome (toxic epidermal necrolysis).

Violations from the blood and lymphatic system

Rarely: leukopenia.

Rarely: agranulocytosis (including cases with a lethal outcome), thrombocytopenia.

Frequency unknown: aplastic Anemia, pancytopenia, including cases with a lethal outcome. These reactions are immunological in their nature. They can arise even in case, if previously the drug was used many times without any complications.

Typical symptoms agranulocytosis are lesions mucous membranes (oral cavity and pharynx, anorectal area and genital organs), sore throat, fever. It should be taken into account that if a patient receives antibiotic therapy, typical manifestations of agranulocytosis may be minimally expressed.

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 petechiae on the skin and mucous membranes.

In the case of the development of the above violations from the blood and lymphatic system, it is necessary to stop the use of the drug and conduct a detailed clinical analysis of the blood (see section "Special instructions").

Vascular disorders

Isolated hypotonic reactions

Infrequently: during or after administration of the drug, an isolated transient decrease in blood pressure is possible (possibly pharmacologically

conditioned and not accompanied by other manifestations of anaphylactic / anaphylactoid reactions).

Rarely: lowering of arterial pressure can be very dramatic expressed. Rapid intravenous Introduction may increase the risk development of such an antihypertensive reaction.

General disorders and disorders at the site of administration

Infrequently: at the injection site is possible soreness and local reactions (hyperemia).

Rarely: phlebitis.

Infringements from kidneys and urinary tract

Infrequently: possible staining urine in red color due to presence in the urine metabolite - gt;

Rarely: possibly acute impairment of kidney function (acute kidney failure), especially in patients with kidney disease, in some cases with oliguria, anuria or proteinuria; at individual cases may arise

acute interstitial nephritis.

Overdose:

Symptoms

In overdose may cause the following symptoms: nausea, vomiting, abdominal pain, decreased renal function / acute renal failure with oliguria (e.g., due to the development of interstitial nephritis), more rarely symptoms from the central nervous system (dizziness, somnolence, tinnitus, delirium, impaired consciousness, coma, convulsions) and a sharp decrease in blood pressure (sometimes progressing to shock), as well as cardiac arrhythmia (tachycardia), hypothermia, dyspnea, acute agranulocytosis, hemorrhagic syn rum, acute liver failure, paralysis of respiratory muscles. 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 concentration of cyclosporine in serum, so when The joint application should monitor concentrations cyclosporine.
With other non-narcotic analgesic agents
Simultaneous application metamizole sodium with other non-narcotic analgesic agents can lead to mutual increased toxic effects.
With tricyclic antidepressants, oral contraceptives, allopurinol
Tricyclic antidepressants, oral contraceptives, allopurinol disrupt metabolism 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 are highly associated with plasma proteins (oral hypoglycemic agents, indirect anticoagulants, glucocorticosteroids and indomethacin)

Metamizole sodium, displacing from the connection with plasma proteins, oral
hypoglycemic agents, indirect anticoagulants, glucocorticosteroids and indomethacin, enhances their effect.
With myelotoxic drugs
Myelotoxic medicinal means increase manifestation hematotoxicity of metamizole sodium.
With methotrexate
Addition of metamizole sodium to can be treated with methotrexate hematotoxic action of methotrexate, especially in elderly patients.
Therefore, this combination follows to avoid.
With thiamazole and sarcolysin
Thiamazole and sarcolysin increase the risk of developing leukopenia.
With codeine, blockers H2-histamine receptors and propranolol
Codeine, blockers H₂-gistaminovyh receptors and propranolol reinforce effects of metamizole sodium

With radiopaque substances, colloidal blood substitutes and penicillin
Radiopaque substances, colloid blood substitutes and Penicillin should not be used during treatment with metamizole sodium (increased risk of developing 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 acids 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 cytotoxic drugs, and children up to 5 years treatment with metamizole sodium should only be conducted under supervision of a doctor.

Anaphylactic / anaphylactoid reactions

When choosing the mode of administration should be taken into account that parenteral application is associated with higher risk emergence 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 is necessary strict medical supervision of their state, and it is necessary to have means to provide them with urgent development assistance anaphylactic / anaphylactoid reactions.

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, possibly 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 1500 / mm³), it is necessary to stop treatment with the drug and consult a doctor.

Pancytopenia

In the case of pancytopenia, treatment should be stopped immediately, need to monitor exponents of detailed analysis

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 of treatment. blood up to 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 seek medical help immediately.Hypotensive reactions The introduction of metamizole sodium can induce individual hypotensive reaction. These reactions, perhaps, depend on the dose of the drug and more often occur after parenteral introduction. In order to avoid development severe hypotensive reactions must adhere to following recommendations:

- intravenous administration of the drug should be implemented slowly; patients with hypotension, decrease in volume circulating blood,

dehydration, instability hemodynamics or with the initial stage of insufficiency blood circulation is required normalization of hemodynamics;
- in the treatment of patients with high body temperature should be respected caution.
In these patients, the indication of use of metamizole sodium should be chosen especially Caution.
With the administration of the drug Baralgin® M in similar conditions need a close medical supervision. For reduce the risk of hypotensive reactions may be required preventive activities (stabilization hemodynamics). Metamizole sodium follows use only with careful control of hemodynamics of patients, which should be avoided blood pressure, for example, patients with severe ischemic heart disease or stenosis vessels that supply blood brain.

Acute abdominal pain

It is inadmissible to use the drug to relieve acute pain in the abdomen (until finding out their cause). Impaired liver and kidney function

In patients with impaired liver and kidney function, it is recommended that metamizole sodium should not be taken at high doses due to a decrease in the rate of drug clearance.

For intramuscular injection, a needle should be used for intramuscular injection.

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 high doses are used, consideration should be given to the possible violation of concentration and reactivity,which poses a risk when performing manipulations of particular importance (for example, driving a vehicle or machinery), especially after taking alcohol.

Form release / dosage:

Solution for intravenous and intramuscular injection 500 mg / ml.

Packaging:5 ml in dark glass ampoules (type I). 5 ampoules per plastic circuitcell packaging without a coating (pallet). 1 pallet together 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 / 02

Date of registration:06.05.2016

The owner of the registration certificate:Sanofi India LimitedSanofi India Limited India

Manufacturer: & nbsp

SANOFI INDIA, Limited India

Information update date: & nbsp28.08.2016

Illustrated instructions

Instructions

Baralgin® M (Baralgin® M)

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