Analgin - instructions for use, dose, side effects, contraindications

Metamizole sodium - 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 Burdach beams, raises the threshold of excitability 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. Has analgesic, antipyretic and some spasmolytic (with respect to the smooth muscles of the urinary and bile ducts) action.

The effect develops 20-40 minutes after ingestion and reaches a maximum after 2 hours.

Pharmacokinetics:

Good and quickly absorbed in the gastrointestinal tract. After oral administration metamizol sodium 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 renal clearance for 4-N-methylaminoantipyrine was 5 ± 2 ml / min. Half-life is 2.7 hours.

In therapeutic concentrations 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, with colic, with oncological diseases and other conditions, where other therapeutic measures are contraindicated.

Fever resistant to other methods of treatment.

Contraindications:

- Hypersensitivity to the components of the drug;

- oppression of hematopoiesis (agranulocytosis, cytostatic or infectious neutropenia);

- hepatic and / or renal insufficiency;

- hereditary hemolytic anemia associated with a deficiency of glucose-6-phosphate dehydrogenase;

- 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 history);

- leukopenia;

- anemia;

- intolerance to fructose, glucose-galactose malabsorption;

- pregnancy (the first and third trimester), the period of breastfeeding;

- children's age till 15 years.

Carefully:

Kidney disease (pyelonephritis, glomerulonephritis, including in the anamnesis), alcoholism, a predisposition to the development of arterial hypotension, the onset of heart failure, high fever (increased risk of a sharp decrease in blood pressure), bronchial asthma, especially in conjunction with concomitant polyposis rhinosinusitis, chronic urticaria and other types of atopy (allergic diseases, in the development of which a significant role belongs to the genetic predisposition to sensitization), alcohol intolerance , intolerance to dyes or preservatives, 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.

Metamizole sodium penetrates the placenta. During the first trimester of pregnancy, you can not take Analgin. In the second trimester of pregnancy, the preparation of Analgin should be administered according to strict medical indications, and if the expected benefit for the mother exceeds the potential risk to the fetus.The use of sodium metamizole in the third trimester of pregnancy is also contraindicated: it is impossible to exclude the possibility of premature closure of the arterial (botallova) duct and perinatal complications due to influence on the ability of platelets of the mother and fetus to aggregate metamizol sodium is an inhibitor of cyclooxygenase, although it is weak).

Breastfeeding period

Metabolites of metamizole sodium are excreted in breast milk. In the case of taking the drug during breastfeeding, breastfeeding should be discontinued for at least 48 hours.

Dosing and Administration:

Inside, after eating, adults and children over 15 years of age (with a body weight> 53 kg) are prescribed 250-500 mg 2-3 times a day. The maximum single dose is 1000 mg, the daily dose is 4000 mg. The maximum effect of the drug develops, usually after 30-60 minutes. after ingestion.

Do not use (without consulting a doctor) more than 3 days when prescribed as an antipyretic agent and more than 5 days - when prescribed as an anesthetic.

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%); frequency is unknown (according to the present 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 milder anaphylactic or anaphylactoid reactions manifest themselves as skin symptoms and symptoms from the mucous membranes (itching, burning, flushing, urticaria, edema),shortness of breath 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 can 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 taking the drug and conduct a detailed clinical blood test (see section "Special instructions").

Vascular disorders

Isolated hypotonic reactions

Infrequently: after taking 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: decrease in blood pressure can be very pronounced.

Disorders from the kidneys and urinary tract

Infrequently: it is possible to stain the urine red due to the presence in the urine of the metabolite - rubanzonic acid.

Rarely: possibly acute deterioration of kidney function (acute renal failure), especially in patients with kidney disease, in some cases with oliguria, anuria or proteinuria; in some cases, acute interstitial nephritis may occur.

If any of the side effects listed in the manual are aggravated or any other side effects not indicated in the instructions are noted, the doctor should be informed immediately.

Overdose:

Symptoms: nausea, vomiting, abdominal pain, gastralgia, oliguria, hypothermia, lowering of arterial pressure, tachycardia, dyspnea, tinnitus,drowsiness, delirium, impaired consciousness, acute agranulocytosis, hemorrhagic syndrome, acute renal and / or hepatic insufficiency, convulsions, paralysis of the respiratory musculature.

Treatment: gastric lavage, saline laxatives, Activated carbon; carrying out forced diuresis, hemodialysis, 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 the drug.

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 capcolizin

Timazol 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 cytotoxic drugs, metamizole sodium intake should only be performed under the supervision of a physician.

Anaphylactic / anaphylactoid reactions

An increased risk of hypersensitivity reactions metamizol sodium stipulate the following states:

- chronic urticaria;

- Alcohol intolerance (hypersensitivity to alcohol), against which, even with the intake of a small amount of some alcoholic beverages, patients experience sneezing, lacrimation and severe reddening of the face. Alcohol intolerance may indicate a previously unidentified syndrome of aspirin asthma;

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

Before using metamizole sodium it is necessary to conduct a thorough questioning of the patient. If the risk of developing an anaphylactoid reaction is detected, admission may be possible only after determining the risk / benefit ratio.

In the case of sodium metamizole, these patients need strict medical supervision of theircondition and it is necessary to have means for rendering them emergency aid in case of development of 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

With the use of metamizole sodium, life-threatening skin reactions, such as Stevens-Johnson syndrome (SSD) and toxic epidermal necrolysis (TEN), have been described. When symptoms of SSD or TENS (such as a progressive skin rash, often with blisters or mucosal lesions) appear, treatment with methamizole should be stopped immediately, and should not be re-started. Patients should be aware of the symptoms of these diseases. They should carefully monitor skin reactions, especially during the first weeks of treatment.

Agranulocytosis

With prolonged use, it is necessary to monitor the picture of peripheral blood. At any time against the background of metamizole sodium treatment may develop agranulocytosis. It occurs very rarely, lasts at least a week, does not depend on the dose, can be severe, threaten life and even lead to death.

In this regard, the manifestation of symptoms that may be associated with neutropenia (fever, chills, sore throat, difficulty swallowing, stomatitis, erosive-ulcerous lesions of the oral cavity, vaginitis, or proctitis, reducing the number of neutrophils in the peripheral blood of less than 1500 / mm³), it is necessary to stop treatment with the drug and consult a doctor.

Pancytopenia

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

All patients should be aware that when symptoms of abnormal blood changes (eg, general malaise, infections, persistent fever, formation of hematomas, bleeding, pallor) occur with metamizole sodium, medical attention should be sought immediately.

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.

Effect on the ability to drive transp. cf.and fur:

The adverse effect of the drug on the ability to drive vehicles and other mechanisms that require concentration of attention and speed of psychomotor reactions was not reported.

Form release / dosage:

Tablets 500 mg.

Packaging:

For 20 or 30 tablets in cans of polymer complete with lids or cans of polyethylene terephthalate with the means of corking.

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

Each jar, 1, 2, 5, 10 or 20 contour mesh packages together with the instruction for use is placed in a pack of cardboard.

For 10 tablets in a contour non-cellular package of paper with a polymer coating.

It is allowed to pack 30 or 40 cans without a bundle with an equal number of instructions for use in group packaging (for hospitals).

300 or 500 contiguous cell-free packages or contiguous cell packs with an equal number of instructions for use are placed in a group package (for hospitals).

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-004375

Date of registration:12.07.2017

Expiration Date:12.07.2022

The owner of the registration certificate:IVANOVSKAYA Pharmaceutical Factory, OAO IVANOVSKAYA Pharmaceutical Factory, OAO Russia

Manufacturer: & nbsp

IVANOVSKAYA Pharmaceutical Factory, OAO Russia

Information update date: & nbsp03.10.2017

Illustrated instructions

Instructions

Analgin (Analgin)