Tempalgin® [Metamizole Sodium, Tempidone]

Pharmacological properties

metamizole sodium as an analgesic has an analgesic and anti-inflammatory effect. it inhibits the synthesis of prostaglandins, inhibiting cog, has a known membrane-stabilizing effect, inhibits the formation of endogenous pyrogens.

Tempidone has a pronounced anxiolytic activity and eliminates the state of anxiety, fear and tension. Reduces motor excitation, has a central N-anticholinergic effect, strengthens and lengthens the analgesic effect of metamizole. Tempidone favorably affects the emotional component of pain.

The combination of metamizole sodium and tempidone enhances the analgesic effect of metamizole and increases its duration of action.

Pharmacokinetics Resorption. After oral administration, metamizole is hydrolyzed in the digestive tract. Active metabolites are 4-methyl-aminoantipyrine (MAA) and 4-aminoantipyrine (AA). MAA is characterized by rapid and complete resorption. C_max in blood plasma is reached within 1-2 hours. The bioavailability of MAA is about 90%. Food does not affect the pharmacokinetics of metamizole.

Tempidone is resorbed in the upper gastrointestinal tract. Therapeutic plasma concentrations are established 30 minutes after administration.

C_max in blood plasma, 0.8 μg / ml is reached within 60 minutes.

Distribution. Metamizole sodium partially binds to plasma proteins.

Data obtained in experimental studies on animals show that the distribution of tempidone in the tissues is significant.

Metabolism. Metamizole sodium undergoes intensive metabolism in the liver. Its main metabolites - 4-MAA, 4-AA - are pharmacologically active.

It is excreted in the urine in the form of metabolites, and only 3% of the allocated amount of metamizole is detected unchanged. Metamizole metabolites are excreted in breast milk.

Tempidone is excreted unchanged in the urine, in the amount of ⅔ applied dose.

Patients with impaired liver function: T_½ active metabolite of MAA in patients with impaired liver function is lengthened by approximately 3 times. These patients are recommended treatment with metamizole in lower doses.

Patients with impaired renal function: in patients with impaired renal function, the degree of excretion of certain metabolites is reduced. These patients are recommended treatment with metamizole in lower doses.

Indications

Short-term symptomatic treatment of a mild to moderate pain syndrome in the following conditions: headache, toothache and dental procedures, myalgia, neuralgia, arthralgia.

Application

Tablets are taken orally, washed down with water, mainly after a meal.

The course of treatment should not be more than 3 days. The use of the drug for a longer period or in higher doses is possible only after consulting a doctor.

The dose depends on the severity of pain and individual sensitivity to the drug.

Adults The usual dose is 1 tablet 1-2 times a day, depending on the severity of the clinical symptoms. The maximum single dose should not exceed 1 tablet. The maximum daily dose is 2 tablets.

For dental procedures - 1 tablet 30 minutes before the intervention.

Children over the age of 15. 1 tablet per day. The maximum daily dose is 1 tablet.

Patients over the age of 65. Usually no dose reduction is required. In patients with age-related renal and hepatic impairment, treatment with the drug should be short-lived. The maximum daily dose should not exceed 2 tablets.

Patients with impaired liver function. In such patients, an increase in T is possible_½ metabolites of metamizole.In patients with moderate or severe liver damage, it is recommended to use ½ of the recommended dose for adults (maximum daily dose is 1 tablet).

Patients with impaired renal function. Metamizole and its metabolites are excreted by the kidneys. In patients with impaired renal function, treatment with Tempalgin should be carried out using ½ of the recommended dose for adults (maximum daily dose is 1 tablet).

Contraindications

Hypersensitivity to the active or auxiliary substances of the drug; hypersensitivity to other pyrazolone derivatives; acute hepatic porphyria; congenital deficiency of glucose-6-phosphate dehydrogenase (threat of hemolysis); severe kidney and / or liver disease; bone marrow dysfunction (for example, after treatment with cytostatics); diseases of the blood system (aplastic anemia, leukopenia and agranulocytosis), a change in the composition of peripheral blood; anemia of any etiology, cytostatic or infectious neutropenia; arterial hypotension with values ​​of hell 100 mm RT. st .; suspicion of acute surgical pathology.

Side effects

When using the drug tempalgin, possible side effects are more often caused by metamizole sodium.

Adverse reactions are classified by organs and systems.

From the blood system and lymphatic system: agranulocytosis, leukopenia, aplastic anemia, thrombocytopenia, hemolytic anemia. The risk of developing agranulocytosis cannot be foreseen. Agranulocytosis can also occur in patients who have used metamizole in the past without side effects. The risk of agranulocytosis increases with prolonged use (1 week) of metamizole.

On the part of the immune system: fixed drug exanthema, maculopapular rash, anaphylactic or anaphylactoid reactions. Lighter actions are manifested by typical reactions from the skin and mucous membranes - itching, burning, redness, urticaria, edema (generalized or local), dyspnea and rarely gastrointestinal disorders. Such mild reactions can go into more severe forms with generalized urticaria, severe angioedema (including laryngeal edema), severe bronchospasm, cardiac arrhythmias, decreased blood pressure (sometimes with a previous increase in blood pressure), asthmatic attack (in patients with aspirin asthma), Stevens syndrome - Johnson and Lyell, circulatory shock.

From the side of metabolism and nutrition: decreased appetite.

From the nervous system: headache, dizziness.

From the cardiovascular system: palpitation, tachycardia, cyanosis, arterial hypotension.

From the digestive tract: nausea, vomiting, pain and discomfort in the abdomen; in isolated cases - ulceration and bleeding.

On the part of the hepatobiliary system: increased levels of liver enzymes (AsAT, AlAT), cholestasis, hyperbilirubinemia.

From the kidneys and urinary tract: polyuria, oliguria, anuria, proteinuria, interstitial nephritis. When using the drug in high doses - impaired renal function.

special instructions

Tempalgin treatment (due to the content of metamizole) is carried out only for a short period when there is no alternative method of therapy.

Before treatment, patients should be warned that if bleeding from the gums, blanching of the skin, asthenia, rashes on the skin and mucous membranes occur, the drug should be stopped and a doctor should be consulted immediately.

With longer treatment with Tempalgin, it is necessary to control the blood picture, including the leukocyte formula, because of the increased risk of developing agranulocytosis.

Do not exceed recommended doses of the drug.Since metamizole has anti-inflammatory and analgesic properties, it can mask signs of infection, symptoms of noncommunicable diseases and complications of pain, which can complicate their diagnosis.

In children, it should be used under the constant supervision of a physician. It is necessary to control the qualitative and quantitative composition of peripheral blood.

It is necessary to carefully use in patients with allergic diseases, hypersensitivity to analgesics and antirheumatic drugs (intolerance to analgesics) and other drugs or food products due to an increased risk of allergic reactions and asthmatic attacks.

Caution should be used in patients of the following categories: elderly - can lead to an increase in the frequency of adverse reactions, especially from the digestive tract; with impaired renal function, with a history of kidney disease (pyelonephritis, glomerulonephritis); with inflammatory bowel diseases, including ulcerative colitis and Crohns disease; with cardiovascular failure; with chronic alcoholism.

Metamizole can provoke hypotensive reactions. Treatment with Tempalgin should be carried out with extreme caution in patients with arterial hypotension, volume deficiency or dehydration, unstable blood circulation.

With simultaneous use with alcohol, the risk of developing side effects increases.

It should be used with caution in patients with moderate to moderate hepatic impairment or renal impairment.

When taking the drug, it is possible to stain urine in red due to the excretion of the metabolite of metamizole sodium.

Do not use the drug longer than the prescribed period without consulting a doctor!

If the signs of the disease do not begin to disappear or, conversely, the health condition worsens, or undesirable effects appear, it is necessary to stop taking the drug and seek medical advice regarding further use.

Wheat starch, which is part of the drug, may contain only traces of gluten and is considered safe for people with celiac disease.

Do not exceed recommended doses of the drug.

Use in children should be under the constant supervision of a doctor.

Use during pregnancy and lactation

Pregnancy. There were no controlled clinical trials in pregnant women and there are no observational data on the use of the drug in this group. Despite the fact that metamizole is a weak inhibitor of prostaglandin synthesis, there is a possibility of premature closure of the botallal duct and perinatal complications as a result of a decrease in platelet aggregation in the fetus and mother. Treatment with the drug is contraindicated in pregnant women.

Lactation. Metamizole metabolites pass into breast milk. If treatment with Tempalgin is necessary, breast-feeding should be discontinued.

Children. Do not use in children under the age of 15 years.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. Tempalgin reduces the ability to concentrate and slows down conditioned reflexes, so it should not be prescribed to drivers of vehicles and persons whose work requires a high speed of mental and physical reactions.

Interactions

The action of tricyclic antidepressants (imipramine, amitriptyline), oral contraceptives, analgesics, allopurinol and alcohol is potentiated with the simultaneous use of tempalgin.

The simultaneous use with other analgesics and NSAIDs increases the risk of developing manifestations of hypersensitivity and other side effects.

Barbiturates, glutethimide and phenylbutazone reduce the severity and time of the pharmacodynamic effects of metamizole due to the induction of liver enzymes.

Metamizole reduces the activity of coumarin anticoagulants while using hepatic enzymes as a result of induction.

The analgesic effect of the drug is enhanced by sedatives and tranquilizers (diazepam, combined preparations containing phenobarbital, ethyl bromisovalerianate, codeine, etc.).

Metamizole reduces the concentration of cyclosporine in blood plasma.

With simultaneous use with chlorpromazine, hypothermia may occur.

Cytostatics (sacrolisin, methotrexate), gold preparations, tiamazole, chloramphenicol and other drugs that inhibit hematopoiesis enhance the myelotoxic effect of metamizole.

Caution is needed when used simultaneously with diuretics (furosemide).

Radiopaque drugs, colloidal blood substitutes, and penicillin should not be used during treatment with metamizole sodium.

Tempidone potentiates the sedative effect of sleeping pills, general anesthetics, narcotic and non-narcotic analgesics.

When used simultaneously with NSAIDs, including metamizole sodium, the hypoglycemic effect of sulfonamide oral hypoglycemic drugs is enhanced.

Overdose

Symptoms: gastrointestinal syndrome (nausea, vomiting, pain in the stomach, at high doses - hemathemesis and melena); cerebral syndrome (lesser-like phenomena, tinnitus, weakness, ataxia, drowsiness, apnea, impaired consciousness, delirium, coma with arterial hypotension and tonic-clonic convulsions); hematological syndrome (agranulocytosis, aplastic or hemolytic anemia, hemorrhagic diathesis); metabolic syndrome (metabolic alkalosis); renal (renal) syndrome (from oliguria to anuria); acute liver failure and ARF; toxic-allergic syndrome (bullous-urticarial and petechial, sometimes bark or typhoid-like rash; some patients may develop toxic-allergic shock); hypothermia, palpitations, marked decrease in hell, tachycardia, dysphagia, shortness of breath, gastralgia / gastritis, respiratory muscle paralysis.

At the first symptoms of an overdose, you must immediately seek medical help!

Treatment: symptomatic therapy - gastric lavage, monitoring of the respiratory and cardiovascular systems, fluid injection, forced diuresis, if necessary - hemodialysis.

Storage conditions

In the original packaging at a temperature not exceeding 25 ° C.