Sedalgin

Pharmacological properties

metamizole sodium is a pyrazolone derivative that belongs to the group of non-narcotic analgesics. It has a pronounced analgesic and antipyretic effect. does not show a hypnotic effect, does not inhibit the respiratory center, does not lead to euphoria and addiction. metamizole has an analgesic effect both of the peripheral type, inhibiting the synthesis of endogenous algogens, and the central type, inhibiting the activity of nociceptive neurons in the posterior roots of the spinal cord. an important role in the pharmacological effects of metamizole is played by its ability to suppress the activity of cog-1 and especially cog-2, which leads to a decrease in the synthesis of prostaglandins. metamizole also has a membrane stabilizing effect.

Caffeine has a slight stimulating activity relative to the central nervous system. The main effect of caffeine is a vasoconstrictor, which affects certain types of headache and hypotension. It is believed that in some painful conditions, it has a direct analgesic effect. Caffeine potentiates the action of metamizole, facilitating its penetration into the brain tissue. When combining caffeine with analgesics, a synergistic effect occurs.

Thiamine Hydrochloride (Vitamin B₁) has multilateral functions in the metabolism of the body. It is part of a number of enzymes and is the main part of the cocarboxylase molecule, which catalyzes the combustion of pyruvic acid and facilitates the breakdown of carbohydrates. Through phosphorylation, thiamine is converted into the active form, thiamine pyrophosphate, which participates as a coenzyme in the pentose phosphate cycle, decarboxylation of α-keto acids and the formation of acetyl coenzyme A in the Krebs cycle. In the nervous system, about 90% of thiamine is contained in axon mitochondria, and 10% are included in axon membranes. Contributing to the decarboxylation of pyruvic acid, it has a positive effect on the elimination of inflammatory processes of the nervous system. Thiamine facilitates the synthesis of the acetylcholine mediator and suppresses the enzyme that breaks it down - cholinesterase, thus improving the conduction of nerve impulses. When used in high doses, it has some analgesic effect.

Due to the presence of metamizole acting on the enzymes responsible for the metabolism of drugs, the pharmacokinetics of the individual components used in the complex are somewhat different from the pharmacokinetics of the drugs when they are used independently.

Pharmacokinetics The combined drug Sedalgin plus is rapidly absorbed, and its therapeutic effect appears after 1 hour.

Indications

Symptomatic treatment of pain with:

• migraines, tension headache;
• inflammatory and degenerative diseases of the musculoskeletal system;
• postoperative conditions;
• diseases of the peripheral nervous system (sciatica, plexitis, neuritis, neuralgia, polyneuritis, polyneuropathy);
• dysmenorrhea.

Application

Sedalgin plus tablets are taken orally after a meal, washed down with water.

Recommended dose for adults and children over the age of 16 years: 1 tablet 3 times a day.

The maximum dose should not exceed 6 tablets per day.

Recommended dose for children aged 12–16 years: ½ – 1 tablet 3 times a day.

The maximum dose should not exceed 4 tablets per day.

The course of treatment with Sedalgin plus is no more than 3 days.

Contraindications

Hypersensitivity to the active or excipients that make up the drug; hypersensitivity to pyrazolone derivatives (butadion, tribuzon, antipyrine) and xanthine; children under 12 years of age, old age, pregnancy and lactation; ba; leukopenia; anemia; thrombocytopenia; cytostatic or infectious neutropenia, agranulocytosis,hepatic porphyria; congenital deficiency of glucose-6-phosphate dehydrogenase; marked increase in hell, organic diseases of the cardiovascular system, including severe atherosclerosis, severe ag, acute myocardial infarction; decompensated heart failure, paroxysmal tachycardia; glaucoma; severe renal and hepatic insufficiency; irritability, insomnia; suspicion of acute surgical pathology, allergic diseases, idiosyncrasy; do not use simultaneously with monoamine oxidase inhibitors (MAO) and within 2 weeks after stopping the use of MAO inhibitors.

Side effects

Adverse reactions to the drug may be noted:

• on the part of the central nervous system: insomnia, dizziness, increased irritability, anxiety, anxiety, mild tremor, visual impairment, headache, seizures, increased reflexes, tachypnea. With prolonged uncontrolled use of the drug in high doses, addiction is possible (a decrease in the analgesic effect), dependence, therefore, with a sudden withdrawal of the drug after prolonged use, an increase in the effect on the central nervous system, increased fatigue, drowsiness, muscle tension, and depression are noted.
• hypersensitivity reactions, including a rash on the skin and mucous membranes; conjunctivitis, itching, redness, urticaria, angioedema, bronchospasm, anaphylactic shock, Lyell and Stevens-Johnson syndrome, other allergic reactions;
• on the part of the cardiovascular system: a feeling of constriction in the chest, arrhythmias, tachycardia, palpitation (flutter), increased / decreased blood pressure;
• from the hemopoietic system: with prolonged use, passing leukopenia, granulocytopenia, agranulocytosis, hemolytic and aplastic anemia, purpura, thrombocytopenia are possible;
• from the digestive and hepatobiliary system: loss of appetite, nausea, gastrointestinal discomfort, vomiting, diarrhea, cholestasis, jaundice, impaired liver function, hepatitis, exacerbation of gastritis and gastric ulcer;
• from the urinary system: the development of acute renal failure, interstitial nephritis, oliguria, anuria, increased diuresis / increased urination frequency, increased creatinine clearance, increased excretion of sodium and calcium, proteinuria, reddening of urine;
• others: nasal congestion;
• influence on laboratory test results: hypo- or hyperglycemia; effects on laboratory tests (see SPECIAL INSTRUCTIONS).

special instructions

Do not exceed recommended doses of the drug.

Use with caution in case of impaired renal and / or liver function; in the presence of a stomach ulcer and duodenal ulcer in the history of stomach diseases (achalasia, gastroesophageal reflux, stenosis of the pyloric stomach), inflammatory bowel diseases, including ulcerative colitis and Crohns disease; with prostatic hyperplasia; with chronic bronchitis and bronchospasm in the presence of hyperthyroidism; with cardiac arrhythmias, coronary heart disease, severe arterial hypotension, cardiovascular failure, severe headache of unknown etiology, with a long history of alcohol.

Do not use to eliminate acute abdominal pain (until the cause is clarified). Since metamizole sodium has anti-inflammatory and analgesic properties, the drug can mask the signs of infection, the symptoms of noncommunicable diseases and complications with pain, and may complicate their diagnosis.

The drug can affect the psychophysical state of patients while using alcohol and drugs that inhibit the central nervous system. Given this, when using the drug should refrain from drinking alcoholic beverages.

The drug can affect the central nervous system - both on the excitation and inhibition of nervous activity, as well as blood pressure, and stimulate or suppress the activity of the heart.

Do not use simultaneously with other NSAIDs and metamizole.

When using analgesics every other day or more often, the appearance or increase in the severity of an existing headache after prolonged treatment with analgesics (more than 3 months) is possible. Headache caused by overuse of analgesics should not be treated by increasing the dose. In such cases, treatment should be discontinued after consulting a doctor.

When using the drug, excessive consumption of coffee, strong tea, other tonic drinks and medicines containing caffeine should be avoided. It can cause sleep problems, tremors, tension, irritability, palpitations.

When used in children, constant medical monitoring should be carried out. It is necessary to control the qualitative and quantitative composition of peripheral blood.

Regular long-term use of the drug is not recommended due to the myelotoxicity of metamizole sodium salt.

When prescribing a longer course of treatment (more than 7 days), it is necessary to control the blood picture / qualitative and quantitative composition of peripheral blood (especially leukocyte formula), kidney and liver function.

Patients should be warned before starting treatment that if unmotivated chills, fever, sore throat, difficulty swallowing, bleeding gums, blanching of the skin, asthenia, the development of vaginitis or proctitis occur, the drug should be discontinued immediately. Also, the use of the drug must be stopped when a rash appears on the skin and mucous membranes. If these symptoms occur, consult a doctor immediately.

Excipients. Sedalgin Plus contains wheat starch, so the use of this drug is dangerous for patients with celiac disease (celiac enteropathy).

Influence on laboratory research. Metamizole sodium metabolites can change the color of urine to red, which does not have clinical significance.

Caffeine may interfere with adenosine or dipyridamole tests. Therefore, Sedalgin Plus should not be used for at least 12 hours before testing.

Caffeine can cause a false increase in the level of uric acid in the blood plasma, which is determined by the Bittner method.

Caffeine can lead to a slight increase in the concentration of 5-hydroxyindole acetic acid (5-HIAA), vanillyl mandelic acid (VMA) and catecholamines in the urine, which can lead to false-positive diagnostic results for pheochromocytoma and neuroblastoma.

Use during pregnancy and lactation. The drug is not used during pregnancy or lactation.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. During treatment, care should be taken when driving vehicles and working with mechanisms due to the possibility of developing adverse reactions from the nervous system.

Children. Do not prescribe to children under the age of 12 years.

Interactions

Ethanol enhances the analgesic effect of the drug, and caffeine reduces the effect of inhibition of central nervous system. the simultaneous use of other hepatotoxic drugs and agents that inhibit hematopoiesis should be avoided. due to the induction of liver enzymes, the activity of coumarin anticoagulants decreases. tempidone enhances and lengthens its effect. the therapeutic effect is enhanced by tricyclic antidepressants, oral contraceptives, allopurinol as a result of inhibition of enzymes and slower biotransformation of the drug. the drug does not affect the effect of uterokinetic and uterotonic agents.with simultaneous use with NSAIDs enhances their effect and toxicity in relation to the gastrointestinal tract and hematopoiesis.

The combination of Sedalgin plus with other drugs requires special attention, since metamizole, which is part of the drug, is an enzymatic inducer. With simultaneous use with other antipyretic, analgesic and anti-inflammatory drugs, the risk of developing allergic reactions and side effects increases. With the combined use of Sedalgin plus and drugs that inhibit bone marrow function, there is a possibility of damage to white blood cell cells. Antipsychotics and tranquilizers potentiate the analgesic effect of Sedalgin plus. Concomitant use with chlorpromazine can lead to hypothermia.

Some antidepressants, oral contraceptives, allopurinol slow down the breakdown of metamizole and, thus, can increase the toxicity of the drug.

The drug reduces the concentration of cyclosporin A in the blood, so it can be dangerous in the presence of transplants.

Simultaneous use with sympathomimetics may lead to central nervous system excitement.

Caffeine may enhance the effects of ergotamine; reduce the effect of opioid analgesics, anxiolytics, sleeping pills and sedatives. Caffeine is an antagonist of drugs for anesthesia and other drugs that depress the central nervous system, and a competitive antagonist of adenosine drugs. Enhances the absorption, action and toxicity of glycosides. When used with xanthine derivatives, psychostimulating agents - potentiation of their effects. It is possible to increase the thyroid effect while using caffeine with thyrotropic drugs. Cimetidine, isoniazid enhance the effect of caffeine. Caffeine reduces the concentration of lithium in the blood.

Overdose

If you accidentally take a large number of tablets, the following clinical symptoms are noted: bullous-urticaria and petechial, sometimes morbid and typhoid rashes; in some cases, anaphylactic shock, hallucinations, tremors, lesser phenomena, coma and tonic-clonic convulsions, nausea, vomiting, agitation, insomnia, headache, dizziness, tinnitus, palpitations, weakness, melena and hematemosis, in more severe cases - oliguria, up to anuria, epileptiform convulsions, agranulocytosis, aplastic and hemolytic anemia, hemorrhagic diathesis.

With an overdose of metamizole, hypothermia, a marked decrease in blood pressure, dysphagia, shortness of breath, gastralgia / gastritis, weakness, drowsiness, delirium, hemorrhagic syndrome, acute renal and hepatic failure, and respiratory muscle paralysis are also possible.

High doses of caffeine can cause pain in the epigastric region, effects on diuresis, rapid breathing, extrasystole, tachycardia or cardiac arrhythmia, effects on the central nervous system (dizziness, insomnia, nervous excitement, irritability, affect state, anxiety, tremor, convulsions).

Treatment. General measures to reduce absorption: the introduction of agents that provoke vomiting, gastric lavage, the use of activated carbon, laxatives. Symptomatic treatment is carried out. There is no specific antidote.

Storage conditions

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

Medicinal product information for healthcare professionals.