Caffeine, Metamizole Sodium

Instruction manual

For medical use of the drug

Structure:

Active substances:

1 tablet contains metamizole sodium salt (in terms of 100% dry matter) - 300 mg, caffeine-sodium benzoate (with 40% caffeine content) (in terms of 100% dry matter) - 50 mg;

excipients: microcrystalline cellulose, povidone, magnesium stearate.

Dosage form.

Tablets.

Basic physical and chemical properties: round tablets, white or yellowish-white, with beveled edges (chamfered) and notch.

Pharmacotherapeutic group.

Analgesics and antipyretics. metamizole sodium, combinations without psycholeptics. code atx n02b b52.

Pharmacological properties.

Pharmacodynamics

Cofalgin is a combined drug whose action is due to the properties of the components that make up its composition.

Metamizole sodium - an analgesic-antipyretic, a derivative of pyrazolone, has an analgesic, antipyretic and weak anti-inflammatory effect, the mechanism of which is associated with inhibition of prostaglandin synthesis mainly in the central nervous system.

Caffeine, a derivative of methylxanthine, stimulates the psychomotor centers of the brain, has an analeptic effect, enhances the effect of metamizole sodium, eliminates drowsiness and a feeling of fatigue, and increases physical and mental performance.

Pharmacokinetics

Not studied.

Clinical characteristics.

Indications.

Moderately expressed pain syndrome, headache, neuralgia, arthritis, myositis, rheumatism; as an antipyretic for fever of various origins.

Contraindications

• Hypersensitivity to any component of the drug; hypersensitivity to pyrazolone derivatives, other xanthine derivatives (theophylline, aminophylline, theobromine); arterial hypertension; glaucoma; increased irritability; sleep disturbances; severe impaired liver and kidney function; inhibition of hematopoiesis, blood diseases: anemia of any etiology, cytostatic or infectious neutropenia, agranulocytosis, leukopenia; bronchial asthma; suspected acute surgical pathology; organic diseases of the cardiovascular system (including acute myocardial infarction, severe atherosclerosis); prostate hypertrophy with urinary retention; glucose-6-phosphate dehydrogenase deficiency; elderly age.

Do not use with monoamine oxidase inhibitors (MAOs) and within 2 weeks after discontinuation of MAO inhibitors.

Interaction with other drugs and other types of interactions.

Barbiturates, codeine, paracetamol, H2-blockers of histamine receptors, anaprilin: enhancing their effects.

Sarkolizin, merkazolil, Thiamazole, drugs that inhibit bone marrow activity, including gold preparations: an increase in the likelihood of hematotoxicity, including the development of leukopenia.

Ketoconazole, disulfiram, ciprofloxacin, norfloxacin, enoxacin, pipemidic acid: it is possible to slow down the release of caffeine and increase its concentration in the blood.

Oral antidiabetic agents: increase their hypoglycemic activity.

Alcohol: increase its sedative effect.

Cyclosporine: a decrease in its concentration in blood plasma.

Ergotamine: Caffeine may enhance its effect.

Fluvoxamine: increased plasma caffeine levels.

Mexiletine: 50% reduction in caffeine excretion.

Nicotine: increased caffeine excretion rate.

Methoxalen: a decrease in the excretion of caffeine from the body with a possible increase in its effect and the development of toxic effects.

Clozapine: increased plasma concentration of clozapine.

Theophylline and other xanthines: reduced clearance of these drugs, increased risk of additive pharmacodynamic and toxic effects.

Lithium: increased excretion of lithium in the urine.

Other drugs whose effect can be changed when interacting with caffeine: idrocylamide, phenylpropanolamine, phenytoin, pentobarbital, diazepam.

MAO inhibitors, furazolidone, procarbazine and Selegiline: a dangerous increase in blood pressure is possible.

Analgesics, antipyretics: caffeine enhances their effect (improves bioavailability).

Psychostimulants, α- and β-adrenergic agonists: potentiation of their effects.

Cimetidine, hormonal contraceptives, isoniazid: increased action of caffeine.

Opioid analgesics, anxiolytics, sleeping pills and sedatives: caffeine reduces their effect.

Caffeine is an antagonist of drugs for anesthesia and other drugs that inhibit the central nervous system, a competitive antagonist of drugs of adenosine, ATP.

Thyrotropic drugs: increased thyroid effect.

Drinks and medicines containing caffeine, when used together with the drug, can lead to excessive stimulation of the central nervous system. High doses of caffeine can cause tremors and palpitations. Patients should avoid excessive consumption of coffee or tea.

Interactions that may be due to the presence of metamizole sodium

Chlorpromazine or other phenothiazine derivatives: severe hypothermia may develop.

X-ray contrast agents, colloidal blood substitutes and penicillin: should not be used during treatment with metamizole sodium.

Indirect anticoagulants, glucocorticosteroids and indomethacin: metamizole sodium increases the activity of these drugs by displacing them from their protein bond.

Phenylbutazone, other hepatoinductors: a decrease in the effectiveness of metamizole sodium.

Tricyclic antidepressants, hormonal contraceptives and allopurinol: possibly increased toxicity of metamizole sodium.

Sedatives and tranquilizers (sibazon, trioxazine), valocordin: increased analgesic effect of metamizole sodium.

Non-narcotic analgesics, other non-steroidal anti-inflammatory drugs (NSAIDs): their analgesic and antipyretic effects are potentiated and the likelihood of additive unwanted side effects increases.

Methotrexate: Metamizole in high doses can lead to an increase in the concentration of methotrexate in blood plasma and an increase in its toxic effects (primarily on the digestive tract and blood formation system).

Sulfonylamide oral hypoglycemic drugs: it is possible to enhance their hypoglycemic effect when used together with NSAIDs, including sodium metamizole.

Diuretics (furosemide): a decrease in the diuretic effect is possible.

Features of the application.

Long-term use is not recommended. do not use the drug to relieve acute abdominal pain (until the cause is clarified).

Since metamizole sodium has anti-inflammatory and analgesic properties, it can mask signs of infection, symptoms of noncommunicable diseases and complications with pain, which can complicate their diagnosis.

With caution, prescribe the drug to patients with hyperthyroidism, epilepsy, chronic respiratory tract infection, impaired renal function, with a history of kidney diseases (pyelonephritis, glomerulonephritis), with inflammatory bowel diseases, including ulcerative colitis and Crohns disease; with severe hypotension, cardiovascular insufficiency, with increased sensitivity to analgesics and NSAIDs, with allergic reactions (including hay fever) or with a preliminary history of these diseases (the risk of allergic reactions increases), while the use of cytostatic drugs (only under the supervision of a physician), with alcoholism.

With prolonged use of the drug (more than 7 days), it is necessary to control the composition of peripheral blood (due to the myelotoxicity of metamizole), kidney and liver function.

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

When using the drug, excessive consumption of coffee, strong tea, other tonic drinks, alcohol and medicines containing caffeine should be avoided.

In the case of prolonged use of the drug, the development of mental dependence is possible. A sharp cessation of treatment leads to increased inhibition of the central nervous system (drowsiness, depression).

Caffeine can cause a false increase in uric acid in the blood, as determined by the Bittner method.

Caffeine can increase levels of 5-hydroxyindoleacetic acid (5-HIAA), vanillyl mandelic acid (VMA) and urinary catecholamines, which can lead to false-positive diagnostic results for pheochromocytoma and neuroblastoma.

Use the drug with caution in patients with a history of peptic ulcer.

Patients should be warned at the beginning of treatment that with unmotivated chills, fever, sore throat, difficulty swallowing, bleeding gums, blanching of the skin, asthenia, with the development of vaginitis or proctitis, the drug should be stopped immediately. Also, the drug should be stopped at the first rash on the skin and mucous membranes. If these symptoms appear, consult a doctor immediately.

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

Use during pregnancy or lactation.

The use of the drug during pregnancy is contraindicated.

If it is necessary to use the drug, breast-feeding should be discontinued.

The ability to influence the reaction rate when driving vehicles or other mechanisms.

There is no data on the effect of the drug on the reaction rate when driving motor vehicles or other mechanisms, but the likelihood of dizziness should be considered.

Dosage and administration.

Cofalgin is prescribed for adults and children from the age of 14, 1 tablet 2-3 times a day. do not chew tablets, drink with a small amount of water. the maximum daily dose is 3 tablets.

The duration of treatment is no longer than 3 days.

If the symptoms of the disease do not disappear within 3 days, you should consult a doctor regarding further administration of the drug.

Children.

Children under 14 years of age should not be prescribed.

Overdose.

An overdose of metamizole sodium: hypothermia, palpitations, tremors, marked decrease in blood pressure, tachycardia, dysphagia, shortness of breath, tinnitus, nausea, vomiting, gastralgia / gastritis, weakness, drowsiness, delirium, impaired consciousness, convulsive syndrome; acute agranulocytosis, hemorrhagic syndrome, oliguria, anuria, acute renal or hepatic failure, and paralysis of the respiratory muscles are possible.

Caffeine overdose: gastralgia, anxiety, agitation, nervousness, dizziness, insomnia, irritability, affect state, facial flushing, psychomotor agitation, confusion, delirium, dehydration, tachycardia, arrhythmias, hyperthermia, increased urination frequency, increased respiratory rate, headache, increased tactile or pain sensitivity, tremor, or muscle twitching; nausea and vomiting, sometimes with blood, pain in the epigastric region; ringing in the ears, convulsive seizures (with acute overdose - tonic-clonic convulsions).

Treatment: gastric lavage, forced diuresis, administration of enterosorbents, support for lung ventilation and oxygenation; with convulsive seizures - intravenously diazepam, phenobarbital or phenytoin; maintaining fluid and salt balance.In severe cases, hemodialysis, hemoperfusion, peritoneal dialysis are possible. Symptomatic therapy is aimed at maintaining vital functions.

Adverse Reactions

From the immune system: possible manifestations of hypersensitivity reactions, including rashes on the skin and mucous membranes, conjunctivitis, itching, urticaria, angioedema (angioedema), bronchospasm, anaphylactic shock, Stevens-Johnson syndrome, Lyell syndrome.

From the alimentary canal: nausea, vomiting, epigastric pain, exacerbation of peptic ulcer.

From the cardiovascular system: a feeling of compression in the chest, a feeling of palpitations, tachycardia, arrhythmias, increased / decreased blood pressure.

From the side of the nervous system: dizziness, anxiety, irritability, tremor, anxiety, headache, sleep disturbances, muscle twitching, seizures, increased reflexes, tachypnea; with sudden cancellation - increased inhibition of the central nervous system with the appearance of feelings of increased fatigue, drowsiness, muscle tension, depression.

From the urinary system: usually in patients with impaired renal function and / or when excessive doses are used, transient oliguria, anuria, interstitial nephritis, proteinuria, increased creatinine clearance, increased sodium and calcium excretion are observed. It is possible to stain urine in red.

From the hepatobiliary system: hepatitis.

On the part of the blood system: with prolonged use, leukopenia, thrombocytopenia, hemolytic anemia, granulocytopenia / agranulocytosis are possible.

Laboratory indicators: there may be a false increase in uric acid in the blood, as determined by the Bittner method, hypoglycemia / hyperglycemia, a slight increase in 5-hydroxyindoleacetic acid (5-HIAA), vanillylindic acid (VMA) and catecholamines in the urine.

Others: nasal congestion, with prolonged use - a decrease in the effect of caffeine associated with the formation of new adenosine receptors, drug dependence.

Shelf life.

2 years.

Storage conditions.

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

Keep out of the reach of children.

Packaging.

10 tablets in a blister, 1 blister in a pack; 10 tablets in a blister, 2 blisters in a pack.

Vacation category.

Over the counter.

Manufacturer.

Public Joint Stock Company “Scientific-Production Center“ Borgashchov Chemical and Pharmaceutical Plant ”.

LLC Agrofarm.

The location of the manufacturer and the address of the place of business.

Ukraine, 03134, Kiev, st. peace, 17.

Ukraine, 08200, Kiev region, Irpin city, st. Central, 113-A.