Tetralganol^® (Tablets) Instructions for Use

Marketing Authorization Holder

FPK PharmVILAR, JSC (Russia)

Manufactured By

PharmVILAR NPO, LLC (Russia)

ATC Code

N02BB72 (Metamizole sodium in combination with psycholeptics)

Dosage Form

Tetralganol®

Tablets

Dosage Form, Packaging, and Composition

Tablets

10 pcs. – blister packs – cardboard packs (10 pcs.) – Prescription only
10 pcs. – blister packs (2 pcs.) – cardboard packs (20 pcs.) – Prescription only

Clinical-Pharmacological Group

Combination analgesic-antipyretic

Pharmacotherapeutic Group

Analgesics; other analgesics and antipyretics; pyrazolones

Pharmacological Action

A combined medicinal product that has analgesic, antipyretic, vasodilating, and antimigraine action. It relieves symptoms of the common cold and influenza.

Metamizole is an analgesic-antipyretic, a pyrazolone derivative, and has analgesic, antipyretic, and antispasmodic effects on the smooth muscles of the urinary and biliary tracts.

Codeine has a central antitussive effect (by suppressing the excitability of the cough center), as well as an analgesic effect due to the excitation of opiate receptors in various parts of the CNS, leading to the stimulation of the antinociceptive system and a change in the emotional perception of pain. It depresses respiration less than morphine and less frequently causes miosis, nausea, vomiting, and constipation (activation of opioid receptors in the intestine causes relaxation of smooth muscles, decreased peristalsis, and spasm of all sphincters). It enhances the effect of analgesics.

Caffeine stimulates the psychomotor centers of the brain, has an analeptic effect, enhances the effect of analgesics, eliminates drowsiness and fatigue, and increases physical and mental performance.

Phenobarbital is an antiepileptic agent that has sedative, hypnotic, antispasmodic, and muscle relaxant effects.

Pharmacokinetics

The components of the drug are well absorbed from the gastrointestinal tract.

Codeine binds slightly to plasma proteins. It undergoes biotransformation in the liver (10% is converted to morphine via demethylation). It is excreted by the kidneys (5-15% unchanged).

Caffeine is well absorbed in the intestine, T_1/2 is 5 hours (sometimes up to 10 hours). It is excreted mainly by the kidneys as metabolites, about 10% unchanged.

Sodium metamizole is hydrolyzed in the intestinal wall to form an active metabolite, 4-methyl-amino-antipyrine, which in turn is metabolized to 4-formyl-amino-antipyrine and other metabolites. The binding level of the active metabolite to proteins is 50-60%. Metabolites are excreted through the kidneys. In addition, they are excreted in breast milk.

Phenobarbital has a bioavailability of 80%. It is 50% bound to plasma proteins and penetrates the placenta well. It is biotransformed in the liver. The main metabolite has no pharmacological activity. It is excreted by the kidneys, including 20-25% unchanged.

Indications

Headache; toothache; myalgia; arthralgia; neuralgia; algodysmenorrhea; symptomatic therapy of influenza and acute respiratory viral infections (ARVI).

ICD codes

Dosage Regimen

Take Tetralganol^® tablets orally with a sufficient amount of water.

For adults and adolescents over 12 years of age, administer one tablet per dose.

If pain or fever persists, a second tablet may be taken after 4-6 hours.

Do not exceed three tablets within a 24-hour period.

The maximum duration of self-administered treatment without medical supervision is 3 days for fever and 5 days for pain.

Discontinue use immediately and consult a physician if symptoms persist or worsen.

For elderly patients, use with caution, considering potential for reduced drug clearance.

Avoid concomitant use with alcohol or other CNS depressants.

Do not crush or chew the tablets; swallow them whole.

Adverse Reactions

From the digestive system: nausea, vomiting, constipation.

From the CNS: dizziness, drowsiness.

From the hematopoietic system: leukopenia, granulocytopenia, agranulocytosis.

From the cardiovascular system: tachycardia.

Allergic reactions: rash, itching, urticaria.

With long-term uncontrolled use of the drug in high doses, a weakening of the analgesic effect, the development of drug dependence due to the presence of codeine, and hepatic and/or renal failure are possible.

Contraindications

Hepatic and/or renal failure; hypersensitivity to the components of the drug; bronchospasm; glucose-6-phosphate dehydrogenase deficiency; anemia, leukopenia; conditions accompanied by respiratory depression; intracranial hypertension; traumatic brain injury; arrhythmias; arterial hypotension; alcohol intoxication; pregnancy, breastfeeding period, children under 12 years of age.

With caution: elderly age.

Use in Pregnancy and Lactation

Contraindicated during pregnancy and breastfeeding.

Use in Hepatic Impairment

Contraindicated in hepatic failure.

Use in Renal Impairment

Contraindicated in renal failure.

Pediatric Use

Contraindication: children under 12 years of age.

Geriatric Use

With caution, the drug should be prescribed to elderly patients.

Special Precautions

With long-term (more than 1 week) treatment, monitoring of the peripheral blood picture and the functional state of the liver is necessary.

The drug may change the results of doping control in athletes.

Patients with atopic bronchial asthma and hay fever have an increased risk of developing allergic reactions.

Effect on the ability to drive vehicles and machinery

It is necessary to refrain from potentially hazardous activities requiring increased attention, as it slows down the speed of reactions and causes drowsiness.

Drug Interactions

With simultaneous use of drugs that depress the CNS, an enhancement of the sedative effect and a depressant effect on the respiratory center are possible.

It enhances the effect of ethanol on the psychomotor reaction.

Concomitant use with phenothiazine derivatives may lead to the development of severe hyperthermia.

With simultaneous administration of cyclosporine, its concentration in the blood decreases.

Sodium metamizole, displacing oral hypoglycemic drugs, indirect anticoagulants, corticosteroids, and indomethacin from protein binding, increases their activity.

Phenylbutazone, barbiturates, and other inducers of microsomal liver enzymes reduce the effectiveness of sodium metamizole when administered simultaneously.

Tricyclic antidepressants, oral contraceptives, allopurinol disrupt the metabolism of sodium metamizole in the liver and increase its toxicity.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.