Theophedrin-N^® (Tablets) Instructions for Use

Marketing Authorization Holder

Endocrine Technologies, LLC (Russia)

Manufactured By

Moscow Endocrine Plant FSUE (Russia)

Contact Information

MOSKHIMFARMPREPARATY im. N.A.Semashko JSC (Russia)

ATC Code

R03DA54 (Theophylline in combination with other drugs, except psycholeptics)

Dosage Form

Theophedrin-N®

Tablets: 10 or 20 pcs.

Dosage Form, Packaging, and Composition

Tablets white with a grayish or beige tint, with inclusions, flat-cylindrical in shape, with a bevel and a score line.

Excipients: calcium stearate, potato starch, polyvinylpyrrolidone (povidone), stearic acid.

10 pcs. – contour cell packs (1) – cardboard packs.
10 pcs. – contour cell packs (2) – cardboard packs.

Clinical-Pharmacological Group

Bronchodilator drug

Pharmacotherapeutic Group

Combined bronchodilator agent

Pharmacological Action

A combined drug that has a bronchodilating and antispasmodic effect.

The bronchodilating effect of the drug is due to the combination of methylxanthine derivatives (theophylline, caffeine) with the sympathomimetic ephedrine and the m-cholinolytic atropine, which is the main active principle of the belladonna extract.

Phenobarbital eliminates CNS excitation.

The drug increases the lumen of the bronchi, dilates the vessels of the lungs and lowers pressure in the pulmonary circulation, stimulates the respiratory center, dilates the coronary vessels and increases the frequency and strength of heart contractions, increases renal blood flow and has a moderate diuretic effect. Due to the presence of paracetamol in the composition, Theophedrin-N^® has antipyretic and analgesic effects.

Pharmacokinetics

After oral administration, Paracetamol is well absorbed from the gastrointestinal tract. C_max in blood plasma is reached within 1 hour. Paracetamol metabolites are excreted within 1-4 hours, mainly in the urine. T_1/2 of the unchanged drug from blood plasma is about 3 hours. This indicator increases in case of liver and/or kidney failure, as well as in case of overdose.

C_max of theophylline in the blood is reached 2.5 hours after taking the tablet. T_1/2 of theophylline is 11 hours, the therapeutic concentration of theophylline in the blood is 20 mcg/ml.

Atropine after oral administration is 18% bound to blood proteins, 50% is excreted by the kidneys in the urine unchanged.

Ephedrine is well absorbed from the gastrointestinal tract, creating and maintaining the necessary therapeutic level in the blood plasma. It is metabolized in the liver and excreted mainly in the urine.

Indications

As an auxiliary agent for respiratory diseases accompanied by bronchospasm, including:

• Bronchial asthma;
• Chronic obstructive bronchitis;
• Pulmonary emphysema.

ICD codes

Dosage Regimen

The drug is taken orally.

For relief of bronchial asthma attacks as an auxiliary agent, take 2 tablets of Theophedrin-N once. If necessary, the drug is used 2-3 times/day. The maximum daily dose is 3 tablets.

For preventive purposes, Theophedrin-N^® is taken orally, 1/2-1 tablet once/day after meals.

To avoid sleep disturbance, the drug should be taken in the morning or during the day. The duration of use of the drug depends on the nature, characteristics of the course of the disease and the therapeutic effect provided.

Adverse Reactions

From the cardiovascular system in isolated cases – tachycardia, cardiac arrhythmias.

From the central nervous system in isolated cases – mental agitation, tremor, headache, sleep disturbance, insomnia.

From the digestive system in isolated cases – decreased appetite, heartburn, nausea, vomiting.

Other in isolated cases – dry mouth, increased sweating, urinary retention, allergic reactions.

Contraindications

• Chronic heart failure;
• Angina pectoris;
• Impaired coronary circulation;
• Cardiac arrhythmias;
• Angle-closure glaucoma;
• Prostatic hyperplasia;
• Hyperthyroidism;
• Arterial hypertension;
• Epilepsy and other convulsive conditions;
• Pregnancy;
• Lactation period;
• Children under 18 years of age;
• Hypersensitivity to the components of the drug.

Use with caution in renal or hepatic insufficiency, diabetes mellitus, urinary disorders, tendency to develop drug dependence.

Use in Pregnancy and Lactation

The use of the drug is contraindicated during pregnancy and lactation.

Use in Hepatic Impairment

Use with caution in renal insufficiency.

Use in Renal Impairment

Use with caution in hepatic insufficiency.

Pediatric Use

Contraindicated: children under 18 years of age.

Special Precautions

To avoid sleep disturbance, the drug should not be taken in the evening.

To avoid toxic liver damage, the drug should not be combined with the intake of alcoholic beverages, and should not be taken by persons prone to regular alcohol consumption.

It is not recommended to prescribe the drug to patients with diabetes mellitus, since ephedrine, used in doses exceeding therapeutic ones, increases metabolism, thus leading to an increase in blood glucose levels.

Effect on the ability to drive vehicles and operate machinery

During the treatment period, caution should be exercised when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions. The drug contains potent components.

Overdose

Symptoms of acute poisoning: nausea, vomiting, stomach pain, insomnia, epileptiform seizures, visual impairment.

Ephedrine, used in high doses, leads to an increase in blood glucose levels. The lethal oral dose of ephedrine is 1 g.

Overdose due to paracetamol (with the development of hepatonecrosis, increased activity of liver transaminases and increased prothrombin time) manifests after taking more than 10-15 g of the latter and is unlikely due to the presence of other active components in the drug.

Treatment: gastric lavage, induced vomiting, symptomatic therapy.

Drug Interactions

Beta-blockers (propranolol), indirect anticoagulants (acenocoumarol, phenindione), carbamazepine, furosemide, cimetidine, verapamil, antibiotics (lincomycin, macrolides), fluoroquinolones (ciprofloxacin, norfloxacin), MAO inhibitors, hormonal contraceptives, glucocorticosteroids increase the concentration of theophylline in the blood and therefore may increase the risk of its side effects.

Belladonna extract weakens the effect of m-cholinomimetics and anticholinesterase agents.

Paracetamol enhances the effect of anticoagulants. The risk of hepatotoxic action of paracetamol increases with simultaneous administration of barbiturates, phenytoin, carbamazepine, rifampicin, zidovudine and other inducers of liver microsomal enzymes.

When ephedrine is used in combination with MAO inhibitors, severe hypertensive crises may occur due to suppression of the metabolism of these vasopressor substances. Ephedrine weakens the effect of opioid analgesics and other agents that depress the central nervous system. When used simultaneously with non-selective beta-blockers, the bronchodilator effect of the drug is reduced.

Storage Conditions

List of potent substances.

The drug should be stored out of the reach of children, in a dry, light-protected place at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 2 years.

Dispensing Status

The drug is dispensed by prescription.

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.