Pharmacode (Syrup) Instructions for Use

Marketing Authorization Holder

Pharmera LLC (Russia)

ATC Code

R05DB13 (Butamirate)

Active Substance

Butamirate (Rec.INN registered by WHO)

Dosage Form

Pharmacode

Syrup 1.5 mg/1 ml: bottle 100 ml or 200 ml

Dosage Form, Packaging, and Composition

Syrup as a colorless or slightly yellowish transparent liquid.

Excipients: liquid sorbitol (non-crystallizing) – 405 mg, glycerol – 290 mg, sodium saccharin – 0.6 mg, sodium benzoate – 1.15 mg, citric acid monohydrate – 1.2 mg, purified water – up to 1 ml.

100 ml – bottles (1) – cardboard packs.
200 ml – bottles (1) – cardboard packs.

Clinical-Pharmacological Group

Antitussive drug

Pharmacotherapeutic Group

Central antitussive agent

Pharmacological Action

Antitussive agent of central action. Butamirate is not an opium alkaloid. It does not cause dependence or addiction.

It suppresses cough by directly affecting the cough center. It has a moderate bronchodilatory effect. It facilitates breathing, improves spirometry parameters (reduces airway resistance) and blood oxygenation.

Pharmacokinetics

After oral administration, Butamirate is rapidly and completely absorbed; measurable concentrations are detected in the blood 5-10 minutes after administration.

C_max in blood plasma is reached within 1 hour. Mean plasma concentrations of 2-phenylbutyric acid are reached within 1.5 hours.

Butamirate has a large V_d in the range of 81-112 L (adjusted for body weight in kg), as well as a high degree of binding to plasma proteins. 2-phenylbutyric acid has a high degree of binding to plasma proteins – on average 89.3 – 91.6%. The ability of diethylaminoethoxyethanol to bind to plasma proteins is also detected, with average rates ranging from 28.8% to 45.7%. It is not known whether Butamirate crosses the placenta or is excreted in breast milk.

Hydrolysis of butamirate, resulting in the formation of 2-phenylbutyric acid and diethylaminoethoxyethanol, which have antitussive activity, occurs very rapidly. 2-phenylbutyric acid undergoes further partial metabolism by hydroxylation in the para position.

Excretion of the three metabolites occurs mainly through the kidneys; after conjugation in the liver, acid-reaction metabolites are largely bound to glucuronic acid. Conjugates of 2-phenylbutyric acid are detected in urine in significantly higher concentrations than in blood plasma. Butamirate is detected in urine for 48 hours. Butamirate is excreted in the urine in greater amounts as diethylaminoethoxyethanol than as unchanged Butamirate or as unconjugated 2-phenylbutyric acid.

The measured T_1/2 of 2-phenylbutyric acid, butamirate, and diethylaminoethoxyethanol is 23.26-24.42 h, 1.48-1.93 h, and 2.27-2.90 h, respectively.

Indications

Treatment of dry cough of various etiologies: for cough suppression in the pre- and postoperative period, during surgical interventions, bronchoscopy, and whooping cough.

ICD codes

Dosage Regimen

Administer orally. Use the provided measuring cup for accurate dosing.

For children aged 2 months to 3 years: administer 5 ml twice daily.

For children aged 3 to 6 years: administer 5 ml three times daily.

For children aged 6 to 12 years: administer 10 ml three times daily.

For adolescents over 12 years and adults: administer 15 ml three times daily.

Adjust the frequency of administration based on the intensity of the cough. For persistent nocturnal cough, a dose may be administered before bedtime.

The duration of treatment is typically 2-3 days. If cough persists beyond this period, consult a physician.

Do not administer to children under 2 months of age due to risk of respiratory depression.

Avoid concomitant use with mucolytics or expectorants.

Adverse Reactions

From the central nervous system rarely – drowsiness, dizziness.

From the digestive system rarely – nausea, vomiting, diarrhea.

From the skin rarely – exanthema.

Other possible development of allergic reactions.

Contraindications

Hypersensitivity to butamirate; first trimester of pregnancy, lactation period (breastfeeding); children under 2 months of age; children under 3 years of age (for syrup), children under 6 years of age (for tablets); children under 18 years of age (for modified-release tablets).

With caution

Second and third trimesters of pregnancy. Use dosage forms containing ethyl alcohol with caution in patients prone to drug dependence, with liver diseases, alcoholism, epilepsy, brain diseases, and in children.

Use in Pregnancy and Lactation

Contraindicated in the first trimester of pregnancy and during lactation (breastfeeding). In the second and third trimesters of pregnancy, use with caution and only in cases where the expected therapeutic benefit for the mother outweighs the potential risk to the fetus.

Pediatric Use

Contraindication: children under 2 months of age (for drops), under 3 years of age (for syrup), under 12 years of age (for modified-release tablets).

Special Precautions

In children, use only in dosage forms that are specifically intended for this category of patients according to age.

Effect on ability to drive vehicles and operate machinery

Butamirate can cause drowsiness, so during treatment, patients should exercise caution when driving vehicles and engaging in other activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

Since Butamirate suppresses the cough reflex, the simultaneous use of expectorants should be avoided to prevent the accumulation of sputum in the airways.

During treatment with butamirate, it is not recommended to use drugs that have a depressant effect on the central nervous system (including hypnotics, antipsychotics, tranquilizers).

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

Over-the-Counter

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.