Butamirate (Solution, Drops, Syrup) Instructions for Use

Instructions
Dosage forms

ATC Code

R05DB13 (Butamirate)

Active Substance

Butamirate (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antitussive drug

Pharmacotherapeutic Group

Drugs used for cough and colds; antitussives, excluding combinations with expectorants; other antitussives

Pharmacological Action

Butamirate is a centrally acting antitussive agent. It 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 helps to facilitate 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 achieved 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.

The hydrolysis of butamirate, which results 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, metabolites with an acidic reaction 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 hours, 1.48-1.93 hours, and 2.27-2.90 hours, respectively.

Indications

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

ICD codes

Open the list of ICD codes

ICD-10 code	Indication
A37	Whooping cough
R05	Cough
Z51.4	Preparatory procedures for subsequent treatment or examination, not elsewhere classified

ICD-11 code	Indication
1C12.Z	Whooping cough, unspecified
MD12	Cough
QB9A	Preparatory procedures for subsequent treatment

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

Administer orally. Adhere strictly to the dosing schedule based on the specific formulation and patient age.

For oral drops: Children aged 2 to 6 months: administer 10 drops four times daily. Children aged 6 months to 1 year: administer 15 drops four times daily. Children aged 1 to 3 years: administer 25 drops four times daily.

For syrup: Children aged 3 to 6 years: administer 5 ml three times daily. Children aged 6 to 12 years: administer 10 ml three times daily. Adults and children over 12 years: administer 15 ml three times daily.

Measure doses accurately using the provided measuring cup or dropper. Do not exceed the recommended daily frequency or duration of treatment.

Space doses evenly throughout the day. The duration of therapy is typically short-term; do not use for persistent chronic cough without medical consultation.

Adverse Reactions

From the CNS 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 disease, 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 benefit of therapy for the mother outweighs the potential risk to the fetus.

Pediatric Use

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

Special Precautions

In children, only dosage forms specifically intended for this category of patients according to age should be used.

Effect on ability to drive vehicles and 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 30°C (86°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.

Medical Disclaimer

Brand (or Active Substance), Marketing Authorisation Holder, Dosage Form

Butamirate [Ivanovo Pharmaceutical Factory PJSC (Russia)]
Oral solution 1.5 mg/ml: 100 ml, 150 ml, or 200 ml bottle or jar

Marketing Authorization Holder

Ivanovo Pharmaceutical Factory PJSC (Russia)

Dosage Form

Butamirate

Oral solution 1.5 mg/ml: 100 ml, 150 ml, or 200 ml bottle or jar

Dosage Form, Packaging, and Composition

Oral solution transparent, colorless to pale brownish-yellow, with a vanilla odor.

	100 g
Butamirate citrate	0.15 g

Excipients : sorbitol solution non-crystallizing 70%, glycerol (glycerin), sodium saccharin dihydrate, benzoic acid, vanillin, ethanol (ethyl alcohol) 95%, sodium hydroxide solution 30%, purified water.

100 ml – bottles – cardboard packs.
100 ml – bottles (for hospitals).
150 ml – bottles – cardboard packs.
150 ml – bottles (for hospitals).
200 ml – bottles – cardboard packs.
200 ml – bottles (for hospitals).
100 ml – jars – cardboard packs.
100 ml – jars (for hospitals).
150 ml – jars – cardboard packs.
150 ml – jars (for hospitals).
200 ml – jars – cardboard packs.
200 ml – jars (for hospitals).

Butamirate [Kirov Pharmaceutical Factory, JSC (Russia)]
Oral solution 0.8 mg/ml: 50 ml, 100 ml, 150 ml, or 200 ml bottle
Oral solution 1.5 mg/ml: 50 ml, 100 ml, 150 ml, or 200 ml bottle

Marketing Authorization Holder

Kirov Pharmaceutical Factory, JSC (Russia)

Dosage Forms

	Butamirate	Oral solution 0.8 mg/ml: 50 ml, 100 ml, 150 ml, or 200 ml bottle
		Oral solution 1.5 mg/ml: 50 ml, 100 ml, 150 ml, or 200 ml bottle

Dosage Form, Packaging, and Composition

Oral solution in the form of a colorless, transparent or slightly yellowish liquid, with a characteristic odor.

	1 ml
Butamirate (as citrate)	0.8 mg

Excipients : sorbitol solution 70%, glycerol, sodium saccharin, benzoic acid, vanillin, ethanol 96%, sodium hydroxide solution 30%, purified water.

50 ml – dark glass bottles (1) – cardboard packs.
50 ml – dark glass bottles (1) – cardboard packs (with a measuring spoon or measuring cup, or measuring syringe, or cap).
50 ml – dark glass bottles (1) – cardboard packs (with a measuring syringe, adapter).
100 ml – dark glass bottles (1) – cardboard packs.
100 ml – dark glass bottles (1) – cardboard packs (with a measuring spoon or measuring cup, or measuring syringe, or cap).
100 ml – dark glass bottles (1) – cardboard packs (with a measuring syringe, adapter).
150 ml – dark glass bottles (1) – cardboard packs.
150 ml – dark glass bottles (1) – cardboard packs (with a measuring spoon or measuring cup, or measuring syringe, or cap).
150 ml – dark glass bottles (1) – cardboard packs (with a measuring syringe, adapter).
200 ml – dark glass bottles (1) – cardboard packs.
200 ml – dark glass bottles (1) – cardboard packs (with a measuring spoon or measuring cup, or measuring syringe, or cap).
200 ml – dark glass bottles (1) – cardboard packs (with a measuring syringe, adapter).

Oral solution in the form of a colorless, transparent or slightly yellowish liquid, with a characteristic odor.

	1 ml
Butamirate (as citrate)	1.5 mg

Excipients : sorbitol solution 70%, glycerol, sodium saccharin, benzoic acid, vanillin, ethanol 96%, sodium hydroxide solution 30%, purified water.

Butamirate [Kirov Pharmaceutical Factory, JSC (Russia)]
Oral drops 5 mg/ml: 20 ml or 40 ml bottle

Marketing Authorization Holder

Kirov Pharmaceutical Factory, JSC (Russia)

Dosage Form

Butamirate

Oral drops 5 mg/ml: 20 ml or 40 ml bottle

Dosage Form, Packaging, and Composition

Oral drops in the form of a transparent, colorless to slightly yellowish liquid, with a characteristic odor.

	1 ml
Butamirate (as citrate)	5 mg

Excipients : sorbitol solution 70%, glycerol, sodium saccharin, benzoic acid, vanillin, ethanol 96%, sodium hydroxide solution 30%, purified water.

20 ml – dark glass bottles (1) – cardboard packs.
20 ml – dark glass bottles (1) – cardboard packs (with a dropper/dropper cap).
40 ml – dark glass bottles (1) – cardboard packs.
40 ml – dark glass bottles (1) – cardboard packs (with a dropper/dropper cap).

Butamirate [Sintez PJSC (Russia)]
Syrup 1.5 mg/1 ml: 100 ml bottle with or without a dosing spoon.

Marketing Authorization Holder

Sintez PJSC (Russia)

Dosage Form

Butamirate

Syrup 1.5 mg/1 ml: 100 ml bottle with or without a dosing spoon.

Dosage Form, Packaging, and Composition

Syrup transparent, colorless or with a slight yellowish tint, with a vanilla odor.

	100 ml
Butamirate citrate	0.15 g

Excipients : sorbitol, glycerol (glycerin), sodium saccharin dihydrate, benzoic acid, vanillin, ethanol (ethyl alcohol), sodium hydroxide solution 30%, purified water.

100 ml – dark glass bottles (1) – cardboard packs.
100 ml – dark glass bottles (1) with a double-sided dosing spoon – cardboard packs.

Butamirate [Usolye-Sibirskiy Chemical and Pharmaceutical Plant, JSC (Russia)]
Oral solution 1.5 mg/ml: 50 ml or 100 ml bottle

Marketing Authorization Holder

Usolye-Sibirskiy Chemical and Pharmaceutical Plant, JSC (Russia)

Manufactured By

Usolye-Sibirskiy Chemical and Pharmaceutical Plant, JSC (Russia)

Dosage Form

Butamirate

Oral solution 1.5 mg/ml: 50 ml or 100 ml bottle

Dosage Form, Packaging, and Composition

Oral solution transparent colorless or with a slight yellowish tint, with a vanilla odor.

	100 ml
Butamirate citrate	0.15 g

Excipients : sorbitol liquid non-crystallizing 70% – 40.5 g, glycerol (glycerin) 85% – 29 g, sodium saccharin dihydrate – 0.06 g, benzoic acid – 0.115 g, vanillin – 0.06 g, ethanol 96% – 0.25 g, sodium hydroxide solution 30% – 0.031 g, purified water – up to 100 ml.

50 ml – dark glass bottles (1) with a measuring spoon – cardboard packs.
100 ml – dark glass bottles (1) with a measuring spoon – cardboard packs.

Butamirate Avva [Avva Rus, JSC (Russia)]
Oral solution 1.5 mg/ml

Marketing Authorization Holder

Avva Rus, JSC (Russia)

Dosage Form

Butamirate Avva

Oral solution 1.5 mg/ml

Dosage Form, Packaging, and Composition

Oral solution

	1 ml
Butamirate (as citrate)	1.5 mg

100 ml – bottles – cardboard packs /with a double-sided measuring spoon or measuring cup/ – Over-the-Counter
200 ml – bottles – cardboard packs /with a double-sided measuring spoon or measuring cup/ – Over-the-Counter

Butamirate-Pharmstandard [Pharmstandard-Lexredstva OJSC (Russia)]
Oral solution 1.5 mg/1 ml: 100 ml or 200 ml bottle with measuring spoon

Marketing Authorization Holder

Pharmstandard-Lexredstva OJSC (Russia)

Dosage Form

Butamirate-Pharmstandard

Oral solution 1.5 mg/1 ml: 100 ml or 200 ml bottle with measuring spoon

Dosage Form, Packaging, and Composition

Oral solution in the form of a transparent, colorless or with a yellowish, or with a brownish-yellow tint, viscous liquid with a cinnamon odor.

	1 ml
Butamirate (as citrate)	1.5 mg

Excipients : sorbitol (sorbitol solution 70% non-crystallizing), glycerol (glycerin), benzoic acid, sodium saccharin, sodium hydroxide*, vanillin, cinnamon flavor**, purified water.

* sodium hydroxide solution 30% is used.
** the flavor contains 1,2-propylene glycol.

100 ml – dark glass bottles (1) with a measuring spoon – cardboard packs.
200 ml – dark glass bottles (1) with a measuring spoon – cardboard packs.

Butamirate-Teva [Teva Pharmaceutical Industries, Ltd. (Israel)]
Oral solution 1.5 mg/1 ml: 100 ml or 200 ml bottle with measuring cup

Marketing Authorization Holder

Teva Pharmaceutical Industries, Ltd. (Israel)

Manufactured By

Balkanpharma-Troyan, AD (Bulgaria)

Dosage Form

Butamirate-Teva

Oral solution 1.5 mg/1 ml: 100 ml or 200 ml bottle with measuring cup

Dosage Form, Packaging, and Composition

Oral solution as a colorless or slightly yellowish liquid with a chocolate and caramel odor.

	1 ml
Butamirate (as citrate)	1.5 mg

Excipients: sorbitol (E420) – 450 mg, citric acid monohydrate, sucralose (E955), glycerol, sodium benzoate (E211) – 1 mg, caramel flavor, bitter chocolate flavor F2428, purified water.

100 ml – dark glass bottles (1) with a measuring cup – cardboard packs^×.
200 ml – dark glass bottles (1) with a measuring cup – cardboard packs^×.

^× protective stickers may be applied on the pack.