Sinekod, syrup 1.5 mg/ml 200 ml

Pharmacotherapeutic group
Anticough agent of central action.

Pharmacodynamics
Butamirat, the active ingredient of Sinekod, is an anti-cough medicine of central action. It does not relate to opium alkaloids neither chemically nor pharmacologically. It is not addictive or addictive.

It suppresses cough, has a direct effect on the coughing center. It has a bronchodilator effect (dilates the bronchi). Helps ease breathing, improving spirometry (reduces airway resistance) and blood oxygenation (saturates blood with oxygen).

Pharmacokinetics

Intake

Based on available data, butamyrate ester is believed to be rapidly and completely absorbed and hydrolyzed in plasma, converting to 2-phenyl butyric acid and diethylaminoethoxyethanol. The effect of food on absorption has not been studied. Changes in the concentration of 2-phenyl butyric acid and diethylaminoethoxyethanol are proportional to the amount of dose taken, ranging from 22.5 mg to 90 mg. Butamirate is rapidly and completely absorbed when ingested, with measurable concentrations detected in the blood 5 to 10 minutes after doses of 22.5 mg, 45 mg, 1 hour at all 4 dose levels, averaging 16.1 ng/ml at an oral dose of 90 mg.

Average plasma concentrations of 2-phenyl butyric acid are reached within 1.5 hours; maximum concentration was observed after 90 mg dose (3052 ng/ml); average plasma concentrations of diethylaminoethoxyethanol are reached within 0.67 h; Cmax is observed after 90 mg dose (160 ng/ml).

Distribution

Butamirate has a large volume of distribution in the range of 81 – 112 L (adjusted for body weight in kg), and a high degree of binding to plasma proteins. 2-phenyl butyric acid has a high degree of binding to plasma proteins at all dosage levels (22.5 to 90 mg) and averages 89.3% to 91.6%. Diethylaminoethoxyethanol’s ability to bind to plasma proteins is also found, averaging between 28.8% and 45.7%. It is not known whether butamyrate penetrates the placenta or is excreted with the mother’s milk.

Metabolism

Hydrolysis of butamyrate, which produces 2-phenyl butyric acid and diethylaminoethoxyethanol, which have anti-cough effects, occurs very rapidly. 2-phenyl butyric acid undergoes further partial metabolism by hydroxylation at the para-position.

The excretion of the three metabolites occurs mainly through the kidneys; after conjugation in the liver, the acidic metabolites are largely bound to glucuronic acid. Conjugates of 2-phenyl butyric acid are detected in the urine in much higher concentrations than in plasma. Butamirate is detectable in the urine within 48 hours; butamirate excreted in the urine during the 96-hour sampling period accounts for approximately 0.02, 0.02, 0.03 and 0.03% of the 22.5 mg, 45 mg, 67.5 mg and 90 mg doses, respectively.

The percentage of butamirate excreted in the urine is greater in the form of diethylaminoethoxyethanol than butamirate unchanged or unconjugated 2-phenyl butyric acid.

The measured half-life of 2-phenyl butyric acid, butamyrate, and diethylaminoethoxyethanol is 23.26-24.42, 1.48-1.93, and 2.72-2.90 h, respectively.

Indications

Active ingredient

Composition

Active ingredient – butamirate citrate – 0.150 (1.5 mg/ml).

Auxiliary substances: sorbitol solution 70% m/m 40.50, glycerol 29.00, sodium saccharinate 0.06, benzoic acid 0.115, vanillin 0.06, ethanol 96% vol./vol.t0.25, sodium hydroxide 30% m/m 0.031, water to 100 ml.

How to take, the dosage

Special Instructions

Synopsis

Contraindications

Side effects

Overdose

Symptoms: drowsiness, nausea, vomiting, diarrhea, dizziness and decreased blood pressure.

Treatment: gastric lavage, administration of activated charcoal, maintenance of vital body functions. There is no special antidote.

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