Properties
What is it?
Sinecod Trade Name: Sinecod Active Ingredient (INN): Butamirate Dosage Form: Oral drops Composition Active ingredient: Butamirate citrate - 5 mg/ml. Excipients: Sorbitol solution 70% (w/w), Glycerin, Sodium saccharin, Benzoic acid (E 210), Vanillin, Ethanol 96% (v/v), Sodium hydroxide 30% (w/w), Purified water. Description: Clear solution, colorless, with vanilla aroma, sweet and slightly bitter. Pharmacotherapeutic group: Other antitussives. ATC code: R05DB13. See Sinecod in syrup form here: Sinecod - Sinecod Syrup 100ml Pharmacological Properties Pharmacodynamics The active ingredient of Sinecod, butamirate citrate, is an antitussive agent that is neither chemically nor pharmacologically related to opium alkaloids. Sinecod is considered a centrally acting antitussive. The exact mechanism of action is unknown. In addition to its antitussive effect, a tendency to reduce airway resistance is observed, which is manifested by a slight increase in spirometry parameters. Pharmacokinetics Pharmacokinetics are not fully known. Absorption. Based on available data, it is believed that butamirate ester is hydrolyzed to 2-phenylbutyric acid and diethylaminoethoxyethanol, and is rapidly and completely absorbed. There is no data on the alcoholic metabolite in humans. The effect of food on absorption has not been studied. The change in concentration of 2-phenylbutyric acid and diethylaminoethoxyethanol is proportional to the dose administered in the range of 22.5-90 mg. Butamirate citrate is rapidly absorbed after oral administration, with measurable concentrations detected in the blood within 5 to 10 minutes after administration of doses of 22.5 mg, 45 mg, 67.5 mg, and 90 mg. Peak plasma concentrations are reached within 1 hour for all dosage levels, with the mean value for a 90 mg oral dose being 16.058 ng/ml. Peak plasma concentrations of the main metabolite, 2-phenylbutyric acid, are reached within 1.5 hours, with the highest value observed after a 90 mg dose (3051.569 ng/ml). The mean plasma concentration of diethylaminoethoxyethanol is reached within 0.67 hours; the highest value is observed after a 90 mg dose (160.297 ng/ml). Distribution Butamirate has a large volume of distribution ranging from 80.51 to 112.339 L (adjusted for body weight in kg), as well as a high degree of plasma protein binding. 2-phenylbutyric acid has a high degree of plasma protein binding at all doses (22.5-90 mg), averaging 89.28-91.55%. Diethylaminoethoxyethanol has a lower degree of plasma protein binding, with mean values ranging from 28.80-45.72%. Metabolism Hydrolysis of butamirate, resulting in the formation of 2-phenylbutyric acid and diethylaminoethoxyethanol, occurs very rapidly. Based on studies, it is believed that both metabolites have antitussive effects. 2-phenylbutyric acid undergoes further partial metabolism by hydroxylation at the para-position. It is unknown whether butamirate crosses the placental barrier or is excreted in breast milk. Excretion. All three metabolites are primarily excreted by the kidneys; after conjugation in the liver, the acidic metabolites are significantly bound to glucuronic acid. Conjugates of 2-phenylbutyric acid are found in urine at significantly higher concentrations than in blood plasma. Butamirate is detected in urine for up to 48 hours. Butamirate excreted in urine over a 96-hour collection period accounts for approximately 0.02%, 0.02%, 0.03%, and 0.03% of the administered doses of 22.5 mg, 45 mg, 67.5 mg, and 90 mg, respectively. As a percentage, butamirate is excreted in urine in larger amounts as diethylaminoethoxyethanol or conjugated 2-phenylbutyric acid. The measured half-lives of 2-phenylbutyric acid, butamirate, and diethylaminoethoxyethanol are 23.26-24.42, 1.48-1.93, and 2.72-2.90 hours, respectively. Kinetics in Special Patient Groups. It is unknown whether impaired liver or kidney function affects the pharmacokinetic parameters of butamirate. Indications for Use Symptomatic treatment of cough of various origins. Method of Administration and Dosage For oral use only. The following dosage information is based on experience of use. There is no data from relevant studies on dose determination. The maximum duration of treatment without a doctor's prescription is 1 week (see "Special Instructions"). The lowest effective doses and the shortest duration of use should be used. For infants from 2 months to 1 year - up to 10 drops 4 times a day; For children from 1 year to 3 years - 15 drops 4 times a day; For children from 3 years and older - 25 drops 4 times a day. The use of the preparation in children under 2 years of age is possible only on the prescription of a doctor (see "Special Instructions"). 1 ml of the preparation = 20 drops. Take before meals. The drops contain saccharin and sorbitol as sweeteners, therefore they can be prescribed to patients with diabetes mellitus. Side Effects The following side effects may occur during the use of the preparation: Nervous system: Infrequently (0.1-1.0%): dizziness, drowsiness. Gastrointestinal tract: Infrequently (0.1-1.0%): nausea, diarrhea. Skin: Rarely (0.01-0.1%): rash, urticaria. If an adverse event occurs, including one not listed in this instruction, discontinue the use of the preparation and consult a doctor. Contraindications Children under 2 months of age. Hypersensitivity to the components of the preparation, fructose intolerance (the preparation contains sorbitol, a sweetener, which is metabolized to fructose). Simultaneous use of expectorants is irrational (see "Special Instructions"). Interactions with Other Medicinal Products Simultaneous use of expectorants and mucolytics should be avoided (see "Special Instructions"). Specific interaction studies have not been conducted. Due to the possible mechanism of action on the central nervous system, the potentiation of the effects of other CNS depressants, including preparations containing ethanol, cannot be excluded. Special Instructions Butamirate inhibits the cough reflex, therefore, the simultaneous use of expectorants should be avoided, as this can lead to the accumulation of sputum in the respiratory tract, increasing the risk of bronchospasm and respiratory tract infections. The use of the preparation in children under 2 years of age is possible only on the prescription of a doctor. If the condition does not improve within 7 days, or if symptoms worsen and/or fever, rash, or persistent headache occur, consult a doctor to determine the underlying causes of the symptoms. Due to the presence of sorbitol in the composition, the drops should not be taken by patients with rare hereditary disorders associated with fructose intolerance. This medicinal product contains ethanol (2.81 mg/ml). Use during pregnancy and lactation Pregnancy. No adverse effects on the fetus were observed in animal reproductive studies. Controlled studies in pregnant women have not been conducted. Therefore, Sinecod should not be used during pregnancy, except in cases of extreme necessity. Lactation. Due to the lack of data on the excretion of butamirate in breast milk, Sinecod should not be used during lactation. Effects on ability to drive or use machinery. The medicinal product may cause fatigue and affect the ability to drive or use machinery. Overdose Accidental overdose of the preparation may cause the following symptoms: drowsiness, nausea, loss of balance, vomiting, diarrhea, hypotension. Treatment: Treatment is carried out according to the clinical situation. General supportive emergency measures, observation, and maintenance of vital functions of the body if necessary are indicated. There is no specific antidote. Dosage Form 20 ml in a dark glass bottle with a dropper dispenser and a cap equipped with a first-opening control system. The bottle, along with the instructions for medical use, is placed in a cardboard box. Storage Conditions Store below 30°C. Protect from high temperatures. Keep out of reach of children. Shelf Life 3 years. Do not use after the expiry date indicated on the packaging. Dispensing from Pharmacy Pharmaceutical product group III, available without a prescription.
