Gripocitron-broncho

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT GRIPOCITRON-BRONHO (Gripocitron-BRONHO)

Composition:

Active substance: butamirate;

1 ml of syrup contains 1.5 mg of butamirate citrate;

Excipients: sorbitol (E 420), glycerin, sodium saccharin, benzoic acid (E 210), vanillin, ethanol 96%, sodium hydroxide, purified water.

Pharmaceutical form. Syrup.

Main physicochemical properties: a clear, colorless solution with a specific odor.

Pharmacotherapeutic group.

Medicinal products used for cough and colds. Antitussives.

ATC code R05D B13.

Pharmacological Properties.

Pharmacodynamics.

A non-opioid antitussive agent with central action. However, the exact mechanism of action remains unknown.

The active ingredient of the medicinal product is butamirate citrate, which suppresses cough and differs in its structure and pharmacological action from opium alkaloids. The substance is believed to act on the central nervous system. Butamirate citrate produces a non-specific anticholinergic and bronchospasmolytic effect, which improves respiratory function.

The medicinal product does not cause habituation or dependence.

Butamirate citrate has a wide therapeutic range; therefore, the medicinal product is well tolerated at therapeutic doses and is suitable for the treatment of cough in children.

Pharmacokinetics.

Butamirate is rapidly absorbed, distributed throughout the body, and subsequently hydrolyzed predominantly into 2-phenylbutyric acid and diethylaminoethoxyethanol, both of which also possess antitussive activity. 2-Phenylbutyric acid is further partially metabolized via hydroxylation. Butamirate and 2-phenylbutyric acid are highly bound to plasma proteins.

The effect of food on bioavailability has not been confirmed. The metabolism of butamirate into 2-phenylbutyric acid and diethylaminoethoxyethanol is completely proportional within the dose range of 22.5–90 mg.

Measurable plasma concentrations of butamirate are detected within 5 to 10 minutes after administration of 22.5 mg, 45 mg, 67.5 mg, and 90 mg. Maximum plasma concentrations are reached within 1 hour for all four doses; the mean maximum plasma concentration is 16.1 ng/mL following a 90 mg dose.

The mean maximum plasma concentration of 2-phenylbutyric acid is reached within 1.5 hours, with the highest exposure observed after the 90 mg dose (3052 ng/mL).

The mean maximum plasma concentration of diethylaminoethoxyethanol is reached within 0.67 hours, with the highest exposure observed after the 90 mg dose (160 ng/mL).

Metabolites are primarily excreted by the kidneys. Butamirate is detectable in urine up to 48 hours after administration. According to measurement results, the elimination half-life is 1.48–1.93 hours for butamirate, 23.26–24.42 hours for 2-phenylbutyric acid, and 2.72–2.90 hours for diethylaminoethoxyethanol.

There is no evidence of the impact of hepatic or renal impairment on the pharmacokinetic parameters of butamirate.

Clinical characteristics.

Indications.

Symptomatic treatment of cough (including dry cough) of various origins.

Contraindications.

Hypersensitivity to the active or excipient ingredients of the drug.

Interaction with other medicinal products and other forms of interaction.

Concomitant use of expectorants should be avoided. The exact mechanism of interaction with other medicinal products has not been studied, but the central mechanism of action of the drug in suppressing cough may be enhanced by the effects of strong depressants, including alcohol.

Special precautions.

Since butamirate suppresses the cough reflex, concomitant use of expectorants should be avoided, as this may lead to mucus accumulation in the airways, increasing the risk of bronchospasm and respiratory tract infection.

The syrup contains sweeteners – sodium saccharin and sorbitol, and can be prescribed to patients with diabetes. Sorbitol may cause gastrointestinal discomfort and has mild laxative effect. Should not be used in patients with fructose intolerance.

If cough persists for more than 7 days, medical advice should be sought.

Patients whose symptoms worsen or do not improve within 7 days and/or are accompanied by fever, rash, or persistent headache should undergo additional investigations to identify the underlying cause.

Keep out of reach and sight of children.

The product contains sorbitol (E 420). If the patient has known intolerance to certain sugars, consult a physician before taking this medicinal product.

This medicinal product contains a small amount of ethanol (alcohol), less than 100 mg per dose.

Use during pregnancy or breastfeeding.

The safety of using the drug during pregnancy or breastfeeding has not been evaluated in specific studies. Animal studies do not indicate direct or indirect adverse effects on pregnancy or fetal health.

During pregnancy, the drug may be used only on a physician's prescription and only when there are clear medical indications. If the expected benefit to the pregnant woman outweighs the potential risk to the fetus, the lowest effective dose and shortest possible duration of treatment should be considered.

It is unknown whether the active substance and/or its metabolites pass into breast milk.

For safety reasons, the benefits and risks of using the drug during breastfeeding should be carefully weighed. Use during breastfeeding may be considered if, in the physician’s opinion, the expected benefit to the mother exceeds the potential risk to the infant. In such cases, the lowest effective dose and shortest possible duration of treatment should be considered.

Effect on the ability to drive and operate machinery.

May cause fatigue and affect reaction ability while driving or operating machinery.

Method of Administration and Dosage

For oral use only.

Children aged 3 to 6 years: 5 mL (7.5 mg) three times daily; maximum daily dose — 15 mL (22.5 mg).

Children aged 6 to 12 years: 10 mL (15 mg) three times daily; maximum daily dose — 30 mL (45 mg).

Adolescents aged 12 years and older: 15 mL (22.5 mg) three times daily; maximum daily dose — 45 mL (67.5 mg).

Adults: 15 mL (22.5 mg) four times daily; maximum daily dose — 60 mL (90 mg).

The dosing device should be washed and dried after each use and after use by another person.

The maximum duration of treatment without a physician's prescription should not exceed 1 week.

The medicine should preferably be taken before meals.

The lowest dose necessary to achieve the therapeutic effect should be used for the shortest possible duration of treatment.

Do not exceed the recommended dose.

Children.

This medicinal formulation should not be used in children under 3 years of age. An alternative medicinal form may be used (oral drops containing butamirate citrate).

Overdose.

Overdose may cause the following symptoms: drowsiness, nausea, vomiting, diarrhea, dizziness, and arterial hypotension.

Further treatment should be carried out according to clinical indications.

There is no specific antidote for butamirate overdose. In case of overdose, symptomatic treatment and monitoring of vital functions are required.

Adverse reactions.

From the nervous system (rare: ≥ 1/10,000, < 1/1,000): dizziness, somnolence.

From the gastrointestinal tract (rare: ≥ 1/10,000, < 1/1,000): nausea, diarrhea.

From the immune system (rare: ≥ 1/10,000, < 1/1,000): anaphylactic shock.

From the skin and subcutaneous tissue (rare: ≥ 1/10,000, < 1/1,000): angioneurotic edema, skin rashes, urticaria, pruritus.

Reporting of adverse reactions.

Reporting of adverse reactions after drug registration is of great importance. It enables continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmaceutical professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of efficacy through the Automated Information System for Pharmacovigilance at the following link: https://aisf.dec.gov.ua.

Shelf life.

2 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach and sight of children.

Packaging.

100 or 200 ml in a bottle with a dosing device, in a carton.

Prescription status.

Over-the-counter.

Manufacturer.

Limited Liability Company "Kharkiv Pharmaceutical Enterprise "Zdorov'ya Narodu"".

Manufacturer's address and location of its business activities.

Ukraine, 61002, Kharkiv Oblast, Kharkiv, Kulikovska Street, 41.

Packaging from bulk produced by Limited Liability Company "Pharmaceutical Company "Zdorov'ya", Ukraine.