Gripocitron-broncho

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

Composition:

Active substance: butamirate;

1 ml of syrup contains 1.5 mg of citric acid butamirate;

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

Pharmaceutical form. Syrup.

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

Pharmacotherapeutic group. Agents used for cough and colds. Antitussives. ATC code R05DB13.

Pharmacological Properties

Pharmacodynamics

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

The active ingredient of the drug is butamirate citrate, which suppresses cough and differs in structure and pharmacological action from opium alkaloids. The substance is believed to act on the central nervous system. Butamirate citrate produces a nonspecific anticholinergic and bronchospasmolytic effect, thereby improving respiratory function. The drug does not cause habituation or dependence.

Butamirate citrate has a wide therapeutic range; therefore, the drug is well tolerated at therapeutic doses and is highly suitable as an antitussive agent for 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 protein-bound in the bloodstream.

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 concentrations of butamirate in blood appear within 5 to 10 minutes after administration of 22.5 mg, 45 mg, 67.5 mg, and 90 mg doses. Maximum plasma concentrations are reached within 1 hour for all four doses, with a mean peak plasma concentration of 16.1 ng/mL observed after the 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 excreted primarily via 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 influence 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 substance or to any of the excipients of the medicinal product.

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 medicinal product, which suppresses cough, may be enhanced by the effects of strong depressants, including alcohol.

Special precautions for use

Since butamirate suppresses the cough reflex, concomitant use of expectorants should be avoided, as this may lead to mucus stasis 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 mild laxative effects. 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 medicinal product contains sorbitol (E 420). If the patient has known sugar intolerance, 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 this medicinal product during pregnancy or breastfeeding has not been evaluated in specific studies. Animal studies do not indicate direct or indirect harmful effects on pregnancy or fetal health.

During pregnancy, the medicinal product should be used only on a physician's prescription and only when there are clear indications for such treatment. 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 are excreted in breast milk.

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

Ability to influence reaction speed when driving or operating machinery

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

Method of administration and dosage.

For oral use only.

Children aged 3 to 6 years: 5 ml (7.5 mg or 1 measuring spoon or 1 sachet of 5 ml) three times a day; maximum daily dose — 15 ml (22.5 mg or 3 measuring spoons or 3 sachets of 5 ml).

Children aged 6 to 12 years: 10 ml (15 mg or 2 measuring spoons or 2 sachets of 5 ml) three times a day; maximum daily dose — 30 ml (45 mg or 6 measuring spoons or 6 sachets of 5 ml).

Adolescents aged 12 years and older: 15 ml (22.5 mg or 3 measuring spoons or 3 sachets of 5 ml, or 1 sachet of 15 ml) three times a day; maximum daily dose — 45 ml (67.5 mg or 9 measuring spoons or 9 sachets of 5 ml or 3 sachets of 15 ml).

Adults: 15 ml (22.5 mg or 3 measuring spoons or 3 sachets of 5 ml, or 1 sachet of 15 ml) four times a day; maximum daily dose — 60 ml (90 mg or 12 measuring spoons or 12 sachets of 5 ml or 4 sachets of 15 ml).

The measuring spoon should be washed and dried after each use and after use by another person.

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

The medicine should preferably be taken before meals.

The lowest effective dose should be used for the shortest duration necessary to achieve the desired effect.

Do not exceed the stated dose.

Children.

The drug in this pharmaceutical form is not intended for children under 3 years of age. An alternative pharmaceutical form, namely Grippocitron-BRONCHO, oral drops, solution, may be used.

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, the patient requires symptomatic treatment and monitoring of vital functions.

Side effects.

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

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 rash, urticaria, pruritus.

Shelf life. 2 years.

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

Keep out of the reach of children.

Packaging. 100 ml or 200 ml in a bottle; 1 bottle with a measuring spoon in a cardboard box; 5 ml or 15 ml in sachets; 20 sachets in a cardboard box.

Availability category. Over-the-counter.

Manufacturer.

LIMITED LIABILITY COMPANY "CORPORATION "ZDOROV'YA".

Manufacturer's address and place of business.

22 Shevchenko Street, Kharkiv, Kharkiv Oblast, Ukraine, 61013.