GRIPOSITRON RINIS

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT GRIPOCITRON RINOSE (GRIPOCITRON RINOSE)

Composition:

Active substances: dimethindene maleate, phenylephrine;

1 ml of the preparation contains dimethindene maleate 0.25 mg, phenylephrine 2.5 mg;

Excipients: citric acid monohydrate; sodium hydrogen phosphate anhydrous; sorbitol (E 420); benzalkonium chloride; peppermint oil; purified water.

Pharmaceutical form. Nasal drops, solution.

Main physicochemical properties: clear solution, colorless to slightly yellowish, with a characteristic odor. Slight opalescence may occur.

Pharmacotherapeutic group. Decongestants and other rhinological preparations for topical use. Sympathomimetics, combinations, excluding corticosteroids. ATC code R01A B.

Pharmacological properties.

Pharmacodynamics.

A combination drug containing phenylephrine and dimetindene.

The drug reduces nasal discharge and promotes nasal decongestion without disrupting the physiological functions of the ciliated epithelium and nasal mucosa.

Phenylephrine belongs to sympathomimetic amines. It is used as a nasal decongestant with moderate vasoconstrictive action, selectively stimulating α1-adrenergic receptors of the cavernous venous tissue of the nasal mucosa. Thus, it rapidly and long-lastingly reduces swelling of the nasal mucosa and paranasal sinuses.

Dimetindene is a histamine H1-receptor antagonist with antiallergic action. It is effective at low doses and is well tolerated.

Pharmacokinetics.

The drug is administered locally; therefore, its activity does not correlate with the concentration of active substances in blood plasma.

Following accidental oral absorption, the bioavailability of phenylephrine is reduced and amounts to approximately 38% due to first-pass metabolism in the intestine and liver; the elimination half-life is approximately 2.5 hours.

Systemic bioavailability of dimetindene after oral administration in solution is approximately 70%, with an elimination half-life of approximately 6 hours.

Clinical characteristics.

Indications.

In adults and children aged 2 years and older:

symptomatic treatment of common cold, nasal congestion, acute and chronic rhinitis, seasonal (hay fever) and non-seasonal allergic rhinitis, acute and chronic sinusitis, vasomotor rhinitis. Adjunctive therapy in acute otitis media.

Preparation for nasal surgery and reduction of mucosal edema in the nose and paranasal sinuses after surgical intervention.

Contraindications.

Hypersensitivity to phenylephrine, dimetindene maleate, or any of the excipients of the medicinal product. Due to the presence of phenylephrine, the product, like other vasoconstrictive agents, is contraindicated in atrophic rhinitis, closed-angle glaucoma, and in patients receiving monoamine oxidase inhibitors (MAOIs) or who have received them within the previous 14 days.

Interaction with other medicinal products and other forms of interaction.

Concomitant use of the medicinal product with MAO inhibitors and within 14 days after their discontinuation is contraindicated.

Vasoconstrictive agents should be prescribed with caution together with tricyclic and tetracyclic antidepressants and antihypertensive agents such as β-adrenoblockers, since their concomitant use may potentiate the pressor effect of phenylephrine.

Special precautions for use.

The drug, like other sympathomimetics, should be used with caution in patients who show a marked reaction to adrenergic agents, manifested by such symptoms as insomnia, dizziness, tremor, cardiac arrhythmias, or increased arterial pressure.

The drug should not be used continuously for more than 3 days. If symptoms persist for more than 3 days or worsen, medical advice should be sought. Prolonged or excessive use of the drug may lead to tachyphylaxis and rebound effect ("rebound rhinitis").

As with other vasoconstrictive agents, the recommended dose of the drug should not be exceeded. Excessive use of the drug, especially in children and elderly patients, may result in systemic effects of the drug.

The drug should be prescribed with caution to patients with cardiovascular disorders, arterial hypertension, hyperthyroidism, diabetes mellitus, and to patients with bladder neck obstruction (e.g., prostate hyperplasia).

Due to the presence of the H1-antihistamine dimetindene maleate, the drug should be used with caution in patients with epilepsy.

Use during pregnancy or breastfeeding.

Studies on the use of phenylephrine and dimetindene maleate during pregnancy or breastfeeding have not been conducted. Due to the potential systemic vasoconstrictive effect of phenylephrine, the use of the drug during pregnancy is not recommended.

It is recommended to avoid using the drug during breastfeeding.

Fertility.

There are no adequate data on the effect of phenylephrine and dimetindene maleate on human fertility.

Ability to influence reaction speed when driving or operating machinery.

Data not available.

Method of Administration and Dosage

Before administering the medication, the nose should be thoroughly cleaned.

The patient should tilt the head backward while sitting or standing, or to the side if lying in bed. After instilling the drops, it is advisable to keep the head tilted for several minutes to allow the medication to spread within the nasal cavity.

The dropper cap should be washed and dried before screwing it back onto the bottle.

Children aged 2 to 6 years.

1–2 drops into each nostril 3–4 times daily.

Children aged 6 years and older, and adults.

3–4 drops into each nostril 3–4 times daily.

The duration of continuous treatment should not exceed 3 days and depends on the course of the illness.

Use of the medication in children aged 2 to 12 years should be performed under adult supervision.

Children. The medication is not recommended for use in children under 2 years of age.

Overdose.

In case of overdose, the medication may cause sympathomimetic and anticholinergic effects such as increased heart rate, premature ventricular contractions, occipital pain, tremor or shaking, mild tachycardia, elevated blood pressure, mydriasis, numbness, excitement, hallucinations, seizures, insomnia, and pallor. Overdose may also lead to moderate sedation, increased fatigue, coma, stomach pain, nausea, and vomiting.

No serious adverse effects have been reported following accidental ingestion of the medication. Accidental ingestion of up to 20 mg of dimetindene has not led to severe symptoms.

Treatment: administration of activated charcoal; in younger children, laxatives may be considered (gastric lavage is not required); adults and older children should be given large amounts of fluids to drink.

Phenylephrine-induced arterial hypertension, which responds poorly to benzodiazepines, can be managed using an α-adrenergic blocker.

Central anticholinergic symptoms can be treated with physostigmine. It is advisable to consult a physician regarding the use of antidotes. Since data on ingestion of dimetindene doses exceeding 20 mg are lacking, patients with significant overdose should receive medical supervision and, if deemed necessary by a physician, a single dose of activated charcoal. Severe cases of agitation and seizures should be treated with benzodiazepines.

Side effects.

The product is usually well tolerated. The side effects listed below are categorized by frequency as follows: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1000 to < 1/100), rare (≥ 1/10000 to < 1/1000), very rare (< 1/10000), frequency not known (cannot be estimated from the available data).

Respiratory system, thoracic organs and mediastinum disorders: rare – nasal discomfort, dryness of the nasal cavity, nosebleed.

General disorders and administration site conditions: rare – burning sensation at the application site, very rare – general weakness, development of allergic reactions (including local skin reactions, body itching, eyelid swelling, facial swelling).

Shelf life. 3 years.

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

Keep out of reach of children.

Packaging. 15 ml in a bottle with a dropper cap and a glass pipette, in a box.

Pharmaceutical category. Over-the-counter (without prescription).

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVIYA".

Manufacturer's address and location of business activity.

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