Gripocitron rinis

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

Composition:

Active substances: dimetindene maleate, phenylephrine;

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

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

Pharmaceutical form. Nasal spray, solution.

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

Pharmacotherapeutic group. Decongestants and other nasal 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 passage clearance without impairing 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 persistently 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%, with a half-life of about 2.5 hours.

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

Clinical characteristics.

Indications.

Symptomatic treatment in children aged 6 years and older, and adults, of colds, 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 relief of mucosal edema of the nasal cavity and paranasal sinuses following surgical intervention.

Contraindications.

Hypersensitivity to any component of the medicinal product.

Due to the presence of phenylephrine, the medicinal 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.

The medicinal product is contraindicated in patients receiving MAO inhibitors or who have received them within the previous 14 days.

Vasoconstrictive agents should be used with caution in patients taking tricyclic and tetracyclic antidepressants and antihypertensive agents such as β-adrenoblockers, as 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 exhibit pronounced reactions to adrenergic agents, manifested by symptoms such 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 longer than 3 days or worsen, medical advice should be sought. Prolonged or excessive use of the drug may lead to tachyphylaxis and rebound effect (drug-induced 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., due to prostate hyperplasia).

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

Use during pregnancy or breastfeeding.

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

Use of the drug during breastfeeding is not recommended.

Fertility. There are no adequate data on the effects of phenylephrine and dimetindene on human fertility.

Ability to influence reaction speed when driving or operating machinery.

Not studied.

Method of Administration and Dosage

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

For children aged 6 years and older, and adults: 1–2 sprays into each nostril 3–4 times daily.

The bottle/canister should be held vertically with the spray nozzle pointing upwards. With the head held upright, insert the nozzle into the nostril and press the spray pump once with a short, sharp motion; then withdraw the nozzle from the nose and release the pump. A gentle inhalation through the nose is recommended during spraying. The duration of treatment should not exceed 3 days and depends on the severity of the illness.

Use in children aged 6 to 12 years should be under adult supervision.

Children.

This medication in the current pharmaceutical form must not be used in children under 6 years of age. An alternative pharmaceutical form should be used, namely, Grippocitron RINIS nasal drops, solution.

Overdose.

No serious adverse effects have been reported following accidental use of the medication. Accidental ingestion of up to 20 mg of dimetindene did not result in severe symptoms.

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

Treatment: administration of activated charcoal; possibly laxatives in younger children (gastric lavage is not required); in adults and older children, administration of large amounts of fluids for drinking.

Phenylephrine-induced arterial hypertension can be managed by using an alpha-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 prescribed by a physician, a single dose of activated charcoal.

Severe agitation and seizures should be treated with benzodiazepines.

Side effects.

The medicinal product is usually well tolerated. The adverse reactions listed below are categorized by frequency as follows: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1,000 to < 1/100), rare (≥ 1/10,000 to < 1/1,000), very rare (< 1/10,000), frequency not known (cannot be estimated from the available data).

Respiratory, thoracic and mediastinal disorders: rare – nasal discomfort, dryness of the nasal cavity, epistaxis (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, pruritus, 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 spray nozzle and protective cap in a box; 15 ml in a canister with a spray nozzle and protective cap in a box.

Classification. Over-the-counter (without prescription).

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVIYA".

Manufacturer's address and location of business activity.

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