Dimetindene-zdorovya

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT DIMETINDENE-ZDOROVYE

Composition:

Active substance: dimetindene maleate;

1 ml (20 drops) of the preparation contains 1 mg of dimetindene maleate;

Excipients: sodium hydrogen phosphate, citric acid, sodium saccharin, propylene glycol, disodium edetate, benzoic acid (E 210), purified water.

Pharmaceutical form. Oral drops, solution.

Main physicochemical characteristics: colorless clear solution.

Pharmacotherapeutic group. Antihistamines for systemic use.

ATC code R06A B03.

Pharmacological properties.

Pharmacodynamics.

Dimetindene maleate is a histamine antagonist at the H1-receptor level. At low concentrations, it exerts a stimulating effect on histamine methyltransferase, leading to histamine inactivation. It exhibits high affinity for H1-receptors and acts as a mast cell stabilizer. Dimetindene maleate has no effect on H2-receptors. It also possesses local anesthetic properties.

Dimetindene maleate is an antagonist of bradykinin, serotonin, and acetylcholine. It exists as a racemic mixture with R-(-)-dimetindene, which has more pronounced H1-antihistaminic activity.

Dimetindene maleate significantly reduces capillary hyperpermeability associated with immediate-type hypersensitivity reactions.

In combination with histamine H2-receptor antagonists, it inhibits virtually all types of histamine effects on the circulation.

Studies have shown that the effect of a single 4 mg dose of dimetindene in the form of drops on skin reactions persists up to 24 hours after administration.

Pharmacokinetics.

Systemic bioavailability of dimetindene in the form of drops is approximately 70%. After administration of the drops, maximum plasma concentration of dimetindene is reached within 2 hours.

At concentrations ranging from 0.09 to 2 mcg/mL, plasma protein binding of dimetindene is approximately 90%. Metabolic reactions of dimetindene include hydroxylation and methoxylation.

Its elimination half-life is nearly 6 hours. Dimetindene and its metabolites are excreted via the liver and kidneys.

Preclinical studies revealed no risk associated with the use of the drug at recommended doses. Dimetindene maleate showed no mutagenic or clastogenic properties.

Clinical characteristics.

Indications.

Symptomatic treatment of allergic diseases: urticaria, seasonal (hay fever) and perennial allergic rhinitis, drug and food allergies.

Pruritus of various origins, except that associated with cholestasis. Pruritus in skin disorders with rashes, such as chickenpox. Insect bites.

An adjunctive agent in eczema and other pruritic dermatoses of allergic origin.

Contraindications.

Hypersensitivity to dimethindene maleate or to any other component of the medicinal product. Duodenal or pyloric stenosis.

Contraindicated in children under 1 month of age, especially premature infants.

Interaction with other medicinal products and other forms of interaction.

Concomitant use of drugs that depress the central nervous system (CNS), such as opioid analgesics, anticonvulsants, antidepressants (tricyclic antidepressants and monoamine oxidase inhibitors), other antihistamines, antiemetics, antipsychotics, anxiolytics, hypnotics, scopolamine, and ethanol, may enhance CNS depression, potentially leading to adverse effects or even life-threatening consequences.

Tricyclic antidepressants and anticholinergic drugs, such as bronchodilators, gastrointestinal spasmolytics, mydriatics, and urological antimuscarinic agents, may produce an additive antimuscarinic effect when taken together with antihistamines, thereby increasing the risk of worsening glaucoma and urinary retention.

To minimize the risk of CNS depression or possible potentiation, concomitant use of procarbazine and antihistamines should be performed with caution.

Special precautions for use.

As with other antihistamines, caution should be exercised when using Dimetinden-Zdorovya in patients with glaucoma, bladder neck contracture and/or urinary retention, including those with prostatic hyperplasia, as well as in patients with chronic obstructive lung diseases.

Like all H1-receptor antagonists and partially H2-receptor antagonists, this medication should be used with caution in patients with epilepsy. Antihistamines may cause excitation in young children.

The drug should be used cautiously in elderly patients, in whom the risk of adverse reactions, including excitation and increased fatigue, is higher. Avoid accidental misuse of the drug by elderly patients. Do not exceed the recommended dosage and duration of treatment without a physician's recommendation.

The drop formulation of the drug should be administered with caution to children under 1 year of age: sedative effects may be accompanied by episodes of nocturnal apnea. In young children, antihistamines may cause excitation.

The drug may be used in children aged 1 month to 1 year only upon a physician's recommendation and when there are clear indications for antihistamine therapy. The recommended dose must not be exceeded.

Use during pregnancy or breastfeeding.

Pregnancy. There are no clinical data on the use of the drug in pregnant women. In animal studies, the drug did not cause harmful effects (either direct or indirect) on the course of pregnancy, fetal development, or subsequent offspring development. However, during pregnancy, the drug should not be used except when the therapeutic benefit outweighs the potential risk to the fetus. In such cases, the drug may be used only under a physician's prescription.

Breastfeeding. It is highly likely that dimethindene maleate is excreted into breast milk. The drug is not recommended during breastfeeding. If treatment is necessary, breastfeeding should be discontinued for the duration of therapy.

Ability to affect reaction speed when driving or operating machinery.

The use of the drug may result in slowed psychomotor reaction speed, drowsiness, and dizziness; therefore, patients should refrain from driving a vehicle or operating machinery.

Method of Administration and Dosage.

The duration of use of the medication without consulting a doctor should not exceed 14 days.

For adults, children aged 12 years and older, and elderly patients.

The recommended daily dose is 3–6 mg, divided into 3 doses – 20–40 drops three times a day. For patients prone to drowsiness, it is recommended to take 40 drops at bedtime and 20 drops in the morning during breakfast.

Dose adjustment is not required for elderly patients.

Children.

Administration of the medication is recommended only after prior consultation with a physician. For children aged 1 month to 1 year, the medication should be used only upon a physician's recommendation. The recommended daily dose is 0.1 mg (i.e., 2 drops) per kg of body weight per day, divided into 3 doses.

20 drops = 1 ml = 1 mg of dimetindene maleate.

The medication should not be exposed to high temperatures. When adding to warm infant food, it should be mixed immediately before feeding. If the child is fed with a spoon, the medication can be administered undiluted in a teaspoon. The medication has a pleasant taste.

Children.

Do not administer to children under 1 month of age, especially premature infants. Use the drop formulation with caution in children under 1 year of age: sedative effects may be accompanied by episodes of nocturnal apnea. In younger children, antihistamine medications may cause excitation.

Dimetindene-Zdorovya can be used in children aged 1 month to 1 year only upon a physician's recommendation and when there are clear indications for antihistamine therapy. The recommended dose must not be exceeded.

Overdose.

In case of overdose with Dimetindene-Zdorovya, as with other antihistamine medications, the following symptoms may occur: central nervous system (CNS) depression and drowsiness (mainly in adults), CNS stimulation and antimuscarinic effects (especially in children and elderly patients), including excitement, ataxia, tachycardia, hallucinations, seizures, tremor, dilated pupils, dry mouth, facial flushing, urinary retention, and fever. Additionally, arterial hypotension, coma, and cardiopulmonary collapse may develop.

In case of overdose, measures recommended by the healthcare facility should be taken, depending on the symptoms that occur.

Adverse reactions.

The main adverse effect of the drug is drowsiness, especially at the beginning of treatment. In very rare cases, allergic reactions may occur.

Possible adverse effects.

Immune system.

Rare: anaphylactic reactions, including facial swelling, pharyngeal swelling, rash; muscle spasms and shortness of breath.

Psychiatric disorders.

Single cases: excitement.

Nervous system.

Very common: increased fatigue.

Common: drowsiness, nervousness.

Single cases: headache, dizziness.

Gastrointestinal disorders.

Single cases: gastrointestinal disturbances, nausea, dry mouth and throat.

Reporting of adverse reactions

Reporting of adverse reactions after drug registration is important. It allows continuous monitoring of the benefit-risk balance of the drug. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of drug efficacy via 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 of children.

Packaging. 20 mL of the drug in a bottle closed with a dropper plug and sealed with a cap. The bottle is placed in a box.

Category of supply. Over-the-counter.

Manufacturer. Limited liability company "Pharmaceutical Company "Zdorovya".

Manufacturer's address and location of business activity. 22 Shevchenko Street, Kharkiv, Kharkiv Oblast, 61013, Ukraine.