Foristal

INSTRUCTIONS for medical use of the medicinal product FORISTAL (FORISTAL)

Composition:

active substance: dimetindene maleate;

1 ml contains dimetindene maleate 1 mg;

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

Pharmaceutical form. Oral drops, solution.

Main physicochemical properties: clear colorless solution, practically odorless.

Pharmacotherapeutic group. Antihistamines for systemic use.

ATC code R06A B03.

Pharmacological Properties

Pharmacodynamics

Dimetindene maleate is an antagonist of histamine at H1-receptors. 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 does not affect H2-receptors and 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.

According to study data, the effect of a single 4 mg dose of dimetindene maleate in the form of drops on skin reactions persists up to 24 hours after administration.

Pharmacokinetics

The systemic bioavailability of dimetindene in the form of drops is approximately 70%. The onset of therapeutic effect is expected within 30 minutes after administration of the drops, and maximum plasma concentration of dimetindene is reached within 2 hours.

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

Its elimination half-life is approximately 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 conditions: 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 dimetindene maleate or to any other component of the medicinal product. Presence of pyloric or duodenal stenosis in the patient.

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

Interaction with other medicinal products and other forms of interaction

Concomitant use of central nervous system (CNS) depressants, 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 agents, such as bronchodilators, gastrointestinal spasmolytics, mydriatics, and urological antimuscarinics, may produce an additional antimuscarinic effect when used concomitantly 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 administering Foristal oral drops to patients with glaucoma, patients with bladder neck contracture and/or urinary retention, including those with benign prostatic hyperplasia, as well as patients with chronic obstructive pulmonary 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 with caution in elderly patients, in whom the risk of adverse reactions, including excitation and increased fatigue, is higher. Avoid accidental misuse of the medication by elderly patients. The recommended dosage and duration of use must not be exceeded without a physician's recommendation.

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

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

The medicinal product contains less than 1 mmol (23 mg) of sodium per dose, i.e. it is practically sodium-free.

Use during pregnancy or breastfeeding

Pregnancy. There are no clinical data on the use of the drug in pregnant women. Animal studies have shown no harmful effects (either direct or indirect) on the course of pregnancy, fetal development, or subsequent offspring development. However, the drug is not recommended during pregnancy except when the expected benefit outweighs the potential risk to the fetus. In such cases, the drug may be used only under medical supervision.

Breastfeeding period. It is highly likely that dimetindene 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

When taking Foristal, psychomotor reaction speed may be slowed, and drowsiness or dizziness may occur. Therefore, patients should refrain from driving or operating machinery.

Method of Administration and Dosage

The duration of use of the medication without medical consultation should not exceed 14 days.

Method of Administration

To administer drops, hold the bottle vertically with the dropper tip facing downwards. If you experience difficulty in dispensing the drops, tap the bottom of the bottle several times with your finger.

The drops should be taken undiluted (e.g., in a teaspoon).

Adults, children aged 12 years and older, and elderly patients

The recommended daily dose is 3–6 mg, divided into 3 doses of 20–40 drops taken three times a day. For patients prone to drowsiness, it is recommended to take 40 drops before 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. Children aged 1 month to 1 year may be treated only after consultation with a physician. The recommended daily dose is 0.1 mg (i.e., 2 drops) per kilogram of body weight per day, divided into 3 doses.

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

Forstal oral drops should not be exposed to high temperatures. They should be added directly to warm infant food immediately before feeding. If the child is fed with a spoon, the drops can be administered undiluted, using a teaspoon. The drops have a pleasant taste.

Children

Do not administer to children under 1 month of age, especially premature infants. Use oral drops form with caution in children under 1 year of age: sedative effects may be accompanied by episodes of nocturnal apnea. In young children, antihistamines may cause excitation.

Forstal oral drops may be administered to children aged 1 month to 1 year only after consultation with a physician and when there are clear indications for antihistamine therapy. Do not exceed the recommended dose.

Overdose

In case of overdose of Forstal oral drops, as with other antihistamines, the following symptoms may occur: central nervous system (CNS) depression, drowsiness (mainly in adults), CNS stimulation and antimuscarinic effects (especially in children and elderly individuals), including excitement, ataxia, tachycardia, hallucinations, convulsions, tremor, dilated pupils, dry mouth, facial flushing, urinary retention, and fever. Arterial hypotension, coma, and cardiorespiratory collapse may also develop.

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

Adverse Reactions

The main side effect associated with the use of the medicinal product is somnolence, particularly at the beginning of treatment. Allergic reactions may occur very rarely.

Possible adverse reactions

Immune system disorders

Rare: anaphylactic reactions, including facial swelling, pharyngeal swelling, rash; muscle spasms and dyspnea.

Psychiatric disorders

Isolated cases: excitement.

Nervous system disorders

Very common: increased fatigue.

Common: somnolence, nervousness.

Isolated cases: headache, dizziness.

Gastrointestinal disorders

Isolated cases: gastrointestinal disturbances, nausea, dryness of mouth and throat.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorization of the medicinal product is important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmaceutical professionals, as well as patients or their legal representatives, are encouraged to report all suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.

Shelf life: 2 years.

Storage conditions

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

Keep out of the reach of children.

Packaging

20 ml or 50 ml in a bottle with a dropper cap, 1 bottle per cardboard package.

Supply classification: Over-the-counter (without prescription).

Manufacturer

MIFARM S.P.A. / MIPHARM S.P.A.

Manufacturer's address

Via Bernardo Quaranta 12, Milan, 20141, Italy.

Marketing Authorization Holder

Glenmark Pharmaceuticals s.r.o.

Address of the Marketing Authorization Holder

Hvezdova 1716/2b, 140 78, Prague 4, Czech Republic.