Fenimax

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT FENIMAX (FENIMAX)

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.

Main physicochemical characteristics: clear solution, colorless or slightly brownish-yellow.

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 stimulatory effect on histamine methyltransferase, resulting in 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 permeability associated with immediate-type hypersensitivity reactions.

In combination with histamine H2-receptor antagonists, it inhibits virtually all circulatory effects of histamine.

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 µg/mL, plasma protein binding of dimetindene is approximately 90%. Metabolic reactions of dimetindene include hydroxylation and methoxylation.

The elimination half-life of dimetindene 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 disorders: urticaria, seasonal (hay fever) and perennial allergic rhinitis, drug and food allergies.

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

As 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. When used concomitantly with 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, an enhanced CNS depression may occur, potentially leading to adverse effects or even life-threatening consequences.

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

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

Special precautions for use.

Caution is required when administering antihistamines, particularly Phenimax, 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.

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

Use of the medicinal product in elderly patients should be cautious, as the risk of adverse reactions, including excitation and increased fatigue, is higher in this population. Misuse of the medicinal product by elderly patients should be avoided. The recommended dosage and duration of treatment must not be exceeded 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.

Phenimax oral drops 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.

This medicinal product contains 0.05 mmol (or 1.15 mg) / mL of sodium. Caution is advised when administering to patients on a sodium-restricted diet.

Use during pregnancy or breastfeeding

Pregnancy. Clinical data on the use of dimethindene maleate in pregnant women are lacking. Administration of the drug during animal studies did not reveal any harmful effects (either direct or indirect) on pregnancy progression, 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 on a physician's prescription.

Breastfeeding. Dimethindene maleate is very likely excreted into breast milk. The use of the drug during breastfeeding is not recommended. If treatment is necessary, breastfeeding should be discontinued for the duration of therapy.

Ability to affect reaction speed when driving or operating machinery.
During treatment with Phenimax, psychomotor reaction speed may be reduced and symptoms such as drowsiness and dizziness may occur; therefore, patients should refrain from driving or operating machinery.

Method of Administration and Dosage

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

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 three times a day. For patients prone to drowsiness, it is recommended to take 40 drops at bedtime and 20 drops in the morning with breakfast.

Dosage adjustment is not required for elderly patients.

Children. Administration of the drug is recommended only after prior consultation with a physician. For children aged 1 month to 1 year, use is allowed only upon physician's recommendation. The recommended daily dose is 0.1 mg (i.e., 2 drops) of dimetindene maleate per kilogram of body weight per day, divided into 3 doses.

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

Fenimax oral drops should not be exposed to high temperatures. When adding to warm infant food, the drops should be mixed immediately before feeding. If the child is fed with a spoon, the drops can be administered undiluted in 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 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.

Fenimax oral drops may be used in children aged 1 month to 1 year only upon 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 Fenimax oral drops, as with other antihistamines, 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 individuals), including excitement, ataxia, tachycardia, hallucinations, seizures, tremor, pupil dilation, dry mouth, facial flushing, urinary retention, and fever. Subsequently, arterial hypotension, coma, and cardiopulmonary collapse may develop.

In case of overdose, measures recommended by healthcare institutions should be taken according to the symptoms that occur.

Adverse Reactions

The frequency of adverse reactions is classified as follows: very common (≥1/10), common (≥1/100, <1/10), uncommon (≥1/1000, <1/100), rare (≥1/10,000, <1/1000), very rare (<1/10,000), and frequency not known.

The main adverse effect of dimetindene maleate is drowsiness, especially at the beginning of treatment. Allergic reactions may occur very rarely.

Possible adverse effects:

Immune system

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

Psychiatric disorders

Uncommon: excitement.

Nervous system

Very common: increased fatigue.

Common: drowsiness, nervousness.

Uncommon: headache, dizziness.

Gastrointestinal tract

Uncommon: gastrointestinal disturbances, nausea, dryness of mouth and throat.

Reporting of suspected adverse reactions after drug registration is of great importance. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmacy professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of drug efficacy via the Automated Pharmacovigilance Information System at: https://aisf.dec.gov.ua

Shelf life. 2 years.

Storage conditions. Store at temperatures not exceeding 25 °C.

Keep out of reach of children.

Packaging. 20 mL in a bottle, 1 bottle per cardboard pack.

Prescription status. Over-the-counter.

Manufacturer/Marketing Authorization Holder. LLC "Ternopharm".

Address of manufacturer and location of its business activity / address of marketing authorization holder. 4, Fabrychna St., Ternopil, Ukraine, 46010.

Tel./fax: (0352) 521-444, www.ternopharm.com.ua