Properties
What is it?
1. Drug Name Fenistil New, 0.1% Oral Drops 1.1 International Nonproprietary Name: Dimetindene. 2. Qualitative and Quantitative Composition Active substance: Dimetindene maleate 1.0 mg/ml. Excipients: Disodium phosphate dodecahydrate - 16.0 mg/ml, Benzoic acid - 1.0 mg/ml, Disodium edetate - 1.0 mg/ml, Propylene glycol - 100.0 mg/ml. The full list of excipients is given in section 6.1. 3. Dosage Form Oral drops. A clear, colorless or pale yellowish-brown solution. See blog: Fenistil - A drug for the treatment of allergic reactions and itching. 4. Clinical Data 4.1 Indications for Use Symptomatic treatment of allergic diseases: urticaria, allergic diseases of the upper respiratory tract, e.g., hay fever and seasonal allergic rhinitis, food and drug allergies. Itching of various origins, except for itching associated with cholestasis. Itching accompanying diseases with rash, e.g., chickenpox. Itching after insect bites. As an adjunct in eczema and other allergic dermatoses accompanied by itching. 4.2 Method of Administration and Dosage Dosage regimen Adults The recommended daily dose is 3-6 mg of dimetindene maleate, divided into 3 doses, i.e., 20-40 drops 3 times a day. Patients prone to drowsiness are advised to take 40 drops before bedtime and 20 drops in the morning with breakfast. The maximum duration of use without consulting a doctor is 14 days. Children Children from 1 month to 1 year of age The use of Fenistil New drops in children from 1 month to 1 year of age is possible only after consulting a doctor and only for established medical indications for antihistamines. Exceeding the recommended dose is not allowed. Fenistil New drops should be used with caution in children under 1 year of age, as the sedative effect may be accompanied by episodes of nocturnal apnea. The recommended daily dose is approximately 0.1 mg/kg of body weight, i.e., 2 drops/kg of body weight per day. The daily dose should be divided into 3 administrations. Children from 1 to 12 years of age In children from 1 month to 12 years of age, the daily dose is usually prescribed according to body weight (kg) as shown in the table. Age/Body weight, kg | Dose in mg | Dose in drops 1 month - 1 year / 4.5 kg - 15 kg | 0.15-0.5 mg 3 times a day | 3-10 drops 3 times a day 1 - 3 years / 15 kg - 22.5 kg | 0.5-0.75 mg 3 times a day | 10-15 drops 3 times a day 3 - 12 years / 22.5 kg - 30 kg | 0.75-1 mg 3 times a day | 15-20 drops 3 times a day 20 drops = 1 ml = 1 mg dimetindene maleate. 1 drop = 0.05 mg dimetindene maleate. Children over 12 years of age The dosage regimen is the same as for adult patients. Method of administration For oral administration. When used in children, Fenistil New drops can be added to a bottle of warm baby food just before feeding, as exposure to high temperatures on the drops is not allowed. If the child is already being fed with a spoon, the drops can be given undiluted. The drops have a pleasant taste. 4.3 Contraindications Hypersensitivity to dimetindene and other components of the preparation. Children under one month of age, especially premature newborns. 4.4 Precautions The preparation should be used with caution in patients with glaucoma, with urinary retention on the background of benign prostatic hyperplasia, and in chronic obstructive pulmonary diseases. H1 and H2 histamine receptor blockers should be used with caution in patients with epilepsy. In young children, the use of antihistamines can cause agitation. Use of the preparation in children from 1 month to 1 year of age Fenistil New drops are prescribed with caution in children under 1 year of age, as the sedative effect may be accompanied by episodes of nocturnal apnea. In children from 1 month to 1 year of age, the preparation is used only on the recommendation of a doctor and only in cases of strict medical indications. Exceeding the recommended dose is not allowed. Use with caution in elderly patients, as this age group is more sensitive to side effects such as agitation and fatigue. Use in elderly patients with impaired consciousness should be avoided. It is not recommended to exceed the prescribed dose and duration of use without a doctor's prescription. The medicinal product contains propylene glycol (100 mg/ml), benzoic acid (1 mg/ml), less than 1 mmol of sodium (23 mg/ml), i.e., it practically does not contain sodium. 4.5 Interactions with Other Medicinal Products and Other Types of Interactions Concomitant use of medicinal products with a depressant effect on the central nervous system may enhance their effect, which can lead to the development of undesirable and life-threatening events. Such medicinal products include opioid analgesics, anticonvulsants, antidepressants (tricyclic antidepressants and monoamine oxidase inhibitors), other antihistamines and antiemetics, neuroleptics, anxiolytics and hypnotics, scopolamine, and alcohol. Tricyclic antidepressants and anticholinergic agents (e.g., bronchodilators, gastrointestinal antispasmodics, mydriatics, urological antimuscarinics) in combination with antihistamines may cause an additional antimuscarinic effect, as well as increase the risk of glaucoma exacerbation or urinary retention. To reduce and minimize the risk of possible potentiation of CNS depression syndrome, antihistamines are used with particular caution with procarbazine. 4.6 Fertility, Pregnancy and Lactation Pregnancy Animal studies have not revealed teratogenic effects of dimetindene; nor have direct or indirect adverse effects on pregnancy, embryonic development, fetal development, and postnatal development been revealed. Studies involving pregnant women have not been conducted. The preparation may be used during pregnancy only if absolutely necessary. Lactation Dimetindene may pass into breast milk. The use of the preparation during breastfeeding is not recommended. Fertility No data on fertility are available. 4.7 Effects on Ability to Drive and Use Machines The use of Fenistil New may reduce the ability to react quickly. Caution should be exercised by patients whose activities are associated with a high degree of concentration and the ability to react quickly (operating machinery) when using the preparation. 4.8 Adverse Reactions Adverse reactions include drowsiness, which is particularly evident at the beginning of treatment. In very rare cases, allergic reactions may develop. Information on adverse reactions is presented according to organ and system classes and by frequency of occurrence according to the following categories: very common (≥1/10), common (≥1/100 but <1/10), uncommon (≥1/1000 but <1/100), rare (≥1/10,000 but <1/1,000), very rare (<1/10,000). Within each group, adverse events are listed in order of decreasing seriousness. Immune system disorders: Very rare: manifestations of anaphylactoid reactions, including facial edema, laryngeal edema, rash, muscle spasms, and shortness of breath. Psychiatric disorders: Rare: agitation. Nervous system disorders: Very common: fatigue (11.8%). Common: drowsiness, nervousness. Rare: headache, dizziness. Gastrointestinal disorders: Rare: gastrointestinal disturbances, nausea, dry mouth and throat. Reporting of suspected adverse reactions It is important to report suspected adverse reactions after the medicinal product has been registered to continuously monitor the benefit-risk balance of the medicinal product. Healthcare professionals are recommended to report any suspected adverse reactions of the medicinal product through the national system for reporting adverse reactions and ineffectiveness of medicinal products. If the patient develops any adverse reaction, it is recommended to consult a doctor. This recommendation applies to any possible adverse reaction, including side effects not listed in this leaflet. You can also report adverse reactions, including ineffectiveness of medicinal products, to the database of adverse reactions (effects) of medicinal products. By reporting adverse reactions, you help us gather more information about the safety of the preparation. 4.9 Overdose Overdose of H1-histamine receptor blockers is characterized by the following symptoms: central nervous system (CNS) depression and drowsiness (mainly in adults), CNS stimulation and anticholinergic effects (mainly in children), including agitation, ataxia, tachycardia, hallucinations, tonic-clonic seizures, mydriasis, dry mouth, facial hyperemia, urinary retention, and fever. Possible consequences include hypotension, coma, and collapse. In case of overdose with the medicinal product, general measures of medical assistance should be taken according to clinical symptoms. 5. Pharmacological Properties 5.1 Pharmacodynamic Properties Pharmacotherapeutic group: Antihistamine for systemic use. Mechanism of action Dimetindene is an H1-histamine receptor blocker, a competitive antagonist of histamine. At low concentrations, it stimulates histamine methyltransferase, which leads to histamine deactivation. Dimetindene has a high affinity for H1 receptors and is a potent stabilizer of mast cells. In addition, it has a local anesthetic effect. Dimetindene does not affect H2 receptors. Furthermore, dimetindene acts as an antagonist of bradykinin, serotonin, and acetylcholine. It is a racemic mixture in which R-(-)-dimetindene has a higher H1-antihistamine effect. This leads to a reduction in increased capillary permeability, which is observed in immediate-type allergic reactions. In combination with H2-antihistamine preparations, dimetindene suppresses almost all effects of histamine in the blood. 5.2 Pharmacokinetic Properties Absorption The systemic bioavailability of dimetindene in drops is approximately 70%. The effect begins approximately 30 minutes after administration, with the main effect lasting for 5 hours. After oral administration of drops, the maximum concentration of dimetindene in blood plasma is reached within 2 hours. Distribution At concentrations from 0.09 μg/ml to 2 μg/ml, the binding of dimetindene to plasma proteins is approximately 90%. Biotransformation Metabolized by hydroxylation and methoxylation. Elimination The half-life in blood serum is approximately 6 hours. It is excreted with metabolites in bile and urine. 5-10% of the administered dose is excreted unchanged in the urine. 5.3 Preclinical Safety Data According to standard preclinical studies on pharmacological safety, toxicity upon repeated administration, and genotoxicity, no particular risks have been identified for the use of the preparation in humans. In studies on rats and rabbits, no teratogenic effects were observed. Administration of a dose 250 times higher than the recommended human dose does not affect fertility in rats, nor their perinatal and postnatal development. 6. Pharmaceutical Properties 6.1 List of Excipients Disodium phosphate dodecahydrate Citric acid monohydrate Benzoic acid Disodium edetate Sodium saccharin Propylene glycol Purified water 6.2 Incompatibilities Not applicable. 6.3 Shelf Life 2 years. 6.4 Special Precautions for Storage Store at a temperature not exceeding 25 °C. Keep the bottle in its original carton. Keep out of reach of children. Once opened, the bottle should be stored for no more than 24 months. 6.5 Primary Packaging Material and Contents 20 ml in a dark glass bottle with a low-density polyethylene dropper-dispenser and a polypropylene cap with a child-resistant feature and a first-opening control system. 1 bottle is placed in a cardboard box along with the instructions for use. 6.6 Special Precautions for Disposal There are no special disposal requirements for any unused medicinal product or waste materials obtained after using the preparation, or for other manipulations with the preparation. 6.7 Dispensing Category Pharmaceutical product group III, available without a prescription.
