Phenkarol

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT PHENCAROL® (PHENCAROL)

Composition:

Active substance: hifenadine;

1 tablet contains hifenadine hydrochloride 10 mg;

Excipients: sucrose, potato starch, calcium stearate.

Pharmaceutical form. Tablets.

Main physicochemical properties: flat cylindrical white or almost white tablets with a bevel.

Pharmacotherapeutic group. Antihistamines for systemic use.

ATC code R06A X.

Pharmacological properties.

Pharmacodynamics.

The active ingredient of the medicinal product Fenkarol® is a derivative of quinuclidinylcarbinol, which reduces the effects of histamine on organs and systems. Hydropheniramine is a competitive H1-receptor blocker. In addition, it activates the enzyme diamine oxidase, which degrades approximately 30% of endogenous histamine. This explains the efficacy of hydropheniramine in patients unresponsive to other antihistamines. Hydropheniramine poorly penetrates the blood-brain barrier and has minimal effect on serotonin deamination processes in the brain, with weak influence on monoamine oxidase activity. The antihistaminic properties of hydropheniramine are associated with the presence of a quinuclidine cyclic nucleus in its structure and the distance between the diphenylcarbinol group and the nitrogen atom. In terms of antihistaminic activity and duration of action, hydropheniramine exceeds diphenhydramine. Hydropheniramine reduces the toxic effects of histamine, eliminates or diminishes its bronchoconstrictive action and spasmogenic effects on intestinal smooth muscles, and has moderate anti-serotonin and weak anticholinergic effects, as well as well-expressed antipruritic and desensitizing properties.

Hydropheniramine reduces the hypotensive effect of histamine and its influence on capillary permeability, does not directly affect cardiac activity or arterial pressure, and has no protective effect against aconitine-induced arrhythmias.

Hydropheniramine does not have a central nervous system depressant effect; however, in individuals with increased sensitivity, a mild sedative effect may occur. The drug has low lipophilicity, resulting in low brain tissue concentrations (less than 0.05%), which explains the absence of central nervous system depressant effects.

Pharmacokinetics.

Hydropheniramine is rapidly absorbed from the gastrointestinal tract and appears in body tissues within 30 minutes. Maximum plasma concentration is reached within 1 hour.

Metabolites and unchanged portions of hydropheniramine are primarily excreted in urine, bile, and via the lungs within 48 hours. Fenkarol® is metabolized in the liver.

Clinical characteristics.

Indications.

Pollinosis, food and drug allergy, other allergic diseases, acute and chronic urticaria, angioedema (angioneurotic edema) of Quincke, hay fever, allergic rhinopathy, dermatoses (eczema, neurodermatitis, pruritus), as well as infectious-allergic reactions with bronchospastic component.

Contraindications.

Hypersensitivity to hydropheniramine hydrochloride or to any excipients of the drug.

Interaction with other medicinal products and other forms of interaction.

The drug does not enhance the CNS depressant effects of alcohol and hypnotics. Fenkarol® has weak M-cholinoblocking properties, but in cases of reduced gastrointestinal motility, absorption of slowly absorbed drugs may be enhanced (e.g., indirect-acting anticoagulants – coumarins).

Special precautions for use.

The drug should be prescribed with caution in patients with severe cardiovascular, gastrointestinal, hepatic and/or renal diseases.

The drug contains sucrose, which should be taken into account in patients with diabetes mellitus.

The drug should not be administered to patients with rare hereditary disorders such as fructose intolerance or sucrase-isomaltase deficiency.

Use during pregnancy or breastfeeding

The drug is contraindicated during the first trimester of pregnancy.

Use of the drug is not recommended during the second and third trimesters of pregnancy.

There are no data on the penetration of the drug into breast milk; therefore, the use of the drug is contraindicated during breastfeeding.

Ability to affect reaction rate when driving or operating machinery

Patients should refrain from driving, operating complex machinery, or performing other potentially hazardous activities until individual sensitivity to the drug has been established (through short-term administration), as the drug may cause sedative effects.

Dosage and Administration

The medication should be taken orally immediately after a meal.

Children aged 3 to 7 years – 10 mg twice daily (daily dose should not exceed 20 mg).

Children aged 7 to 12 years – 10–15 mg 2–3 times daily (daily dose should not exceed 50 mg).

Children aged 12 years and older – 25 mg 2–3 times daily (daily dose should not exceed 100 mg).

Adults and children aged 12 years and older are advised to use the medication in another dosage form (Phencarol®, 25 mg tablets).

The duration of treatment is 10–15 days. If necessary, the course may be repeated.

If a dose is missed, it should be taken as soon as possible. However, if the next scheduled dose is within a few hours, only the next dose should be taken. Double dosing should be avoided. If in doubt, consult a physician.

Children

The medication may be used in children aged 3 years and older.

Overdose

Cases of overdose have not been reported. Daily doses up to 300 mg/day do not cause serious clinically evident adverse effects. Higher doses may cause dryness of mucous membranes, headache, vomiting, epigastric pain, and dyspeptic symptoms.

If necessary, symptomatic treatment should be administered.

Adverse Reactions.

Nervous system disorders: dizziness, headache.

A mild sedative effect may occasionally occur, manifested as weakness, drowsiness, and slowed reaction times.

Gastrointestinal disorders: dryness of oral mucous membranes, dyspeptic symptoms (nausea, vomiting, bitter taste in the mouth), which usually resolve upon dose reduction or discontinuation of the drug.

Respiratory, thoracic and mediastinal disorders: sneezing, difficult breathing.

Psychiatric disorders: anxiety.

Renal and urinary disorders: proteinuria, interstitial nephritis.

Musculoskeletal and connective tissue disorders: joint pain.

Eye disorders: lacrimation.

In patients with gastrointestinal disorders, the likelihood of adverse effects is increased.

If any adverse effects occur, administration of the drug should be discontinued and a physician should be consulted.

Shelf life: 5 years.

Storage conditions.

Store in a dry, light-protected place at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging.

10 tablets per blister pack. 2 blisters per cardboard box.

Supply category. Over-the-counter.

Manufacturer.

JSC "Olfa" / Olpha AS.

Manufacturer's address and place of business.

5 Rupnicu Street, Olaine, Olaine region, LV-2114, Latvia / Rupnicu iela 5, Olaine, Olaines novads, LV-2114, Latvia.