Phenkarol

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT PHENCAROL®

Composition:

Active substance: chifenadine;

1 tablet contains chifenadine hydrochloride 25 mg;

Excipients: potato starch, sucrose, calcium stearate.

Pharmaceutical form. Tablets.

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

Pharmacotherapeutic group. Antihistamines for systemic use.

ATC code R06AX31.

Pharmacological Properties.

Pharmacodynamics.

Hiphenadine is a derivative of quinuclidinylcarbinol that reduces the effects of histamine on organs and systems. Hiphenadine 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 hiphenadine in patients unresponsive to other antihistamines. Hiphenadine poorly penetrates the blood-brain barrier and has minimal effect on serotonin deamination processes in the brain, exerting only weak influence on monoamine oxidase activity. The antihistaminic properties of hiphenadine are associated with the presence of the 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, hiphenadine is superior to dimedrol. Hiphenadine reduces the toxic effects of histamine, alleviates or diminishes its bronchoconstrictive action and spasmogenic effects on intestinal smooth muscles, exerts moderate antiserotonin activity and slight cholinolytic effects, and has well-expressed antipruritic and desensitizing properties. Hiphenadine reduces the hypotensive effect of histamine and its influence on capillary permeability. It does not directly affect cardiac function or arterial pressure and does not provide protective effects against aconitine-induced arrhythmias.

Hiphenadine does not suppress the central nervous system; however, in individuals with increased sensitivity, a mild sedative effect may occur. The drug is poorly lipophilic, and its concentration in brain tissues is low (less than 0.05), which explains the absence of central nervous system depressant effects.

Pharmacokinetics.

Hiphenadine is rapidly absorbed from the gastrointestinal tract, and already within 30 minutes it can be detected in body tissues. Maximum concentration is reached within 1 hour.

Metabolites and unchanged portions of hiphenadine are primarily excreted via urine, bile, and through the lungs within 48 hours.

Clinical characteristics.

Indications.

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

Contraindications.

Hypersensitivity to hydrophenhydramine or to any excipients of the medicinal product.

Interaction with other medicinal products and other forms of interaction.

Phencarol® does not potentiate the CNS depressant effects of alcohol and sedatives; it 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 to patients with severe cardiovascular, gastrointestinal, renal, or hepatic disorders.

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

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

Use during pregnancy or breastfeeding.

There are insufficient animal studies to evaluate the effect of the medicinal product on pregnancy.

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 regarding the penetration of the drug into breast milk; therefore, Fenkarolum® is contraindicated during breastfeeding.

Ability to affect reaction rate while driving or operating machinery.

Individuals whose work requires rapid physical or mental responses (e.g., drivers of vehicles) should first determine their individual sensitivity to the sedative effect (by short-term use). If increased sensitivity is observed, such individuals must exercise particular caution when using the drug.

Dosage and Administration.

Phenkarol® should be taken orally immediately after meals.

The single dose for adults is 25–50 mg 2–4 times daily.

For pollinosis, a daily dose of less than 75 mg is ineffective. The maximum daily dose is 200 mg. The duration of treatment course is 10–15 days.

For children aged 12 years and older – 25 mg 2–3 times daily. The duration of treatment course is 10–20 days. If necessary, the course may be repeated (after consultation with a physician).

If a dose has been missed, continue treatment according to the previously prescribed schedule. If necessary, consult a physician.

Children.

The drug can be used in children aged 12 years and older.

For children under 12 years of age, it is recommended to use the drug in another dosage form (Phenkarol®, 10 mg tablets).

Overdose.

Cases of overdose have not been reported. A daily dose of up to 300 mg/day does 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.

There is no specific antidote.

Adverse reactions.

Nervous system disorders: dizziness, headache.

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

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

Respiratory, thoracic and mediastinal disorders: sneezing, difficulty 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, the use of the medicinal product should be discontinued and medical advice should be sought.

Shelf life. 5 years.

Storage conditions.

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

Keep out of reach of children.

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

Pharmaceutical category.

Over-the-counter (without prescription).

Manufacturer.

JSC "Olpha" / Olpha AS.

Manufacturer's address and place of business.

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