PHENCAROL

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

Composition:

Active substance: hifenadine;

1 tablet contains 50 mg of hifenadine hydrochloride;

Excipients: sucrose, potato starch, modified corn starch, 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.

Cyphenadine is a derivative of quinuclidinylcarbinol that reduces the effects of histamine on organs and systems. Cyphenadine 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 cyphenadine in patients who are unresponsive to other antihistamines. Cyphenadine 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 cyphenadine 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, cyphenadine is superior to dimedrol. Cyphenadine reduces the toxic effects of histamine, alleviates or diminishes its bronchoconstrictive action and spasmogenic effects on intestinal smooth muscles, has moderate anti-serotonin activity and weak cholinolytic effects, and pronounced anti-pruritic and desensitizing properties. Cyphenadine 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 action against aconitine-induced arrhythmias.

Cyphenadine 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 tissue is low (less than 0.05), which explains the absence of suppressive effects on the central nervous system.

Pharmacokinetics.

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

Metabolites and unchanged portions of cyphenadine 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, angioneurotic (Quincke's) edema, hay fever, allergic rhinopathy, dermatoses (eczema, psoriasis, neurodermatitis, pruritus), as well as infectious-allergic reactions with bronchospastic component.

Contraindications.

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

Interaction with other medicinal products and other forms of interaction.

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

Special precautions for use.

The drug should be prescribed with caution in patients with severe cardiovascular, gastrointestinal, and liver diseases.

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

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

Use during pregnancy or breastfeeding.

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

The drug is contraindicated during the first trimester of pregnancy. Use of the drug during the second and third trimesters of pregnancy is not recommended.

There are no data on the passage of the drug into breast milk; therefore, the use of Fenkarol® 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) should first determine their individual sensitivity to the sedative effect (by short-term use). If increased sensitivity is observed, such individuals should exercise particular caution when using the drug.

Administration and Dosage

Phencarol® is taken orally immediately after meals.

Adults – 50 mg 3–4 times daily. The maximum daily dose is 200 mg. The treatment course lasts 10–15 days.

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

Children

The drug should not be administered to children due to the high content of the active substance.

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. Large 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.

Side effects.

Central nervous system: dizziness, headache.

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

Gastrointestinal tract: 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 system, thoracic organs and mediastinum: sneezing, difficulty breathing.

Psychiatric disorders: anxiety.

Renal and urinary system: proteinuria, interstitial nephritis.

Musculoskeletal and connective tissue: joint pain.

Eye disorders: lacrimation.

In patients with pre-existing gastrointestinal disorders, the likelihood of adverse effects increases.

If any adverse effects occur, discontinue use of the medicinal product and consult a physician.

Shelf life. 4 years.

Storage conditions.

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

Keep out of reach of children.

Packaging. 15 tablets in a blister. 2 blisters in a cardboard box.

Prescription status.

Over-the-counter.

Manufacturer.

JSC «Olpha» / Olpha AS.

Manufacturer's address and place of business.

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