Suprostilin

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT SUPROSTILIN (Suprostilin)

Composition:

Active substance: chloropyramine hydrochloride;

1 tablet contains: chloropyramine hydrochloride 0.025 g;

Excipients: lactose monohydrate, potato starch, magnesium stearate, talc.

Pharmaceutical form. Tablets.

Main physicochemical properties: white or almost white tablets.

Pharmacotherapeutic group. Antihistamines for systemic use.

ATC code R06A C03.

Pharmacological Properties.

Pharmacodynamics.

Chloropyramine belongs to the group of first-generation antihistamine agents, H1-receptor blockers. It exhibits antihistaminic activity. The drug affects smooth muscles, alleviates the course of allergic reactions, and reduces capillary permeability. The drug also has peripheral anticholinergic, sedative, and hypnotic effects.

Pharmacokinetics.

After oral administration, it is rapidly and completely absorbed from the gastrointestinal tract. Maximum blood concentration is reached within the first 2 hours; the therapeutic concentration level is maintained for 4–6 hours. Regardless of the route of administration, it is well distributed in body tissues and crosses the blood-brain barrier. It is intensively metabolized in the liver. It is excreted mainly by the kidneys in urine as inactive metabolites.

Clinical Characteristics.

Indications.

Allergic diseases – seasonal allergic rhinitis, conjunctivitis, urticaria, dermographism, contact dermatitis, alimentary allergy, allergic reactions caused by drugs, insect bite allergy, pruritus.

As an adjunctive therapy in systemic anaphylactic reactions and angioneurotic edema.

Contraindications.

• Hypersensitivity to any component of the drug;
• acute attacks of bronchial asthma;
• closed-angle glaucoma;
• urinary retention, benign prostatic hyperplasia;
• peptic ulcer;
• acute myocardial infarction;
• arrhythmia;
• concomitant use of monoamine oxidase inhibitors (MAOIs);
• hypersensitivity to other ethylenediamine derivatives.

Interaction with other medicinal products and other forms of interaction.

Monoamine oxidase inhibitors (MAOIs) enhance and prolong the anticholinergic effect of Suprastin. Particular caution should be exercised when prescribing the drug concomitantly with sedatives, tranquilizers, sedative analgesics, tricyclic antidepressants, atropine, and muscarinic parasympatholytics due to the possibility of mutual potentiation of effects.

Alcohol enhances the depressant effect of chloropyramine hydrochloride on the central nervous system; therefore, consumption of alcoholic beverages should be avoided during treatment with this drug.

When used in combination with ototoxic drugs, early warning signs of ototoxicity may be masked.

Antihistamines may suppress skin reactions in allergy testing; therefore, these drugs should be discontinued several days before planned skin allergy testing.

Special precautions for use

The drug should be prescribed with particular caution to patients with hepatic impairment, cardiovascular disorders, elderly patients, and debilitated patients, since they are more sensitive to certain adverse effects of antihistamines (dizziness, drowsiness, decreased arterial pressure).

Dosage adjustment is required in patients with renal impairment, as the active ingredient is predominantly excreted by the kidneys.

If Suprostilin tablets are taken late in the evening, symptoms of gastroesophageal reflux may be intensified.

When Suprostilin tablets are used in combination with ototoxic agents, warning signs of ototoxicity may be masked.

Prolonged use of antihistamines rarely may cause hematopoietic system disorders (leukopenia, agranulocytosis, thrombocytopenia, hemolytic anemia). If adverse effects occur during long-term treatment (fever, laryngitis, development of ulcers on the oral mucosa, pallor, jaundice, bruising, bleeding), treatment must be discontinued and blood parameters monitored.

Alcohol may enhance the sedative effect of antihistamines on the central nervous system.

Suprostilin tablets contain lactose and therefore should not be administered to patients with rare hereditary conditions of galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption.

In hepatic insufficiency, chloropyramine metabolism is slowed, necessitating dosage adjustment.

Dosage reduction may be required in patients with hepatic dysfunction, as the metabolism of the active ingredient is decreased.

Use during pregnancy or breastfeeding

Suprostilin must not be used during pregnancy or breastfeeding.

Adequate and well-controlled studies in pregnant women have not been conducted. However, it has been reported that retrolental fibroplasia (RLF) occurred in newborns whose mothers received antihistamines during the last two weeks of pregnancy.

Ability to influence reaction rate while driving or operating machinery

Due to possible adverse reactions, patients are advised to avoid driving vehicles or operating machinery while taking this medication.

Method of administration and dosage.

The tablets should be taken orally during meals, without chewing, with sufficient amount of liquid.

The usual daily dose for adults is 75–100 mg (3–4 tablets per day).

The dose for children aged 6 to 14 years is 1 tablet per day.

The dose may be increased depending on the patient's response and the development of adverse effects.

However, the daily dose for children should not exceed 2 mg/kg of body weight.

The maximum daily dose is 4 tablets (100 mg).

Treatment is considered complete after the symptoms of the disease have disappeared. If adverse reactions listed in the relevant section occur, treatment must be discontinued.

Children. Suprostilin tablets are indicated for children aged 6 years and older.

Overdose.

Intentional or accidental overdose of antihistamines may be fatal, especially in children. Overdose leads to symptoms similar to atropine intoxication: hallucinations, restlessness, ataxia, impaired motor coordination, athetosis, and convulsions. In children, excitation is predominant. Dry mouth, dilated pupils, flushing, sinus tachycardia, urinary retention, and hyperthermia may also occur. In adults, fever and flushing are not always observed; the excitation phase is accompanied by convulsions and postictal depression. Additionally, coma and cardiopulmonary collapse may occur, potentially leading to fatal outcome within 2–18 hours.

Due to the anticholinergic effect of the drug, gastric emptying may be delayed; therefore, gastric lavage and administration of activated charcoal are required within 12 hours after overdose.

Cardiopulmonary function monitoring is recommended. Treatment is symptomatic. There is no specific antidote.

Adverse reactions.

Central nervous system: sedative effect, increased fatigue, drowsiness, general weakness, dizziness, ataxia, restlessness, tremor, seizures, headache, euphoria, encephalopathy, blurred vision, impaired psychomotor performance.

Cardiovascular system: arterial hypotension, tachycardia, arrhythmia.

Gastrointestinal tract: epigastric pain and discomfort, dry mouth, nausea, vomiting, diarrhea, constipation, anorexia, increased and decreased appetite.

Hematopoietic system: rarely – leukopenia, agranulocytosis, hemolytic anemia, thrombocytopenia, other pathological blood changes.

Other adverse reactions: dysuria, urinary retention, myopathy, increased intraocular pressure, glaucoma, photosensitivity, allergic reactions including skin hyperemia, rash, itching, urticaria, angioneurotic edema.

Shelf life.

5 years.

Storage conditions.

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

Keep out of reach of children.

Packaging.

10 tablets in a blister; 1 or 2 blisters per carton.

Availability.

Over-the-counter.

Manufacturer.

Private Joint-Stock Company "Lekhim-Kharkiv".

Manufacturer's address.

36 Severina Pototskoho Street, Kharkiv, Kharkiv Region, Ukraine, 61115.