SUPRASTIN

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT CUPRAGIN® (SUPRAGIN®)

Composition:

Active substance: chloropyramine;

One tablet contains 25 mg of chloropyramine hydrochloride;

Excipients: stearic acid, gelatin, sodium starch glycolate (type A), talc, potato starch, lactose monohydrate.

Pharmaceutical form. Tablets.

Main physico-chemical properties:

white or greyish-white tablet in the shape of a disk with a bevel, engraved "SUPRASTIN" on one side and a line on the other, odorless or nearly odorless.

Pharmacotherapeutic group. Antihistamines for systemic use.

Chloropyramine. ATC code R06A C03.

Pharmacological properties.

Chloropyramine, a chlorinated analogue of tripelenamine (pyribenzamine), is a first-generation antihistamine belonging to the ethylenediamine group. In preclinical and clinical studies—as with tripelenamine—chloropyramine has demonstrated efficacy in the treatment of hay fever and other allergic conditions. The mechanism of action of the drug involves blockade of histamine H1-receptors.

Very low doses of chloropyramine administered to guinea pigs protected the animals against histamine effects, even when the histamine dose exceeded the lethal dose by 120 times. The drug also affects smooth muscles, capillary permeability, and the central nervous system.

After oral administration, chloropyramine is rapidly absorbed from the gastrointestinal tract. The therapeutic effect develops within 15–30 minutes after administration, reaches its maximum within the first hour, and lasts for 3–6 hours. The drug is metabolized in the liver. It is excreted primarily in the urine as metabolites. In children, the drug may be eliminated more rapidly than in adult patients.

In renal impairment, elimination of the active substance may be reduced.

In hepatic insufficiency, metabolism of chloropyramine is slowed, requiring dose adjustment of the drug.

Clinical characteristics.

Indications.

• Allergic diseases such as seasonal allergic rhinitis; conjunctivitis; urticaria; dermographism; contact dermatitis; alimentary allergy; allergic reactions caused by drugs; insect bite-induced 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;
• peptic ulcer disease;
• acute myocardial infarction;
• arrhythmia;
• concomitant use of monoamine oxidase inhibitors (MAOIs);
• urinary retention, prostate hyperplasia;
• hypersensitivity to other ethylenediamine derivatives.

Interaction with other medicinal products and other types of interactions.

MAOIs increase and prolong the anticholinergic effect of Suprastin®. Particular caution should be exercised when prescribing the drug concomitantly with sedatives, barbiturates, hypnotics, tranquilizers, opioid analgesics, tricyclic antidepressants, atropine, and muscarinic parasympatholytics due to the possibility of mutual potentiation of effects.

Alcohol enhances the depressant effects of the drug 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 responses in allergy testing; therefore, administration of such drugs should be discontinued several days prior to planned skin allergy testing.

Special precautions for use

Elderly and debilitated patients

Use the drug with special caution in these patient groups, as they are more sensitive to certain adverse effects of antihistamines (dizziness, drowsiness, decreased blood pressure).

Hepatic function impairment

Dosage adjustment is required in patients with impaired liver function: dose reduction may be necessary, since the metabolism of the active substance is decreased in liver disease.

Due to the anticholinergic and sedative effects of the drug, particular caution should be exercised when administering it to elderly patients, patients with hepatic dysfunction, or those with cardiovascular disorders.

If the drug is taken late in the evening, symptoms of gastroesophageal reflux may be intensified.

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

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

One tablet contains 116 mg of lactose. The drug should not be administered to patients with hereditary galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption.

Use during pregnancy or breastfeeding

No preclinical studies in animals have been conducted.

The use of the medicinal product during pregnancy or breastfeeding is contraindicated.

Adequate and well-controlled clinical studies involving pregnant women have not been performed, although cases have been reported in which newborns whose mothers received antihistamines during the last 2 weeks of pregnancy developed retrolental fibroplasia (RLF).

Ability to influence reaction rate while driving or operating machinery

During use of the drug, especially at the beginning of treatment, drowsiness and impaired psychomotor function may occur (see section «Special precautions for use**»** ). Therefore, considering the possible adverse reactions affecting the central nervous system, driving vehicles or operating machinery is prohibited at the beginning of therapy, for a period individually determined in each specific case.

Method of Administration and Dosage

Tablets should be taken orally during meals, without chewing, and with sufficient amount of liquid.

Adults.

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

Children.

For children aged:

• 3 to 6 years: 1/2 tablet twice daily;
• 6 to 14 years: 1/2 tablet 2–3 times daily.

The dose may be increased depending on patient response and development of adverse effects; however, the daily dose for children must never exceed 2 mg/kg of body weight.

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

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

Children.

The drug should be administered to children aged 3 years and older.

Overdose.

Intentional or accidental overdose of antihistamines may be fatal, especially in children. Overdose of Suprastin® causes symptoms similar to atropine intoxication: hallucinations, restlessness, ataxia, impaired motor coordination, athetosis, and convulsions. In children, excitation predominates. Dry mouth, dilated pupils, flushing, sinus tachycardia, urinary retention, diaphoresis, and increased body temperature may also occur. In adults, diaphoresis and flushing are not always observed; the excitation phase is followed by seizures and postictal depression. Additionally, coma and cardiopulmonary collapse may develop, 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.

Monitoring of cardiopulmonary function is recommended. Treatment is symptomatic. No specific antidote is known.

Side effects.

Central nervous system: sedative effect, increased fatigue, dizziness, ataxia, nervousness, tremor, seizures, headache, euphoria, encephalopathy, blurred vision, drowsiness, worsening of psychomotor functions.

Cardiovascular system: arterial hypotension, tachycardia, arrhythmia.

Gastrointestinal tract: epigastric pain and discomfort, dry mouth, nausea, vomiting, diarrhea, constipation, anorexia, increased appetite, worsening of gastroesophageal reflux symptoms.

Blood system: leukopenia, agranulocytosis, thrombocytopenia, hemolytic anemia, other blood abnormalities.

Eyes: increased intraocular pressure, glaucoma.

Kidneys and urinary system: dysuria, urinary retention.

Skin and subcutaneous tissue: photosensitivity, allergic reactions.

Musculoskeletal system and connective tissue: myopathy.

Immune system: allergic reactions, including skin hyperemia, rash, pruritus, urticaria, angioedema.

Shelf life. 5 years.

Storage conditions.

Store at a temperature not exceeding 25°C, in a place inaccessible to children.

Packaging.

10 tablets in a blister; 2 blisters in a cardboard box.

Dispensing category.

Over-the-counter.

Manufacturer.

EGIS Pharmaceuticals Plc.

Manufacturer's address.

1165 Budapest, Bokenyfoldi ut. 118-120, Hungary.