SUPRASTIN

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT CUPRATIN® (SUPRATIN®)

Composition:

Active substance: chloropyramine;

1 ml contains 20 mg of chloropyramine hydrochloride;

Excipients: water for injections.

Pharmaceutical form. Solution for injection.

Main physicochemical properties: colorless transparent aqueous solution with a faint characteristic odor.

Pharmacotherapeutic group.
Antihistamines for systemic use.

ATC code R06A C03.

Pharmacological properties.

Pharmacodynamics.

Chloropyramine, a chlorinated analogue of tripelenamine (pyribenzamine), is a first-generation antihistamine belonging to the ethylenediamine group.

The mechanism of action of the drug involves blockade of histamine H1-receptors.

The drug relieves general symptoms of allergic diseases and, in addition to its antiallergic effect, has sedative, hypnotic, and antipruritic actions.

Pharmacokinetics.

Chloropyramine is metabolized in the liver. It is excreted mainly in the urine as metabolites. In children, the drug may be eliminated faster than in adult patients.

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

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

Clinical characteristics.

Indications.

• Allergic diseases – seasonal allergic rhinitis; conjunctivitis; urticaria; contact dermatitis; alimentary allergy; allergic reactions caused by drugs; allergy caused by insect bites.
• As an adjunctive therapy in systemic anaphylactic reactions and angioneurotic edema.

Contraindications.

• Hypersensitivity to any component of the medicinal product;
• Acute attacks of bronchial asthma;
• Closed-angle glaucoma;
• Peptic ulcer disease;
• Acute myocardial infarction;
• Arrhythmia;
• Concomitant use of monoamine oxidase inhibitors (MAOIs);
• Urinary retention, benign prostatic hyperplasia;
• Hypersensitivity to other ethylenediamine derivatives;
• Pregnancy and lactation period.

Interaction with other medicinal products and other forms of interactions.

MAOIs increase and prolong the anticholinergic effect of the drug. Particular caution should be exercised when prescribing the drug concomitantly with sedatives, barbiturates, hypnotics, tranquilizers, opioid analgesics, tricyclic antidepressants, atropine, muscarinic parasympatholytics, due to possible 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 agents, signs of ototoxicity may be masked.

Antihistamines may suppress skin reactions during allergy testing; therefore, administration of such medicinal products should be discontinued several days before planned skin allergy testing.

Special precautions for use.

Elderly and debilitated patients.

Suprastin® should be prescribed with particular caution to these patient groups, as they are more sensitive to certain adverse effects of antihistamines (dizziness, drowsiness, decreased blood pressure).

Due to the anticholinergic and sedative effects of the drug, particular caution should be exercised when administering it to elderly patients, as well as to patients with impaired liver function or cardiovascular disorders.

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

When Suprastin® is used in combination with ototoxic agents, symptoms of ototoxicity may be masked.

Alcohol may enhance the central nervous system depressant effects of antihistamines.

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

Use during pregnancy or breastfeeding.

There are no preclinical studies available.

Adequate and well-controlled clinical studies involving pregnant women have not been conducted, although cases have been reported in which retrolental fibroplasia developed in newborns whose mothers had received antihistamines during the last months of pregnancy.

Therefore, the use of this medicinal product during pregnancy or breastfeeding is contraindicated.

Effect on ability to drive or operate machinery.

During treatment with this medicinal product, particularly at the beginning of therapy, somnolence and impaired psychomotor function may occur (see section "Special precautions for use"). Therefore, considering the possible adverse reactions affecting the nervous system, driving a vehicle or operating machinery should be prohibited at the beginning of therapy for a period individually determined for each specific case. Later, the extent of restriction or prohibition should be individually assessed and determined by a physician.

Administration and Dosage

Suprastin® injection solution must be administered only by a physician or nurse. The solution is administered intramuscularly. In cases of anaphylactic shock or acute, severe allergic reactions, treatment should be initiated with intravenous administration of Suprastin®, followed by transition to intramuscular injections or oral administration of tablets. The duration of treatment is determined by the physician.

Adults

The usual daily dose for adults is 1–2 mL (1–2 ampoules) administered intramuscularly.

Children

Recommended initial doses:

• Children aged 1–12 months: 1/4 ampoule (0.25 mL) intramuscularly;
• Children aged 1–6 years: 1/2 ampoule (0.5 mL) intramuscularly;
• Children aged 6–14 years: 1/2–1 ampoule (0.5–1 mL) intramuscularly.

In these cases, an insulin syringe with a needle suitable for intramuscular injection should be used.

The daily dose for a child must not exceed 2 mg/kg of body weight.

Elderly patients and debilitated patients

Exercise particular caution when prescribing the drug to these patient groups, as they are more sensitive to certain adverse effects of antihistamines (dizziness, somnolence, decreased arterial blood pressure) (see section "Special Warnings and Precautions for Use").

Hepatic impairment

Dosage reduction may be necessary, as hepatic disease reduces the metabolism of the active substance.

Renal impairment

Dosage reduction is required in patients with impaired renal function, since the active substance is primarily excreted by the kidneys.

Children. Suprastin® can be used in children from the age of 1 month. It is contraindicated in newborns and premature infants.

Overdose

Symptoms

Intentional or accidental overdose of antihistamines may be fatal, especially in infants and children. Overdose of Suprastin® produces symptoms similar to atropine intoxication: hallucinations, restlessness, ataxia, motor coordination disturbances, athetosis, and convulsions. In children, excitation predominates. Dry mouth, mydriasis, flushing, sinus tachycardia, urinary retention, and hypothermia may also occur. Flushing and hypothermia are not always observed in adults; the excitation phase may be followed by postictal depression. Additionally, coma and cardiorespiratory collapse may develop, potentially leading to fatal outcome within 2–18 hours.

Cardiorespiratory function monitoring is recommended. Treatment is symptomatic.

No specific antidote is known.

Adverse reactions.

The following adverse effects may occur during the use of Suprastin®.

Cardiovascular system: arterial hypotension, tachycardia, arrhythmia.

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

Central nervous system: sedative effect, increased fatigue, dizziness (vertigo), ataxia, nervousness, tremor, seizures, headache, euphoria, encephalopathy, blurred vision, somnolence, impaired psychomotor performance.

Eye disorders: increased intraocular pressure, glaucoma.

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

Kidneys and urinary system: dysuria, urinary retention.

Skin and subcutaneous tissue: photosensitivity, allergic reactions.

Musculoskeletal and connective tissue: myopathy.

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

Other: injection site reactions.

Shelf life.

5 years.

Storage conditions.

Store at a temperature not exceeding 25 °C. Keep ampoules in the original packaging to protect from light. Keep out of reach of children.

Packaging.

1 ml in an ampoule; 5 ampoules in a blister pack, 1 blister pack in a cardboard box.

Prescription category. Prescription only.

Manufacturer.

Egis Pharmaceuticals Ltd.

Address.

1165 Budapest, Bekenyfoldi str. 118-120, Hungary.