Chloropyramine hydrochloride

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT CHLOROPYRAMINE HYDROCHLORIDE

Composition:

Active substance: chloropyramine;

1 ml of solution contains 20 mg of chloropyramine hydrochloride;

Excipient: water for injections.

Pharmaceutical form. Injection solution.

Main physicochemical properties: clear, colorless liquid.

Pharmacotherapeutic group. Antihistamines for systemic use.

ATC code R06A C03.

Pharmacological properties.

Pharmacodynamics.

Chloropyramine, a chlorinated analogue of tripelennamine (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 also affects smooth muscles, capillary permeability, and the central nervous system.

The drug relieves the 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, requiring dose adjustment.

Clinical characteristics.

Indications.

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

Contraindications. Hypersensitivity to any component of the drug; acute asthma attacks; acute myocardial infarction, arrhythmias; benign prostatic hyperplasia; closed-angle glaucoma; urinary retention; concomitant use of MAO inhibitors.

Interaction with other medicinal products and other forms of interaction. MAO inhibitors 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, and muscarinic parasympatholytics due to the possibility of mutual potentiation of effects.

Alcohol enhances the CNS depressant effect of chloropyramine hydrochloride; 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 can suppress skin reactions in allergy testing; therefore, these medications should be discontinued several days before planned skin allergy testing.

Special precautions for use.

Geriatric and debilitated patients.

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

Due to the anticholinergic and sedative effects of the drug, particular caution is required when administering the drug to elderly patients, as well as to patients with hepatic impairment or cardiovascular disorders.

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

When chloropyramine hydrochloride is used concomitantly with ototoxic agents, warning signs of ototoxicity may be masked.

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

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 oral mucosal ulcers, pallor, jaundice, ecchymoses, bleeding), treatment should be discontinued and blood parameters monitored.

Use during pregnancy or breastfeeding. Due to the lack of adequate and well-controlled studies, the use of the drug during pregnancy or breastfeeding is contraindicated.

Effect on ability to drive or operate machinery. During treatment with this drug, especially at the beginning of therapy, the drug may cause drowsiness and impaired psychomotor performance. Therefore, considering the possible adverse reactions affecting the nervous system, driving vehicles or operating machinery should be prohibited at the beginning of therapy for a period determined individually for each patient. Later, the extent of restriction or prohibition should be determined on an individual basis.

Method of administration and dosage.

Chloropyramine hydrochloride injection solution should be administered only by a physician or nurse. Injections should be given intramuscularly. In cases of anaphylactic shock or acute severe allergic reactions, treatment should be initiated with intravenous administration of chloropyramine hydrochloride, 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.

Children.

Recommended initial dose:

• children aged 1–12 months – 1/4 vial (0.25 mL);
• children aged 1–6 years – ½ vial (0.5 mL);
• children aged 6–14 years – ½ to 1 vial (0.5–1 mL).

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

The daily dose for children must not exceed 2 mg/kg body weight.

Liver function impairment.

Dosage reduction may be necessary, as the metabolism of the active substance is reduced in liver disease.

Kidney function impairment.

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

Children. Chloropyramine hydrochloride may be used in children from 1 month of age.

It is contraindicated in newborns and premature infants.

Overdose. Intentional or accidental overdose of antihistamines can be fatal, especially in children. Overdose of chloropyramine hydrochloride leads to 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, and hyperthermia may also occur. In adults, hyperthermia and flushing are not always observed; the excited phase is followed by convulsions and postictal depression. Additionally, coma and cardiopulmonary collapse may develop, potentially leading to fatal outcomes within 2–18 hours.

Cardiopulmonary function monitoring 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 or decreased appetite, exacerbation of gastroesophageal reflux symptoms.

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

Eyes: increased intraocular pressure, glaucoma.

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. 4 years.

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

Keep out of reach of children.

Packaging. 1 ml in ampoules, 5 ampoules per pack; 5 ampoules in blister pack in a carton.

Prescription status. Prescription only.

Manufacturer.

Limited Liability Company "Experimental Plant "GNCLS".

LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVTYA".

Manufacturer's location and address of business activity.

8 Vorobiova Street, Kharkiv, Kharkiv Oblast, Ukraine.

(Limited Liability Company "Experimental Plant "GNCLS")

22 Shevchenka Street, Kharkiv, Kharkiv Oblast, 61013, Ukraine.

(LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVTYA")