Chloropyramine is a blocker of H1-histamine receptors. Its chemical structure is related to ethylenediamine derivatives. Chloropyramine selectively blocks H1-histamine receptors and reduces capillary permeability.
It prevents the development and facilitates allergic reactions. It has sedative, antihistamine, m-cholinoblocking and pronounced antipruritic effect. It has moderate antispasmodic and antiemetic activity.
Pharmacokinetics
It is evenly distributed in the body including the central nervous system. Penetrates through the blood-brain barrier. Binding of chloropyramine with blood plasma proteins is 7.9%. Peak binding is noted at pH 6.8-7.4.
Therapeutic concentration is retained for 4-6 hours. It is intensively metabolized in the liver.
It is eliminated mainly through the kidneys with the urine as metabolites. Excretion of chloropyramine in children may be faster than in adults.
Indications
Treatment of symptoms of year-round and seasonal allergic rhinitis and allergic conjunctivitis;
hay fever (hay fever);
hives;
allergic dermatoses;
drug allergies;
allergic reactions to insect bites;
angioedema;
serum sickness.
Pharmacological effect
Pharmacodynamics
Chloropyramine is an H1-histamine receptor blocker. According to its chemical structure, it belongs to ethylenediamine derivatives. Chloropyramine selectively blocks H1-histamine receptors and reduces capillary permeability.
Prevents the development and facilitates the course of allergic reactions. It has a sedative, antihistamine, m-anticholinergic and pronounced antipruritic effect. Has moderate antispasmodic activity and antiemetic effect.
Pharmacokinetics
Evenly distributed throughout the body, including the central nervous system. Penetrates the blood-brain barrier. The binding of chloropyramine to plasma proteins is 7.9%. Peak binding was observed at pH 6.8-7.4.
The therapeutic concentration lasts 4-6 hours. It is intensively metabolized in the liver.
It is excreted primarily through the kidneys with urine in the form of metabolites. Elimination of chloropyramine may occur more rapidly in children than in adults.
Special instructions
During treatment, drinking alcoholic beverages is prohibited. Taking the drug at night may increase the symptoms of reflux esophagitis.
If during long-term use of the drug there is an unreasonable increase in body temperature, laryngitis, pallor of the skin, jaundice, the formation of ulcers of the oral mucosa, the appearance of hematomas, unusual and difficult to stop bleeding, you should consult a doctor, since prolonged therapy with antihistamines can lead to hematopoietic disorders.
Antihistamines can distort the manifestation of the reaction when performing allergy skin tests, therefore, a few days before the planned test, the use of the drug should be discontinued. When combined with ototoxic drugs, chloropyramine may mask early manifestations of ototoxicity.
Impact on the ability to drive vehicles and machinery
Active ingredient
Chloropyramine
Composition
1 ampoule (1 ml) contains chloropyramine hydrochloride as an active substance (in terms of 100% substance) – 20 mg;
excipients: water for injection – up to 1 ml.
Contraindications
Individual hypersensitivity to the drug or its components;
acute attack of bronchial asthma;
simultaneous use of monoamine oxidase inhibitors;
newborn children (up to 1 month);
pregnancy and lactation;
gastric ulcer in the acute stage;
prostatic hyperplasia;
severe respiratory failure.
With caution
The drug should be prescribed with caution to elderly patients, with insufficient liver function and/or heart disease, with peptic ulcer of the stomach and/or duodenum, when taking medications that depress the central nervous system (CNS), urinary retention, and angle-closure glaucoma.
Side Effects
From the central nervous system: lethargy, weakness, drowsiness, dizziness, headache, euphoria, feeling of fatigue, irritability, tremor, convulsions, impaired coordination of movements, blurred vision; in children there may be some stimulating effect on the central nervous system, manifested by anxiety, increased irritability, insomnia.
From the digestive system: dry mouth, nausea, vomiting, gastralgia, diarrhea/constipation, loss or increase of appetite.
From the urinary system: difficulty urinating.
From the cardiovascular system: decreased blood pressure (more often in elderly patients), tachycardia, arrhythmia.
From the hematopoietic system: very rarely – leukopenia, agranulocytosis.
On the part of the visual organs, increased intraocular pressure.
Allergic reactions to the drug.
Other: photosensitivity, muscle weakness.
Interaction
Enhances the effect of drugs for general anesthesia, sleeping pills, sedatives, tranquilizers, anticholinergic drugs, opioid analgesics, local anesthetics.
Tricyclic antidepressants and monoamine oxidase inhibitors enhance the m-anticholinergic and inhibitory effect on the central nervous system.
Caffeine and phenamine reduce the inhibitory effect on the central nervous system.
Concomitant use with ethanol is not recommended (risk of severe CNS depression).
Overdose
Symptoms: in children – agitation, anxiety, hallucinations, athetosis, ataxia, convulsions, mydriasis, pupillary immobility, facial skin flushing, hyperthermia; then – collapse, coma.
In adults – depression (lethargy, depression) or excitation of the central nervous system (psychomotor agitation), very rarely – hallucinations, loss of coordination, dilated pupils and lack of reaction to light, dry mouth, hyperthermia and redness of the skin, convulsions, in severe cases – coma.
Treatment: symptomatic therapy (including the prescription of antiepileptic drugs, caffeine, phenamine), resuscitation measures, artificial ventilation – according to indications. There is no specific antidote.
Storage conditions
In a place protected from light at a temperature not exceeding 25 °C.
Keep out of the reach of children.
Shelf life
5 years.
Manufacturer
Ozon, Russia
Shelf life | 5 years. |
---|---|
Conditions of storage | In the dark place at a temperature not exceeding 25 ° C. Keep out of reach of children. |
Manufacturer | Ozon, Russia |
Medication form | solution |
Brand | Ozon |
Other forms…
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