Suprilamin, tablets 25 mg 20 pcs

Pharmacotherapeutic group:

anti-allergic agent – H1-histamine receptor blocker

ATX code: R06AC03

Pharmacological properties

Pharmacodynamics

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

A blocker of H1-histamine receptors, it has antihistamine and m-cholin-blocking effects. This drug also acts on smooth muscles, on capillary permeability and on the central nervous system (CNS).

When taken orally, the effect occurs as early as 15-30 minutes, the maximum effect develops within 1 hour and lasts for about 3-6 hours.

Pharmacokinetics

Intake

In oral administration, it is almost completely absorbed from the gastrointestinal tract (GIT). The therapeutic effect of chloropyramine develops within 15-30 minutes after oral administration, reaches its maximum within the first hour after administration and lasts for at least 3-6 hours.

Distribution

It is well distributed in the body, including the CNS.

Metabolism

Intensively metabolized in the liver.

Elimination

Extracted mainly by the kidneys as metabolites.

Particular patient populations

Children and adolescents

The drug is eliminated faster in children than in adult patients.

Patients with impaired liver function

In patients with impaired liver function, the metabolism of chloropyramine is decreased, so the dose of the drug may be reduced.

Patients with impaired renal function

In patients with impaired renal function, the excretion of chloropyramine is decreased, so the dose of the drug may be reduced.

Indications

Urticaria, serum sickness, seasonal and year-round allergic rhinitis, allergic conjunctivitis, contact dermatitis, skin itching, acute and chronic eczema, atopic dermatitis, food and drug allergies, insect bite allergies.

Active ingredient

Chloropyramine

Composition

Active ingredient: chloropyramine hydrochloride – 25,0 mg

Excipients: lactose monohydrate (milk sugar), microcrystalline cellulose, sodium carboxymethyl starch (sodium glycolate starch, primogel), povidone K25 (collidon K25), magnesium stearate.

How to take, the dosage

Tablets are taken orally with food, without chewing and with plenty of water.

Adults are prescribed 1 tablet 3-4 times a day (75-100 mg per day).

Children:

• In the age of 3 to 6 years: 1/2 tablet (12.5 mg) 2 times a day, the daily dose is 25 mg;
• In the age of 6 to 14 years: 1/2 tablet (12.5 mg) 2 to 3 times daily; daily dose is 25 to 37.5 mg;
• Aged 14 to 18 years: 1 tablet (25 mg) 3 to 4 times daily; daily dose is 75 to 100 mg.

The dose for children may be gradually increased in the absence of side effects in the patient, but the maximum dose should never exceed 2 mg/kg body weight. The duration of treatment depends on the nature, symptoms, degree of their manifestation, duration and course of the disease.

Special patient groups

Elderly patients and patients with significant weight deficit

Use of chloropyramine requires extreme caution because in these patients antihistamines are more likely to cause side effects (dizziness, drowsiness, drop in blood pressure (BP)).

Patients with impaired liver function

Dose reduction may be required due to decreased metabolism of chloropyramine in liver disease.

Patients with impaired renal function

The drug regimen and dose reduction may be required due to the fact that chloropyramine is mainly excreted by the kidneys.

Interaction

Monoamine oxidase inhibitors increase and prolong the anticholinergic effects of chloropyramine.

Particular caution should be exercised when using chloropyramine tablets simultaneously with barbiturates, hypnotics, anxiolytics and sedatives, tranquilizers, opioid analgesics, tricyclic antidepressants, atropine, muscarinergic parasympatholytics (chloropyramine and any of these drugs may increase the effects of each other).

Alcoholic beverages are prohibited during treatment (alcohol increases the CNS depressant effect of chloropyramine).

In combination with ototoxic drugs, chloropyramine may mask the early signs of ototoxicity.

Antihistamines inhibit skin reactions in response to allergic skin tests, thus, chloropyramine should be discontinued several days before the skin tests.

Special Instructions

The use of chloropyramine in the late evening hours may worsen symptoms of gastroesophageal reflux disease.

In combination with ototoxic drugs, chloropyramine may mask early signs of ototoxicity.

Hepatic and renal disease may require modification (reduction) of the drug dose, and therefore, the patient should inform the physician if he or she has hepatic and renal disease.

Because of its anticholinergic and sedative effect, chloropyramine should be prescribed with caution in elderly patients, patients with liver dysfunction, cardiovascular disease, closed-angle glaucoma, urinary retention and prostatic hyperplasia.

Chloropyramine may increase the effects of alcohol on the CNS, therefore, drinking alcoholic beverages while taking the drug is prohibited.

Long-term use of antihistamines may lead to disorders of the blood system and hematopoiesis (leukopenia, agranulocytosis, thrombocytopenia, hemolytic anemia). If during long-term use unexplained increase in body temperature, laryngitis, pale skin, jaundice, formation of mouth ulcers, appearance of bruises, unusual and prolonged bleeding it is necessary to conduct a clinical blood test with determination of the number of enzyme elements. If the test results indicate a change in blood count, the drug should be discontinued.

Each tablet contains 130 mg of lactose monohydrate. The drug is contraindicated in patients with lactase deficiency, lactose intolerance, glucose/galactose malabsorption.

Influence on ability to drive vehicles, mechanisms

The drug, especially in the initial period of treatment, may cause drowsiness, fatigue and dizziness. Therefore, during the initial period, the duration of which is determined individually, it is forbidden to drive vehicles or perform work associated with an increased risk of accidents. After that the degree of restriction to drive vehicles and work with mechanisms should be determined for each patient individually by a physician.

Contraindications

Hypersensitivity to chloropyramine and other components of the drug, acute onset of bronchial asthma, lactose intolerance, lactase deficiency or glucose-galactose malabsorption, pregnancy, lactation, children under 3 years (for this dosage form).

With caution

Closed-angle glaucoma, urinary retention, prostatic hyperplasia, impaired liver and/or renal function, cardiovascular disease elderly patients.

Side effects

Side effects are usually extremely rare, temporary and disappear after discontinuation of the drug.

Side effects are presented according to the lesions of organs and organ systems in the sequence of the Medical Dictionary of Regulatory Affairs (MedDRA).

There are no clinical studies to determine the frequency of adverse reactions.

Blood and lymphatic system disorders: leukopenia, agranulocytosis, hemolytic anemia and other changes in blood cell composition (e.g., thrombocytopenia in long-term use of the drug).

Immune system disorders: allergic reactions.

Nervous system disorders: drowsiness, fatigue, dizziness with a sense of rotation (vertigo), nervous agitation, ataxia, tremor, headache, euphoria, seizures, encephalopathy.

Visual disorders: blurred vision, glaucoma attacks, increased intraocular pressure.

Cardio-vascular system disorders: decrease in blood pressure, tachycardia, arrhythmia.

Gastrointestinal tract disorders: discomfort in the stomach, dry mouth, nausea, vomiting, diarrhea, constipation, loss or increase in appetite, pain in the upper abdomen.

Musculoskeletal and connective tissue disorders: myopathy.

Renal and urinary tract disorders: difficulty in urination, urinary retention.

Skin and subcutaneous tissue disorders: photosensitization.

If any of the above effects occur, discontinue the drug and immediately consult a physician.

Reports of side effects

If you have any side effects specified in the instruction, or they become aggravated, or you notice any other side effects not specified in the instructions, inform your physician.

During the post-registration period, any information about possible adverse reactions is important because these reports help assess the safety of the drug. Health care professionals are required to report any suspected adverse reactions to the contacts listed at the end of the instructions, as well as to local pharmacovigilance agencies.

Overdose

Overdose of antihistamines especially in children can be fatal, especially in infants.

Symptoms: in overdose chloropyramine causes symptoms similar to atropine poisoning, such as hallucinations, anxiety, ataxia, coordination disorders, athetosis, seizures. In young children, agitation predominates. Dry mouth, fixed dilation of the pupils, facial hyperemia, sinus tachycardia, urinary retention, and fever sometimes occur. In adults, fever and facial hyperemia may be absent; the period of agitation is followed by convulsions and post-convulsive depression with possible development of coma and cardiovascular and respiratory failure, which may result in the death of the patient within 2-18 hours.

Treatment: due to the anticholinergic effect of this drug, gastric emptying is delayed. Thus, inducing vomiting, gastric lavage and administration of activated charcoal are recommended within 12 hours after overdose. Monitoring of cardiovascular and respiratory system parameters, symptomatic therapy are recommended.

Specific antidote is unknown.

Pregnancy use

Pregnancy

There have been no adequately controlled clinical trials of antihistamines in pregnant women. However, cases of retrolental fibroplasia have been described in neonates whose mothers took antihistamines in the last months of pregnancy. Accordingly, the use of chloropyramine during pregnancy is contraindicated.

Breast-feeding

The use of chloropyramine is contraindicated during breast-feeding.

If the drug must be used during lactation, breast-feeding should be stopped.

Similarities

Suprastin, Chloropyramine