Subrestine (Solution) Instructions for Use

Marketing Authorization Holder

Bryntsalov-A, JSC (Russia)

ATC Code

R06AC03 (Chloropyramine)

Active Substance

Chloropyramine (Rec.INN registered by WHO)

Dosage Form

Subrestine

Injection solution 20 mg/1 ml: amp. 5 pcs.

Dosage Form, Packaging, and Composition

1 ml – ampoules (5) – contour cell packs (1) – cardboard packs.

Clinical-Pharmacological Group

Histamine H₁-receptor blocker. Antiallergic drug

Pharmacotherapeutic Group

H1 histamine receptor blocker

Pharmacological Action

Histamine H₁-receptor blocker, an ethylenediamine derivative. It has an antiallergic and antipruritic effect. It causes a sedative effect. It has peripheral anticholinergic activity and moderate antispasmodic properties.

Pharmacokinetics

After oral administration, chloropyramine hydrochloride is rapidly and completely absorbed from the gastrointestinal tract. C_max in blood plasma is reached within the first 1-2 hours, and the therapeutic concentration level is maintained for 3-6 hours.

Regardless of the route of administration, it is well distributed in the body, including the CNS.

The binding of chloropyramine to plasma proteins is 7.9%. The peak of binding is noted at pH 7.4.

It is metabolized in the liver.

It is excreted mainly by the kidneys in the form of metabolites. Elimination in children occurs faster than in adults.

Indications

Allergic diseases, including urticaria, serum sickness, angioneurotic edema, hay fever, allergic rhinopathies, allergic conjunctivitis.

Skin diseases, including contact dermatitis, acute and chronic eczema, drug rashes, pruritic dermatoses.

Itching from insect bites.

ICD codes

Dosage Regimen

Administer the solution by intramuscular or slow intravenous injection.

For adults, administer 20-40 mg (1-2 ml) as a single dose.

The maximum daily dose for adults is 150 mg.

For children, base the dose on age and body weight; a typical single dose is 0.3-0.5 mg/kg.

Do not administer to newborns under 1 month of age.

For elderly patients or those with hepatic impairment, use a reduced dose with caution.

Adjust the dosing frequency based on clinical response and tolerability, typically 2-3 times daily.

Monitor for sedation and other adverse reactions, especially during initial therapy.

Avoid concurrent use of alcohol and other CNS depressants.

Adverse Reactions

From the nervous system: lethargy, drowsiness, weakness, mild tremor, dizziness may occur. In children, some stimulating effect on the CNS is possible, manifested by anxiety, increased irritability, and insomnia.

From the digestive system: dry mouth, nausea, vomiting, diarrhea, or constipation may occur.

From the cardiovascular system: rarely – decreased blood pressure (more often in elderly patients), tachycardia, arrhythmia.

Allergic reactions: skin rash, itching may occur.

Other: rarely – difficult urination.

Contraindications

Glaucoma (for parenteral administration), benign prostatic hyperplasia, urinary retention (for parenteral administration), simultaneous use of MAO inhibitors (for parenteral administration), gastric ulcer in the acute phase (for parenteral administration), acute attack of bronchial asthma, pregnancy, lactation period, early childhood under 1 month, hypersensitivity to chloropyramine or other ethylenediamine derivatives.

Use in Pregnancy and Lactation

Contraindicated during pregnancy and lactation.

Use in Hepatic Impairment

Should be used with caution in cases of hepatic insufficiency.

Pediatric Use

Contraindicated in early childhood under 1 month.

Use with caution in children due to the increased sensitivity of this category of patients to antihistamines.

Geriatric Use

Should be used with caution in elderly patients.

Special Precautions

Should be used with caution in elderly patients, in cases of hepatic insufficiency and/or heart disease.

Use with caution in children due to the increased sensitivity of this category of patients to antihistamines.

Oral administration should be used with particular caution in patients with angle-closure glaucoma, urinary retention, and prostatic hypertrophy.

When taken at night, Chloropyramine may intensify the symptoms of reflux esophagitis.

Alcohol consumption should be avoided during treatment.

Effect on ability to drive vehicles and operate machinery

During the initial, individually determined period of chloropyramine use, driving vehicles and engaging in other potentially hazardous activities requiring speed of psychomotor reactions are not permitted. During further treatment, the degree of restrictions is determined depending on treatment tolerance.

Drug Interactions

With simultaneous use, Chloropyramine potentiates the effects of anesthetics, hypnotics, tranquilizers, analgesics, MAO inhibitors, tricyclic antidepressants, atropine, and sympatholytics (such a combination requires caution).

With simultaneous use of chloropyramine and caffeine or phenamine, a decrease or elimination of the inhibitory effect of chloropyramine on the CNS is noted.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.