RIMAZIN [Cetirizine] 10 mg/1 ml Drops for oral administration

Инструкция по медицинскому применению лекарственного препарата

RIMAZIN

Tradename

Rimazin, Римазин

International non-proprietary name or generic name

Cetirizine, Цетиризин

Dosage form

Drops for oral administration.

Composition

1 ml of the preparation contains:

active substance: cetirizine dihydrochloride 10 mg;

excipients: propylene glycol, glycerin, methyl parahydroxybenzoate, propyl parahydroxybenzoate, sodium acetate, glacial acetic acid, sodium saccharin, banana flavor, purified water.

Pharmacotherapeutic group

Antiallergic agent - H1-histamine receptor blocker.

Code АТХ  R06AE07

Pharmacological properties

Pharmacodynamics

Antiallergic drug. Histamine H1 receptor blocker, competitive histamine antagonist, hydroxyzine metabolite. Prevents development and participation in providing assistance to persons with antipruritic and antiexudative measures.

Affects the early histamine-dependent stage of the preceding stage, limits the release of stage mediators at a late stage of development, reduces the migration of eosinophils, neutrophils and basophils, stabilizes mast cell membranes. Reduces capillary permeability, prevents the development of tissue edema, relieves spasm of smooth muscle tissue. Eliminates skin reaction to the introduction of histamine, typical allergens, as well as to cooling (with "cold" urticaria). Reduces histamine-induced bronchoconstriction in mild bronchial asthma. It has virtually no anticholinergic or antiserotonin effect. In therapeutic doses, it has virtually no sedative effect.

After a single dose of cetirizine at a dose of 10 mg, the onset of the effect is observed after 20 minutes (in 50% of patients) and after 60 minutes (in 95% of patients), the effect lasts for more than 24 hours. Tolerance to antihistamine treatment with cetirizine has not been developed against the background of a course of treatment. After treatment, the treatment continues for up to 3 days.

Pharmacokinetics

The pharmacokinetic parameters of cetirizine change linearly.

After oral administration, the drug is rapidly and completely absorbed from the gastrointestinal tract. In adults, after a single dose of the drug at a therapeutic dose, Cmax in plasma is achieved after 1±0.5 hours and is 300 ng/ml. Taking the drug with food does not affect the amount of absorption.

Cetirizine binds to plasma proteins by 93±0.3%. Vd - 0.5 l/kg.

When taking the drug at a dose of 10 mg for 10 days, accumulation of cetirizine is not observed.

In small quantities, it is metabolized in the liver by O-dealkylation to form a pharmacologically inactive metabolite (unlike other histamine H1 receptor blockers, which are metabolized in the liver with the participation of cytochrome P450 isoenzymes).

T1/2 in adults is approximately 10 hours. Approximately 2/3 of the administered dose is excreted unchanged by the kidneys.

Indications for use

• Treatment of symptoms of perennial and seasonal allergic rhinitis and allergic conjunctivitis, such as itching, sneezing, rhinorrhea, lacrimation, conjunctival hyperemia;

• hay fever (pollinosis);

• urticaria (including chronic idiopathic urticaria);

• Quincke's edema;

• other allergic dermatoses (including atopic dermatitis), accompanied by itching and rashes.

Contraindications

• hypersensitivity to the components of the drug;

• hypersensitivity to hydroxyzine;

• end-stage renal failure (CC < 10 ml/min);

• pregnancy;

• lactation period (breastfeeding);

• children under 6 months (safety and efficacy have not been established).

Method of administration and dosage

Orally, regardless of food intake.

Adults: 10 mg (20 drops) once a day. Alternatively, the dose can be divided into two doses (10 drops in the morning and evening).

Children from 6 to 12 months: 2.5 mg (5 drops) once a day. Use in children from 6 to 12 months is possible only on prescription and under strict medical supervision!

Children from 1 year to 6 years: 2.5 mg (5 drops) 2 times a day in the morning and evening. The duration of treatment should not exceed 4 weeks.

Children from 6 to 12 years: 10 mg (20 drops) once a day. Alternatively, the dose can be divided into two doses (10 drops in the morning and evening). The duration of treatment should not exceed 4 weeks.

Children over 12 years: 10 mg (20 drops) once a day.

Sometimes a starting dose of 5 mg (10 drops) may be sufficient if this achieves satisfactory control of symptoms.

Special patient groups

Children with renal insufficiency - the dose is adjusted taking into account CC and body weight.

Elderly patients. Due to a possible decrease in renal function, the dosage regimen of the drug should be adjusted.

Patients with renal insufficiency. Since cetirizine is excreted from the body mainly by the kidneys, if alternative treatment of patients with renal insufficiency is impossible, the dosage regimen of the drug should be adjusted depending on renal function (SCF).

When using the table for dose adjustment, CC should be calculated in ml/min.

CC for men can be calculated based on serum creatinine concentration using the following formula:

CC for women can be calculated by multiplying the obtained value by a factor of 0.85.

Dosage in adult patients with renal insufficiency

Patients with impaired liver function. In patients with impaired liver function only, no dosage adjustment is required. In patients with impaired liver and kidney function, dosage adjustment is recommended (see table above).

If there is no improvement after treatment or new symptoms appear, a doctor should be consulted.

The drug should be used only according to the method of administration and in the doses indicated in the instructions.

Special instructions and precautions

Consult a doctor before using the drug. Due to the potential depressant effect on the central nervous system, caution should be exercised when prescribing the drug to children aged 6 months to 1 year. In patients with spinal cord injury, prostatic hyperplasia, and other predisposing factors to urinary retention, caution is required, since cetirizine may increase the risk of urinary retention. Caution is recommended when using cetirizine simultaneously with alcohol, since cetirizine can lead to increased drowsiness. In patients with renal insufficiency, the dosage regimen of the drug should be adjusted. Due to the possible decrease in renal function in elderly patients, the dosage regimen of the drug should be adjusted. Caution should be exercised in patients with epilepsy and increased seizure readiness. Before prescribing allergy tests, a three-day "washout" period is recommended due to the fact that H1-histamine receptor blockers inhibit the development of skin allergic reactions.

Side effect

When using the drug in recommended doses, side effects develop in very rare cases.

From the nervous system: drowsiness, dizziness, headache, agitation, depression.

From the digestive system: dry mouth, nausea, abdominal pain, diarrhea, liver dysfunction (increased levels of transaminases, alkaline phosphatase, GGT, bilirubin).

From the cardiovascular system: tachycardia.

From the respiratory system: rhinitis, pharyngitis.

From the organ of vision: accommodation disorder, blurred vision, nystagmus.

From the urinary system: urination disorder, enuresis.

Allergic reactions: itching, rash, urticaria, angioedema, hypersensitivity, up to the development of anaphylactic shock.

From the hematopoietic system: thrombocytopenia.

Others: fatigue, asthenia, malaise, edema.

Interaction with other medicinal products

No clinically significant drug interactions have been observed.

Alcohol: No enhancement of effect has been observed, but caution is advised.

Theophylline: Clearance is slightly reduced with high doses of cetirizine.

Overdose

Symptoms observed after apparent overdose of the drug affected the central nervous system or were related to a possible anticholinergic effect. Symptoms observed after taking at least five times the recommended daily dose included the following: confusion, diarrhea, fatigue, headache, malaise, mydriasis, pruritus, restlessness, sedation, somnolence, stupor, tachycardia, tremor, urinary retention. Treatment: There is no specific antidote. In case of overdose, symptomatic or supportive treatment is recommended. Gastric lavage and/or activated charcoal may be effective if the overdose is recent. Cetirizine is partially removed by dialysis.

Storage conditions

Store at a temperature not exceeding 25ºС.

Keep out of reach of children!

Shelf life

2 years.

Shelf life after opening the bottle is 3 months.

Do not use after the expiration date.

Vacation conditions

By prescription.

Release form

10 ml in a glass bottle with a dropper stopper, sealed with a plastic cap. 1 bottle together with instructions for use in a cardboard box.