Cetrifast (Drops) Instructions for Use

Marketing Authorization Holder

Stmfarm LLC (Russia)

Manufactured By

Kirov Pharmaceutical Factory, JSC (Russia)

ATC Code

R06AE07 (Cetirizine)

Active Substance

Cetirizine (Rec.INN WHO registered)

Dosage Form

Cetrifast

Oral drops 10 mg/1 ml: 10 ml, 20 ml, 25 ml, or 30 ml vial.

Dosage Form, Packaging, and Composition

Oral drops in the form of a transparent, colorless or slightly brownish solution with a characteristic odor.

Excipients: propylene glycol – 350 mg, glycerol – 250 mg, sodium saccharin – 10 mg, sodium acetate trihydrate – 10 mg, methylparaben – 1.35 mg, glacial acetic acid – 0.53 mg, propylparaben – 0.15 mg, purified water – up to 1 ml.

10 ml – dark glass bottles (1) with a dropper cap – cardboard packs.
20 ml – dark glass bottles (1) with a dropper cap – cardboard packs.
25 ml – dark glass bottles (1) with a dropper cap – cardboard packs.
30 ml – dark glass bottles (1) with a dropper cap – cardboard packs.

Clinical-Pharmacological Group

Histamine H₁-receptor blocker. Antiallergic drug

Pharmacotherapeutic Group

Antiallergic agent – H₁-histamine receptor blocker

Pharmacological Action

A third-generation histamine H₁-receptor blocker. It affects the “early” stage of the allergic reaction and reduces eosinophil migration; it limits the release of mediators at the “late” stage of the allergic reaction. It has practically no anticholinergic or antiserotonin action. It does not cause a sedative effect at therapeutic doses.

Pharmacokinetics

It is rapidly absorbed from the gastrointestinal tract, C_max after oral administration is reached after 1 hour. The bioavailability of cetirizine when taken as tablets and syrup is the same. Food does not affect the completeness of absorption (AUC), but prolongs the time to reach C_max by 1 hour and reduces the C_max value by 23%.

When taken at a dose of 10 mg once a day for 10 days, the C_ss in plasma is 310 ng/ml and is noted 0.5-1.5 hours after administration. Plasma protein binding is 93% and does not change with cetirizine concentration in the range of 25-1000 ng/ml. The pharmacokinetic parameters of cetirizine change linearly when prescribed in a dose of 5-60 mg. V_d is 0.5 l/kg.

It is metabolized in small amounts in the liver by O-dealkylation to form a pharmacologically inactive metabolite (unlike other H₁-histamine receptor antagonists, which are metabolized in the liver by the cytochrome system). It does not accumulate. 2/3 of the dose is excreted unchanged by the kidneys and about 10% in the feces. Systemic clearance is 53 ml/min. T_1/2 in adults is 7-10 hours, in children aged 6 to 12 years – 6 hours, from 2 to 6 years – 5 hours, from 6 months to 2 years – 3.1 hours.

In elderly patients, T_1/2 increases by 50%, and systemic clearance decreases by 40% (decreased renal function). In patients with impaired renal function (creatinine clearance <40 ml/min), the clearance of the drug decreases, and T_1/2 is prolonged (for example, in patients on hemodialysis, total clearance decreases by 70% and is 0.3 ml/min/kg, and T_1/2 is prolonged by 3 times), which requires an appropriate change in the dosage regimen.

It is practically not removed during hemodialysis. In patients with chronic liver diseases (hepatocellular, cholestatic or biliary cirrhosis), a prolongation of T_1/2 by 50% and a decrease in total clearance by 40% are noted (dose adjustment is required only with a concomitant decrease in the glomerular filtration rate). It penetrates into breast milk.

Indications

Hay fever; allergic rhinitis, conjunctivitis, dermatitis; urticaria, angioedema.

ICD codes

Dosage Regimen

Administer the drops orally. Use the provided dropper for accurate dosing. Shake the vial well before each use.

For adults and children over 12 years, the standard dose is 10 mg once daily. Alternatively, administer 5 mg twice daily.

For children aged 6 to 12 years, administer 5 mg once daily. Alternatively, administer 2.5 mg twice daily.

For children aged 2 to 6 years, administer 5 mg once daily. Alternatively, administer 2.5 mg twice daily.

For children aged 1 to 2 years, administer 2.5 mg twice daily (total 5 mg/day).

For infants 6 to 12 months, administer 2.5 mg once daily. Use only under direct medical supervision.

Measure the dose precisely. One milliliter (1 ml) of solution contains 10 mg of cetirizine. The dropper is marked for 0.25 ml (2.5 mg), 0.5 ml (5 mg), and 1 ml (10 mg) doses.

For patients with moderate renal impairment (creatinine clearance 30-49 ml/min), administer the standard dose every 48 hours.

For patients with severe renal impairment (creatinine clearance 10-29 ml/min), administer half the standard dose every 48 hours.

For patients with end-stage renal disease (creatinine clearance <10 ml/min) or on hemodialysis, the drug is contraindicated.

For elderly patients with age-related renal decline, base the dose on actual creatinine clearance. No dose adjustment is needed for patients with hepatic impairment alone.

Take the dose with or without food. If drowsiness occurs, consider an evening dose. Do not exceed the recommended daily dose.

Adverse Reactions

Possible dry mouth, drowsiness, headache, fatigue.

Rarely skin manifestations of allergic reactions, angioedema.

In isolated cases dyspepsia, agitation.

Contraindications

Renal failure, pregnancy, lactation period, hypersensitivity to cetirizine.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation.

Use in Renal Impairment

Contraindicated in renal failure.

Cetirizine should be prescribed with caution to patients with chronic renal failure (moderate and severe – dose adjustment is required).

Pediatric Use

Cetirizine should be prescribed with caution to children (experience of use in children under 1 year is insufficient).

Geriatric Use

Cetirizine should be prescribed with caution to elderly patients (a decrease in glomerular filtration is possible).

Elderly patients with normal renal function do not require dose adjustment.

Special Precautions

Cetirizine should be prescribed with caution to patients with chronic renal failure (moderate and severe – dose adjustment is required), to elderly patients (a decrease in glomerular filtration is possible).

Elderly patients with normal renal function do not require dose adjustment.

Use in pediatrics

Cetirizine should be prescribed with caution to children (experience of use in children under 1 year of age is insufficient).

Effect on the ability to drive vehicles and machinery

When the dose exceeds 10 mg/day, the ability for rapid reactions may deteriorate. During the treatment period, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

No pharmacokinetic interaction was found with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, diazepam and glipizide.

Concomitant administration with theophylline (400 mg/day) led to a 16% decrease in the total clearance of cetirizine (the kinetics of theophylline did not change).

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

Over-the-Counter

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.