Cetirinax^® (Tablets) Instructions for Use

Marketing Authorization Holder

Actavis Group PTC ehf. (Iceland)

Manufactured By

Actavis hf. (Iceland)

ATC Code

R06AE07 (Cetirizine)

Active Substance

Cetirizine (Rec.INN registered by WHO)

Dosage Form

Cetirinax®

Film-coated tablets, 10 mg: 7 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, biconvex, oval, with a score on one side.

Excipients: microcrystalline cellulose, lactose monohydrate, crospovidone, colloidal silicon dioxide, magnesium stearate.

Shell composition: hypromellose, macrogol stearate, microcrystalline cellulose, propylene glycol, titanium dioxide (E171).

7 pcs. – blisters (1) – cardboard packs.

Clinical-Pharmacological Group

Histamine H₁-receptor blocker. Antiallergic drug

Pharmacotherapeutic Group

Antiallergic agent – H₁-histamine receptor blocker

Pharmacological Action

Blocker of peripheral histamine H₁-receptors. A competitive histamine antagonist, a metabolite of hydroxyzine. Prevents the development and alleviates the course of allergic reactions, has antipruritic and anti-exudative effects. It affects the early stage of allergic reactions, limits the release of inflammatory mediators at the late stage of allergic reactions, and reduces the migration of eosinophils, neutrophils, and basophils.

It reduces capillary permeability, prevents the development of tissue edema, and relieves smooth muscle spasm. It eliminates the skin reaction to the administration of histamine, specific allergens, as well as to cooling (in cold urticaria).

It has practically no anticholinergic or antiserotonin action. In therapeutic doses, it does not cause a sedative effect.

The onset of action of the drug after a single dose of 10 mg is noted after 20 minutes (in 5% of patients), after 60 minutes (in 95% of patients), the duration of action of the drug is more than 24 hours. Tolerance does not develop during course treatment.

After discontinuation of treatment, the effect persists for up to 3 days.

Pharmacokinetics

Absorption

Cetirizine is rapidly absorbed from the gastrointestinal tract.

C_max in blood plasma is reached 1 hour after oral administration. Simultaneous food intake does not affect the degree of absorption of the drug but prolongs the time to reach C_max by 1 hour and reduces C_max by 23%.

Distribution

Plasma protein binding is 93% and does not change at cetirizine concentrations in the range of 25-1000 ng/ml. The pharmacokinetic parameters of cetirizine change linearly when administered at doses from 5 mg to 60 mg.

When taking the drug at a dose of 10 mg once a day for 10 days, C_ss in blood plasma is noted after 0.5-1.5 hours and is 310 ng/ml.

V_d is about 0.5 l/kg. Cetirizine penetrates into breast milk.

Metabolism

Cetirizine is metabolized in small amounts in the liver by O-dealkylation to form a pharmacologically inactive metabolite (unlike other histamine H₁-receptor blockers that are metabolized in the liver with the participation of the cytochrome P₄₅₀ system).

The drug does not accumulate.

Excretion

Two-thirds of the administered dose of cetirizine is excreted unchanged by the kidneys and about 10% in the feces. The systemic clearance of cetirizine is 53 ml/min. T_1/2 in adults is 7-10 hours, in children aged 6-12 years – 6 hours, in children aged 2-6 years – 5 hours.

Pharmacokinetics in special clinical cases

In elderly patients, T_1/2 increases by 50%, systemic clearance decreases by 40% (due to decreased renal function).

In renal failure (creatinine clearance less than 40 ml/min), the systemic clearance of the drug decreases, T_1/2 is prolonged (for example, in patients on hemodialysis, systemic clearance decreases by 70% and is 0.3 ml/min/kg, and T_1/2 is prolonged by 3 times), which requires appropriate adjustment of the dosage regimen.

In chronic liver diseases (hepatocellular, cholestatic, or biliary cirrhosis), there is a prolongation of T_1/2 of cetirizine by 50% and a decrease in systemic clearance by 40% (adjustment of the dosage regimen is required only with a corresponding decrease in the glomerular filtration rate).

Cetirizine is practically not removed by hemodialysis.

Indications

• Seasonal and perennial allergic rhinitis and conjunctivitis (itching, sneezing, rhinorrhea, lacrimation, conjunctival hyperemia);
• Urticaria (including chronic idiopathic urticaria);
• Pollinosis (hay fever);
• Angioneurotic edema;
• Pruritic allergic dermatoses.

ICD codes

Dosage Regimen

Adults and children over 6 years of age are prescribed 10 mg (1 tablet) once a day or 5 mg (1/2 tablet) twice a day.

Patients with impaired renal function (creatinine clearance from 30 to 49 ml/min) are prescribed 5 mg/day, for severe chronic renal failure (creatinine clearance from 10 to 29 ml/min) 5 mg every other day.

The tablets are taken orally with a small amount of water.

Adverse Reactions

From the digestive system: dry mouth, abdominal discomfort.

From the central nervous system: headache, dizziness, migraine.

Allergic reactions: urticaria, angioneurotic edema, skin itching, skin rash.

Contraindications

• Lactase deficiency;
• Galactosemia;
• Glucose-galactose malabsorption syndrome;
• Children under 6 years of age;
• Pregnancy;
• Lactation period (breastfeeding);
• Hypersensitivity to the components of the drug.

With caution, the drug should be prescribed to elderly patients, patients with chronic renal failure.

Use in Pregnancy and Lactation

Cetirinax^® is contraindicated for use during pregnancy and lactation (breastfeeding).

Use in Renal Impairment

Patients with impaired renal function (creatinine clearance from 30 to 49 ml/min) are prescribed 5 mg/day, for severe chronic renal failure (creatinine clearance from 10 to 29 ml/min) 5 mg every other day.

Pediatric Use

The drug is contraindicated in children under 6 years of age.

Children over 6 years of age are prescribed 10 mg (1 tablet) once a day or 5 mg (1/2 tablet) twice a day.

Geriatric Use

It should be prescribed with caution to elderly patients.

Special Precautions

When the daily dose exceeds 10 mg, a decrease in the ability to perform rapid reactions is noted.

It should be taken into account that in moderate and severe chronic renal failure, adjustment of the dosage regimen is required.

In recommended doses, the drug does not enhance the effect of ethanol (at a concentration not exceeding 0.8 g/l). However, it is recommended to refrain from drinking alcohol while using Cetirinax^®.

Effect on the ability to drive vehicles and mechanisms

During treatment with Cetirinax^®, one should refrain from engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Overdose

Symptoms: when taking a single dose of the drug of 50 mg, drowsiness, anxiety, increased irritability, urinary retention, dry mouth, and constipation develop.

Treatment: gastric lavage, intake of activated charcoal; if necessary, symptomatic therapy is carried out. There is no specific antidote. Hemodialysis is ineffective.

Drug Interactions

No pharmacokinetic interaction of cetirizine with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, diazepam, glipizide has been established.

With the simultaneous administration of cetirizine with theophylline (400 mg/day), the systemic clearance of cetirizine decreases. At the same time, the pharmacokinetics of theophylline does not change.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C (77°F).

Shelf Life

The shelf life is 3 years.

Dispensing Status

The drug is approved for use as an over-the-counter product.

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.