Cetirizine Sandoz, 10 mg 10 pcs

Pharmacodynamics:

Cetirizine has a pronounced anti-allergic effect. It has practically no sedative effect in pharmacologically active doses, belongs to selective antagonists of H1-histamine receptors and has practically no anticholinergic and antiserotonin action, prevents development and facilitates allergic reactions.

It has an antipruritic and antiexudative effect. It affects the early stage of allergic reactions and also reduces migration of inflammatory cells; it inhibits the release of mediators involved in late allergic reactions.

Limits capillary permeability, prevents the development of tissue edema, relieves smooth muscle spasm. It eliminates the skin reaction to the introduction of histamine, specific allergens and also to cooling (in case of cold urticaria).

Cetirizine significantly reduces bronchial hyperresponsiveness arising in response to histamine release in patients with bronchial asthma. The therapeutic effect of the drug is manifested on average 60 minutes after intake. Tolerance does not develop during a course of administration.

Pharmacokinetics:

Intake: After oral administration cetirizine is quickly and well absorbed from the gastrointestinal tract. The maximum level of concentration is determined after about 40 – 60 minutes.
Food intake has no significant effect on the amount of absorption, but in this case the absorption rate is slightly reduced.

Distribution: Cetirizine binds with blood plasma proteins by about 93%. Volume of distribution (Vd) is low (0.5 l/kg), the drug does not penetrate into cells.
The drug does not penetrate through the blood-brain barrier.

Metabolism: cetirizine is slightly metabolized in liver with formation of inactive metabolite.
When administered in 10-day dose of 10 mg there is no accumulation of preparation.
Elimation: approximately 70% of drug is kidney-acquired mostly unchanged.
Systemic clearance is approximately 54 ml/min.

After a single single single dose the half-life is about 10 hours. In children aged 2 to 12 years, the half-life is reduced to 5-6 hours.

In patients with impaired renal function (creatinine clearance less than 11-31 ml/min) and in patients on hemodialysis (creatinine clearance less than 7 ml/min) the value of half-life is increased by 3 times, clearance is decreased by 70%.

In chronically ill and elderly patients half-life increases by 50% and clearance decreases by 40%.

Hemodialysis is ineffective.

Indications

Year-round and seasonal allergic rhinitis (symptomatic therapy);
urticaria, incl. chronic idiopathic;
dermatoses that occur with itching (atopic dermatitis, neurodermatitis);
allergic conjunctivitis.

Pharmacological effect

Pharmacodynamics:

Cetirizine has a pronounced antiallergic effect. It has virtually no sedative effect in pharmacologically active doses, is a selective antagonist of H1-histamine receptors and has virtually no anticholinergic and antiserotonin effects, prevents the development and facilitates the course of allergic reactions.

Has antipruritic and antiexudative effect. Affects the early stage of allergic reactions, and also reduces the migration of inflammatory cells; inhibits the release of mediators involved in a late allergic reaction.

Reduces capillary permeability, prevents the development of tissue edema, relieves spasm of smooth muscles. Eliminates skin reactions to the introduction of histamine, specific allergens, as well as to cooling (with cold urticaria).

Cetirizine significantly reduces the hyperreactivity of the bronchial tree that occurs in response to the release of histamine in patients with bronchial asthma. The therapeutic effect of the drug appears on average 60 minutes after administration. During the course of treatment, tolerance does not develop.

Pharmacokinetics:

Absorption: after oral administration, cetirizine is quickly and well absorbed from the gastrointestinal tract. The maximum concentration level is determined after approximately 40 – 60 minutes.
Food intake does not have a significant effect on the amount of absorption, but in this case the rate of absorption is slightly reduced.

Distribution: cetirizine is approximately 93% bound to plasma proteins. The volume of distribution (Vd) is low (0.5 l/kg), the drug does not penetrate into the cell.
The drug does not penetrate the blood-brain barrier.

Metabolism: cetirizine is poorly metabolized in the liver to form an inactive metabolite.
With 10-day use at a dose of 10 mg, no accumulation of the drug is observed.
Excretion: approximately 70% occurs by the kidneys, mainly unchanged.
The systemic clearance is about 54 ml/min.

After a single dose, the half-life is about 10 hours. In children aged 2 to 12 years, the half-life decreases to 5-6 hours.

In case of impaired renal function (creatinine clearance below 11-31 ml/min) and in patients on hemodialysis (creatinine clearance less than 7 ml/min), the half-life increases 3 times, clearance decreases by 70%.

Against the background of chronic diseases and in elderly patients, there is an increase in the half-life by 50% and a decrease in clearance by 40%.

Hemodialysis is ineffective.

Special instructions

During the treatment period, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

The simultaneous use of drugs that depress the central nervous system and alcohol is not recommended.

Instructions for patients with diabetes mellitus:
1 tablet corresponds to less than 0.01 bread. units

Active ingredient

Cetirizine

Composition

1 film-coated tablet contains:

Contraindications

Hypersensitivity to cetirizine or other components of the drug;
severe kidney disease.
children under 6 years of age.
pregnancy,
lactation period.

With caution: chronic pyelonephritis of moderate and severe severity (correction of the dosage regimen is required), old age (possible decrease in glomerular filtration).

Side Effects

From the digestive system: dry mouth, dyspepsia.

From the central nervous system: headache, drowsiness, fatigue, dizziness, agitation, migraine.

Allergic reactions: skin rash, angioedema, urticaria, itching.

The drug is usually well tolerated. Side effects are rare and transient.

Interaction

No clinically significant interactions of cetirizine with other drugs have been established.

Combined use with theophylline (400 mg/day) leads to a decrease in the total clearance of cetirizine (theophylline kinetics does not change).

Overdose

Symptoms: possible drowsiness, lethargy, weakness, headache, tachycardia, increased irritability, urinary retention, fatigue (most often when taking 50 mg of cetirizine per day).

Treatment: carry out symptomatic therapy. A specific antidote has not been identified. Hemodialysis is ineffective. Gastric lavage is performed and activated charcoal is prescribed.

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

3 years

Manufacturer

Salutas Pharma GmbH, Germany