Cetirizine Sandoz, 10 pcs., 10 mg, film-coated tablets

Cetirizine Sandoz, 10 pcs., 10 mg, film-coated tablets

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.

CETIRIZINE SANDOZ 10MG N10 TAB P/O

Inside,

with water, regardless of meals.

Adults and teenagers over 12 years of age:

It is recommended to take 20 drops (10 mg) or 1 tablet. daily, preferably in the evening.

Children aged 6–12 years:

10 drops (5 mg) 2 times a day in the morning and evening or 20 drops (10 mg) in the evening; for tablets - with body weight less than 30 kg - 1/2 tablet, coated, in the evening; for body weight more than 30 kg - 1 tablet, coated, in the evening. You can take 2 times a day (morning and evening), 1/2 tablet.

Children aged 2–6 years:

10 drops (5 mg) in the evening or 5 drops (2.5 mg) in the morning and evening.

Children aged 1–2 years:

5 drops (2.5 mg) 2 times a day.

Elderly patients

with normal renal function no dose adjustment is required.

Patients with renal failure

The dose of cetirizine should be adjusted depending on the creatinine Cl value.

Creatinine Cl for men can be calculated based on plasma creatinine concentration using the formula:

Cl creatinine, ml/min = ([140? age, years] ? body weight, kg): 72 ? Plasma creatinine Cl, mg/dL

Creatinine Cl for women can be calculated by multiplying the resulting value by a factor of 0.85.

Dose adjustment is carried out taking into account the table data.

Table

For children with renal failure, dose adjustment of cetirizine in drops for oral administration is carried out individually, taking into account creatinine Cl, age and body weight.

For adult patients with both renal and hepatic insufficiency, dose adjustment is carried out according to the table above.

Patients with impaired liver function alone do not require dose adjustment of cetirizine drops for oral administration.

In case of liver dysfunction

it is necessary to select the dose of cetirizine tablets individually, especially carefully with simultaneous renal failure.

The duration of treatment is determined individually; usually, for seasonal allergic rhinitis, the duration of therapy is from 3 to 6 weeks, and for short-term exposure to pollen, 1 week is sufficient.

The duration of therapy for children over 6 years of age ranges from 2 to 4 weeks, and for short-term exposure to the allergen, 1 week is sufficient.

Cetirizine Sandoz film-coated tablets 10 mg No. 10

pharmachologic effect

Cetirizine is a competitive histamine antagonist, a metabolite of hydroxyzine, and blocks H1-histamine receptors.
Prevents the development and facilitates the course of allergic reactions, has antipruritic and antiexudative effects. Affects the early stage of allergic reactions, limits the release of inflammatory mediators at the late stage of the allergic reaction, reduces the migration of eosinophils, neutrophils and basophils. Reduces capillary permeability, prevents the development of tissue edema, relieves spasm of smooth muscles. relieves skin reactions to the introduction of histamine, specific allergens, as well as to cooling (with cold urticaria). It has virtually no anticholinergic and antiserotonin effects. In therapeutic doses it practically does not cause a sedative effect. The onset of action after a single dose of 10 mg of cetirizine is 20 minutes (in 50% of patients) and 60 minutes (in 95% of patients), lasting more than 24 hours. During a course of treatment, tolerance to the antihistamine effect of cetirizine does not develop. After stopping treatment, the effect lasts up to 3 days. Pharmacokinetics: Rapidly absorbed from the gastrointestinal tract, time to reach Cmax after oral administration is 1 hour. Food does not affect the completeness of absorption (AUC), but prolongs the time to reach Cmax by 1 hour and reduces Cmax by 23%. When taken at a dose of 10 mg 1 time/day for 10 days, the equilibrium concentration in plasma is 310 ng/ml and is observed 0.5-1.5 hours after administration. Plasma protein binding is 93% and does not change with cetirizine concentrations in the range of 25-1000 ng/ml. The pharmacokinetic parameters of cetirizine change linearly when administered at a dose of 5-60 mg. Vd - 0.5 l/kg. In small quantities, it is metabolized in the liver by O-dealkylation to form a pharmacologically inactive metabolite (unlike other H1-histamine receptor blockers, which are metabolized in the liver with the participation of the cytochrome P450 system). Does not accumulate. 2/3 of the drug is excreted unchanged by the kidneys and about 10% through the intestines. Systemic clearance is 53 ml/minute. T1/2 in adults - 7-10 hours, in children 6-12 years old - 6 hours, in children 2-6 years old - 5 hours, in children from 6 months to 2 years - 3 hours. In elderly patients, T1/2 increases by 50%, systemic clearance decreases by 40% (decreased renal function).

In patients with impaired renal function (creatinine clearance below 40 ml/min), drug clearance decreases and T1/2 lengthens (for example, in patients on hemodialysis, the total clearance decreases by 70% and is 0.3 ml/min/kg, and T1/2 is extended by 3 times), which requires a corresponding change in the dosage regimen. In patients with chronic liver diseases (hepatocellular, cholestatic or biliary cirrhosis), an increase in T1/2 by 50% and a decrease in total clearance by 40% are observed (adjustment of the dosage regimen is required only with a concomitant decrease in glomerular filtration rate). Passes into breast milk.

Indications

• seasonal and year-round allergic rhinitis and conjunctivitis (itching, sneezing, rhinorrhea, lacrimation, conjunctival hyperemia);
• urticaria (including chronic idiopathic urticaria);
• hay fever (hay fever);
• itching;
• angioedema (Quincke's edema);
• itchy allergic dermatoses.

Contraindications

• decreased renal function (creatinine clearance 30-49 ml/min);
• chronic renal failure;
• children under 6 years of age;
• pregnancy;
• lactation period;
• hypersensitivity to cetirizine, other components of the drug, hydroxyzine.

With caution: older age (possibly decreased glomerular filtration rate).

Use during pregnancy and breastfeeding

Contraindicated during pregnancy and lactation.

special instructions

Concomitant use with alcohol and drugs that depress the central nervous system is not recommended.

Impact on the ability to drive vehicles and operate machinery: During the treatment period, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions. If the dose exceeds 10 mg/day, the ability to react quickly may deteriorate.

Compound

1 film-coated tablet contains: active substance: cetirizine dihydrochloride 10 mg; excipients: microcrystalline cellulose, lactose monohydrate, crospovidone, magnesium stearate, colloidal silicon dioxide. shell composition: [hypromellose, talc, titanium dioxide, macrogol 4000] or [dry white film shell containing hypromellose, talc, titanium dioxide, macrogol 4000].

Directions for use and doses

Inside, the tablets are washed down with 200 ml of water, the drops are dissolved in water before taking. Adults and children over 6 years old - 10 mg once a day or 5 mg 2 times a day, children 2-6 years old - 5 mg once a day or 2.5 mg 2 times a day, children 1-2 years old - 2.5 mg (5 drops) 2 times a day. In patients with reduced renal function (creatinine clearance 30-49 ml/min) 5 mg/day is prescribed; for severe chronic renal failure (creatinine clearance 10-30 ml/min) - 5 mg/day every other day.

Side effects

Cetirizine is usually well tolerated. Side effects occur rarely and are transient.

From the digestive system: dry mouth, dyspepsia.

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

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

Drug interactions

Combined use with theophylline (400 mg/day) leads to a decrease in the overall clearance of cetirizine (theophylline kinetics does not change). Myelotoxic drugs increase the manifestations of hematotoxicity of the drug. No clinically significant interactions were found with other drugs (pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, diazepam, glipizide).

Overdose

Symptoms: taking the drug once in a dose of over 50 mg may be accompanied by signs of intoxication in the form of drowsiness, anxiety and increased irritability; signs of anticholinergic action may appear in the form of urinary retention, dry mouth, constipation. Treatment: induce vomiting, rinse the stomach, take activated charcoal, consult a doctor immediately. There is no specific antidote. Hemodialysis is ineffective.

Storage conditions

In a place protected from light, at a temperature of 2-25°C.

Best before date

2 years.

Active substance

Cetirizine

Conditions for dispensing from pharmacies

Over the counter

Dosage form

pills

Purpose

For adults, Children over 6 years old