Xizal, 7 pcs., 5 mg, film-coated tablets

Xizal, 7 pcs., 5 mg, film-coated tablets

Inside,

during meals or on an empty stomach. Swallow film-coated tablets whole with a small amount of water. To take the drug in the form of drops, use a teaspoon. If necessary, the dose of the drug can be diluted in a small amount of water immediately before use.

Adults and children over 6 years of age:

The daily dose is 5 mg (1 tablet or 20 drops) once.

Children from 2 to 6 years old:

1.25 mg (5 drops) 2 times a day; daily dose - 2.5 mg (10 drops).

Since levocetirizine is excreted from the body by the kidneys, when using the drug in patients with renal failure and elderly patients, the dose should be adjusted depending on the creatinine clearance. Creatinine clearance for men can be calculated from serum creatinine concentration using the following formula:

Creatinine Cl, ml/min

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

Elderly patients with normal renal function do not require dose reduction; in patients with chronic renal failure, dose calculation should be carried out taking into account creatinine clearance according to the table below.

For patients with renal and hepatic insufficiency, dosing is carried out according to the table above.

In patients with impaired liver function only, no dosage adjustment is required.

Duration of taking the drug:

when treating seasonal (intermittent) rhinitis (the presence of symptoms less than 4 days a week or their total duration less than 4 weeks), the duration of treatment depends on the nature of the disease; Treatment may be stopped when symptoms disappear and resumed when symptoms appear. When treating year-round (persistent) allergic rhinitis (the presence of symptoms more than 4 days a week and their total duration of more than 4 weeks), treatment is possible throughout the entire period of exposure to allergens. There is clinical experience with the continuous use of Xyzal® tablets in adult patients for up to 6 months.

Xyzal®

The pharmacokinetic parameters of levocetirizine change linearly.

Suction

After oral administration, the drug is quickly and completely absorbed from the gastrointestinal tract. Eating does not affect the completeness of absorption, although it reduces its speed. The maximum concentration (Cmax) in blood plasma is reached after 0.9 hours and is 270 ng/ml, the equilibrium concentration is reached after 2 days.

Distribution

Levocetirizine is 90% bound to plasma proteins. The volume of distribution (Vd) is 0.4 l/kg. Bioavailability reaches 100%.

Metabolism

In small quantities (<14%) it is metabolized in the body by N- and O-dealkylation (unlike other H1-histamine receptor antagonists, which are metabolized in the liver using the cytochrome system) to form a pharmacologically inactive metabolite. Due to negligible metabolism and lack of metabolic potential, interaction of levocetirizine with other drugs is unlikely.

Removal

The half-life (T1/2) in adults is 7.9 ± 1.9 hours.

In young children, the half-life is shorter. In adults, the total clearance is 0.63 ml/min/kg.

About 85.4% of the administered dose of the drug is excreted unchanged by the kidneys through glomerular filtration and tubular secretion; about 12.9% - through the intestines.

Selected patient groups

Patients with kidney failure

In patients with renal failure (creatinine clearance (CC) < 40 ml/min), drug clearance is reduced. In hemodialysis patients, total clearance is reduced by 80%. Less than 10% of the drug is removed during a standard 4-hour hemodialysis procedure.

Patients with liver failure

The pharmacokinetics of levocetirizine in patients with hepatic impairment have not been studied.

In patients with chronic liver diseases (hepatocellular, cholestatic and biliary cirrhosis) receiving the racemic compound cetirizine at a dose of 10 or 20 mg as a single dose, an increase in half-life by 50% and a decrease in clearance of the drug by 40% were observed, compared with healthy people.

Children

Data from a study of the pharmacokinetics of the drug in 14 children aged 6 to 11 years weighing from 20 to 40 kg with a single oral dose of 5 mg of levocetirizine showed that Cmax and area under the curve (AUC) were approximately twice as high as in healthy adults with cross-control. The mean Cmax was 450 ng/ml, the maximum concentration was reached after an average of 1.2 hours, the total body weight-adjusted clearance was 30% higher, and the half-life was 24% shorter in children than in adults.

Specific pharmacokinetic studies have not been conducted in children under 6 years of age. A retrospective pharmacokinetic analysis was conducted in 323 patients (181 children aged 1 to 5 years, 18 children aged 6 to 11 years, and 124 adults aged 18 to 55 years) who received one or more doses of levocetirizine 1.25 mg. up to 30 mg.

Data obtained during the analysis showed that taking the drug at a dose of 1.25 mg in children aged 6 months to 5 years leads to plasma concentrations similar to those in adults when taking 5 mg of the drug once a day.

Elderly patients

Pharmacokinetic data in elderly patients is limited. When repeated dosing of levocetirizine 30 mg once daily for 6 days in 9 elderly patients (ages 65 to 74 years) total clearance was approximately 33% lower than that in younger adults. The distribution of cetirizine racemate has been shown to be more dependent on renal function than on age. This statement may also apply to levocetirizine, since both levocetirizine and cetirizine are excreted primarily in the urine. Therefore, in elderly patients, the dose of levocetirizine should be adjusted depending on renal function.

Xyzal 5 mg, 7 film-coated tablets

Registration Certificate Holder

UCB FARCHIM (Switzerland)

Dosage form

Medicine - Xyzal®

Description

Drops for oral administration

in the form of an almost colorless, slightly opalescent solution.

1 ml

Levocetirizine dihydrochloride 5 mg

Excipients

: sodium acetate, acetic acid, propylene glycol, glycerol 85%, methyl parahydroxybenzoate, propyl parahydroxybenzoate, sodium saccharinate, purified water.

10 ml - dark glass bottles with a dropper (1) - cardboard packs. 20 ml - dark glass bottles with a dropper (1) - cardboard packs.

Indications

Symptomatic treatment of allergic diseases and conditions:

• year-round (persistent) and seasonal (intermittent) allergic rhinitis and allergic conjunctivitis (itching, sneezing, rhinorrhea, lacrimation, conjunctival hyperemia, nasal congestion);
• hay fever (hay fever);
• urticaria (including chronic idiopathic urticaria);
• Quincke's edema;
• other allergic dermatoses, accompanied by itching and rashes.

Contraindications for use

• end-stage renal failure (creatinine clearance less than 10 ml/min);
• children under 6 years of age (for tablets);
• children under 2 years of age (for oral drops);
• pregnancy;
• hypersensitivity to the components of the drug, especially in patients with galactosemia or severe lactose intolerance (for tablets);
• hypersensitivity to levocetirizine or piperazine derivatives.

Carefully _

The drug should be used for chronic renal failure (dosage regimen adjustment is required), in elderly patients (with an age-related decrease in glomerular filtration).

pharmachologic effect

The histamine H1 receptor blocker, an enantiomer of cetirizine, belongs to the group of competitive histamine antagonists. The affinity for histamine H1 receptors of levocetirizine is 2 times higher than that of cetirizine.

Levocetirizine has an effect on the histamine-dependent stage of allergic reactions, and also reduces the migration of eosinophils, reduces vascular permeability, and limits the release of inflammatory mediators. Prevents the development and facilitates the course of allergic reactions, has an antiexudative, antipruritic effect, and has virtually no anticholinergic and antiserotonin effects. In therapeutic doses it has virtually no sedative effect.

Drug interactions

The interaction of levocetirizine with other drugs has not been studied.

When studying the drug interactions of cetirizine racemate with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam, no clinically significant adverse interactions were identified.

When used simultaneously with theophylline (400 mg/day), the total clearance of cetirizine is reduced by 16%, the pharmacokinetic parameters of theophylline do not change.

In some cases, with simultaneous use of levocetirizine with ethanol or drugs that have a depressant effect on the central nervous system, their effect on the central nervous system may be enhanced, although cetirizine racemate has been proven to potentiate the effect of alcohol.

Dosage regimen

The drug is prescribed orally during meals or on an empty stomach.

The tablets are taken with a small amount of water, without chewing.

Drops for oral administration are taken with a teaspoon. If necessary, the dose of the drug can be diluted in a small amount of water immediately before use.

Adults and children over 6 years old

: daily dose 5 mg (1 tablet or 20 drops).

Children aged 2 to 6 years:

1.25 mg (5 drops) 2 times/day; daily dose - 2.5 mg (10 drops).

Since levocetirizine is excreted by the kidneys, when prescribing the drug to elderly patients and patients with renal failure

the dose should be adjusted depending on the CC value.

CC can be calculated based on serum creatinine concentration using the following formula.

For men:

CC (ml/min)= [140-age (years)] × body weight (kg)/72 × serum creatinine (mg/dl)

For women:

obtained value × 0.85

Renal failure CC (ml/min) Dose and frequency of administration

Normal>805 mg/dayMild50-795mg/dayModerate30-495mg/day once every 2 daysSevere<305 mg/day once every 3 daysTerminal stage (patients on hemodialysis)<10 The drug is contraindicated

For patients with
renal and hepatic insufficiency,
dosing is carried out according to the table above.
Patients with impaired liver function alone
do not require dosage adjustment.

The duration of use depends on the indications. Treatment course for hay fever

averages 1-6 weeks.
For chronic diseases (year-round rhinitis, atopic dermatitis
), the duration of treatment can increase to 18 months.

Overdose

Symptoms:

drowsiness (in adults), agitation and anxiety, followed by drowsiness (in children).

Treatment:

immediately after taking the drug, perform gastric lavage or induce artificial vomiting. It is recommended to prescribe activated carbon and carry out symptomatic and supportive therapy. There is no specific antidote. Hemodialysis is ineffective.

Side effect

Possible side effects are listed below by body system and frequency of occurrence: often (≥1/10); uncommon (from ≥1/100 to <1/10); rare (from ≥1/1000 to <1/100); very rare (from ≥1/10,000 to <1/1000).

From the side of the central nervous system:

infrequently - headache, fatigue, drowsiness; rarely - asthenia; very rarely - aggression, agitation, convulsions, hallucinations, depression, visual impairment.

From the cardiovascular system:

very rarely - tachycardia.

From the respiratory system:

very rarely - dyspnea.

From the digestive system:

uncommon - dry mouth; rarely - abdominal pain; very rarely - nausea, diarrhea, hepatitis, changes in liver function tests.

From the musculoskeletal system:

very rarely - myalgia.
Metabolic:
very rarely - weight gain.

Allergic reactions:

very rarely - itching, rash, urticaria, angioedema, anaphylaxis.

special instructions

The patient should be careful when taking the drug and drinking alcohol at the same time.
Effect on the ability to drive vehicles and operate machinery.
An objective assessment of the ability to drive vehicles and operate machinery did not reliably reveal any adverse events when the drug was prescribed at the recommended dose. However, during the treatment period, it is advisable to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Storage conditions

Tablets should be stored out of the reach of children, in a dry place at a temperature not exceeding 25°C.

Best before date

Shelf life – 4 years.

Drops for oral administration should be stored out of the reach of children, protected from light at a temperature not exceeding 30°C. Shelf life – 3 years. After opening the bottle, the shelf life is 3 months.

Use during pregnancy and breastfeeding

Restrictions during pregnancy - Contraindicated. Restrictions when breastfeeding - Contraindicated.

Adequate and strictly controlled clinical studies on the safety of the drug in pregnant women have not been conducted, therefore Xyzal® should not be prescribed during pregnancy.

Levocetirizine is excreted in breast milk, so if it is necessary to use the drug during lactation, breastfeeding should be discontinued while taking it.

Experimental studies
on animals did not reveal any direct or indirect adverse effects of levocetirizine on the developing fetus (including in the postnatal period), the course of pregnancy and childbirth also did not change.

Use for renal impairment

Restrictions for impaired renal function - With caution.

Contraindicated in end-stage renal failure (creatinine clearance less than 10 ml/min).

For patients with
chronic renal failure, with a CC of 49-30 ml/min,
the dose is reduced by 2 times (1 tablet every other day),
with a CC of 29-10 ml/min,
the dose is reduced by 3 times (1 tablet 1 time in 3 days ).

Use for liver dysfunction

Restrictions for liver dysfunction - No restrictions.

Patients with hepatic insufficiency do not require dose adjustment.

Use in elderly patients

Restrictions for elderly patients - Use with caution.

Since levocetirizine is excreted by the kidneys, when prescribing the drug to elderly patients, the dose should be adjusted depending on the value of CC.

Use in children

Restrictions for children - With caution.

Contraindicated in children under 6 years of age (for tablets); in children under 2 years of age (for oral drops).

Children over 6 years old

: daily dose 5 mg (1 tablet or 20 drops).
Children aged 2 to 6 years:
1.25 mg (5 drops) 2 times/day; daily dose - 2.5 mg (10 drops).

Terms of sale

The drug is available with a prescription.

Contacts for inquiries

YUSB PHARMA S.A. (Belgium)

YUSB Pharma LLC

105082 Moscow, Perevedenovsky per. 13, p. 21 Tel.; Fax