Xizal, 5 mg 14 pcs

Levocetirizine, the active ingredient in Xizal® , is the R-enantiomer of cetirizine, a powerful and selective histamine antagonist that blocks H1-histamine receptors.

Levocetirizine influences the histamine-dependent stage of allergic reactions and also reduces migration of eosinophils reduces vascular permeability and limits the release of inflammatory mediators.

Levocetirizine prevents and facilitates the development of allergic reactions has antiexudative antipruritic action with practically no anticholinergic and antiserotonin action. In therapeutic doses has practically no sedative effect.

Pharmacokinetics:

The pharmacokinetic parameters of levocetirizine change linearly.

Intake

After oral administration, the drug is quickly and completely absorbed from the gastrointestinal tract. Food intake does not affect the completeness of absorption, although it reduces its rate. Maximal concentration (Cmax) in blood plasma is reached after 09 hours and equals 270 ng/ml Equilibrium concentration is reached after 2 days.

Distribution

Levocetirizine is 90% bound to plasma proteins. The volume of distribution (Vd) is 04 l/kg. Bioavailability reaches 100%.

Metabolism

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

Elimination

The elimination half-life (T1/2) in adults is 79 ±19 hours.

The elimination half-life is shorter in young children. In adults, the total clearance is 063 ml/min/kg.

About 854% of the taken dose of the drug is excreted unchanged by the kidneys through glomerular filtration and tubular secretion; about 129% – through the intestine.

Patients with renal impairment

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

Patients with hepatic impairment

Pharmacokinetics of levocetirizine in patients with hepatic impairment has not been studied.

In patients with chronic liver disease (hepatocellular cholestatic and biliary cirrhosis) who received racemic cetirizine compound in dose of 10 or 20 mg once, a 50% increase in half-life and 40% decrease in clearance of the drug were observed compared to healthy subjects.

Children

The data from a study of the pharmacokinetics of the drug in 14 children aged 6 to 11 years with a body weight of 20 to 40 kg when 5 mg of levocetirizine was taken orally once showed that the Cmax and area under the curve (AUC) were approximately twice that of healthy adults in a cross-match control. The mean Cmax was 450 ng/mL and maximum concentration was reached after an average of 12 hours total body weight-adjusted clearance was 30% higher and the half-life was 24% shorter in children than in adults.

Special pharmacokinetic studies in children younger than 6 years have not been conducted. A retrospective pharmacokinetic analysis was performed 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) receiving one or more doses of levocetirizine from 125 mg to 30 mg.

The data obtained in the analysis showed that administration of the drug in a dose of 125 mg in children aged 6 months to 5 years resulted in plasma concentrations corresponding to those in adults when 5 mg of the drug was taken once daily.

Elderly patients

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

Indications

For adults and children over 6 years: Treatment of symptoms of year-round and seasonal allergic rhinitis and allergic conjunctivitis, such as conjunctival hyperemia, itching, sneezing, lacrimation,; hay fever (pollinosis); urticaria, including chronic idiopathic urticaria, Quincke’s edema; other allergic dermatoses accompanied by itching and rashes.

Active ingredient

Composition

1 tablet contains:

The core:

the active ingredient: levocetirizine dihydrochloride 5.0 mg;

the excipients: lactose monohydrate 63.50 mg, microcrystalline cellulose 30.00 mg, colloidal silicon dioxide 0.50 mg, magnesium stearate 1.00 mg.

The shell: opadray Y-1-7000 3.00 mg (contains hypromellose 62.5%, titanium dioxide (E171) 31.25%, macrogol 400 6.25%).

How to take, the dosage

It is taken orally with food or on an empty stomach with a small amount of water, without chewing. Adults and children over 6 years of age: daily dose is 5 mg (1 tablet).

Elderly patients (with normal renal function) do not need dose reduction.

For patients with chronic renal failure, the dose is reduced by half (1 tablet every other day) for CKR of 30 to 49 ml/min and by 3 times (1 tablet every 3 days) for CKR of 10 to 29 ml/min.

Patients with hepatic insufficiency do not require dosage regimen correction.

The duration of treatment depends on the disease. For the treatment of pollinosis it is prescribed for 1-6 weeks on average. In chronic diseases (year-round rhinitis, atonic dermatitis) the treatment duration may be increased up to 18 months.

Interaction

The study of interaction of levocetirizine with other medicinal products has not been conducted.

In the study of drug interactions of cetirizine racemate with azithromycin cimetidine diazepam erythromycin glipizide ketoconazole and pseudoephedrine no clinically significant adverse interactions were found.

Concomitant use with theophylline (400 mg/day) decreases total clearance of cetirizine by 16% (theophylline kinetics is not changed).

In a study with concomitant administration of ritanovir (600 mg twice daily) and cetirizine (10 mg daily) it was shown that exposure to cetirizine increased by 40% and exposure to ritanovir changed only slightly (-11%).

In sensitive patients, concomitant use of levocetirizine and alcohol or medications that have an inhibitory effect on the central nervous system (CNS) may cause lethargy and impaired performance.

Special Instructions

Dose intervals should be adjusted individually depending on renal function.

Cautious use with alcohol is recommended.

Patients with predisposing factors to urinary retention (e.g., spinal cord injury, prostatic hyperplasia) should be cautious because levocetirizine may increase the risk of urinary retention.

Caution should be exercised in patients with epilepsy and increased seizure readiness because levocetirizine may cause exacerbation of seizures.

The reaction to skin allergy tests is suppressed with antihistamines and the drug must be withheld for 3 days before testing.

Itching may occur after discontinuation of levocetirizine even if there were no such symptoms at the beginning of treatment. The symptoms may go away on their own. In some cases the symptoms may be severe and may require resumption of treatment. Once treatment is resumed, the symptoms should go away.

In children

Levocetirizine film-coated tablets are contraindicated in children under 6 years of age because this dosage form does not allow for a suitable dosage for this age group. It is recommended to use the pediatric dosage form (orally administered drops).

Levocetirizine may cause increased somnolence; therefore, Xizal® may affect ability to drive or operate machinery. During the treatment period it is necessary to refrain from potentially dangerous activities requiring high concentration and quick psychomotor reactions.

Contraindications

Hypersensitivity to the active substance cetirizine hydroxyzine any piperazine derivative or any other excipient of the drug.

Lactase deficiency lactose intolerance glucose-galactose malabsorption.

The terminal stage of renal failure (creatinine clearance < 10 ml/min).

Children under 6 years of age.

In chronic renal failure (dosing regimen must be adjusted).

In elderly patients (with age-related decrease in glomerular filtration).

In patients with spinal cord injury, prostatic hyperplasia and other predisposing factors to urinary retention because levocetirizine may increase the risk of urinary retention.

In concomitant use with alcohol (see Interaction with other drugs).

Pregnancy and the period of breastfeeding.

Caution should be exercised in patients with epilepsy and increased seizure readiness because levocetirizine may cause exacerbation of seizures.

Side effects

Headache, fatigue, drowsiness, dry mouth.

Rarely – migraine, dizziness, dyspeptic disorders, allergic reactions (angioedema, rash, urticaria, itching).

Overdose

Symptoms: may be accompanied by signs of intoxication in the form of drowsiness, in children overdose of the drug may be accompanied by anxiety and increased irritability.

Treatment: in case of overdose symptoms (especially in children) the drug should be stopped, gastric lavage, activated charcoal, symptomatic therapy should be used. There is no specific antidote.

Pregnancy use

Pregnancy

The data on the use of levocetirizine during pregnancy are almost non-existent or limited (less than 300 pregnancy outcomes). However, the use of cetirizine racemate levocetirizine in pregnancy (more than 1000 pregnancy outcomes) was not accompanied by malformations and intrauterine and neonatal toxic effects. No direct or indirect adverse effects on fetal and foetal development and postnatal development were found in animal studies.

The administration of levocetirizine in pregnancy may be considered if necessary.

Breastfeeding period

The cetirizine racemate levocetirizine is excreted with breast milk. Therefore, excretion of levocetirizine with breast milk is also likely. Breast-fed children may have adverse reactions to levocetirizine. Therefore it is necessary to observe caution when prescribing levocetirizine during breastfeeding.

Fertility

There are no clinical data on levocetirizine.

Consult your doctor before using the drug if you are pregnant or think you might be pregnant or are planning to become pregnant.

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