Xizal - instructions for use, dose, side effects, contraindications

Excipients: lactose monohydrate 63.50 mg, cellulose microcrystalline 30.00 mg, silicon dioxide colloid 0.50 mg, magnesium stearate 1.00 mg, opadrai Y-1-7000 3.00 mg (contains hypromellose 62.5%, titanium dioxide (E171) 31.25%, macrogol 400 6.25%).

Description:

Oval-shaped tablets, coated with a film coat of white or almost white. On one side of the tablet the "Y".

Pharmacotherapeutic group:Antiallergic agent - H1-histamine receptor blocker

ATX: & nbsp

R.06.A.E. Piperazine derivatives

E.06.A.E.09 Levocetirizine

Pharmacodynamics:

Levocetirizine, the active substance of Xisal®, is R-enantiomer of cetirizine, which belongs to the group of competitive histamine antagonists and blocks H₁ histamine receptors.

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

Levocetirizine prevents the development and facilitates the course of allergic reactions, has antiexudative, antipruritic effect, practically does not exert anticholinergic and antiserotonin action. In therapeutic doses, it practically does not have a sedative effect.

Pharmacokinetics:

The pharmacokinetic parameters of levocetirizine vary linearly.

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

Levocetirizine binds to blood plasma proteins by 90%. Volume of distribution (Vd) is 0.4 l / kg. Bioavailability reaches 100%.

Less than 14% of the drug is metabolized in the liver with the formation of a pharmacologically inactive metabolite.

The half-life (T1 / 2) in adults is 7.9 ± 1.9 hours. In adults, the total clearance is 0.63 ml / min / kg. About 85,4% of the accepted dose of the drug is excreted by the kidneys, about 12,9% - through the intestine. In patients with renal failure with creatinine clearance less than 40 ml / min, the clearance of the drug decreases. In patients on hemodialysis, the total clearance is reduced by 80%, which requires a change in the appropriate dosing regimen. Less than 10% of the drug is removed during a standard 4-hour hemodialysis procedure.

Indications:

Treatment of symptoms of year-round (persistent) and seasonal (intermittent) allergic rhinitis and allergic conjunctivitis such as itching, sneezing, nasal congestion, rhinorrhea,lacrimation, hyperemia of the conjunctiva;

Pollinosis (hay fever);

Hives;
Other allergic dermatoses, accompanied by itching and rashes.

Contraindications:

Hypersensitivity to levocetirizine or piperazine derivatives, as well as other components of the drug;

Deficiency of lactase, lactose intolerance, glucose-galactose malabsorption;

Terminal stage of renal failure (creatinine clearance <10 ml / min);

Children under 6 years of age (due to limited safety and efficacy data);

Pregnancy and the period of breastfeeding.

Carefully:

In chronic renal failure (correction of the dosing regimen is necessary);

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

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

When used concomitantly with alcohol (see Interaction with other medicinal products).

Pregnancy and lactation:

Preclinical studies did not reveal any direct or indirect adverse effects of levocetirizine on the developing fetus, as well as on development in the postnatal period; the course of pregnancy and childbirth also did not change.

Adequate and strictly controlled clinical trials on the safety of the drug during pregnancy have not been conducted.

The use of the drug during pregnancy is contraindicated.

Levocetirizine is excreted in breast milk, so if it is necessary to use the drug in lactation it is recommended to stop breastfeeding.

Dosing and Administration:

Film coated tablets are taken orally, swallowing whole, with food or on an empty stomach, with a small amount of water.

Adults and children over 6 years of age: The daily dose is 5 mg (1 tablet) once.

Because the levocetirizine is excreted from the body by the kidneys, when the drug is used in patients with renal insufficiency and elderly patients The dose should be adjusted depending on the degree of renal failure.

Patients with mild renal impairment (creatinine clearance 50-79 ml / min) dose adjustment is not required.

In patients with moderate renal insufficiency (clearance of creatinine from 30 to 49 ml / min) the recommended dose of 5 mg every other day.

In patients with severe renal insufficiency (creatinine clearance less than 30 ml / min) the recommended dose of 5 mg once every 3 days.

Patients with renal and hepatic impairment dosing is carried out according to the above scheme.

Patients with a violation of only liver function correction of the dosing regimen is not required.

Duration of the drug:

In the treatment of seasonal (intermittent) rhinitis (the presence of symptoms less than 4 days a week or their total duration is less than 4 weeks), the duration of treatment depends on the duration of the symptomatology; Treatment can be stopped if symptoms disappear and are resumed when symptoms appear.

In the treatment of 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 can continue throughout the exposure period of allergens.

There is a clinical experience of the continuous use of Xisal® in adult patients lasting up to 6 months.

If you are taking (or have recently taken) other drugs, including over-the-counter drugs, tell your doctor about it.

If you forget to take Xisal®, do not take a double dose to compensate for missed, take the next dose at the usual time.

Side effects:

During clinical trials in men and women 12-71 years, the most often (≥1 / 100, <1/10), the following side effects occurred: headache, drowsiness, dry mouth, fatigue, infrequently (≥1 / 1000, <1/100) met asthenia and abdominal pain.

During clinical trials in children aged 6 to 12 years, the most often (≥1 / 100, <1/10) there was a headache and drowsiness.

During the post-marketing use of the drug, the following side effects were observed, the frequency of which is unknown due to insufficient data.

From the immune system

Hypersensitivity reactions, including anaphylaxis

From metabolism and eating disorders

Increased appetite

From the side of the psyche

Anxiety, aggression, agitation, insomnia, hallucinations, depression, suicidal thoughts

From the nervous system

Convulsions, thrombosis of the dura of the dura mater, paresthesia, dizziness, fainting, tremor, dysgeusia

From the side of hearing

Vertigo

From the side of the organ of vision

Visual impairment, blurred vision, inflammatory manifestations

From the cardiovascular system:

Angina pectoris, tachycardia, palpitations, jugular vein thrombosis

From the respiratory system:

Shortness of breath, increased symptoms of rhinitis

From the digestive system:

Nausea, vomiting

Hepatobiliary disorders:

Hepatitis, changes in functional liver samples

From the side of the kidneys and the urinary system:

Dysuria, urinary retention

From the skin and soft tissues:

Angioedema, persistent drug erythema, rash, itching, urticaria, hypotrichosis, fissures, photosensitivity

From the musculoskeletal system:

Muscle pain

General disorders:

Peripheral edema, weight gain

Other:

Cross reactivity

If any of the side effects indicated in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

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

Treatment: wash your stomach or take Activated carbon, if after the drug has passed a little time. Symptomatic and maintenance therapy is recommended. There is no specific antidote. Hemodialysis is not effective.

Interaction:

The interaction of levocetirizine with other drugs has not been studied. In the study of the drug interaction of the racemate cetirizine with phenazone, pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam, no clinically relevant undesirable interactions have been identified.

With simultaneous application with theophylline (400 mg / day), the total clearance of cetirizine is reduced by 16% (theophylline kinetics does not change).

In a study with simultaneous administration of ritanovir (600 mg twice daily) and cetirizine (10 mg per day), it was shown that the exposure of cetirizine increased by 40%, and the exposure of ritanovir slightly changed (-11%).

In a number of cases, with simultaneous application of levocetirizine with alcohol or drugs,having an inhibitory effect on the central nervous system (CNS), it is possible to enhance their effect on the central nervous system, although it has not been proven that the racemate of cetirizine potentiates the effect of alcohol.

Effect on the ability to drive transp. cf. and fur:

Levocetirizine can lead to increased drowsiness, therefore, Xisal ® may affect the ability to drive or work with machinery. During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Film coated tablets 5 mg.

Packaging:

For 7 or 10 tablets in a blister of PVC - aluminum foil. 1 or 2 blisters together with instructions for use in a cardboard bundle.

Storage conditions:

In a dry place at a temperature of no higher than 25 °. Keep out of the reach of children!

Shelf life:

4 years

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:П N016137 / 01

Date of registration:19.11.2009

The owner of the registration certificate:FSB Farshim S.A.FSB Farshim S.A. Switzerland

Manufacturer: & nbsp

UCB FARCHIM, S.A. Switzerland

Representation: & nbspYUSB FARMA LLC YUSB FARMA LLC Russia

Information update date: & nbsp02.11.2015

Illustrated instructions

Instructions

Xizal® (Xyzal®)