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

Excipients: sodium acetate 5.70 mg, acetic acid 0.53 mg, propylene glycol 350.00 mg, glycerol 85 % 294.10 mg, methyl parahydroxybenzoate 0.3375 mg, propyl parahydroxybenzoate 0, 0375 mg, sodium saccharinate 10.00 mg, water purified to 1.00 ml.

Description:

Practically colorless slightly opalescent solution.

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

Pharmacokinetics:

Pharmacokinetic parameters of levocetirizine vary linearly and practically do not differ from the pharmacokinetics of cetirizine.

Suction. After ingestion, the drug is quickly and completely absorbed from the gastrointestinal tract.The intake of food does not affect the completeness of absorption, although its rate decreases. In adults, after a single dose at a therapeutic dose (5 mg), the maximum concentration (C_m_Oh) in the blood plasma is achieved after 0.9 hours and is 270 ng / ml, after repeated administration at a dose of 5 mg-308 ng / ml. The equilibrium concentration is achieved after 2 days.

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

Metabolism. In small amounts (<14%) is metabolized in the body by N- and O-dealkylation (as opposed to other antagonists H₁-gistaminovyh receptors, which are metabolized in the liver with the help of a system of cytochromes) to form a pharmacologically inactive metabolite. Due to the insignificant metabolism and lack of metabolic potential, the interaction of levocetirizine with other drugs is unlikely.

Excretion. In adults, the half-life (T_1/2) is 7.9 ± 1.9 hours; in young children T_1/2is shortened. 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 in unchanged form by glomerular filtration and tubular secretion; about 12.9% through the intestine.

In patients with renal insufficiency (creatinine clearance (CK) <40 ml / min), the clearance of the drug decreases, and T_1/2lengthens (for example, in patients on hemodialysis, the total clearance is reduced by 80%), which requires a corresponding change in the dosing regimen. Less than 10% of levocetirizine 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, conjunctival hyperemia;

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;

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

Children under 2 years of age (due to limited data on efficacy and safety of the drug);

Pregnancy and the period of breastfeeding

Carefully:

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

In elderly people (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 {cm. 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, therefore, if it is necessary to use the drug during pregnancy, it is recommended to stop breastfeeding.

Dosing and Administration:

The drug is taken orally during meals or on an empty stomach. To take the drug should 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 (20 drops) once.

Children from 2 to 6 years: for 1.25 mg (5 drops) 2 times a day; daily dose of 2.5 mg (10 drops).

Because the levocetirizine is excreted from the body by the kidneys, when the drug is used patients with renal insufficiency and elderly patients The dose should be adjusted depending on the amount of creatinine clearance (CC).

The creatinine clearance for men can be calculated based on the serum creatinine concentration, according to the following formula:

[140 - age (years)] х body weight (kg)

KK (ml / min) = ------------------------------------------- ----------------

72 х КК_serum (mg / dL)

KK for women can be calculated by multiplying the obtained value by a factor of 0.85.

Renal insufficiency	CK (ml / min)	Dosing regimen
Norm	>80	5 mg / day
Lightweight	50-79	5 mg / day
Average	30-49	5 mg / day x every 2 days
Heavy	<30	5 mg / day x every 3 days
Terminal stage - patients on dialysis	< 10	The drug is contraindicated

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

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 of less than 4 weeks) duration of treatment depends on the nature of the disease; 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 tablets in adult patients lasting up to 6 months.

Side effects:

At the time of clinical trials in males and females 12-71 years often (≥1 / 100, <1/10), the following adverse events were observed: headache, drowsiness, dry mouth, fatigue, infrequently (≥1 / 1000, <1/100) - there were asthenia and abdominal pain. Children aged 6 to 12 years often there was a headache and drowsiness.

During the post-marketing use of the drug, the following side effects were observed, frequency of which 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:

Feeling heart palpitations, tachycardia, jugular vein thrombosis

From the respiratory system:

Shortness of breath, increased symptoms of rhinitis

From the digestive system:

Nausea, vomiting

Hepatobiliary disorders:

Hepatitis

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 side of the musculoskeletal system:

Muscle pain

General disorders:

Peripheral edema

Other:

Increase in body weight, change in functional liver samples, cross reactivity

If any of the side effects indicated in the manual are aggravated, or if you notice other side effects, 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 a simultaneous appointment 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)that the exposure of cetirizine increased by 40%, and the exposure of ritanovir slightly changed (-10%).

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

Special instructions:

Methyl parahydroxybenzoate and propyl parahydroxybenzoate, which are part of the drops for oral administration, can cause allergic reactions (possibly delayed type).

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 practicing potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Drops for ingestion 5 mg / ml.

Packaging:

To 10.0 ml of the solution in bottles of dark glass (type III, Heb.F.) with a nominal capacity of 15 ml, equipped with a dropper of low density polyethylene, with a screw cap made of white polypropylene with "child protection".

To 20.0 ml of the solution in bottles of dark glass (type III, Hebrew F.) with a nominal capacity of 20 ml, equipped with a dropper of low density polyethylene, with a screw cap made of white polypropylene with "child protection".

One bottle together with the instruction for use is placed in a cardboard box.

Storage conditions:

At a temperature of no higher than 30 ° C in a dark place.

Keep out of the reach of children!

Shelf life:

3 years in the original packaging; after the first opening of the vial - 3 months.

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

Terms of leave from pharmacies:On prescription

Registration number:LSR-001308/08

Date of registration:29.02.2008

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

Manufacturer: & nbsp

Aesica Pharmaceuticals Srl Italy

Representation: & nbspYUSB FARMA LLC YUSB FARMA LLC Russia

Information update date: & nbsp02.11.2015

Illustrated instructions

Instructions

Xizal® (Xyzal®)