COMPOSITION:

Active substance: Levocetirizine dihydrochloride;

1 film coated tablet contains Levocetirizine hydrochloride 5 mg.

Excipients:

microcystalline cellulose, croscarmellose sodium, colloidal silicon dioxide anhydrous, magnesium stearate, Opadry II 85G 51300 green coating.

INDICATIONS:

Symptomatic treatment of seasonal allergic rhinitis including whole-year allergic , the chronic idiopathic urticaria.

DOSAGE:

The preparation is taken internally, without chewing, following with some water. The preparation effect is more rapid if used on an empty stomach. The recommended dose for adults and children above 6 years old is 5 mg (1 tablet 1 time per day). The course of the treatment of hay fever (pollinosis) is from 1 to 6 weeks. In chronic allergic diseases the course of the treatment can continue up to 12 months.

ADVERSE REACTIONS:

Central nervous system:

headache, drowse, fatiguability, weakness.

Cardio-vascular system:

palpitation sensation.

Visual organ:

visual impairment.

Hepatobiliary system:

hepatitis.

Immune system:

hypersensitivity, including anaphylaxis and angioneurotic edema.

Respiratory system:

short breath.

Digestive system: dry mouth, nausea.

Skin and subcutaneous tissue:

skin itch, rash and urticaria.

Others:

body weight enlargement; gastric pain; mialgia; liver function test can be increased.

Drug interactions:

Concurrent usage of the preparation with teophylline reduces the total Levocetirizine clearance. In studies of concomitant usage of Levocetirizine with ketoconazole and macrolides there were not any significant changes of cardiac function in electrocardiograms. In case of synchronous usage of Levocetirizine with central nervous system depressive medicines (tranquilizers, tricyclic antidepressants, MAO inhibitors) and alcohol it may occur a drowse.

Pregnancy and lactation:

There is no data indicating the safety of the preparation during pregnancy that’s why the administration in pregnant women is contraindicated. Levocetirizine is secreted into the breast milk. If there is a need the usage of the preparation during the breast feeding should be stopped.

Children:

The preparation is not used in children under 16 years old.

PRECAUTIONS:

As the preparation is mainly excreted via kidneys it is necessary to administer L-CET® with caution to patients with renal pathology. In patients with renal insufficiency (creatinine clearance < 40 ml/min) Levocetirizine excretion is decreased (up to 80% in hemodialysis patients).

In renal insufficiency the therapeutic dose depends on creatinine clearance (CC). If CC is 50 – 80 ml/min and more it is used 1 tablet per day, if CC is 30 – 49 ml/min – 1 tablet every other day, if CC is 30 ml/min – 1 tablet every other three days. If CC is less than 10 ml/min the preparation use is contraindicated.

In renal insufficiency the therapeutic dose is not corrected.

Overdose:

Symptoms:

drowse, headache, dry mouth, nausea and gastric pain.

Treatment:

Removing the preparation from gastro-intestinal tract via gastric lavage and administration of sorbents with further symptomatic therapy. Less than 10% of Levocetirizine is excreted via hemodialysis. There is no specific antidote. Hemodyalisis is ineffective.

Ability to influence reaction velocity while driving or operating any other mechanisms.

Taking into consideration the possibility of side effects development (drowse, fatigability, asthenia) ability to drive and operate other machines should determine a doctor after studying an individual patient’s reaction to the preparation.

CONTRAINDICATIONS:

Symptomatic treatment of allergic rhinitis, including year-round allergic rhinitis; chronic idiopathic urticaria.

PHARMACOLOGICAL PROPERTIES:

Antihistaminic drugs for system use. ATC Code R06A Е09.

Levocetirizine is H1-histamine receptors blocker, cetirizine enantiomer and competitive antagonist of histamine. Levocetirizine influences on histamine dependent stage of allergic reactions, reduces the vessels penetrability and eosinophil migration, limits the release of inflammatory mediators and in this way prevents the allergic reactions development and significantly relieves their course, removes the exudation and itch. Levocetirizine has almost no anticholinergic and antiserotonin action. It does not pass through hematoencephalic barrier. Levocetirizine has almost no sedative effect if therapeutic doses used. After oral administration of single dose the preparation effect begins in 15 minutes and continues for 24 hours.

Levocetirizine is rapidly absorbed in internal administration; the simultaneous use of meal decreases the absorption rate, but does not influence on its completeness. Levocetirizine bioavailability is 100%. Peak concentration is 207 ng/ml, TCmax – 0.9 hours, distribution volume – 0.4 l/kg. Binding with plasma proteins is 90%. The period of half-life is 7 – 10 hours. More than 85% of the preparation is eliminated via kidneys. Levocetirizine is secreted in the breast milk.

PHARMACEUTICAL CHARACTERISTICS:

General physic-chemical properties:

Round biconvex tablets coated with green coating.

Shelf-life:

3 years.

Storage:

Store in a dry, protected from light place at a temperature not more than 25°c

Keep it out of reach of children.

Package:

10 tablets are in a blister, 1 or 3 blisters are in a carton pack.

Conditions of supply:

Without prescription.