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Levocetirizine (Tablets, Drops) Instructions for Use

ATC Code

R06AE09 (Levocetirizine)

Active Substance

Levocetirizine (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Histamine H1-receptor blocker. Antiallergic drug

Pharmacotherapeutic Group

Antiallergic agent – H1-histamine receptor blocker

Pharmacological Action

Antiallergic agent. Levocetirizine, the (R)-enantiomer of cetirizine, is a selective antagonist of peripheral histamine H1 receptors. The affinity of levocetirizine (Ki = 3.2 nmol/L) for histamine H1 receptors is 2 times higher than that of cetirizine (Ki = 6.3 nmol/L). Pharmacokinetic studies in healthy volunteers have shown that when applied to the skin and nasal mucosa, the activity of levocetirizine at half the dose is comparable to the activity of cetirizine at the full dose.

Levocetirizine suppresses eotaxin-induced transendothelial migration of eosinophils in skin and lung cells. Pharmacodynamic studies have demonstrated three main inhibitory effects of levocetirizine at a dose of 5 mg within the first 6 hours after pollen exposure: suppression of VCAM-1 release, changes in vascular permeability, and reduction of eosinophil activation. As with cetirizine, the effect on histamine-induced skin reactions does not depend on the plasma concentrations of the drug.

Levocetirizine prevents the development and alleviates the course of allergic reactions, has anti-exudative and antipruritic effects; it has practically no anticholinergic or antiserotonin action.

Levocetirizine at a dose of 5 mg contributes to the suppression of the inflammatory-exudative reaction to histamine to the same extent as cetirizine at a dose of 10 mg. ECG did not reveal a significant effect of levocetirizine on the QT interval.

Pharmacokinetics

After oral administration, Levocetirizine is rapidly absorbed from the gastrointestinal tract. Food intake does not affect the completeness of absorption, although its rate decreases. Cmax in plasma is reached 0.9 hours after a single oral dose. Steady state is achieved after 2 days. Cmax after single and repeated (5 mg daily) administration are 270 ng/ml and 308 ng/ml, respectively.

Plasma protein binding is 90%. Data on the distribution of the drug in tissues and penetration through the blood-brain barrier are not available. Vd is 0.4 L/kg. It is excreted in breast milk.

Less than 14% of the administered dose is metabolized in the liver by oxidation of the aromatic ring, N- and O-dealkylation, and conjugation with taurine. Dealkylation is predominantly catalyzed by CYP3A4, and CYP isoforms are involved in the oxidation of the aromatic ring. Levocetirizine does not affect the activity of CYP1A2, 2C9, 2C19, 2D6, 2E1, and 3A4 isoenzymes at concentrations far exceeding peak concentrations after oral administration of 5 mg. Due to insignificant metabolism and the absence of metabolic suppression, interaction of levocetirizine with other substances is unlikely.

T1/2 is 7.9±1.9 hours. Total clearance is 0.63 ml/min/kg. Levocetirizine and its metabolite are excreted mainly by the kidneys (85.4% of the administered dose), through glomerular filtration and active tubular secretion. Excretion through the intestine is 12.9%.

The pharmacokinetics of levocetirizine are linear, independent of dose and time, and have small variations among different subjects. The pharmacokinetic profiles of the single enantiomer and cetirizine are similar. No chiral inversion occurs during absorption or excretion.

The total clearance of levocetirizine correlates with CrCl (this should be taken into account when determining dosing intervals in patients with moderate or severe renal impairment). In anuria, total clearance decreases by approximately 80% compared to healthy subjects. Less than 10% of levocetirizine is removed during a standard 4-hour hemodialysis procedure.

Indications

Symptomatic treatment of symptoms of perennial and seasonal allergic rhinitis (including persistent allergic rhinitis) and allergic conjunctivitis: sneezing, rhinorrhea, lacrimation, conjunctival hyperemia; hay fever (pollinosis); urticaria (including chronic idiopathic urticaria); other allergic dermatoses accompanied by itching and rash; angioedema.

ICD codes

ICD-10 code Indication
H10.1 Acute atopic (allergic) conjunctivitis
J30.1 Allergic rhinitis due to pollen
J30.3 Other allergic rhinitis (perennial allergic rhinitis)
L20.8 Other atopic dermatitis (neurodermatitis, eczema)
L23 Allergic contact dermatitis
L24 Irritant contact dermatitis
L28.0 Lichen simplex chronicus (circumscribed neurodermatitis)
L29 Pruritus
L50 Urticaria
T78.3 Angioneurotic edema (Quincke's edema)
ICD-11 code Indication
9A06.70 Atopic eczema of the eyelids
9A60.01 Acute atopic conjunctivitis
9A60.02 Allergic conjunctivitis
9A60.0Y Other specified papillary conjunctivitis
9A60.0Z Papillary conjunctivitis, unspecified
CA08.00 Allergic rhinitis due to pollen
CA08.03 Other allergic rhinitis
EA80.0 Infantile atopic eczema
EA80.1 Childhood atopic eczema
EA80.2 Adult atopic eczema
EA80.Z Atopic eczema, unspecified
EA83.00 Lichen simplex of vulva
EA83.01 Lichen simplex of male genital organs
EA83.02 Lichen simplex of perianal area
EA83.0Z Lichen simplex of unspecified location
EA85.20 Atopic hand eczema
EB04 Idiopathic angioedema
EC90.Z Itching, unspecified
EK00.Z Allergic contact dermatitis, unspecified
EK02.Z Irritant contact dermatitis, unspecified

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

Tablets, Drops

Take orally, regardless of meals.

Adults and children over 6 years of age – 5 mg once daily.

Children aged 2-6 years – 1.25 mg twice daily.

The duration of treatment depends on the type, duration, and course of symptoms. For the treatment of hay fever, 3-6 weeks are required, and for short-term pollen exposure, taking the drug for 1 week is usually sufficient.

Adverse Reactions

From the CNS often – headache, drowsiness, increased fatigue; infrequently – asthenia.

From the digestive system often – dry mouth; infrequently – abdominal pain; very rarely – nausea, impaired liver function tests.

Allergic reactions very rarely – angioedema, itching, skin rash, urticaria, anaphylaxis.

Other very rarely – weight gain, dyspnea.

Contraindications

Severe renal failure (CrCl below 10 ml/min); children under 2 years of age; hypersensitivity to levocetirizine.

Use in Pregnancy and Lactation

There are no clinical data on the use of levocetirizine during pregnancy. It is not recommended for use during pregnancy and lactation (breastfeeding).

Special Precautions

Elderly patients with moderate or severe renal impairment may require dose adjustment.

Patients with impaired renal function require dose adjustment depending on CrCl.

Patients with isolated hepatic impairment do not require any dose changes. Patients with combined hepatic and renal impairment are recommended to clarify the dose.

Patients should refrain from consuming alcohol while using levocetirizine.

Use in pediatrics

Levocetirizine is used in children over 2 years of age in a special dosage form.

Effect on ability to drive vehicles and operate machinery

Comparative clinical studies did not reveal signs of impaired alertness, reaction time, or ability to drive vehicles after taking recommended doses of levocetirizine. However, some patients may experience drowsiness, fatigue, or asthenia during use. Use with caution in patients driving vehicles and engaging in activities requiring quick psychomotor reactions.

Drug Interactions

A decrease in the clearance of cetirizine (16%) was observed with multiple administrations of theophylline (400 mg once daily); while the pharmacokinetics of theophylline did not change with simultaneous administration of cetirizine.

In susceptible patients, simultaneous use of levocetirizine and ethanol or other CNS depressants may lead to potentiation of the CNS depressant effect.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.

Medical Disclaimer

Brand (or Active Substance), Marketing Authorisation Holder, Dosage Form

Marketing Authorization Holder

Avva Rus, JSC (Russia)

Dosage Form

Bottle OTC Icon Levocetirizine Avva Oral drops 5 mg/ml: bottle 10 ml or 20 ml

Dosage Form, Packaging, and Composition

Oral drops transparent, colorless or light yellow; slight opalescence is allowed.

1 ml
Levocetirizine (as dihydrochloride) 5 mg

Excipients: propylene glycol, sodium saccharin, sodium acetate trihydrate, glacial acetic acid, methylparaben, propylparaben, purified water.

10 ml – bottles (1) – cardboard packs with insert.
20 ml – bottles (1) – cardboard packs with insert.

Marketing Authorization Holder

Avva Rus, JSC (Russia)

Dosage Form

Bottle OTC Icon Levocetirizine Avva Film-coated tablets 5 mg

Dosage Form, Packaging, and Composition

Film-coated tablets

1 tab.
Levocetirizine dihydrochloride 5 mg

10 pcs. – contour cell packs – cardboard packs (10 pcs.) – Over-the-Counter
10 pcs. – contour cell packs (3 pcs.) – cardboard packs (30 pcs.) – Over-the-Counter

Marketing Authorization Holder

Atoll LLC (Russia)

Manufactured By

Ozon, LLC (Russia)

Dosage Form

Bottle OTC Icon Levocetirizine Film-coated tablets, 5 mg: from 7 to 300 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, round, biconvex; the core is almost white in cross-section.

1 tab.
Levocetirizine dihydrochloride 5 mg

Excipients: lactose monohydrate (milk sugar) – 63.5 mg, microcrystalline cellulose (MCC-102) – 30 mg, magnesium stearate – 1 mg, colloidal silicon dioxide – 0.5 mg.

Film coating composition hypromellose – 1.74 mg, titanium dioxide – 0.75 mg, macrogol-4000 – 0.51 mg.

From 7 to 30 pcs. – contour cell packs (from 1 to 10 pcs.) – cardboard packs.
From 7 to 100 pcs. – jars (1) – cardboard packs.

Marketing Authorization Holder

Obnovlenie Pfc, JSC (Russia)

Dosage Form

Bottle OTC Icon Levocetirizine Renewal Oral drops 5 mg/1 ml: bottle 10 ml or 20 ml

Dosage Form, Packaging, and Composition

Oral drops in the form of a transparent or slightly opalescent, colorless or slightly brownish-yellowish liquid with the smell of acetic acid.

1 ml
Levocetirizine dihydrochloride 5 mg

Excipients: propylene glycol, glycerol (glycerin), sodium saccharin, sodium acetate, acetic acid, methylparaben, propylparaben, purified water.

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

xwith first-opening control or with first-opening control and child resistance.

Marketing Authorization Holder

PFKO-1, LLC (Russia)

Manufactured By

Obnovlenie Pfc, JSC (Russia)

Dosage Form

Bottle OTC Icon Levocetirizine Renewal Film-coated tablets, 5 mg: 10, 20, or 30 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, round biconvex; the core is white or almost white in cross-section.

1 tab.
Levocetirizine dihydrochloride 5 mg

Excipients: lactose monohydrate, microcrystalline cellulose, calcium hydrogen phosphate dihydrate, sodium carboxymethyl starch, povidone K30, magnesium stearate; shell composition – hypromellose, macrogol 6000, titanium dioxide.

10 pcs. – contour cell pack (1) – cardboard packs.
10 pcs. – contour cell pack (2) – cardboard packs.
10 pcs. – contour cell pack (3) – cardboard packs.

Marketing Authorization Holder

Sandoz, d.d. (Slovenia)

Manufactured By

Rottendorf Pharma, GmbH (Germany)

Quality Control Release

SALUTAS PHARMA, GmbH (Germany)

Dosage Form

Bottle OTC Icon Levocetirizine Sandoz® Film-coated tablets, 5 mg: 30 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, oval, biconvex, with engraving “L9CZ” on one side and “5” on the other side; the tablet core is white or almost white in cross-section.

1 tab.
Levocetirizine dihydrochloride 5 mg

Excipients: lactose monohydrate 64.0 mg, microcrystalline cellulose 30.0 mg, magnesium stearate 1.0 mg.
Film coating composition Opadry white 3.0 mg (hypromellose 1.875 mg, titanium dioxide 0.9375 mg, macrogol 400 – 0.1876 mg).

10 pcs. – PVC/PVDC/aluminum foil blisters (3) – cardboard packs.

Marketing Authorization Holder

Teva Pharmaceutical Industries, Ltd. (Israel)

Dosage Form

Bottle OTC Icon Levocetirizine-Teva Film-coated tablets, 5 mg: 7, 10, or 14 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, oval, with engraving “LC5” on one side; tablets must be free of cracks and chips.

1 tab.
Levocetirizine dihydrochloride 5 mg

Excipients: microcrystalline cellulose (grade 102) – 30 mg, lactose monohydrate – 63.5 mg, colloidal silicon dioxide (anhydrous colloidal silicon dioxide) – 0.5 mg, magnesium stearate – 1 mg.

Coating composition Opadry Y1-7000H white: macrogol 400 (polyethylene glycol 400) – 0.1875 mg, titanium dioxide (E171) – 0.9375 mg, hypromellose 2910 (E464) – 1.875 mg.

7 pcs. – blisters made of aluminum laminated foil (1) – cardboard packs×.
7 pcs. – blisters made of aluminum laminated foil (2) – cardboard packs×.
10 pcs. – blisters made of aluminum laminated foil (1) – cardboard packs×.

× protective stickers may be additionally applied.

Marketing Authorization Holder

Vertex, JSC (Russia)

Dosage Form

Bottle OTC Icon Levocetirizine-Vertex Film-coated tablets, 5 mg: 10, 14, 15, 20, 28, or 30 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, round, biconvex; on the cross-section – a core of white or almost white color.

1 tab.
Levocetirizine (as dihydrochloride) 5 mg

Excipients: lactose monohydrate – 62.5 mg, microcrystalline cellulose – 30 mg, sodium carboxymethyl starch (sodium starch glycolate, type A) – 1 mg, magnesium stearate – 1 mg, colloidal silicon dioxide – 0.5 mg.

Film coating composition [hypromellose – 1.8 mg, talc – 0.6 mg, titanium dioxide – 0.33 mg, macrogol 4000 (polyethylene glycol 4000) – 0.27 mg] or [dry mix for film coating, containing hypromellose (60%), talc (20%), titanium dioxide (11%), macrogol 4000 (polyethylene glycol 4000) (9%) – 3 mg].

10 pcs. – contour cell packs (1) – cardboard packs.
10 pcs. – contour cell packs (2) – cardboard packs.
10 pcs. – contour cell packs (3) – cardboard packs.
14 pcs. – contour cell packs (1) – cardboard packs.
14 pcs. – contour cell packs (2) – cardboard packs.
15 pcs. – contour cell packs (1) – cardboard packs.
15 pcs. – contour cell packs (2) – cardboard packs.
30 pcs. – contour cell packs (1) – cardboard packs.

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