Levocetirizine

What is Levocetirizine?

• Levocetirizine is a histamine H1-receptor antagonist used for the treatment of allergic rhinitis (hay fever), chronic idiopathic urticaria.

Levocetirizine structure

Levocetirizine 3D ball

What are the uses of this medicine?

Levocetirizine dihydrochloride tablets are indicated for:

• the relief of symptoms associated with seasonal allergic rhinitis in adults and children 6 years of age and older.
• the relief of symptoms associated with perennial allergic rhinitis in adults and children 6 years of age and older.
• the uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children 6 years of age and older.

How does this medicine work?

• The dihydrochloride salt form of the active levorotatory enantiomer of cetirizine, levocetirizine; a third generation, non-sedating, selective histamine H1 receptor antagonist, with antihistamine, anti-inflammatory and potential anti-angiogenic activities.
• Levocetirizine competes with endogenous histamine for binding at peripheral H1-receptor sites on the effector cell surface.
• This prevents the negative symptoms associated with histamine release and an allergic reaction.
• In addition, as histamine plays an important role in angiogenesis during an allergic inflammatory reaction, blocking the action of histamine may modulate the expression of proangiogenic factors and thus may prevent angiogenesis.
• As a third-generation histamine H1 receptor antagonist, levocetirizine has fewer side effects than most second-generation antihistamines.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• known hypersensitivity to levocetirizine or any of the ingredients of levocetirizine dihydrochloride tablets, or to cetirizine.
• end-stage renal disease (CLCR < 10 mL/min) and patients undergoing hemodialysis.
• Children 6 months to 11 years of age with impaired renal function.

What drug interactions can this medicine cause?

• No in vivo drug-drug interaction studies have been performed with levocetirizine.

Is this medicine FDA approved?

• Levocetirizine was approved for medical use in the United States in 2007.

How should this medicine be used?

Recommended dosage:

• Adults and children 12 years of age and older: 5 mg once daily in the evening.
• Children 6 to 11 years of age: 2.5 mg once daily in the evening.

Renal Impairment:

• Adjust the dose in patients 12 years of age and older with decreased renal function.
• Mild renal impairment (creatinine clearance [CLCR] = 50-80 mL/min): a dose of 2.5 mg once daily is recommended;
• Moderate renal impairment (CLCR = 30-50 mL/min): a dose of 2.5 mg once every other day is recommended;
• Severe renal impairment (CLCR = 10-30 mL/min): a dose of 2.5 mg twice weekly (administered once every 3-4 days) is recommended;
• End-stage renal disease patients (CLCR < 10 mL/min) and patients undergoing hemodialysis should not receive levocetirizine dihydrochloride tablets.

Administration:

• Levocetirizine dihydrochloride tablets are available as 5 mg breakable (scored) tablets, allowing for the administration of 2.5 mg, if needed.
• Levocetirizine dihydrochloride tablets can be taken without regard to food consumption.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Immediate release breakable (scored) tablets, 5 mg

This medicine is available in fallowing brand namesː

• Xyzal ; Xyzal Allergy 24 Hr

What side effects can this medication cause?

The most common side effects of this medicine include:

• somnolence, nasopharyngitis, fatigue, dry mouth, and pharyngitis in subjects 12 years of age and older
• pyrexia, somnolence, cough, and epistaxis in children 6 to 12 years of age.

What special precautions should I follow?

• Avoid engaging in hazardous occupations requiring complete mental alertness such as driving or operating machinery when taking levocetirizine dihydrochloride tablets.
• Avoid concurrent use of alcohol or other central nervous system depressants with levocetirizine dihydrochloride tablets.
• Cetirizine and levocetirizine have been linked to rare, isolated instances of clinically apparent acute liver injury.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• drowsiness in adults and initially agitation and restlessness, followed by drowsiness in children.

Management of overdosage:

• There is no known specific antidote to levocetirizine dihydrochloride tablets.
• Should overdose occur, symptomatic or supportive treatment is recommended.
• Levocetirizine dihydrochloride tablets are not effectively removed by dialysis, and dialysis will be ineffective unless a dialyzable agent has been concomitantly ingested.

Can this medicine be used in pregnancy?

• There are no adequate and well-controlled studies in pregnant women.
• Pregnancy Category B

Can this medicine be used in children?

• The safety of levocetirizine dihydrochloride tablets 5 mg once daily was evaluated in pediatric patients 6 to 12 years of age.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• LEVOCETIRIZINE DIHYDROCHLORIDE

Inactive ingredients:

• CELLULOSE, MICROCRYSTALLINE
• LACTOSE MONOHYDRATE
• MAGNESIUM STEARATE
• HYPROMELLOSES
• TITANIUM DIOXIDE
• POLYETHYLENE GLYCOL 400

Who manufactures and distributes this medicine?

Manufactured by:

• Rottendorf Pharma GmbH
• Ennigerloh, Germany
• Made in Germany

Distributed by:

• Perrigo
• Allegan, MI

What should I know about storage and disposal of this medication?

• Store at 20-25°C (68-77°F); excursions permitted to 15-30°C (59-86°F).

First Generation Antihistamines

• Brompheniramine
• Carbinoxamine
• Chlorcyclizine
• Chlorpheniramine
• Clemastine
• Cyclizine
• Cyproheptadine
• Dexbrompheniramine
• Dexchlorpheniramine
• Dimenhydrinate
• Diphenhydramine
• Doxylamine
• Hydroxyzine
• Meclizine
• Phenyltoloxamine
• Promethazine
• Triprolidine

Second Generation Antihistamines

• Acrivastine
• Cetirizine
• Fexofenadine
• Levocetirizine
• Loratadine
• Desloratadine

• Dailymed label info on Levocetirizine
• FDA Levocetirizine

First Generation Antihistamines

• Brompheniramine
• Carbinoxamine
• Chlorcyclizine
• Chlorpheniramine
• Clemastine
• Cyclizine
• Cyproheptadine
• Dexbrompheniramine
• Dexchlorpheniramine
• Dimenhydrinate
• Diphenhydramine
• Doxylamine
• Hydroxyzine
• Meclizine
• Phenyltoloxamine
• Promethazine
• Triprolidine

Second Generation Antihistamines

• Acrivastine
• Cetirizine
• Fexofenadine
• Levocetirizine
• Loratadine
• Desloratadine