Levocetirizine is a second generation antihistamine drug available over the counter (OTC), used to relieve allergy symptoms, including sneezing, runny nose, watery eyes, hives, and itching. Second generation antihistamines are considered to have a better side effect profile than first generation antihistamines.

Levocetirizine works by blocking the activity of histamine, a natural chemical in the body that causes allergy symptoms. Histamine is released by mast cells and basophils, types of immune cells, in response to allergen exposure. Levocetirizine is a histamine H1 receptor antagonist that binds to histamine H1 receptors in the brain and spinal cord, preventing their activation by histamine and the resultant allergic reaction.

Levocetirizine is used to treat adults and pediatric patients to relieve allergic symptoms from:

• Seasonal and perennial allergic rhinitis (nasal inflammation)
• Chronic idiopathic urticaria (hives)

• Do not take levocetirizine if you are allergic to levocetirizine, cetirizine, or any of the ingredients of levocetirizine
• Do not administer levocetirizine to patients with end-stage renal disease or patients undergoing hemodialysis
• Do not administer levocetirizine to pediatric patients of 6 months to 11 years of age with renal impairment

Side effects of levocetirizine include:

• Dry mouth
• Fatigue
• Runny or stuffy nose
• Sore throat
• Central nervous system (CNS) depression
• Drowsiness
• Sedation
• Dizziness
• Mental or physical weariness
• Disturbed coordination
• Restlessness
• Inability to sleep (insomnia)
• Tremors
• Intense excitement
• Nervousness
• Disturbed state of mind
• Irregular heartbeat
• Seizures
• Upper abdominal distress
• Loss of appetite
• Nausea
• Vomiting
• Diarrhea
• Constipation
• Impaired bile flow (cholestasis)
• Inflammation of the liver (hepatitis)
• Liver failure
• Liver function abnormality
• Fast heart rate
• ECG changes
• Abnormal heart rhythm (extra heartbeat, heart block)
• Low blood pressure (hypotension)
• High blood pressure (hypertension)
• Difficult or painful urination
• Urinary retention
• Impotence
• Spinning sensation (vertigo)
• Visual disturbances
• Blurred vision
• Double vision
• Ringing in the ears (tinnitus)
• Acute inflammation of the inner ear
• Irritability
• Involuntary movement of facial muscles
• Tightness of the chest
• Thickening of bronchial secretions
• Wheezing
• Sweating
• Chills
• Early menses
• Toxic psychosis
• Headache
• Faintness
• Numbness and tingling
• Lowered white blood cell count (leukopenia)
• Low red blood cell count (anemia)
• Deficiency of platelets (thrombocytopenia)

Rare side effects of levocetirizine reported include:

• Yellowing of skin and eyes (jaundice)

Postmarketing side effects of Levocetirizine reported include:

• Skin/Allergy: Hypersensitivity and acute allergic reaction (anaphylaxis), swelling of the skin, fixed drug eruption, itching, rash, skin eruptions with superficial pustules (acute generalized exanthematous pustulosis [AGEP]), and hives
• Neurologic: Convulsion, numbness and tingling, dizziness, aggression and agitation, hallucinations, depression, movement disorders (including dystonia and oculogyric crisis), tic, sudden muscle contractions, extrapyramidal symptoms
• Psychiatric disorders: Aggression and agitation, depression, hallucinations, insomnia, nightmare, suicidal ideation
• Ocular: Visual disturbances, blurred vision
• Cardiovascular: Irregular heartbeat, fast heart rate
• Pulmonary: Shortness of breath
• Gastrointestinal: Nausea, vomiting, hepatitis
• Metabolism and nutrition disorders: Increased appetite
• Genitourinary: Difficult or painful urination
• Musculoskeletal: Muscle pain, joint pain

This is not a complete list of all side effects or adverse reactions that may occur from the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may also report side effects or health problems to the FDA at 1-800-FDA-1088.

Dosages of Levocetirizine

Adult and Pediatric Dosages:

Tablet

• 5 mg

Oral Solution

• 2.5 mg/5 ml

Dosage Considerations

Adult:

Allergic Rhinitis

• Indicated for the relief of symptoms associated with seasonal and perennial allergic rhinitis
• 5 mg orally daily in the evening
• Some patients may respond to 2.5 mg/day

Chronic Hives (Urticaria)

• Indicated for uncomplicated skin manifestations of chronic idiopathic hives
• 5 mg orally daily in the evening

Dosage Modifications

Renal impairment

• Creatinine Clearance 50-80 mL/min: 2.5 mg orally each day
• Creatinine Clearance 30-50 mL/min: 2.5 mg orally every other day
• Creatinine Clearance 10-30 mL/min: 2.5 mg orally 2 times/week (every 3-4 days)
• Creatinine Clearance less than 10 mL/min and or hemodialysis: Contraindicated

Hepatic impairment

• No dose adjustment required

Pediatric:

Allergic Rhinitis

• Indicated for the relief of symptoms associated with seasonal and perennial allergic rhinitis
• Infants under 6 months: Safety and efficacy not established
• Infants over 6 months to Children 5 years: 1.25 mg orally each day in the evening
• Children 6-12 years: 2.5 mg orally each day in the evening
• Children over 12 years: 5 mg orally each day in the evening; some patients may respond to 2.5 mg/day

Chronic Hives (Urticaria)

• Indicated for uncomplicated skin manifestations of chronic idiopathic hives
• Infants under 6 months: Safety and efficacy not established
• Infants over 6 months to Children 5 years: 1.25 mg orally each day in the evening
• Children 6-12 years: 2.5 mg orally each day in the evening
• Children over 12 years: 5 mg orally each day in the evening

Dosage Modifications

Renal impairment

Children 12 years or older:

• Creatinine Clearance 50-80 mL/min: 2.5 mg orally each day
• Creatinine Clearance l 30-50 mL/min: 2.5 mg orally every other day
• Creatinine Clearance 10-30 mL/min: 2.5 mg orally 2 times/week (every 3-4 days)
• Creatinine Clearance less than 10 mL/min and or hemodialysis: Contraindicated

Infants 6 months to children 11 years:

• Any degree of renal impairment: contraindicated

Hepatic impairment

• No dose adjustment required

Symptoms of overdose can include drowsiness in adults and initially restlessness and agitation, followed by drowsiness in pediatric patients. There is no known specific antidote to levocetirizine. In case of overdose, get medical help or contact a Poison Control Center immediately.

Inform your doctor of all medications you are currently taking, who can advise you on any possible drug interactions. Never begin taking, suddenly discontinue, or change the dosage of any medication without your doctor’s recommendation.

Levocetirizine has no known severe interactions with other drugs.

Serious interactions of levocetirizine include:

• isocarboxazid
• tranylcypromine

Moderate interactions of levocetirizine include:

• clobazam
• hyaluronidase
• lurasidone
• phenelzine
• ritonavir

Mild interactions of levocetirizine include:

• dyphylline
• theophylline

The drug interactions listed above are not all of the possible interactions or adverse effects. For more information on drug interactions, visit the RxList Drug Interaction Checker.

It is important to always tell your doctor, pharmacist, or health care provider of all prescription and over-the-counter medications you use, as well as the dosage for each, and keep a list of the information. Check with your doctor or health care provider if you have any questions about the medication.

Levocetirizine is a pregnancy category B drug.

• Use of levocetirizine during pregnancy may be acceptable
• Either animal studies show no risk but human studies are not available or animal studies show minor risks and human studies were done and showed no risk
• Levocetirizine is expected to be excreted in breast milk and not recommended for nursing mothers.

• Levocetirizine may impair mental alertness or physical abilities. Avoid performing tasks that require mental alertness, including driving and operating heavy machinery.
• Levocetirizine may cause central nervous system depression, avoid use of alcohol or other CNS depressants.
• Long term use may result in rebound itching several days after stopping levocetirizine.
• Use levocetirizine with caution if the patient has narrow angle glaucoma, prostatic hyperplasia, stenosing peptic ulcer, pyloroduodenal obstruction or bladder obstruction.