Dosing and uses of Xyzal (levocetirizine)
Adult dosage forms and strengths
tablet
- 5mg
oral solution
- 2.5mg/5mL
Allergic Rhinitis
5 mg PO qDay (evening)
Chronic Urticaria
5 mg PO qDay (evening)
Renal Impairment
CrCl 50-80 mL/min: 2.5 mg PO qDay
CrCl 30-50 mL/min: 2.5 mg PO qOd
CrCl 10-30 mL/min: 2.5 mg PO 2x/wk
CrCl <10 mL/min: contraindicated
Pediatric dosage forms and strengths
tablet
- 5mg
oral solution
- 2.5mg/5mL
Allergic Rhinitis
<6 months: Safety and efficacy not established
6 months to 5 years: 1.25 mg PO qDay (evening)
6-12 years: 2.5 mg PO qDay (evening)
>12 years: 5 mg PO qDay (evening)
Chronic Urticaria
<6 months: Safety and efficacy not established
6 months to 5 years: 1.25 mg PO qDay (evening)
6-12 years: 2.5 mg PO qDay (evening)
>12 years: 5 mg PO qDay (evening)
Renal Impairment
<12 years
- Contraindicated
≥12 years
- CrCl: 50-80 mL/min: 2.5 mg PO qDay
- CrCl: 30-50 mL/min: 2.5 PO qODay
- CrCl: 10-30 mL/min: 2.5 mg every 3-4 days
- CrCl: <10 mL/min, hemodialysis: Contraindicated
Xyzal (levocetirizine) adverse (side) effects
Varies in incidence & severity with the individual drug; also individual patients vary in susceptibility
1-10%
Dry mouth
Fatigue
Nasopharyngitis
Pharyngitis
Frequency not defined
CNS depression
Drowsiness
Sedation ranging from mild drowsiness to deep sleep (most frequent)
Dizziness
Lassitude
Disturbed coordination
Restlessness, insomnia, tremors, euphoria, nervousness, delirium, palpitation, seizures is less common
Epigastric distress
Anorexia
Nausea
Vomiting
Diarrhea
Constipation
Cholestasis, hepatitis, hepatic failure, hepatic function abnormality, jaundice is rare
Tachycardia, palpitation ECG changes (eg, widened QRS)
Arrhythmias (eg, extrasystole, heart block)
Hypotension
Hypertension
Dizziness, sedation, and hypotension may occur in geriatric patients
Dryness of mouth, nose, and throat
Dysuria
Urinary retention
Impotence
Vertigo
Visual disturbances
Blurred vision
Diplopia; tinnitus
Acute labyrinthitis
Insomnia
Tremors
Nervousness
Irritability
Facial dyskinesia
Tightness of the chest
Thickening of bronchial secretions
Wheezing
Nasal stuffiness
Sweating
Chills
Early menses
Toxic psychosis
Headache
Faintness
Paresthesia
Agranulocytosis
Hemolytic anemia
Leukopenia
Thrombocytopenia
Pancytopenia
Postmarketing Reports
Skin/Allergy: Hypersensitivity and anaphylaxis, angioedema, fixed drug eruption, pruritus, rash, and urticaria
Neurologic: Convulsion, paraesthesia, dizziness, aggression and agitation, hallucinations, depression, movement disorders (including dystonia and oculogyric crisis), tic, myoclonus, extrapyramidal symptoms
Ocular: Visual disturbances, blurred vision
Cardiovascular: Palpitations, tachycardia
Pulmonary: Dyspnea
Gastrointestinal: Nausea, vomiting, hepatitis
Genitourinary: Dysuria
Musculoskeletal: Myalgia, arthralgia
Warnings
Contraindications
Documented hypersensitivity
Lower respiratory disease, eg, asthma (controversial)
Preemies and neonates
Nursing women
Hypersensitivity to levocetirizine or cetirizine
ESRD with CrCl <10 mL/min or HD patients
Children with renal impairment
Cautions
Caution in narrow angle glaucoma, prostatic hypertrophy, stenosing peptic ulcer, pyloroduodenal obstruction, or bladder neck obstruction
May impair mental alertness
Avoid alcohol or other CNS depressants
Pregnancy and lactation
Pregnancy category: B
Lactation: expected to be excreted in breast milk, avoid
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Xyzal (levocetirizine)
Mechanism of action
Histamine H1-receptor antagonist
Absorption
Peak Plasma Time: 0.5hr (oral solution); 0.9 hr (tablet)
Peak Plasma Concentration (5 mg x1 dose): 270 ng/mL
Onset: 1 hr (allergic rhinitis); 1 day (seasonal/perennial)
Distribution
Protein Bound: >90%
Vd: 0.4 L/kg
Metabolism
Metabolism: CYP3A4 and other isoforms
Elimination
Half-Lfe: 8 hr
Total Body Clearance: 0.63 mL/kg/min
Excretion: urine: 85%; feces 13%
