Allergic rhinitis (OTC only): Oral: 5 mg once daily (in the evening); some patients with less severe symptoms may experience relief with 2.5 mg once daily; maximum dose: 5 mg/day.
Urticaria, new onset (off-label use) and chronic spontaneous (labeled use):
New onset: Oral: Initial: 5 mg once daily. If symptom control is inadequate, may immediately increase to 5 mg twice daily (Ref).
Chronic spontaneous: Oral: Initial: 5 mg once daily. If symptom control is inadequate, may increase in 5 mg/day increments every 1 to 4 weeks up to 10 mg twice daily; periodically reevaluate necessity for continued treatment (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.
Note: Renally adjusted dose recommendations are based on a usual dose of 5 mg/day.
CrCl >80 mL/minute: No dosage adjustment necessary.
CrCl 50 to 80 mL/minute: 2.5 mg once daily.
CrCl 30 to 50 mL/minute: 2.5 mg once every other day.
CrCl 10 to 30 mL/minute: 2.5 mg twice weekly (every 3 or 4 days).
CrCl <10 mL/minute: Use is contraindicated.
Hemodialysis, intermittent (thrice weekly): Nondialyzable (<10% with 4-hour dialysis session): Use is contraindicated.
Peritoneal dialysis: Use is contraindicated (expert opinion).
No dosage adjustment necessary.
Refer to adult dosing; dosing should begin at the lower end of the dosing range.
(For additional information see "Levocetirizine: Pediatric drug information")
Allergic rhinitis, perennial: Oral:
Infants ≥6 months and Children ≤5 years: 1.25 mg once daily (in the evening); maximum daily dose: 1.25 mg/day; Note: In children >2 years, dosing based on previous FDA approved manufacturer labeling (Ref).
Children ≥6 years and Adolescents: Note: Dosing based on previous FDA approved manufacturer labeling (Ref):
6 to 11 years: 2.5 mg once daily (in the evening); maximum daily dose: 2.5 mg/day
≥12 years: 5 mg once daily (in the evening); some patients may experience relief of symptoms with 2.5 mg once daily
Hay fever and other respiratory allergies: OTC labeling: Oral:
Children 2 to 5 years: 1.25 mg once daily (in the evening); maximum daily dose: 1.25 mg/day
Children 6 to 11 years: 2.5 mg once daily (in the evening); maximum daily dose: 2.5 mg/day
Children ≥12 years and Adolescents: 2.5 to 5 mg once daily (in the evening); dose based on symptom severity; maximum daily dose: 5 mg/day
Urticaria, chronic: Oral:
Infants ≥6 months and Children ≤5 years: 1.25 mg once daily (in the evening); maximum daily dose: 1.25 mg/day
Children 6 to 11 years: 2.5 mg once daily (in the evening); maximum daily dose: 2.5 mg/day
Children ≥12 years and Adolescents: 5 mg once daily (in the evening); some patients may experience relief of symptoms with 2.5 mg once daily
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Allergic perennial rhinitis, chronic urticaria:
Infants ≥6 months and Children ≤11 years: Contraindicated with any degree of renal impairment.
Children ≥12 years and Adolescents:
CrCl >80 mL/minute: No adjustment necessary
CrCl 50 to 80 mL/minute: 2.5 mg once daily
CrCl 30 to 50 mL/minute: 2.5 mg once every other day
CrCl 10 to 30 mL/minute: 2.5 mg twice weekly (every 3 or 4 days)
CrCl <10 mL/minute or on hemodialysis: Contraindicated
Hemodialysis: Nondialyzable
Hay fever and other respiratory allergies (OTC): Children ≥2 years and Adolescents: Use is not recommended.
Infants ≥6 months, Children, and Adolescents: No dosage adjustment necessary.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adolescents and adults unless otherwise indicated.
>10%: Gastrointestinal: Diarrhea (infants: 13%; children: 4%)
1% to 10%:
Gastrointestinal: Constipation (infants: 7%), vomiting (children: 4%), xerostomia (2% to 3%)
Nervous system: Drowsiness (children, adolescents, adults: 3% to 6%), fatigue (4%)
Respiratory: Cough (children: 3%), epistaxis (children: 2%), nasopharyngitis (4% to 6%), pharyngitis (2%)
Miscellaneous: Fever (children: 4%)
<1%:
Cardiovascular: Syncope
Endocrine & metabolic: Weight gain
Hepatic: Increased serum bilirubin, increased serum transaminases
Frequency not defined: Nervous system: Asthenia
Postmarketing (any population):
Cardiovascular: Edema, palpitations, tachycardia
Dermatologic: Fixed drug eruption, pruritus, skin rash, urticaria
Gastrointestinal: Dysgeusia, increased appetite, nausea
Genitourinary: Dysuria, urinary retention
Hepatic: Hepatitis (including cholestatic hepatitis) (Jung 2016)
Hypersensitivity: Hypersensitivity reaction (including anaphylaxis, angioedema)
Nervous system: Aggressive behavior, agitation, depression, dizziness, febrile seizure, hallucination, insomnia, movement disorder (including dystonia, oculogyric crisis), nightmares, paresthesia, seizure, suicidal ideation, tremor, vertigo
Neuromuscular & skeletal: Arthralgia, myalgia
Ophthalmic: Blurred vision, iridocyclitis (Konstantinou 2010), visual disturbances
Respiratory: Dyspnea
Known hypersensitivity to levocetirizine, cetirizine, or any component of the formulation; end-stage renal disease (CrCl <10 mL/minute); hemodialysis; infants and children 6 months to 11 years of age with renal impairment
Concerns related to adverse effects:
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
• Pruritus: Rebound pruritus has been reported within several days after stopping cetirizine, usually after long-term (eg, months to years) use; therefore, this may also occur with levocetirizine since it is the active enantiomer of cetirizine.
Disease-related concerns:
• Renal impairment: Levocetirizine is excreted primarily by the kidneys; use with caution in adults with mild to severe renal impairment; dosage adjustments may be needed.
• Urinary retention: Urinary retention may occur; use with caution in patients with increased risk of urinary retention (including spinal cord lesions or prostatic hyperplasia); discontinue if urinary retention occurs.
Special populations:
• Older adult: Use with caution in older adults.
Safety and efficacy for the use of cough and cold products in pediatric patients <4 years of age is limited; the AAP warns against the use of these products for respiratory illnesses in young children. Serious adverse effects including death have been reported. Many of these products contain multiple active ingredients, increasing the risk of accidental overdose when used with other products. Health care providers are reminded to ask caregivers about the use of OTC cough and cold products in order to avoid exposure to multiple medications containing the same ingredient (AAP 2018; CDC 2007; FDA 2017; FDA 2018).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Oral, as dihydrochloride:
Xyzal Allergy 24HR Childrens: 2.5 mg/5 mL (148 mL) [alcohol free, dye free, sugar free; contains methylparaben, propylparaben, saccharin; tutti-frutti flavor]
Generic: 2.5 mg/5 mL (118 mL, 148 mL)
Tablet, Oral, as dihydrochloride:
Allergy Relief: 5 mg [scored]
Xyzal Allergy 24HR: 5 mg [scored]
Generic: 5 mg
Yes
Solution (Levocetirizine Dihydrochloride Oral)
2.5 mg/5 mL (per mL): $0.62 - $1.62
Solution (Xyzal Allergy 24HR Childrens Oral)
2.5 mg/5 mL (per mL): $0.10
Tablets (Levocetirizine Dihydrochloride Oral)
5 mg (per each): $0.24 - $3.08
Tablets (Xyzal Allergy 24HR Oral)
5 mg (per each): $0.80
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Oral: Administer in the evening with or without food. Use an accurate measuring device for the oral solution; a household teaspoon is not an accurate measuring device.
Oral: Administer without regard to food in the evening.
Allergic rhinitis (OTC only): Temporary relief of symptoms due to hay fever or other respiratory allergies (including rhinitis, sneezing, itchy/watery eyes, or itching of the throat/nose) in adults and pediatric patients ≥2 years of age.
Allergic rhinitis, perennial: Relief of symptoms associated with perennial allergic rhinitis in pediatric patients 6 months to 2 years of age.
Urticaria, chronic spontaneous: Treatment of uncomplicated skin manifestations of chronic spontaneous urticaria in adults and pediatric patients ≥6 months of age.
Urticaria, new onset
Levocetirizine may be confused with cetirizine
The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drugs (pediatric liquid medications requiring measurement) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Community/Ambulatory Care Settings).
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Amezinium: Antihistamines may increase stimulatory effects of Amezinium. Risk C: Monitor
Benzylpenicilloyl Polylysine: Coadministration of Antihistamines and Benzylpenicilloyl Polylysine may alter diagnostic results. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. A histamine skin test may be used to assess persistent antihistaminic effects. Risk D: Consider Therapy Modification
Betahistine: Antihistamines may decrease therapeutic effects of Betahistine. Betahistine may decrease therapeutic effects of Antihistamines. Risk C: Monitor
Certoparin: Antihistamines may increase therapeutic effects of Certoparin. Risk C: Monitor
CNS Depressants: Levocetirizine may increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Hyaluronidase: Antihistamines may decrease therapeutic effects of Hyaluronidase. Risk C: Monitor
Pitolisant: Antihistamines may decrease therapeutic effects of Pitolisant. Risk X: Avoid
Outcome data following maternal use of levocetirizine during pregnancy are available (Kocatürk 2022, Paulus 2004). Based on the limitations of available data, second-generation antihistamines are considered acceptable for use during pregnancy, with preference given to agents with more study (EAACI [Zuberbier 2022]).
Algorithms are available for the treatment of acute rhinitis and urticaria. When treatment with a second-generation oral antihistamine is recommended, agents other than levocetirizine may be preferred for use during pregnancy (AAAAI/ACAAI [Dykewicz 2020], EAACI [Zuberbier 2022]).
Levocetirizine is present in breast milk.
Data related to the presence of levocetirizine in breast milk are available from a study evaluating a method of analyzing breast milk for the presence of cetirizine. As part of the study, breast milk was collected from 219 lactating patients taking cetirizine 5 to 20 mg/day and 9 patients taking levocetirizine 5 mg/day. All patients in the study were at steady state. Cetirizine/levocetirizine breast milk concentration ranged from 0.65 to 65 ng/mL among 228 samples; 24 samples were below the limits of quantification (Wegler 2022).
Drowsiness and irritability have been reported in breastfed infants exposed to antihistamines (Ito 1993). In general, second-generation antihistamines are less sedating as compared to their first-generation counterparts. Infants exposed to a second-generation antihistamine via breast milk, should be monitored for irritability, jitteriness, or drowsiness (Butler 2014).
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother. Use of a second-generation antihistamine is preferred when an oral antihistamine is needed in lactating patients (Butler 2014, EAACI [Zuberbier 2022]).
Levocetirizine is the active enantiomer of cetirizine which is present in breast milk; refer to the cetirizine monograph for additional information.
Creatinine clearance (prior to treatment for dosing adjustment)
Levocetirizine is an antihistamine which selectively competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. Levocetirizine, the active enantiomer of cetirizine, has twice the binding affinity at the H1-receptor compared to cetirizine.
Onset of action: 1 hour (Devillier 2008)
Duration: 24 hours (Devillier 2008)
Absorption: Rapid and extensive
Distribution: Vd: Children 1 to 2 years: Oral solution: 0.37 ± 0.06 L/kg (Cranswick 2005); Children 6 to 11 years: Oral tablet: 0.4 ± 0.02 L/kg (Simons 2005); Adults: ~0.4 L/kg
Protein binding: 91% to 92%
Metabolism: Minimal (<14%); via aromatic oxidation, N and O-dealkylation (via CYPA4), and taurine conjugation
Half-life elimination: Children 1 to 2 years: Oral solution: 4.09 ± 0.67 hours (Cranswick 2005); Children 6 to 11 years: Oral tablet: 5.7 ± 0.2 hours (Simons 2005); Adults: ~8 to 9 hours
Time to peak, plasma: Children 1 to 2 years: Oral solution: Median: 1 hour (range: 1 to 6 hours) (Cranswick 2005); Children 6 to 11 years: Oral tablet: 1.2 ± 0.2 hours (Simons 2005); Adults: Oral solution: 0.5 hours, Tablet: 0.9 hours
Excretion: Urine (85.4 %); feces (12.9%)
Clearance: Children 1 to 2 years: Oral solution: 1.05 ± 0.1 mL/minute/kg (Cranswick 2005); Children 6 to 11 years: Oral tablet: 0.82 ± 0.05 mL/minute/kg (Simons 2005); Adults: 0.63 mL/kg/minute
Altered kidney function: In patients with mild, moderate, severe renal impairment, and end-stage renal disease, the AUC increased by 1.8, 3.2, 4.3, and 5.7-fold, respectively, and the half-life increased by 1.4, 2, 2.9, and 4-fold, respectively.
Older adult: Total body Cl was approximately 33% lower in 9 older adults, compared with younger adults.
Sex: Half-life was slightly shorter in females than in males; however, the body weight-adjusted oral Cl in females appears to be comparable with that in males.