Levocetirizine: Drug information

(For additional information see "Levocetirizine: Patient drug information" and see "Levocetirizine: Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)

Brand Names: US

Allergy Relief [OTC];
Xyzal Allergy 24HR Childrens [OTC];
Xyzal Allergy 24HR [OTC]

Pharmacologic Category

Histamine H₁ Antagonist;
Histamine H₁ Antagonist, Second Generation;
Piperazine Derivative

Dosing: Adult

Allergic rhinitis

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 and chronic spontaneous

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.

Dosing: Kidney Impairment: Adult

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.

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).

Dosing: Hepatic Impairment: Adult

No dosage adjustment necessary.

Dosing: Older Adult

Refer to adult dosing; dosing should begin at the lower end of the dosing range.

Dosing: Pediatric

(For additional information see "Levocetirizine: Pediatric drug information")

Allergic rhinitis, perennial

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

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

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.

Dosing: Kidney Impairment: Pediatric

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.

Dosing: Hepatic Impairment: Pediatric

Infants ≥6 months, Children, and Adolescents: No dosage adjustment necessary.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%: Gastrointestinal: Diarrhea (infants: 13%; children: 4%)

1% to 10%:

Central nervous system: Drowsiness (3% to 6%), fatigue (adolescents and adults: 4%)

Gastrointestinal: Constipation (infants: 7%), vomiting (4%), xerostomia (adolescents and adults: 2% to 3%)

Otic: Otitis media (children: 3%)

Respiratory: Nasopharyngitis (adolescents and adults: 4% to 6%), cough (children: 3%), epistaxis (children: 2%), pharyngitis (adolescents and adults: 2%)

Miscellaneous: Fever (children: 4%)

Frequency not defined: Neuromuscular & skeletal: Weakness

<1%, postmarketing, and/or case reports: Aggressive behavior, agitation, anaphylaxis, angioedema, arthralgia, blurred vision, depression, dizziness, dysgeusia, dyspnea, dysuria, edema, febrile seizures, fixed drug eruption, hallucination, hepatitis, hypersensitivity reaction, increased appetite, increased serum bilirubin, increased serum transaminases, insomnia, movement disorder (including dystonia and oculogyric crisis), myalgia, nausea, nightmares, palpitations, paresthesia, pruritus, seizure, skin rash, suicidal ideation, syncope, tachycardia, tremor, urinary retention, urticaria, vertigo, visual disturbances, weight gain

Contraindications

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

Warnings/Precautions

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. Use is contraindicated in end-stage renal disease (CrCl <10 mL/minute), patients undergoing hemodialysis, and in infants and children 6 months to 11 years of age with renal impairment.

• 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 the elderly.

Warnings: Additional Pediatric Considerations

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).

Dosage Forms: US

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

Generic Equivalent Available: US

Yes

Pricing: US

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.

Administration: Adult

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.

Administration: Pediatric

Oral: Administer without regard to food in the evening.

Use: Labeled Indications

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.

Use: Off-Label: Adult

Urticaria, new onset

Medication Safety Issues

Sound-alike/look-alike issues:

Levocetirizine may be confused with cetirizine

Metabolism/Transport Effects

None known.

Drug Interactions

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 Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Risk C: Monitor therapy

Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy

Alizapride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Amantadine: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Amezinium: Antihistamines may enhance the stimulatory effect of Amezinium. Risk C: Monitor therapy

Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Risk C: Monitor therapy

Azelastine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Benzylpenicilloyl Polylysine: Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. 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 diminish the therapeutic effect of Betahistine. Betahistine may diminish the therapeutic effect of Antihistamines. Risk C: Monitor therapy

Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Management: Use caution if coadministering blonanserin and CNS depressants; dose reduction of the other CNS depressant may be required. Strong CNS depressants should not be coadministered with blonanserin. Risk D: Consider therapy modification

Botulinum Toxin-Containing Products: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Brexanolone: CNS Depressants may enhance the CNS depressant effect of Brexanolone. Risk C: Monitor therapy

Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Bromopride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Bromperidol: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Buprenorphine: CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants. Risk D: Consider therapy modification

Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Risk C: Monitor therapy

Cannabinoid-Containing Products: CNS Depressants may enhance the CNS depressant effect of Cannabinoid-Containing Products. Risk C: Monitor therapy

Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Risk C: Monitor therapy

Chlormethiazole: May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. Risk D: Consider therapy modification

Chlorphenesin Carbamate: May enhance the adverse/toxic effect of CNS Depressants. Risk C: Monitor therapy

Chlorprothixene: Anticholinergic Agents may enhance the anticholinergic effect of Chlorprothixene. Risk C: Monitor therapy

Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Risk X: Avoid combination

CloZAPine: Anticholinergic Agents may enhance the constipating effect of CloZAPine. Management: Consider alternatives to this combination whenever possible. If combined, monitor closely for signs and symptoms of gastrointestinal hypomotility and consider prophylactic laxative treatment. Risk D: Consider therapy modification

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy

Daridorexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dose reduction of daridorexant and/or any other CNS depressant may be necessary. Use of daridorexant with alcohol is not recommended, and the use of daridorexant with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification

DexmedeTOMIDine: CNS Depressants may enhance the CNS depressant effect of DexmedeTOMIDine. Management: Monitor for increased CNS depression during coadministration of dexmedetomidine and CNS depressants, and consider dose reductions of either agent to avoid excessive CNS depression. Risk D: Consider therapy modification

Difelikefalin: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Dimethindene (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Doxylamine: May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended. Risk C: Monitor therapy

DroPERidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification

Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Risk X: Avoid combination

Esketamine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Flunarizine: CNS Depressants may enhance the CNS depressant effect of Flunarizine. Risk X: Avoid combination

Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Management: Reduce the dose of CNS depressants when combined with flunitrazepam and monitor patients for evidence of CNS depression (eg, sedation, respiratory depression). Use non-CNS depressant alternatives when available. Risk D: Consider therapy modification

Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Risk C: Monitor therapy

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Risk C: Monitor therapy

Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Risk X: Avoid combination

Glycopyrronium (Topical): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Hyaluronidase: Antihistamines may diminish the therapeutic effect of Hyaluronidase. Risk C: Monitor therapy

HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Management: Consider a decrease in the CNS depressant dose, as appropriate, when used together with hydroxyzine. Increase monitoring of signs/symptoms of CNS depression in any patient receiving hydroxyzine together with another CNS depressant. Risk D: Consider therapy modification

Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Risk C: Monitor therapy

Ixabepilone: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Kava Kava: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Kratom: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Lemborexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dosage adjustments of lemborexant and of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Risk D: Consider therapy modification

Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Risk X: Avoid combination

Lisuride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Lofexidine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce the usual dose of CNS depressants by 50% if starting methotrimeprazine until the dose of methotrimeprazine is stable. Monitor patient closely for evidence of CNS depression. Risk D: Consider therapy modification

Metoclopramide: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Risk C: Monitor therapy

Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Minocycline (Systemic): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Risk C: Monitor therapy

Nitroglycerin: Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Risk C: Monitor therapy

Olopatadine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Opioid Agonists: CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification

Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Risk X: Avoid combination

Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Oxomemazine: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Oxybate Salt Products: CNS Depressants may enhance the CNS depressant effect of Oxybate Salt Products. Management: Consider alternatives to this combination when possible. If combined, dose reduction or discontinuation of one or more CNS depressants (including the oxybate salt product) should be considered. Interrupt oxybate salt treatment during short-term opioid use Risk D: Consider therapy modification

OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification

Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Risk X: Avoid combination

Perampanel: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Piribedil: CNS Depressants may enhance the CNS depressant effect of Piribedil. Risk C: Monitor therapy

Pitolisant: Antihistamines may diminish the therapeutic effect of Pitolisant. Risk X: Avoid combination

Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Risk X: Avoid combination

Potassium Citrate: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium citrate. Risk X: Avoid combination

Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Risk C: Monitor therapy

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Risk X: Avoid combination

Procarbazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Risk C: Monitor therapy

Revefenacin: Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. Risk X: Avoid combination

Ropeginterferon Alfa-2b: CNS Depressants may enhance the adverse/toxic effect of Ropeginterferon Alfa-2b. Specifically, the risk of neuropsychiatric adverse effects may be increased. Management: Avoid coadministration of ropeginterferon alfa-2b and other CNS depressants. If this combination cannot be avoided, monitor patients for neuropsychiatric adverse effects (eg, depression, suicidal ideation, aggression, mania). Risk D: Consider therapy modification

ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Risk C: Monitor therapy

Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Risk C: Monitor therapy

Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Risk C: Monitor therapy

Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin. Risk D: Consider therapy modification

Suvorexant: CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification

Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Risk X: Avoid combination

Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Risk C: Monitor therapy

Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Risk X: Avoid combination

Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Risk C: Monitor therapy

Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Valerian: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Risk D: Consider therapy modification

Zuranolone: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to the use of zuranolone with other CNS depressants or alcohol. If combined, consider a zuranolone dose reduction and monitor patients closely for increased CNS depressant effects. Risk D: Consider therapy modification

Pregnancy Considerations

Guidelines for the use of antihistamines in the treatment of allergic rhinitis or urticaria in pregnancy are generally the same as in nonpregnant females. Second generation antihistamines may be used for the treatment of allergic rhinitis and urticaria during pregnancy; however, information related to the use of levocetirizine in pregnancy is limited and other medications may be preferred (BSACI [Scadding 2017]; BSACI [Powell 2015]; Zuberbier 2018).

Levocetirizine is the active enantiomer of cetirizine; refer to the cetirizine monograph for additional information.

Breastfeeding Considerations

It is not known if levocetirizine is present in breast milk.

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. When treatment of rhinitis and urticaria in breastfeeding women is needed, other agents are preferred (BSACI [Powell 2015]; BSACI [Scadding 2017]; Zuberbier 2018).

Levocetirizine is the active enantiomer of cetirizine which is present in breast milk; refer to the cetirizine monograph for additional information.

Monitoring Parameters

Creatinine clearance (prior to treatment for dosing adjustment)

Mechanism of Action

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.

Pharmacokinetics (Adult Data Unless Noted)

Onset of action: 1 hour (Devillier 2008)

Duration: 24 hours (Devillier 2008)

Absorption: Rapid and extensive

Distribution: V_d: 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

Pharmacokinetics: Additional Considerations (Adult Data Unless Noted)

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 elderly subjects, compared with younger adults.

Sex: Half-life was slightly shorter in women than in men; however, the body weight-adjusted oral Cl in women appears to be comparable with that in men.

Brand Names: International

International Brand Names by Country

For country code abbreviations (show table)

(AE) United Arab Emirates: Antallos | Evocet | Glencet | Glozal | L cet | Lazine | Levocet | Levozin | Omcet L | Xyzal | Zolix;
(AR) Argentina: Alergical | Analerg | Atopix l | Cetimer L | Levomine | Supraler | Tiriz;
(AT) Austria: Levocetirizin +pharma | Levocetirizin actavis | Levocetirizin Genericon | Levocetirizin hexal | Levocetirizin Krka | Levocetirizin Stada | Xyzall;
(AU) Australia: Xyzal;
(BD) Bangladesh: Acitrin L | Alcet | Cevozin | Clarigen | Curin | Lacer | Lce | Lecet | Lecetrin | Lerex | Levocet | Levotiz | Lingin | Liset | Lozin | Lvc | Megatrol | Polan | Purotrol | Rehaf | Rinocet | Rinotin | Seasonix | Sinacet | Verizin | Vocet;
(BE) Belgium: Levocetirizin ab | Levocetirizin Teva | Levocetirizine actavis | Levocetirizine Apotex | Levocetirizine EG | Levocetirizine mylan | Levocetirizine ratiopharm | Levocetirizine sandoz | Xyzall;
(BF) Burkina Faso: Ceten l | Lazine | Levotriz;
(BG) Bulgaria: Alercit | Bezaleria | Cezera | Ksivozan | L-cetiricon | Revistim | Xyzal | Zenaro;
(BR) Brazil: Dicloridrato de levocetirizina | Rizi | Vocety | Zina;
(CH) Switzerland: Allergo X | Levocet mepha allergie | Levocetirizin mepha | Levocetirizin Sandoz | Levocetirizin spirig hc | Xyzal;
(CI) Côte d'Ivoire: Allergostop | Lazine | Levocetirizina Generis | Levotriz | Supraler | Xylix | Xyzall;
(CL) Chile: Degraler | Dofitex | Lezitar | Neo alertop | Xuzal | Zival;
(CN) China: Di min | Levocetirizine hydrochloride | Qiang yi | Xyzal;
(CO) Colombia: Antiss | Cehaler | Cetimer | Cetrilev | Expotizina | Glencet | Lecetir | Levoc | Levocetirizina | Levopraz | Zyxem;
(CZ) Czech Republic: Alergimed | Analergin neo | Cezera | Contrahist | Levocetirizin actavis | Levocetirizin biofarm | Levocetirizin Ratiopharm | Levocetirizine dr max | Levoxal | Volnostin | Xyzal | Zenaro;
(DE) Germany: Levocetirizin | Levocetirizin abz | Levocetirizin al | Levocetirizin ct | Levocetirizin hexal | Levocetirizin Micro Labs | Levocetirizin Ratiopharm | Levocetirizin Stada | Levocetirizine glenmark | Xusal | Xyzal | Xyzall;
(DO) Dominican Republic: Alercure | Cetimer | Convenil | Elriz | Eurolevocet | Glencet | Lecefar | Lergical | Leskera | Levocetirizina | Levocetirizina if | Levotek | Neocet | Supraler | Tricevol aglf | Xalerg;
(EC) Ecuador: Alergiplus | Antiss | Cetimer | Degraler | Levoc | Levocetirizina | Libbera | Lomazol | Neo alertop | Supraler | Zival;
(EE) Estonia: Cezera | Levocetirizine | Levocetirizine ratiopharm | Xyzal;
(EG) Egypt: Allear | Allevo | Lergicare | Lergopan | Levocitrone | Levoctivan | Levohistam | Modallerge | Orgitrizine | Xaltec | Zalkevor;
(ES) Spain: Aralevo | Levocetirizina | Levocetirizina actavis | Levocetirizina apotex | Levocetirizina cInfa | Levocetirizina cinfamed | Levocetirizina Combix | Levocetirizina krka | Levocetirizina mylan | Levocetirizina normon | Levocetirizina pharma combix | Levocetirizina Sandoz | Levocetirizina stada | Levocetirizina tarbis | Levocetirizina Teva | Levocetirizina vegal | Muntel | Xazal;
(ET) Ethiopia: 1 al | Histachek | Levocet | Levocetirizine | Levozal;
(FI) Finland: Levazyr | Levocetirizin Ratiopharm | Levocetirizin Stada | Levocetirizine sandoz | Nocedan | Xyzal;
(FR) France: Levocetirizine | Levocetirizine actavis | Levocetirizine biogaran | Levocetirizine cristers | Levocetirizine EG | Levocetirizine evolugen | Levocetirizine KRKA | Levocetirizine mylan | Levocetirizine ranbaxy | Levocetirizine ratiopharm | Levocetirizine Teva | Levocetirizine Zentiva | Levocetirizine zydus | Xyzall;
(GB) United Kingdom: Levocetirizine | Xyzal;
(GR) Greece: Contrahist | Levocet | Levocetirizine | Levocetirizine actavis | Levocetirizine glenmark | Xozal;
(HK) Hong Kong: Alercet | Euro zysol | Leocet | Lerizine | Levocet | Levocezal | Levotil | Lisinex | Purotrol | Vick levozy | Xizyne | Xylaclear | Xyzal;
(HR) Croatia: Xyzal;
(HU) Hungary: Cetizal | Cezera | Histisynt | Lertazin | Levocep | Levocetirizin Hetero | Novocetrin | Pollezin | Sefaller | Xyzal | Zilola;
(ID) Indonesia: Avocel | L falergi | Xyzal;
(IE) Ireland: Levocetirizin Teva | Levocetirizine glenmark | Levocetirizine KRKA | Rinozal | Xyzal;
(IN) India: 1 al | Adicure | Adliz | Airitis | Alcet | Alci | Aldbest | Alerfix | Alert L | Alertin | Alertriz | Alidil | Allelin | Allercet l | Allerhin l | Allermed | Allerzine-l | Allrite | Altin le | Alzene | Alzero | Aplev | Astrizine | Betawin Lc | Cefid l | Cerzin-L | Cetalore | Cetcip l | Cetiriz L | Cetiriz-l | Cetley | Cetmet l | Cetoz-l | Cetrezol L | Cetriliv | Cetrina lv | Cetrite | Cetsafe | Cistin l | Covel | Criz | Daylong | Dicet l | Ekon-xl | Elate | Ele | Elriz | Elycet | Elzin | Fitin | Genlevo | Glencet | Hatric | Hicet-l | His-block | Histachek | Ibalert 5 | Ibialert | Intriz 5 | Izi md | Klocet | L Arpicet | L C T | L Cetron | L dio 1 | L zin | L-alerid | L-Cetramac | L-cetridoc | L-cetrizet | L-cetron | L-dio-1 | L-tine | Laveta | Lazine | Lc-5 | Lcet | Lcz | Le one | Le zyncet | Lecet | Lecope | Leday | Leecet | Lency | Leoriv | Lerzin | Leset | Lestal | Levo setride | Levocee | Levocet | Levocetrival | Levodil | Levohext | Levoler | Levolyte | LevoMast | Levomer | Levonitrin | Levoplan | Levorid | Levosetride | Levosiz | Levotiz | Levotrine | Levova | Lezet | Lezine | Lisani | Livozine | Loviroc | Luvle | Lvt | Maxcet | Nexcet | Novolev | Nucet | Nuzil | Okacet-l | Oriel | Palevo | Perizine | Primecet | Provent | Rezin l | Rizi | Rizin lc | Safecet | Sigcet | Starcet | Teczine | Thermal | Uvnil | Verizet | Vocetin | Vociz | Votz | Vozet | Xenocet | Xevor | Xyzac | Xyzal | Zeez | Zilo | Zipcet | Zirlon L | Zocet | Zylera;
(IT) Italy: Levocetirizina actavis | Levocetirizina doc generici | Levocetirizina EG | Levocetirizina fidia | Levocetirizina krka | Levocetirizina mylan | Levocetirizina pensa | Levocetirizina ranbaxy | Levocetirizina ratiopharm | Levocetirizina San | Levocetirizina Tev | Xyzal;
(JO) Jordan: Cetazal | L cet | Layal | Lesonal | Levozal | Xyzal | Zolix;
(JP) Japan: Xyzal;
(KE) Kenya: Alcet | Allerzine | Cetlevo | Maxcet;
(KR) Korea, Republic of: Alcetin | Alcetizine | Alcitec | Alecet | Alecetin | Alefree | Alenan | Allecet | Allecetin | Allefree | Allenex | Allerban | Allercetin | Allerin | Allertop | Allerzal | Allezy | Altirizine | Altiz | Alvorin | Beartilin | Bicozal | Bizal | Boryung levocetirizine hydrochloride | Br ceti | Cellizin | Cenlevo | Cenova-L | Cetinal | Cetinzal | Cetirin | Cetirion | Cetizal | Cezal | Cipen | Citirizine | Cizaron | Cizin | Coalbi | Cocetin | Dialon | Eletin | Hyundai levocetirizine hcl | Kaizal | Ketra | Ketrazin | Korus levocetirizine hydrochloride | L-Tirizine | L-Trizine | Lastrin | Lecer | Leceti | Lecetizal | Lecevo | Lecezal | Leptizine | Leti | Leticin | Letinin | Letirazine | Letirin | Letirizine | Letizal | Letizin | Letizine | Levo-Q | Levocen | Levocera | Levocerin | Levocet | Levocetan | Levoceti | Levocetin | Levocetirin | Levocetirine | Levocetirizine | Levocetirizine 2hcl | Levocetirizine HanAll | Levocetrin | Levocezal | Levocezine | Levoconazine | Levocort | Levones | Levorizin | Levoseltec | Levotil | Levotizal | Levotizine | Levotop | Levotrizine | Levozal | Levozytec | Neocetin | Neorizine | Netizine | New ceretine | Newzal | Repcetin | Ribocetin | Samsung levocetirizine | Serenzal | Starizin | Xarlin | Xezal | Xyzal | Xyzin | Yuyu levocetirizine hcl | Zaltizine | Zarlin;
(KW) Kuwait: Glozal | L cet | Xyzal;
(LB) Lebanon: Aralevo | Calivida | L Cit | Layal | Supraler | Xyzal;
(LT) Lithuania: Cezera | Levocetirizine actavis | Levocetirizine ratiopharm | Xyzal;
(LU) Luxembourg: Levocetirizine EG | Xyzall;
(LV) Latvia: Levocetirizin actavis | Levocetirizine ratiopharm | Xyzal | Zenaro;
(MA) Morocco: Allegra | Aplevax | Supraler | Xycet | Xyzall;
(MX) Mexico: Belazix | Bocetix | Desceristad | Ergizar | Invoker | Komzimba | Lerpilex | Levigrix | Levocetirizina | Olenobran | Vazni | Xuceed | Xuzal | Zetyrel | Zyxem;
(MY) Malaysia: Avozine | Cezera | Egizin | Glencet | Lazine | Levocetirizine | Ranozine;
(NG) Nigeria: Calivida | Cerizine | LCT;
(NL) Netherlands: Cetirigen | Levocetirizine | Levocetirizine 2hcl actavis | Levocetirizine diHCl Mylan | Levocetirizine diHCl PCH | Levocetirizine dihcl ratiopharm | Levocetirizine diHCL Sandoz | Xyzal;
(NO) Norway: Xyzal;
(NZ) New Zealand: Levoclear | Levrix;
(PE) Peru: Alerfix | Alerfort | Alergilab | Alergiplus | Alerliv | Cetriler | Degraler | Gazella | Histalex | Laboxet | Lctimax | Lergial | Lergizina plus | Lertamine | Lesstamin | Levo del | Levoallergy | Levocelip | Levocert | Levogram | Levozalicer | Libbera | Libertium | Lizinaler | Lusaler | Quitaler | Rapiler | Sinalerg | Sprint | Xyzal;
(PH) Philippines: Allerzet | Coalbi | Getcet | Glencet | Histalev | L zet | Le zyncet | Lecetzy | Lerizine | Letrizine | Levocet | Levocetirizine | Levozyr | Lisinex | Nozal | Philcet | Purcet | Sensitrin | Stalevo | Tecovel | Veltir | Xylergic | Xyzal | Zocet;
(PK) Pakistan: Alcivo | Alvozine | Atiza | Belair | Cerigex-l | Citrafast | Etrizine L | Firax levo | Healazin l | Histamizine | Histaset | Hivocet | Invocet | Lcaria | Le vin | Lecetzi | Legozin | Leozin | Leridal | Letrazim | Leve cit | Leviva | Leviz | Levo Deebar | Levocet | Levocit | Levocitrin | Levomelt | Levopraz | Levota | Levozin | Lezet | Licet | Licide | Lirizine | Lixer | Neo sedil | Oakzine | Ocet | Ocitra | Okay | Relair | Selcet | Setrin | Setzine | Shavozin | T day | Velkeno | Voizin | Welcet | Xenocit | Xylizine | Xyzal | Zamocetrin | Zosper;
(PL) Poland: Ahist | Cezera | Contrahist | Contrahist allergy | Lecetax | Levocedo | Levocetirizine dr.max | Levocetirizine Genoptim | Lirra | Lirra gem | Nossin | Votrezin | Xyzal | Zenaro | Zilola | Zyx;
(PR) Puerto Rico: Levocetirizine | Xyzal | Xyzal allergy 24hr;
(PT) Portugal: Levocetiriz Bluefish | Levocetirizina | Levocetirizina actavis | Levocetirizina ciclum | Levocetirizina cInfa | Levocetirizina Fair Med | Levocetirizina Generis | Levocetirizina krka | Levocetirizina ratiopharm | Levocetirizina Sandoz | Levocetirizina tolife | Levocetirizina wynn | Levocetirizina Zentiva | Levrix | Rovinex | Xyzal;
(PY) Paraguay: Aleretic | Alermax | Degraler | Neo alertop | Nofludes | Novo alergina | Recifer | Zival;
(RO) Romania: Cetizal | Cezera | Contrahist | Xyzal | Zenaro;
(RU) Russian Federation: Alercet l | Allerway | Cesera | Elcet | Glencet | Levocetirizin Teva | Levocetirizine | Levocetirizine sandoz | Levocetirizine vertex | Suprastinex | Xyzal | Zenaro | Zodac express;
(SA) Saudi Arabia: Allercet | Glozal | L cet | Layal | Levozal | Levozin | Xyzal | Zolix;
(SG) Singapore: Allerzal | Levozine | Xyzal;
(SI) Slovenia: Cezera | Xyzal;
(SK) Slovakia: Alergimed | Cetizal | Cezera | Contrahist | Levocetirizin Dr.Max | Levocetirizin Ratiopharm | Levocetirizin Sandoz | Levocetirizin Teva | Levocetirizine actavis | Xyzal | Zenaro;
(TH) Thailand: Cetizal | Ellezin | Levocet | Levtrizin | Xyzal | Zyller;
(TN) Tunisia: Allergy stop | Levorgica | Levostamine | Xylix | Xyzall;
(TR) Turkey: Alerinit | Crebros | Leviset | Vivid | Xyzal | Zenaro;
(TW) Taiwan: Beloton | Levocetirizine | Levozal | Levozine | Limino | Locemine | Minlo | Neocetin | Sorimine | Xyzal | Xyzalin | Xyzine;
(UA) Ukraine: Aleron | Alerzin | Allercet | Allergofree | Allergolik | Allerway | Cetlo | Cetrilev | Cetrilev neo | Cetrimac | Ergocetal | Glencet | L cet | Lazine | Levocetirizin astrapharm | Levosetil | Levzirin | Sezonia | Xyzal;
(UG) Uganda: Fitin | Lazine | Levozin | Lezyncet | Welbeen l;
(UY) Uruguay: Histaplen | Levocet | Tiriz;
(VE) Venezuela, Bolivarian Republic of: Aplev | Cenaret | Cetimer | Glencet | Levocetirizina | Levorat;
(VN) Viet Nam: Xytab;
(ZA) South Africa: Allerway | Cetaway | Cetizal | Cetlev | Glencet | Levogex | Texamer | Xyzal

American Academy of Pediatrics (AAP). Cough and cold medicines should not be prescribed, recommended or used for respiratory illnesses in young children. Updated June 12, 2018. Available at http://www.choosingwisely.org/clinician-lists/american-academy-pediatrics-cough-and-cold-medicines-for-children-under-four/
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Xyzal Children’s Allergy 24HR (levocetirizine dihydrochloride) [prescribing information]. Chattanooga, TN: Chattem Inc; received November 2022.
Xyzal Children's liquid (levocetirizine dihydrochloride) [prescribing information]. Chattanooga, TN: Chattem, Inc.; February 2017.
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Topic 9443 Version 427.0

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Levocetirizine: Drug information