24HR ALLERGY RELIEF
  • 24HR ALLERGY RELIEF (Generic for XYZAL)

  • QTY 90 • 5 MG • Tablet • Near 77381

LEVOCETIRIZINE/Xyzal Allergy 24 Hour (LEE voe se TIR i zeen) prevents and treats allergy symptoms, such as red, itchy eyes, sneezing, a runny or stuffy nose, or hives. It works by blocking histamine, a substance released by the body during an allergic reaction. It belongs to a group of medications called antihistamines.

24HR ALLERGY RELIEF (Generic for XYZAL) Pediatric Monographs
  • General Administration Information
    For storage information, see the specific product information within the How Supplied section.

    Route-Specific Administration

    Oral Administration
    -Administer once daily in the evening.
    -May administer with or without food.
    Oral Solid Formulations
    Tablets
    -If tablet is scored it may be split in half if a lower dosage is needed.

    Oral Liquid Formulations
    Oral solution
    -Administer using a calibrated measuring device to ensure accurate dosing.

    Similar to other low-sedating antihistamines, side effects from levocetirizine reported in placebo-controlled trials in adults and children aged 12 years and older, and at incidences greater than with placebo, included: somnolence/drowsiness (5% to 6%) and fatigue (1% to 4%); somnolence/drowsiness (3%) were reported in clinical trials involving children aged 6 to 12 years. The combined incidence of drowsiness, fatigue, and asthenia was 8.1% for levocetirizine versus 3.1% for placebo during clinical study. Discontinuation due to somnolence/drowsiness, fatigue, or asthenia occurred in 2.3% of patients vs. less than 1% with placebo during long-term clinical trials. Adverse reaction profiles are similar regardless of the indication being treated.

    Side effects reported in 2% or more of levocetirizine-treated pediatric patients 12 years of age and older, and at a greater incidence than seen with placebo, included: nasopharyngitis (4% to 6%), xerostomia (2% to 3%), and pharyngitis (1% to 2%). Cough (3%) and epistaxis (2%) have been reported in children 6 to 12 years of age receiving levocetirizine and at a greater incidence than with placebo. In children 1 to 12 years of age, pyrexia (fever) occurred in 4% of levocetirizine recipients. More pediatric patients 1 to 5 years of age receiving levocetirizine reported otitis media infection (3%) than with placebo (0%).

    Although not common, cardiovascular adverse events have been reported during levocetirizine therapy. In placebo-controlled trials of levocetirizine in patients aged 12 years and older (which included adults), more patients experienced syncope (0.2%) with levocetirizine than with placebo. World-wide postmarketing experience includes reports of palpitations, sinus tachycardia, and edema among levocertirizine-treated patients. Severe hypotension has been reported in the postmarketing experience with cetirizine; levocetirizine is the active enantiomer of cetirizine.

    Appetite stimulation has been reported during postmarketing experience with levocetirizine. In placebo controlled trials of levocetirizine involving patients aged 12 years and older, more patients experienced weight gain (0.5%) with levocetirizine than with placebo. Increased appetite has been reported postmarketing.

    Levocetirizine has been reported to cause transient elevations in bilirubin and liver function tests (elevated hepatic enzymes) at an incidence of less than 1%. These elevations were transient in all patients and did not require drug discontinuation. Vomiting and diarrhea have been reported in children aged 1 to 5 years during clinical trials (4% vs. 3% placebo, incidence for both). In infants 6 to 11 months of age, diarrhea (13% vs. 4% placebo) and constipation (7% vs. 4% placebo) were reported. Postmarketing experience includes reports of dysgeusia, nausea, cholestasis, and hepatitis; causal relationships have not been determined.

    Neurologic and psychiatric adverse events have been reported during levocetirizine therapy. In a study of the safety of levocetirizine in children 12 to 24 months of age, the following adverse events occurred more frequently with levocetirizine compared to placebo: agitation (0.4%), seizures (0.4%), febrile seizures (2%), insomnia (1.2%), and nervousness (0.4%). Dizziness, aggression, agitation, depression, febrile seizure, hallucinations, paresthesias, movement disorders (including dystonic reaction, oculogyric crisis), and seizures (in those with a known seizure disorder) have been reported in world-wide postmarketing experience with use of levocetirizine in adults and children. Extrapyramidal symptoms, orofacial dyskinesia, myoclonia, tics, and suicidal ideation have been reported during postmarketing experience with cetirizine; levocetirizine is the active enantiomer of cetirizine.

    Anaphylaxis and hypersensitivity reactions have been noted during postmarketing experience with levocetirizine and/or cetirizine (parent drug), including the following rare but potentially serious allergic or dermatologic events: anaphylactoid reactions, angioneurotic edema (angioedema), dyspnea, acute generalized exanthematous pustulosis (AGEP), fixed drug eruption, pruritus, rash (unspecified), and urticaria. Rebound pruritus may occur within a few days after discontinuation of levocetirizine, usually after long-term use (i.e., months to years). If signs or symptoms of hypersensitivity occur, discontinue levocetirizine.

    Levocetirizine is the active enantiomer of cetirizine; postmarketing side effect reports with cetirizine have included hemolytic anemia and thrombocytopenia.

    In postmarketing experience, dysuria and urinary retention have been reported with levocetirizine use and glomerulonephritis has been reported with cetirizine use; causal relationships have not been established. Discontinue use if urinary retention occurs.

    Unspecified visual impairment/disturbance and blurred vision have been reported with postmarketing use of levocetirizine. Vertigo has been reported as an ear or labyrinth disorder postmarketing. Causal relationships have not been established.

    Musculoskeletal, connective tissues, and bone disorder adverse events reported with levocetirizine use postmarketing have included arthralgia and myalgia.

    Levocetirizine is contraindicated for use in patients with a known hypersensitivity to levocetirizine or to any of the formulation components or who have known cetirizine hypersensitivity. Observed reactions range from urticaria to anaphylaxis. Though not listed in the levocetirizine package labeling, it is recommended to avoid use in patients who have known hydroxyzine hypersensitivity, as cetirizine is a hydroxyzine derivative.

    Levocetirizine is contraindicated for use in pediatric patients less than 12 years of age with any degree of renal impairment and in patients of any age with end stage renal failure (CrCl less than 10 mL/minute) and those undergoing dialysis. Dosage adjustments are required for adolescents than 12 years of age with mild (CrCl 50 to 80 mL/minute), moderate (CrCl 30 to 50 mL/minute), or severe renal impairment (CrCl 10 to 30 mL/minute). Renal excretion is the primary route of levocetirizine elimination and renal clearance of the drug correlates with creatinine clearance. Do not use non-prescription (OTC) levocetirizine products in pediatric patients with renal disease without their care team's approval and prescription due to the needs for dosage adjustment.

    Although levocetirizine causes less sedation than first-generation antihistamines, somnolence, fatigue, and asthenia have been reported by some patients. Patients receiving levocetirizine should not perform activities requiring coordination and concentration, such as gymnastics, riding a bicycle, or for older adolescents, operation of vehicles, until they are aware of how this medication affects them. Because the effects of CNS depressants may be additive with antihistamines, counsel adolescents to avoid ethanol ingestion while taking levocetirizine. Also use caution with the coadministration of other CNS depressants with levocetirizine.

    Use levocetirizine with caution in patients with predisposing risk factors for urinary retention (e.g. bladder obstruction, spinal cord lesion). Discontinue use if urinary retention occurs; urinary retention has been reported postmarketing with levocetirizine. Patients who have trouble urinating or emptying their bladder should consult their care team prior to nonprescription (OTC) use.

    Description: Levocetirizine, the R-enantiomer of cetirizine, is a selective piperazine antihistamine (H1-blocker). Levocetirizine is effective in the treatment of seasonal allergic rhinitis, perennial allergic rhinitis, and chronic idiopathic urticaria in both adult and pediatric patients. Levocetirizine has been used off-label for the symptomatic relief of atopic dermatitis in pediatric patients. Despite reports of drowsiness with levocetirizine, controlled trials did not show it to cause adverse cognitive or psychomotor effects. Like its parent drug cetirizine, levocetirizine is considered "low-sedating", as it causes drowsiness to a lesser degree than first-generation (sedating) antihistamines. Levocetirizine is FDA-approved for prescription use in infants as young as 6 months and nonprescription products are available for children 2 years of age and older.

    For the management of symptoms of seasonal allergies or perennial allergies, including allergic rhinitis:
    Oral dosage (solution):
    Infants and Children 6 months to 1 year: 1.25 mg PO once daily in the evening. Use by prescription only.
    Children 2 to 5 years: 1.25 mg PO once daily in the evening.
    Children 6 to 11 years: 2.5 mg PO once daily in the evening.
    Children and Adolescents 12 to 17 years: 2.5 to 5 mg PO once daily in the evening. Some, such as those with less severe symptoms, experience adequate symptom control with 2.5 mg/day.
    Oral dosage (tablet):
    Children 6 to 11 years: 2.5 mg PO once daily in the evening.
    Children and Adolescents 12 to 17 years: 5 mg PO once daily in the evening. Some, such as those with less severe symptoms, experience adequate symptom control with 2.5 mg/day.

    For the treatment of chronic spontaneous urticaria (chronic idiopathic urticaria):
    Oral dosage (solution):
    Infants and Children 6 months to 5 years: 1.25 mg PO once daily in the evening.
    Oral dosage (tablet or solution):
    Children 6 to 11 years: 2.5 mg PO once daily in the evening.
    Children and Adolescents 12 years and older: 5 mg PO once daily in the evening. Some patients may be adequately controlled by 2.5 mg/day in the evening.

    For the symptomatic treatment of atopic dermatitis*:
    Oral dosage (solution):
    Children 1 to 2 years: 0.125 mg/kg/dose PO twice daily. Total daily dosage range from clinical studies: 2.83 to 3.83 mg/day.

    Maximum Dosage Limits:
    -Neonates
    Safety and efficacy have not been established.
    -Infants
    Less than 6 months: Safety and efficacy have not been established.
    6 to 11 months: 1.25 mg/day PO.
    -Children
    1 to 2 years: 1.25 mg/day PO; up to 0.125 mg/kg/dose PO twice daily has been used off-label for atopic dermatitis.
    3 to 5 years: 1.25 mg/day PO.
    6 to 11 years: 2.5 mg/day PO.
    12 years: 5 mg/day PO.
    -Adolescents
    5 mg/day PO.

    Patients with Hepatic Impairment Dosing
    No dosage adjustment is needed.

    Patients with Renal Impairment Dosing
    Nonprescription use is not recommended. According to the FDA-approved prescription label, the use of levocetirizine in children less than 12 years of age with any renal impairment is contraindicated. For pediatric patients 12 years and older, the following dosage adjustments are recommended :
    CrCl 50 to 80 mL/minute: 2.5 mg PO once daily.
    CrCl 30 to 50 mL/minute: 2.5 mg PO once every other day.
    CrCl 10 to 30 mL/minute: 2.5 mg PO twice a week; administered every 3 to 4 days.
    CrCl less than 10 mL/minute: Use is contraindicated.

    Hemodialysis
    Use of levocetirizine in patients undergoing hemodialysis is contraindicated.

    *non-FDA-approved indication

    Monograph content under development

    Mechanism of Action: Levocetirizine, the R-enantiomer of cetirizine, is highly selective for histamine H1-receptors. In vitro studies have demonstrated that levocetirizine has a 2-fold higher affinity for the H1-receptors than cetirizine. Levocetirizine, similar to other H1-antagonists, does not block the release of histamine, as do cromolyn and nedocromil, but rather competes with free histamine for binding at H1-receptor sites. This competitive antagonism blocks the effects of histamine on H1-receptors in the GI tract, uterus, large blood vessels, and bronchial smooth muscle. Levocetirizine suppresses histamine-induced skin reactions and associated pruritus. Blockade of H1-receptors reduces the edema, flare, and pruritus that result from histaminic activity. Levocetirizine, similar to the parent drug cetirizine, has a lower incidence of sedation compared to older antihistamines.

    The inflammatory response plays a prominent role in the development of nasal obstruction in patients with allergic rhinitis and involves a number of mediators. Initial release of histamine from mast cells is followed by late-phase reactions involving a number of other cells, such as fibroblasts, epithelial cells, neutrophils, eosinophils (especially in conditions with raised IgE levels), macrophages, platelets, and lymphocytes. Cell adhesion can also be part of the inflammatory process. Levocetirizine has demonstrated anti-inflammatory effects in both in vitro and in vivo studies. The anti-inflammatory action appears to be related to a reduction in eosinophils, neutrophils, interleukin-4 and interleukin-8.

    Pharmacokinetics: Levocetirizine is administered orally. Levocetirizine is 91% to 92% protein bound. The mean volume of distribution is approximately 0.4 L/kg in both pediatric and adult patients. Only 14% of levocetirizine undergoes metabolism via aromatic oxidation, N-dealkylation, O-dealkylation, and taurine conjugation; the remaining 86% is excreted unchanged. The elimination half-life in healthy adults is approximately 8 to 9 hours and is somewhat shorter in pediatric patients. Urinary excretion accounts for 85.4% of a dose and the feces for 12.9%. Renal clearance correlates with creatinine clearance; levocetirizine is excreted by both glomerular filtration and active tubular secretion.

    Affected cytochrome P450 isoenzymes: CYP3A4
    CYP3A4 contributes to the metabolism of levocetirizine; however, clinically significant drug interactions are not expected. Only 14% of levocetirizine is metabolized via aromatic oxidation, N-dealkylation, O-dealkylation, and taurine conjugation. The CYP3A4 isoenzyme is responsible for dealkylation; the enzymes responsible for aromatic oxidation have not fully been elucidated. In vitro studies have demonstrated that levocetirizine does not inhibit CYP1A2, 2C9, 2C19, 2A1, 2D6, 2E1, or 3A4. In addition, levocetirizine does not induce CYP1A2, 2C9, or 3A4. Formal drug interaction studies with levocetirizine have not been performed; data have been extrapolated from cetirizine studies.


    -Route-Specific Pharmacokinetics
    Oral Route
    The oral tablet and solution are bioequivalent. Levocetirizine is rapidly absorbed from the GI tract with peak plasma concentrations reached in approximately 0.5 to 0.9 hours after administration. Steady state plasma concentrations are achieved in 2 days. Although the rate of absorption of the tablets may be increased and peak plasma concentrations reduced by 36% when administered with food, levocetirizine may be administered with or without food.


    -Special Populations
    Pediatrics
    Infants and Children less than 6 years
    In a pharmacokinetic study, 15 children (12 to 24 months of age) suffering from recurrent cough and other allergy-related symptoms received levocetirizine 0.125 mg/kg/dose PO twice daily for 90 days. The following mean pharmacokinetic parameters were calculated: Tmax = 1 hour, Vd = 0.37 L/kg, and t1/2 = 4 hours. Pharmacokinetic parameters of children less than 6 years were calculated from a retrospective population pharmacokinetic analysis that included 324 subjects (181 children aged 1 to 5 years, 19 children 6 to 11 years, and 124 adults 18 to 55 years). Single or multiple doses ranging from 1.25 to 30 mg levocetirizine were administered; resultant data indicate that children aged 6 months to 5 years who receive 1.25 mg daily have drug plasma concentrations similar to those of adults who receive 5 mg daily.

    Children 6 years and older
    In a single-dose pharmacokinetic study, 14 children (6 to 11 years of age) with mild allergic rhinitis received levocetirizine 5 mg PO. The following mean pharmacokinetic parameters were calculated: Tmax = 1.2 +/- 0.2 hours, Vd = 0.4 +/- 0.02 L/kg, CL = 0.82 +/- 0.05 mL/kg/minute (30% greater weight-normalized apparent body clearance than that of adults), and t1/2 = 5.7 +/- 0.2 hours (24% reduction when compared to adults). The Cmax and AUC values were about 2-fold greater than those reported in healthy adult subjects who also received a 5 mg dose in a cross-study comparison.

    Hepatic Impairment
    The effects of hepatic impairment on levocetirizine have not been studied. Approximately 72% of levocetirizine is renally cleared leaving only 28% for non-renal clearance; hepatic impairment is unlikely to result in significant change in levocetirizine clearance.

    Renal Impairment
    In patients with mild, moderate, and severe renal impairment, the levocetirizine AUC is increased by 1.8-, 3.2-, and 4.3-fold, respectively, and the half-life is increased by 1.4-, 2-, and 2.9-fold. In patients with renal failure (CrCl less than 10 mL/minute), the AUC and half-life is increased by 5.7- and 4-fold, respectively. Dialysis removes less than 10% of levocetirizine from the blood. Dosage adjustments are necessary in adolescent and adult patients with mild, moderate, or severe renal impairment; due to a lack of data in infants and children, use is not recommended in these patients if renal impairment is present. Levocetirizine should not be administered to patients with renal failure (CrCl less than 10 mL/minute), those on dialysis, and pediatric patients less than 12 years with any degree of renal impairment.

DISCLAIMER: This drug information content is provided for informational purposes only and is not intended to be a substitute for professional medical advice, diagnosis, or treatment. Patients should always consult their physician with any questions regarding a medical condition and to obtain medical advice and treatment. Drug information is sourced from GSDD (Gold Standard Drug Database ) provided by Elsevier.

×

Medicine Chest

24hr allergy relief has been added to your Medicine Chest.

Log In

You need to log into the site to use this feature

More Ways to Save On:

You may find alternative ways to save with this medication. Talk to your pharmacist about the potential option(s) noted below.

Close

Log In

You need to log into the site to use this feature

Create A Free Account To Use Medicine Chest

This feature requires registration. Sign up or log in to your free WellRx account to gain access to this and other tools to help make managing your medications and wellness easier.

Benefits Include:

Store & manage your medication list
Medication pricing updates
Import medication from your pharmacy
Medication information
Pill & refill reminders
Medication journal & mood log

Sign up to use Medicine Chest

Create A Free Account To Use this feature

This feature requires registration. Sign up or log in to your free WellRx account to gain access to this and other tools to help make managing your medications and wellness easier.

Benefits Include:

Store & manage your medication list
Medication pricing updates
Import medication from your pharmacy
Medication information
Pill & refill reminders
Medication journal & mood log

Sign up to use this feature

You will be redirected to your program in 5 seconds.

Hi there.

Our Terms and Conditions and Privacy Policy have recently been updated.

Learn More


I Accept

By declining you will be logged out of your account