levocetirizine (OTC)

Brand and Other Names:Xyzal Allergy 24HR Tablets, Xyzal Allergy 24HR Oral Solution, more...Xyzal
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 5mg

oral solution

  • 2.5mg/5mL

Allergic Rhinitis

Indicated for relief of symptoms associated with seasonal and perennial allergic rhinitis

5 mg PO qDay in evening

Some patients may respond to 2.5 mg/day

Chronic Urticaria

Indicated for uncomplicated skin manifestations of chronic idiopathic urticaria

5 mg PO qDay in evening

Dosage Modifications

Renal impairment

  • CrCl 50-80 mL/min: 2.5 mg PO qDay
  • CrCl 30-50 mL/min: 2.5 mg PO every other day
  • CrCl 10-30 mL/min: 2.5 mg PO 2x/wk (ie, q3-4 days)
  • CrCl <10 mL/min and or hemodialysis: Contraindicated

Hepatic impairment

  • No dose adjustment required

Dosage Forms & Strengths

tablet

  • 5mg

oral solution

  • 2.5mg/5mL

Allergic Rhinitis

Indicated for relief of symptoms associated with seasonal and perennial allergic rhinitis

<6 months: Safety and efficacy not established

6 months to 5 years: 1.25 mg PO qDay in evening

6-12 years: 2.5 mg PO qDay in evening

>12 years: 5 mg PO qDay in evening; some patients may respond to 2.5 mg/day

Chronic Urticaria

Indicated for uncomplicated skin manifestations of chronic idiopathic urticaria

<6 months: Safety and efficacy not established

6 months to 5 years: 1.25 mg PO qDay in evening

6-12 years: 2.5 mg PO qDay in evening

>12 years: 5 mg PO qDay in evening

Dosage Modifications

Renal impairment

  • Aged ≥12 years
    • CrCl 50-80 mL/min: 2.5 mg PO qDay
    • CrCl 30-50 mL/min: 2.5 mg PO every other day
    • CrCl 10-30 mL/min: 2.5 mg PO 2x/wk (ie, q3-4 days)
    • CrCl <10 mL/min and or hemodialysis: Contraindicated
  • Aged 6 months to <12 years
    • Any degree of renal impairment: Contraindicated

Hepatic impairment

  • No dose adjustment required
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Interactions

Interaction Checker

and levocetirizine

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Contraindicated (0)

              Serious - Use Alternative (3)

              • isocarboxazid

                isocarboxazid increases effects of levocetirizine by Other (see comment). Avoid or Use Alternate Drug. Comment: Isocarboxazid should not be administered in combination with antihistamines because of potential additive CNS depressant effects. MAO inhibitors also prolong and intensify anticholinergic effects of antihistamines. .

              • metoclopramide intranasal

                levocetirizine, metoclopramide intranasal. Either increases effects of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Avoid use of metoclopramide intranasal or interacting drug, depending on importance of drug to patient.

              • tranylcypromine

                tranylcypromine increases effects of levocetirizine by Other (see comment). Avoid or Use Alternate Drug. Comment: Tranylcypromine should not be administered in combination with antihistamines because of potential additive CNS depressant effects. MAO inhibitors also prolong and intensify anticholinergic effects of antihistamines.

              Monitor Closely (13)

              • amifampridine

                levocetirizine increases toxicity of amifampridine by Other (see comment). Modify Therapy/Monitor Closely. Comment: Amifampridine can cause seizures. Coadministration with drugs that lower seizure threshold may increase this risk.

              • clobazam

                levocetirizine, clobazam. Other (see comment). Use Caution/Monitor. Comment: Concomitant administration can increase the potential for CNS effects (e.g., increased sedation or respiratory depression).

              • diazepam intranasal

                diazepam intranasal, levocetirizine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration may potentiate the CNS-depressant effects of each drug.

              • esketamine intranasal

                esketamine intranasal, levocetirizine. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely.

              • gabapentin

                gabapentin, levocetirizine. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.

              • gabapentin enacarbil

                gabapentin enacarbil, levocetirizine. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.

              • hyaluronidase

                levocetirizine decreases effects of hyaluronidase by Other (see comment). Use Caution/Monitor. Comment: Antihistamines, when given in large systemic doses, may render tissues partially resistant to the action of hyaluronidase. Patients may require larger amounts of hyaluronidase for equivalent dispersing effect. .

              • lurasidone

                lurasidone, levocetirizine. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Potential for increased CNS depressant effects when used concurrently; monitor for increased adverse effects and toxicity.

              • midazolam intranasal

                midazolam intranasal, levocetirizine. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Concomitant use of barbiturates, alcohol, or other CNS depressants may increase the risk of hypoventilation, airway obstruction, desaturation, or apnea and may contribute to profound and/or prolonged drug effect.

              • phenelzine

                phenelzine increases effects of levocetirizine by Other (see comment). Modify Therapy/Monitor Closely. Comment: Coadministration of phenelzine and antihistamines may result in additive CNS depressant effects. MAO inhibitors also prolong and intensify anticholinergic effects of antihistamines. .

              • pregabalin

                pregabalin, levocetirizine. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration of CNS depressants can result in serious, life-threatening, and fatal respiratory depression. Use lowest dose possible and monitor for respiratory depression and sedation.

              • ritonavir

                ritonavir increases levels of levocetirizine by decreasing metabolism. Use Caution/Monitor.

              • stiripentol

                stiripentol, levocetirizine. Either increases effects of the other by sedation. Use Caution/Monitor. Concomitant use stiripentol with other CNS depressants, including alcohol, may increase the risk of sedation and somnolence.

              Minor (1)

              • theophylline

                theophylline increases levels of levocetirizine by decreasing elimination. Minor/Significance Unknown.

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              Adverse 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

              Cardiac disorders: Palpitations, tachycardia

              Ear and labyrinth disorders: Vertigo

              Eye disorders: Blurred vision, visual disturbances

              Gastrointestinal disorders: Nausea, vomiting

              General disorders and administration site conditions: Edema

              Hepatobiliary disorders: Hepatitis

              Immune system disorders: Anaphylaxis and hypersensitivity

              Metabolism and nutrition disorders: Increased appetite

              Musculoskeletal, connective tissues, and bone disorders: Arthralgia, myalgia

              Nervous system disorders: Dizziness, dysgeusia, febrile seizure, movement disorders (including dystonia and oculogyric crisis), paraesthesia, seizure (reported in subjects with and without a known seizure disorder), tremor

              Psychiatric disorders: Aggression and agitation, depression, hallucinations, insomnia, nightmare, suicidal ideation

              Renal and urinary disorders: Dysuria, urinary retention

              Respiratory, thoracic, and mediastinal disorders: Dyspnea

              Skin and allergy: Hypersensitivity and anaphylaxis, angioedema, fixed drug eruption, pruritus, rash, acute generalized exanthematous pustulosis, and urticaria

              Postmarketing reports of cetirizine

              • Cardiac disorders: Severe hypotension
              • Gastrointestinal disorders: Cholestasis
              • Nervous system disorders: Extrapyramidal symptoms, myoclonus, orofacial dyskinesia, tic
              • Pregnancy, puerperium and perinatal conditions: Stillbirth
              • Renal and urinary disorders: Glomerulonephritis
              • Skin and subcutaneous tissue disorders: acute generalized exanthematous pustulosis (AGEP); rebound pruritus-pruritus within a few days after discontinuation of cetirizine, usually after long-term use (eg, months to years)
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              Warnings

              Contraindications

              Hypersensitivity to levocetirizine or cetirizine

              ESRD (CrCl <10 mL/min) or patients undergoing hemodialysis

              Children aged 6 month to <12 years with renal impairment

              Cautions

              Caution in narrow angle glaucoma, stenosing peptic ulcer, or pyloroduodenal obstruction

              Pruritus may rebound within several days of stopping therapy, following long term use

              May cause CNS depression and impair physical or mental abilities; avoid performin tasks that require mental alertness, including operating heavy machinery or driving

              Urinary retention may occur; use caution in patients at risk of urinary retention, including prostatic hyperplasia and spinal cord injuries

              Use caution in patients with mild to severe renal impairment

              Avoid alcohol or other CNS depressants

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              Pregnancy & Lactation

              Pregnancy

              Available data from published literature and postmarketing experience in pregnant women are insufficient to identify any drug-associated risks of miscarriage, birth defects, or adverse maternal or fetal outcomes

              Animal data

              • In animal reproduction studies, there was no evidence of fetal harm with administration of levocetirizine by oral route to pregnant rats and rabbits, during period of organogenesis, at doses up to 390 times and 470 times, respectively, maximum recommended human dose (MRHD) in adults
              • Rats treated during late gestation and lactation period, had no effects on pup development at oral doses up to approximately 60 times the MRHD in adults; in mice treated during late gestation and lactation period, drug administered by oral route to dams had no effects on pup development at a dose that was approximately 25 times the MRHD in adults; however, lower pup weight gain during lactation was observed at a dose that was 95 times MRHD in adults

              Lactation

              There are no data on presence of levocetirizine in human milk, effects on breastfed infant, or on milk production; however, drug has been reported to be present in human breast milk; in mice and beagle dogs, studies indicated cetirizine was excreted in milk; when a drug is present in animal milk, it is likely the drug will be present in human milk; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from drug or from underlying maternal condition

              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.

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              Pharmacology

              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%

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              Images

              BRAND FORM. UNIT PRICE PILL IMAGE
              levocetirizine oral
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              5 mg tablet
              levocetirizine oral
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              5 mg tablet
              levocetirizine oral
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              levocetirizine oral
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              levocetirizine oral
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              2.5 mg/5 mL solution
              levocetirizine oral
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              5 mg tablet
              levocetirizine oral
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              2.5 mg/5 mL solution
              levocetirizine oral
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              5 mg tablet
              levocetirizine oral
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              2.5 mg/5 mL solution
              levocetirizine oral
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              5 mg tablet
              levocetirizine oral
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              2.5 mg/5 mL solution
              Xyzal oral
              -
              5 mg tablet
              Xyzal oral
              -
              5 mg tablet
              Xyzal oral
              -
              5 mg tablet

              Copyright © 2010 First DataBank, Inc.

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              Patient Handout

              Patient Education
              levocetirizine oral

              LEVOCETIRIZINE - ORAL

              (lee-voh-seh-TEER-ah-zeen)

              COMMON BRAND NAME(S): Xyzal

              USES: Levocetirizine is an antihistamine used to relieve allergy symptoms such as watery eyes, runny nose, itching eyes/nose, and sneezing. It is also used to relieve itching and hives. It works by blocking a certain natural substance (histamine) that your body makes during an allergic reaction.Levocetirizine does not prevent hives or prevent/treat a serious allergic reaction (such as anaphylaxis). If your doctor has prescribed epinephrine to treat allergic reactions, always carry your epinephrine injector with you. Do not use levocetirizine in place of your epinephrine.

              HOW TO USE: If you are taking the over-the-counter product to self-treat, read and follow all directions on the product package before taking this medication. If you have any questions, consult your pharmacist. If your doctor has prescribed this medication, take it as directed.This medication is taken by mouth with or without food, usually once daily in the evening.If you are using the liquid form of this medication, measure the dose carefully using a special measuring device/spoon. Do not use a household spoon because you may not get the correct dose.The dosage is based on your age, medical condition, and response to treatment. Do not increase your dose or take this medication more often than directed.If your condition does not get better or if it gets worse, or if you think you may have a serious medical problem, get medical help right away.

              SIDE EFFECTS: Drowsiness, tiredness, and dry mouth may occur. Fever or cough may also occur, especially in children. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.If your doctor has directed you to use this medication, remember that he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: difficulty urinating, weakness.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

              PRECAUTIONS: Before taking levocetirizine, tell your doctor or pharmacist if you are allergic to it; or to cetirizine; or to hydroxyzine; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: difficulty urinating (such as due to an enlarged prostate), kidney disease.This drug may make you drowsy. Alcohol or marijuana (cannabis) can make you more drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).Liquid products may contain sugar and/or aspartame. Caution is advised if you have diabetes, phenylketonuria (PKU), or any other condition that requires you to limit/avoid these substances in your diet. Ask your doctor or pharmacist about using this medication safely.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.This medication passes into breast milk. Consult your doctor before breast-feeding.

              DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Tell your doctor or pharmacist if you are taking other products that cause drowsiness such as opioid pain or cough relievers (such as codeine, hydrocodone), alcohol, marijuana (cannabis), drugs for sleep or anxiety (such as alprazolam, lorazepam, zolpidem), muscle relaxants (such as carisoprodol, cyclobenzaprine), or other antihistamines (such as diphenhydramine, promethazine).Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.Do not use with any other antihistamines applied to the skin (such as diphenhydramine cream, ointment, spray) because increased side effects may occur.Levocetirizine is very similar to hydroxyzine and cetirizine. Do not use these medications while using levocetirizine.This medication may interfere with certain laboratory tests (including allergy skin testing), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.

              OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe drowsiness. In children, mental/mood changes (such as restlessness, agitation) may occur before drowsiness.

              NOTES: Keep all regular medical and lab appointments.

              MISSED DOSE: If you are taking this medication on a regular schedule and miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

              STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

              Information last revised October 2018. Copyright(c) 2021 First Databank, Inc.

              IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.