Dosing & Uses
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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (4)
- 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.
- olopatadine intranasal
levocetirizine and olopatadine intranasal both increase sedation. Avoid or Use Alternate Drug. Coadministration increases risk of CNS depression, which can lead to additive impairment of psychomotor performance and cause daytime impairment.
- 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 (20)
- acrivastine
acrivastine and levocetirizine both increase sedation. Use Caution/Monitor.
- 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.
- amisulpride
amisulpride and levocetirizine both increase sedation. Use Caution/Monitor.
- asenapine
asenapine and levocetirizine both increase sedation. Use Caution/Monitor.
- asenapine transdermal
asenapine transdermal and levocetirizine both increase sedation. Use Caution/Monitor.
- avapritinib
avapritinib and levocetirizine both increase sedation. Use Caution/Monitor.
- 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).
- daridorexant
levocetirizine and daridorexant both increase sedation. Modify Therapy/Monitor Closely. Coadministration increases risk of CNS depression, which can lead to additive impairment of psychomotor performance and cause daytime impairment.
- 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.
- donepezil transdermal
donepezil transdermal, levocetirizine. Either decreases effects of the other by pharmacodynamic antagonism. Use Caution/Monitor.
- 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.
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)
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
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.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%
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| levocetirizine oral - | 5 mg tablet |  | |
| levocetirizine oral - | 5 mg tablet |  | |
| levocetirizine oral - | 5 mg tablet |  | |
| levocetirizine oral - | 2.5 mg/5 mL solution |  | |
| levocetirizine oral - | 5 mg tablet |  | |
| levocetirizine oral - | 5 mg tablet |  | |
| levocetirizine oral - | 2.5 mg/5 mL solution |  | |
| levocetirizine oral - | 5 mg tablet |  | |
| levocetirizine oral - | 2.5 mg/5 mL solution |  | |
| levocetirizine oral - | 5 mg tablet |  | |
| levocetirizine oral - | 5 mg tablet |  | |
| levocetirizine oral - | 5 mg tablet |  | |
| levocetirizine oral - | 2.5 mg/5 mL solution |  | |
| levocetirizine oral - | 2.5 mg/5 mL solution |  | |
| Xyzal oral - | 5 mg tablet |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
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 last or get worse, tell your doctor or pharmacist promptly.If your doctor has directed you to use this medication, remember that your doctor 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 February 2022. Copyright(c) 2023 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.
