Levocetirizine

Levocetirizine Brand Names

Xyzal | Xyzal Allergy 24 Hour | Xyzal Children’s Allergy 24 Hour

What is Levocetirizine

Levocetirizine the R-enantiomer of cetirizine, is a selective piperazine low-sedating antihistamine (H1-blocker).

Studies have shown that the antihistaminic effects of racemic cetirizine reside in the R-enantiomer, levocetirizine, and not the S-enantiomer, dextrocetirizine.

Based on results of in vitro studies, levocetirizine has demonstrated a 2-fold and 30-fold greater affinity for H1-receptors compared to cetirizine and dextrocetirizine, respectively.

Levocetirizine and cetirizine have been found to have similar efficacy in the inhibition of histamine-induced wheal response, flare response, and nasal resistance.

Levocetirizine is effective in the treatment of seasonal allergic rhinitis, perennial allergic rhinitis, and chronic idiopathic urticaria.

In 1 study, cetirizine demonstrated a longer itch response in patients with chronic idiopathic urticaria when compared to levocetirizine.

Levocetirizine was found to be superior in suppression of histamine-induced skin reactions when compared to loratadine and desloratadine.

Despite reports of drowsiness with levocetirizine, controlled trials did not show it to cause adverse cognitive or psychomotor effects.

Levocetirizine was initially FDA-approved in 2007 and prescription use is approved in adult and pediatric patients as young as 6 months of age; the FDA subsequently approved the nonprescription use of the drug in 2017 for adult and pediatric patients as young as 2 years of age.

Indications

  1. allergic rhinitis
  2. atopic dermatitis
  3. chronic idiopathic urticaria
  4. perennial allergies
  5. seasonal allergies

For the management of symptoms of seasonal allergies or perennial allergies, including allergic rhinitis

Side Effects

  1. acute generalized exanthematous pustulosis (AGEP)
  2. agitation
  3. anaphylactoid reactions
  4. angioedema
  5. arthralgia
  6. asthenia
  7. blurred vision
  8. cholestasis
  9. constipation
  10. cough
  11. depression
  12. diarrhea
  13. dizziness
  14. drowsiness
  15. dysgeusia
  16. dyskinesia
  17. dyspnea
  18. dystonic reaction
  19. dysuria
  20. elevated hepatic enzymes
  21. epistaxis
  22. fatigue
  23. fever
  24. glomerulonephritis
  25. hallucinations
  26. hemolytic anemia
  27. hepatitis
  28. hypotension
  29. infection
  30. insomnia
  31. myalgia
  32. myoclonia
  33. nasal congestion
  34. nausea
  35. palpitations
  36. paresthesias
  37. pharyngitis
  38. pruritus
  39. rash
  40. seizures
  41. sinus tachycardia
  42. suicidal ideation
  43. syncope
  44. thrombocytopenia
  45. tremor
  46. urinary retention
  47. urticaria
  48. vertigo
  49. visual impairment
  50. vomiting
  51. weight gain
  52. xerostomia

Monitoring Parameters

  • laboratory monitoring not necessary

Contraindications

  • bladder obstruction
  • breast-feeding
  • coadministration with other CNS depressants
  • dialysis
  • driving or operating machinery
  • ethanol ingestion
  • geriatric
  • hydroxyzine hypersensitivity
  • infants
  • neonates
  • pregnancy
  • prostatic hypertrophy
  • renal failure
  • renal impairment
  • urinary retention

Interactions

  • Acetaminophen; Butalbital
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Codeine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Pentazocine
  • Acetaminophen; Propoxyphene
  • Acetaminophen; Tramadol
  • Alfentanil
  • Alprazolam
  • Amitriptyline; Chlordiazepoxide
  • Amobarbital
  • Amoxapine
  • Anticholinergics
  • Apomorphine
  • Aripiprazole
  • Asenapine
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Caffeine; Orphenadrine
  • Aspirin, ASA; Carisoprodol
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Oxycodone
  • Atropine; Difenoxin
  • Atropine; Diphenoxylate
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • atypical antipsychotic
  • Baclofen
  • Barbiturates
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Belladonna; Opium
  • Benzhydrocodone; Acetaminophen
  • Benzodiazepines
  • Brexpiprazole
  • Brompheniramine; Guaifenesin; Hydrocodone
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Buprenorphine
  • Buprenorphine; Naloxone
  • Buspirone
  • Butabarbital
  • Butorphanol
  • Cannabidiol
  • Capsaicin; Metaxalone
  • Carbidopa; Levodopa
  • Carbidopa; Levodopa; Entacapone
  • Carbinoxamine; Hydrocodone; Phenylephrine
  • Carbinoxamine; Hydrocodone; Pseudoephedrine
  • Cariprazine
  • Carisoprodol
  • Cenobamate
  • Chloral Hydrate
  • Chlordiazepoxide
  • Chlordiazepoxide; Clidinium
  • Chlorpheniramine; Codeine
  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Hydrocodone
  • Chlorpheniramine; Hydrocodone; Phenylephrine
  • Chlorpheniramine; Hydrocodone; Pseudoephedrine
  • Chlorthalidone; Clonidine
  • Chlorzoxazone
  • Clonazepam
  • Clonidine
  • Clorazepate
  • Clozapine
  • Codeine
  • Codeine; Guaifenesin
  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
  • COMT inhibitors
  • Cyclobenzaprine
  • Dantrolene
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Desloratadine
  • Desloratadine; Pseudoephedrine
  • Deutetrabenazine
  • Dexmedetomidine
  • Diazepam
  • Dihydrocodeine; Guaifenesin; Pseudoephedrine
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Dronabinol
  • Droperidol
  • Enflurane
  • Entacapone
  • Esketamine
  • Estazolam
  • Eszopiclone
  • Ethanol
  • Etomidate
  • Fenfluramine
  • Fentanyl
  • Flibanserin
  • Fluoxetine; Olanzapine
  • Flurazepam
  • Fospropofol
  • Gabapentin
  • General anesthetics
  • Guaifenesin; Hydrocodone
  • Guaifenesin; Hydrocodone; Pseudoephedrine
  • Guanfacine
  • Haloperidol
  • Halothane
  • Heparin
  • Heterocyclic antidepressants
  • Homatropine; Hydrocodone
  • Hydrochlorothiazide, HCTZ; Methyldopa
  • Hydrocodone
  • Hydrocodone; Ibuprofen
  • Hydrocodone; Phenylephrine
  • Hydrocodone; Potassium Guaiacolsulfonate
  • Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
  • Hydrocodone; Pseudoephedrine
  • Hydromorphone
  • Ibuprofen; Oxycodone
  • Iloperidone
  • Isocarboxazid
  • Isoflurane
  • Ketamine
  • Lemborexant
  • Levodopa
  • Levorphanol
  • Lofexidine
  • Lopinavir; Ritonavir
  • Loratadine
  • Loratadine; Pseudoephedrine
  • Lorazepam
  • Loxapine
  • Lumateperone
  • Lurasidone
  • Maprotiline
  • Melatonin
  • Meperidine
  • Meperidine; Promethazine
  • Mephobarbital
  • Meprobamate
  • Metaxalone
  • Methadone
  • Methohexital
  • Methyldopa
  • Midazolam
  • Mirtazapine
  • Molindone
  • Monoamine oxidase inhibitors
  • Morphine
  • Morphine; Naltrexone
  • Nabilone
  • Nalbuphine
  • Nefazodone
  • Olanzapine
  • Ombitasvir; Paritaprevir; Ritonavir
  • Opiate Agonists
  • Orphenadrine
  • Oxazepam
  • Oxycodone
  • Oxymorphone
  • Paliperidone
  • Pentazocine
  • Pentazocine; Naloxone
  • Pentobarbital
  • Perampanel
  • Phenelzine
  • Phenobarbital
  • Pimavanserin
  • Pimozide
  • Pramipexole
  • Pregabalin
  • Primidone
  • Propofol
  • Propoxyphene
  • Quazepam
  • Quetiapine
  • Ramelteon
  • Rasagiline
  • Remifentanil
  • Risperidone
  • Ritonavir
  • Ropinirole
  • Rotigotine
  • Safinamide
  • Secobarbital
  • Sedating H1-blockers
  • Selegiline
  • Sevoflurane
  • Sincalide
  • Skeletal Muscle Relaxants
  • Sodium Oxybate
  • Sufentanil
  • Suvorexant
  • Tapentadol
  • Tasimelteon
  • Temazepam
  • Tetrabenazine
  • Thalidomide
  • Theophylline, Aminophylline
  • Thiopental
  • Thiothixene
  • Tolcapone
  • Tramadol
  • Tranylcypromine
  • Trazodone
  • Triazolam
  • Tricyclic antidepressants
  • Trospium
  • Valerian, Valeriana officinalis
  • Valproic Acid, Divalproex Sodium
  • Zaleplon
  • Ziprasidone
  • Zolpidem