Levocetirizine; Uses, Dosage, Side Effects, Drug Interactions

Levocetirizine; Uses, Dosage, Side Effects, Drug Interactions

Levocetirizine is a third generation, non-sedating, selective histamine H1 receptor antagonist, with an antihistamine, anti-inflammatory, and potential anti-angiogenic activities. Levocetirizine competes with endogenous histamine for binding at peripheral H1-receptor sites on the effector cell surface. This prevents the negative symptoms associated with histamine release and an allergic reaction. In addition, as histamine plays an important role in angiogenesis during an allergic inflammatory reaction, blocking the action of histamine may modulate the expression of proangiogenic factors and thus may prevent angiogenesis. As a third-generation histamine H1 receptor antagonist, levocetirizine has fewer side effects than most second-generation antihistamines.

Levocetirizine is a third-generation non-sedative antihistamine indicated for the relief of symptoms associated with seasonal and perennial allergic rhinitis and uncomplicated skin manifestations of chronic idiopathic urticaria. It was developed from the second-generation antihistamine cetirizine. Levocetirizine is the R-enantiomer of the cetirizine racemate. Levocetirizine is an inverse agonist that decreases activity at histamine H1 receptors. This, in turn, prevents the release of other allergy chemicals and increased blood supply to the area, and provides relief from the typical symptoms of hay fever.

Mechanism of action of Levocetirizine

Levocetirizine, the active enantiomer of cetirizine, is an antihistamine; its principal effects are mediated via selective inhibition of H1 receptors. The antihistaminic activity of levocetirizine has been documented in a variety of animal and human models. In vitro binding studies revealed that levocetirizine has an affinity for the human H1-receptor 2-fold higher than that of cetirizine (Ki = 3 nmol/L vs. 6 nmol/L, respectively). This increased affinity has unknown clinical relevance.

Indications of Levocetirizine

  • Chronic idiopathic urticaria
  • Perennial allergic rhinitis
  • Seasonal allergic rhinitis
  • Urticaria
  • Allergies
  • Allergic rhinitis
  • Perennial allergic rhinitis
  • Pollen allergy
  • Sneezing
  • Runny nose
  • Itchy or watery eyes
  • Itchy throat or nose
  • Upper respiratory tract hypersensitivity reaction, site unspecified
  • Rhinorrhea
  • Postnasal discharge,
  • Nasal pruritus,
  • Ocular pruritus & tearing
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Contra-Indications of Levocetirizine

  • End-Stage Renal Disease
  • enlarged prostate with urination problem
  • Cannot Empty Bladder
  • moderate to severe kidney impairment
  • Hemodialysis with High-Flux Membrane
Allergies to
  • Antihistamines
  • Antihistamines – Piperazine

Dosages of Levocetirizine

Strengths: 2.5 mg; 5 mg; 0.5 mg/mL


  • 5 mg orally once a day in the evening

Allergic Rhinitis

Seasonal Allergic Rhinitis (OTC)

  • 5 mg orally once a day in the evening; some patients may be adequately controlled on 2.5 mg once a day

Pediatric Dose for Allergic Rhinitis

Perennial Allergic Rhinitis

  • 6 months to 2 years: 1.25 mg orally once a day in the evening

Seasonal Allergic Rhinitis (OTC)

  • 6 to 11 years: 2.5 mg orally once a day in the evening
  • 12 years or older: 5 mg orally once a day in the evening; some patients may be adequately controlled on 2.5 mg once a day.


  • 6 months to 5 years: 1.25 mg orally once a day in the evening
  • 6 to 11 years: 2.5 mg orally once a day in the evening
  • 12 years or older: 5 mg orally once a day in the evening; some patients may be adequately controlled on 2.5 mg once a day

Side Effects of Levocetirizine

The most common

More common

Less common

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Drug Interactions of Levocetirizine

Levocetirizine may interact with following drugs, supplement & may change the efficacy of drugs

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, 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.

Pregnancy and Lactation of Levocetirizine

FDA Pregnancy category B


Very rare clinical data on exposed pregnancies are available. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/fetal development, parturition or postnatal development. Caution should be exercised when prescribing to pregnant or breastfeeding women because levocetirizine passes into breast milk.


Levocetirizine is the R-enantiomer of cetirizine. Small occasional doses of levocetirizine are probably acceptable during breastfeeding. Larger doses or more prolonged use may cause drowsiness and other effects in the infant or decrease the milk supply, particularly in combination with a sympathomimetic such as pseudoephedrine or before lactation is well established.




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