Pharmacology of Levocetirizine


Levocetirizine, the R-enantiomer of cetirizine, is a third-generation non-sedating antihistamine. It is used primarily in the management of allergic conditions such as allergic rhinitis and chronic urticaria.

Chemical Structure and Properties


Levocetirizine is chemically known as (R)-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic acid. As a third-generation antihistamine, it is designed to minimize central nervous system penetration, reducing sedative effects.

Mechanism of Action

Levocetirizine acts by selectively inhibiting peripheral histamine H1-receptors. This antagonism prevents histamine from exerting its effects on capillary permeability, vascular dilation, and sensory nerves, thus mitigating allergic symptoms.


  • Absorption: Rapidly and extensively absorbed after oral administration, with peak plasma concentrations occurring within an hour.
  • Distribution: Displays limited penetration into the brain, minimizing sedative effects. It has a moderate volume of distribution and low protein binding.
  • Metabolism: Unlike many other antihistamines, levocetirizine is not extensively metabolized in the liver, which reduces the risk of drug interactions.
  • Excretion: Excreted primarily unchanged in urine.

Clinical Uses

  • Allergic Rhinitis: Effective in treating both seasonal and perennial allergic rhinitis.
  • Chronic Urticaria: Used in the management of chronic idiopathic urticaria for symptomatic relief of itching and hives.
  • Other Allergic Conditions: May be beneficial in other allergic reactions where histamine plays a key role.

Adverse Effects

  • Sedation: Although less sedating than first-generation antihistamines, drowsiness can still occur.
  • Gastrointestinal Disturbances: Symptoms such as dry mouth and nausea may be experienced.
  • Headaches: Some individuals may experience headaches.
  • Rare Effects: Palpitations and blurred vision have been reported but are uncommon.

Contraindications and Precautions

  • End-Stage Renal Disease: Should be used cautiously or avoided in patients with severe renal impairment.
  • Pediatric Use: The safety and effectiveness in children under 6 years of age have not been established.
  • Elderly Patients: Caution is advised due to the potential for increased sensitivity and reduced renal clearance.

Drug Interactions

  • Central Nervous System Depressants: Potential for increased sedation when used with other CNS depressants.
  • Renal Excretion Affecting Drugs: Drugs that affect renal excretion could alter the clearance of levocetirizine.
  • Ritonavir: There’s some evidence that co-administration with ritonavir can increase plasma levels of levocetirizine.

Special Considerations

  • Pregnancy and Breastfeeding: Should be used during pregnancy and breastfeeding only if clearly needed and after assessing the risks and benefits.
  • Impaired Driving: Patients should be cautioned about engaging in activities requiring mental alertness, as levocetirizine can cause drowsiness.


Levocetirizine, as a third-generation antihistamine, offers effective relief from allergic symptoms with a lower risk of sedation. Its utility in various allergic conditions, coupled with a favorable safety profile, makes it a valuable option in allergy management.

Disclaimer: This article is for informational purposes only and does not constitute medical advice. Always seek the advice of a healthcare provider with any questions regarding a medical condition.

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