Drug reference

Levocetirizine

Antihistamine · Corticosteroid

Also known as Levocetirizine dihydrochloride, Levocetirizine HCl

AntihistamineCorticosteroidATC R06AE009

CDSCO approvedSchedule HJan AushadhiATC R06AE009

Pharmacokineticsplasma · t hours

ONSET: 1h · Within 1 hour
PEAK: 1h · Approximately 1 hour
t½: 8.5h · Approximately 7-10 hours (varies with age and renal function)
DURATION: 1d · Up to 24 hours

EXCRETION

—

not curated

INTERACTIONS

—

none in our sources

PREGNANCY

Category B (No evidence of risk in humans based on animal studies and limited human data, but controlled studies in pregnant women are lacking.)

FDA category + note

Mechanism

Levocetirizine, the R-enantiomer of cetirizine, is a potent and highly selective peripheral H1-receptor antagonist. It competitively binds to and inhibits histamine at H1 receptors, thereby preventing histamine-mediated effects such as vasodilation, increased capillary permeability, pruritus, and bronchoconstriction. It has minimal anticholinergic or antiserotonergic activity.

Indications

Perennial allergic rhinitisSeasonal allergic rhinitisChronic idiopathic urticariaAllergic conjunctivitisallergic rhinitisconjunctivitishay feverpollinosisurticariadermographismatopic eczemaacute allergic reactions to drugs and foods

Dosing

Adult: 5 mg orally once daily, in the evening. May be taken with or without food. For patients with mild renal impairment, dose adjustment is required.
Pediatric: 6 months to 5 years: 1.25 mg orally once daily. 6 to 11 years: 2.5 mg orally once daily. 12 years and older: 5 mg orally once daily.
Renal adjustment: For adults and adolescents ≥12 years: Mild impairment (CrCl 50-79 mL/min): 2.5 mg orally once daily. Moderate impairment (CrCl 30-49 mL/min): 2.5 mg orally every other day. Severe impairment (CrCl 10-29 mL/min): 2.5 mg orally twice weekly. Contraindicated in end-stage renal disease (CrCl <10 mL/min).…

Pharmacokinetics

Onset

Within 1 hour

Peak effect

Approximately 1 hour

Duration

Up to 24 hours

Half-life

Approximately 7-10 hours (varies with age and renal function)

Bioavailability

High, approximately 90% (oral)

Protein binding

Approximately 90%

Metabolism

Minimal hepatic metabolism, primarily excreted unchanged

Excretion

Primarily renal, approximately 85.4% of the dose excreted unchanged in urine

Contraindications

Hypersensitivity to levocetirizine, cetirizine, or any piperazine derivatives
End-stage renal disease (CrCl <10 mL/min) or hemodialysis patients
Children aged 6 months to 11 years with impaired renal function
Patients with severe renal impairment (CrCl <30 mL/min)

Side effects

Common

Somnolence (drowsiness)FatigueDry mouthHeadacheNasopharyngitisPharyngitisCoughFeverless sedation and other side effects compared to cetirizine

Serious

Hypersensitivity reactions (including anaphylaxis)
Angioedema
Convulsions
Hepatitis (rare)
Severe drowsiness/sedation (especially with overdose)
Urinary retention

Pregnancy & lactation

Pregnancy

Category B (No evidence of risk in humans based on animal studies and limited human data, but controlled studies in pregnant women are lacking.)

Lactation

Levocetirizine is excreted into breast milk. Although data are limited, there is a potential for adverse effects in breastfed infants (e.g., sedation, irritability). Use with caution and only if the potential benefit outweighs the potential risk. Monitor infant for drowsiness or feeding difficulties.

Drug interactions

Ritonavir

Moderate

Database

Potential for increased plasma concentrations of levocetirizine, leading to increased adverse effects (e.g., sedation).

Monitor for increased adverse effects of levocetirizine. Dose adjustment of levocetirizine may be considered if significant sedation occurs, although this interaction is generally not considered severe.

Source: DDInter

11 additional unreviewed or low-confidence interactions hidden because their provenance or source detail is insufficient.