XYZAL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for XYZAL (XYZAL).

How it works

Levocetirizine is a selective histamine H1-receptor antagonist; it inhibits the histamine-mediated responses in allergic conditions.

What the body does with it

Metabolism	Approximately 86% excreted unchanged in urine; minor hepatic metabolism (oxidative O-dealkylation) via CYP3A4.
Excretion	Approximately 84% of a dose is excreted renally as unchanged drug; 12% in feces via biliary elimination.
Half-life	Terminal elimination half-life is approximately 7 hours in healthy adults; prolonged to 8–11 hours in elderly and in renal impairment.
Protein binding	Approximately 95–96% bound primarily to human serum albumin.
Volume of Distribution	0.3–0.4 L/kg, indicating distribution primarily in extracellular fluid.
Bioavailability	Oral bioavailability is approximately 80–90%.
Onset of Action	Oral: 1 hour (antihistamine effect); intranasal: 15 minutes.
Duration of Action	Approximately 24 hours; clinical effect may persist longer due to high receptor affinity.

Classification & Brands

Action Class	H1 Antihistaminics (second Generation)
Brand Substitutes	Lecope Tablet, LCZ Tablet, 1-AL Tablet, Hatric Tablet, Levocet Tablet, Vocetin 2.5mg Syrup, Grilcet 2.5mg Syrup, Zucet Syrup, 1-AL Syrup, Belrin-LZ Syrup, Levosiz 10 Tablet, LCZ 10 Tablet, Imusun 10mg Tablet, 1-AL 10 Tablet, Valicet 10mg Tablet

Dosing & administration

5 mg orally once daily in the evening.

Dosage form	TABLET
Renal impairment	CrCl 30-50 mL/min: 5 mg every other day; CrCl <30 mL/min or ESRD: contraindicated.
Liver impairment	No adjustment required for mild to moderate impairment; severe impairment not studied.
Pediatric use	6-11 years: 2.5 mg orally once daily in the evening; ≥12 years: 5 mg orally once daily.
Geriatric use	No specific adjustment; use with caution due to potential increased sensitivity and renal impairment.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for XYZAL (XYZAL).

Breastfeeding	Excreted in human breast milk; unknown M/P ratio. Caution in nursing mothers; consider developmental risks vs benefits.
Teratogenic Risk	FDA Pregnancy Category B. Animal studies show no fetal harm; no adequate human studies in first trimester. Risk cannot be ruled out; use only if clearly needed.
Fetal Monitoring	Monitor for maternal sedation and dizziness; fetal heart rate monitoring if used near term.

Warnings & precautions

■ FDA Black Box Warning

None.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to levocetirizine, cetirizine, or any component of the formulation","End-stage renal disease (CrCl < 10 mL/min) requiring dialysis"]

Clinical Precautions

Precautions

["Use with caution in patients with renal impairment (dose adjustment required based on creatinine clearance)","May cause somnolence; avoid activities requiring mental alertness","Caution in elderly patients due to potential increased sensitivity","Avoid concurrent use with alcohol or other CNS depressants"]

Clinical Tips & Counseling

Drug interactions

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XYZAL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for XYZAL (XYZAL).

How it works

Levocetirizine is a selective histamine H1-receptor antagonist; it inhibits the histamine-mediated responses in allergic conditions.

What the body does with it

Metabolism	Approximately 86% excreted unchanged in urine; minor hepatic metabolism (oxidative O-dealkylation) via CYP3A4.
Excretion	Approximately 84% of a dose is excreted renally as unchanged drug; 12% in feces via biliary elimination.
Half-life	Terminal elimination half-life is approximately 7 hours in healthy adults; prolonged to 8–11 hours in elderly and in renal impairment.
Protein binding	Approximately 95–96% bound primarily to human serum albumin.
Volume of Distribution	0.3–0.4 L/kg, indicating distribution primarily in extracellular fluid.
Bioavailability	Oral bioavailability is approximately 80–90%.
Onset of Action	Oral: 1 hour (antihistamine effect); intranasal: 15 minutes.
Duration of Action	Approximately 24 hours; clinical effect may persist longer due to high receptor affinity.

Classification & Brands

Action Class	H1 Antihistaminics (second Generation)
Brand Substitutes	Lecope Tablet, LCZ Tablet, 1-AL Tablet, Hatric Tablet, Levocet Tablet, Vocetin 2.5mg Syrup, Grilcet 2.5mg Syrup, Zucet Syrup, 1-AL Syrup, Belrin-LZ Syrup, Levosiz 10 Tablet, LCZ 10 Tablet, Imusun 10mg Tablet, 1-AL 10 Tablet, Valicet 10mg Tablet

Dosing & administration

5 mg orally once daily in the evening.

Dosage form	TABLET
Renal impairment	CrCl 30-50 mL/min: 5 mg every other day; CrCl <30 mL/min or ESRD: contraindicated.
Liver impairment	No adjustment required for mild to moderate impairment; severe impairment not studied.
Pediatric use	6-11 years: 2.5 mg orally once daily in the evening; ≥12 years: 5 mg orally once daily.
Geriatric use	No specific adjustment; use with caution due to potential increased sensitivity and renal impairment.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for XYZAL (XYZAL).

Breastfeeding	Excreted in human breast milk; unknown M/P ratio. Caution in nursing mothers; consider developmental risks vs benefits.
Teratogenic Risk	FDA Pregnancy Category B. Animal studies show no fetal harm; no adequate human studies in first trimester. Risk cannot be ruled out; use only if clearly needed.
Fetal Monitoring	Monitor for maternal sedation and dizziness; fetal heart rate monitoring if used near term.

Warnings & precautions

■ FDA Black Box Warning

None.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to levocetirizine, cetirizine, or any component of the formulation","End-stage renal disease (CrCl < 10 mL/min) requiring dialysis"]