Levocetirizine Dihydrochloride (levocetirizine dihydrochloride)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Levocetirizine dihydrochloride, the R-enantiomer of cetirizine, is a second generation antihistamine.
Levocetirizine is the active R-enantiomer of cetirizine. The drug exhibits selective antagonism of histamine H1-receptors. In in vitro binding studies, levocetirizine demonstrated a 2-fold higher affinity for H1-receptors than cetirizine; the clinical relevance of this finding is unknown.
Levocetirizine is rapidly and extensively absorbed following oral administration; in adults, peak plasma concentrations are attained 0.9 hour following administration of the tablets. Food had no effect on the AUC of levocetirizine following oral administration as tablets; however, time to peak plasma concentration was delayed by about 1.25 hours and peak plasma concentration was decreased by approximately 36% following administration of levocetirizine dihydrochloride tablets with a high fat meal.
The manufacturer states that aAA 5-mg dose of levocetirizine dihydrochloride administered as the commercially available oral solution containing 2.5 mg/5 mL is bioequivalent to a 5-mg tablet. Following administration of levocetirizine as an oral solution in adults, mean peak plasma concentrations were achieved in approximately 0.5 hours.
Following administration of a single 2.5 or 5-mg dose of levocetirizine dihydrochloride, antihistaminic effects of the drug occur within 1 hour and persist for at least 24 hours. Symptomatic improvement is observed as early as one day after initiation of therapy for allergic rhinitis.
Levocetirizine is metabolized to a limited extent (less than 14% of the dose) by aromatic oxidation, N-dealkylation, O-dealkylation, and taurine conjugation. The plasma half-life of levocetirizine in adults is approximately 8-9 hours. Approximately 85.4% of the dose is excreted in urine (via glomerular filtration and active tubular secretion), and 12.9% is excreted in feces.
USES: Levocetirizine is an antihistamine used to relieve allergy symptoms such as watery eyes, runny nose, itching eyes/nose, and sneezing. It is also used to relieve itching and hives. It works by blocking a certain natural substance (histamine) that your body makes during an allergic reaction.
Levocetirizine does not prevent hives or prevent/treat a serious allergic reaction (such as anaphylaxis). If your doctor has prescribed epinephrine to treat allergic reactions, always carry your epinephrine injector with you. Do not use levocetirizine in place of your epinephrine.
Generic name: levocetirizine dihydrochloride
Pronunciation: (lee-voh-seh-TEER-ah-zeen)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Levocetirizine Dihydrochloride
Indications
The following indications are listed for Levocetirizine Dihydrochloride:
- Allergic Rhinitis
- Chronic Idiopathic Urticaria
Dosing
The manufacturer states that a 5-mg dose of levocetirizine dihydrochloride administered as the commercially available oral solution containing 2.5 mg/5 mL is bioequivalent to a 5-mg tablet.
Levocetirizine dihydrochloride is administered orally once daily in the evening without regard to meals. The drug is commercially available as tablets or an oral solution.
Levocetirizine tablets are scored and can be broken in half (each half providing a dose of 2.5 mg).
Levocetirizine dihydrochloride tablets should be stored at 20-25degreesC. Levocetirizine dihydrochloride oral solution should be stored at 20-25degreesC (excursions permitted to 15-30degreesC).
Levocetirizine is also commercially available in various over-the-counter (OTC) preparations. See the FDA Orange Book and the manufacturer's drug facts for information.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
No formal drug interaction studies have been performed with levocetirizine to date; studies have been performed with racemic cetirizine.
Levocetirizine does not inhibit cytochrome P-450 (CYP) isoenzymes 1A2, 2C9, 2C19, 2A1, 2D6, 2E1, or 3A4. The drug does not induce uridine diphosphate-glucuronosyltransferase (UGT) 1A or CYP isoenzymes 1A2, 2C9, or 3A4. The manufacturer states that levocetirizine is unlikely to produce or be subject to pharmacokinetic interactions associated with metabolic enzyme systems.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity (e.g., urticaria, anaphylaxis) to levocetirizine or any ingredient in the formulation, or to cetirizine.
*Adults and pediatric patients 12 years of age and older with end-stage renal disease (creatinine clearance less than 10 mL/minute) or undergoing hemodialysis.
*Pediatric patients 6 months to 11 years of age with renal impairment.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects reported in 2% or more of patients 12 years of age and older receiving levocetirizine dihydrochloride (2.5 or 5 mg daily) in clinical trials and occurring more frequently than placebo include somnolence, nasopharyngitis, fatigue, dry mouth, and pharyngitis.
Adverse effects reported in 2% or more of pediatric patients 6-12 years of age receiving levocetirizine dihydrochloride (5 mg daily) in clinical trials and occurring more frequently than placebo include pyrexia, cough, somnolence, and epistaxis.
Adverse effects reported in 2% or more of pediatric patients 1-5 years of age receiving levocetirizine dihydrochloride (1.25 mg twice daily) in a safety trial and occurring more frequently than with placebo include pyrexia, diarrhea, vomiting, and otitis media.
Adverse effects reported in 3% or more of pediatric patients 6-11 months of age receiving levocetirizine dihydrochloride (1.25 mg once daily) in a safety trial and occurring more frequently than placebo include diarrhea and constipation.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety of levocetirizine has not been established in children younger than 6 months of age.
Efficacy of levocetirizine dihydrochloride 1.25 mg once daily (in pediatric patients 6 months to 5 years of age) and levocetirizine dihydrochloride 2.5 mg once daily (in pediatric patients 6-11 years of age) for the management of allergic rhinitis is based on extrapolation of the demonstrated efficacy of the 5-mg daily dosage in pediatric patients 12 years of age and older and on pharmacokinetic comparisons in adults and children.
Efficacy of levocetirizine dihydrochloride 1.25 mg once daily (in pediatric patients 6 months to 5 years of age), levocetirizine dihydrochloride 2.5 mg once daily (in pediatric patients 6-11 years of age), and levocetirizine dihydrochloride 5 mg once daily (in pediatric patients 12-17 years of age) for the management of chronic idiopathic urticaria is based on extrapolation of the demonstrated efficacy of the 5-mg daily dosage in adults and/or on pharmacokinetic comparisons in adults and children.
A cross-study comparison of pharmacokinetic data indicate that systemic exposure (i.e., AUC) to levocetirizine was approximately 2-fold higher in pediatric patients 6-11 years of age with seasonal allergic rhinitis receiving a single 5-mg dose compared with that reported in adults receiving the same dose. Data from a retrospective population pharmacokinetic analysis indicate that administration of levocetirizine dihydrochloride 1.25 mg once daily in children 6 months to 5 years of age results in plasma levocetirizine concentrations that are comparable to those observed in adults receiving the drug at a dosage of 5 mg once daily.
Available data are insufficient to establish a drug-associated risk of miscarriage, birth defects, or adverse maternal or fetal outcomes with levocetirizine use during pregnancy.
Animal reproductive studies have shown no evidence of fetal harm with administration of levocetirizine to pregnant rats and rabbits during the period of organogenesis at doses up to 390 times and 470 times, respectively, the maximum recommended human dose (MRHD). In mice who received cetirizine during late gestation and the lactation period, cetirizine administration at a dose 25 times the MRHD had no effects on pup development; however, lower pup weight was observed during lactation when a dose 95 times the MRHD was administered.
Levocetirizine is expected to be distributed into human milk (since cetirizine is distributed into milk). Consider the developmental and health benefits of breast-feeding along with the mother's clinical need for levocetirizine and any potential adverse effects on the breast-fed child from levocetirizine or from the underlying maternal condition.
Dosage of levocetirizine should be selected with caution in geriatric patients (usually starting at the low end of the dosage range) because of the greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy.
Experience from clinical trials in patients 65 years of age and older is insufficient to determine whether geriatric patients respond differently than younger adults. Other reported clinical experience has not identified differences in responses between geriatric and younger patients. Dosage of levocetirizine generally should be selected with caution in geriatric patients because of the greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy. Periodic monitoring of renal function may be useful.
ICD codes
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Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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