Product Information
Registration Status: ActiveXYZAL FILM-COATED TABLET 5 MG is approved to be sold in Singapore with effective from 2020-10-14. It is marketed by GLAXOSMITHKLINE PTE LTD, with the registration number of SIN16028P.
This product contains Levocetirizine 5 mg in the form of TABLET, FILM COATED. It is approved for ORAL use.
This product is manufactured by UCB Farchim SA in SWITZERLAND, andAesica Pharmaceuticals S.r.l. (Primary and Secondary Packager) in ITALY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
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. It does not prevent the actual release of histamine from mast cells. Levocetirizine was approved by the United States Food and Drug Administration on May 25, 2007 and is marketed under the brand XYZAL® by sanofi-aventis U.S. LLC.
Indication
Levocetirizine is indicated for the relief of symptoms associated with allergic rhinitis (seasonal and perennial) in adults and children 6 years of age and older.
Mechanism of Action
Levocetirizine, the active enantiomer of cetirizine, is an anti-histamine; 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.
Pharmacokinetics
- Absorption
- Levocetirizine is rapidly and extensively absorbed following oral administration. In adults, peak plasma concentrations are achieved 0.9 hour after administration of the oral tablet. The accumulation ratio following daily oral administration is 1.12 with steady state achieved after 2 days. Peak concentrations are typically 270 ng/mL and 308 ng/mL following a single and a repeated 5 mg once daily dose, respectively. Food had no effect on the extent of exposure (AUC) of the levocetirizine tablet, but Tmax was delayed by about 1.25 hours and Cmax was decreased by about 36% after administration with a high fat meal; therefore, levocetirizine can be administered with or without food.
- Distribution
- Approximately 0.4 L/kg.
- Metabolism
- Levocetirizine is poorly metabolized and mostly excreted. This is favourable as it is unlikely to be modified by drugs administered concomitantly.
- Elimination
Clearance
about 0.63 mL/kg/min (oral total body clearance).
Active Ingredient/Synonyms
2-(2-{4-[(R)-(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid | Levocetirizine |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.