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RX BIN: 015558RX PCN: HTGroup ID: DDN6600Card Holder ID: DDN6600
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2019 Price of Xyzal

$11.0430 tablets/5 mg
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Levocetirizine volume of distribution

The terminal elimination half-life was 5.7 +/- 0.2 hours, the oral clearance was 0.82 +/- 0.05 mL/min/kg, and the volume of distribution was 0.4 +/- 0.02 L/kg. Compared with predose areas, the wheals and flares produced by histamine phosphate were significantly decreased from 1 to 28 hours, inclusive (P < .05).

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What is Levocetirizine

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.

Levocetirizine 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.

Dosage forms of Levocetirizine

Xyzal5mg100 Tablet$144.00
Xyzal Oral Solution0.5mg/mL200mL Solution$75.00
Levocetirizine5mg100 Tablet$60.00

Prescription Generics


International Brands

Levocetirizine Dihydrochloride


2-(2-{4-[(R)-(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid


Camber Pharmaceuticals, Inc.

CAS number






Affected organisms

Humans and other mammals

Indication of Levocetirizine

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.

Toxicity of Levocetirizine

Uncertainty factor (UF) regarding the uncertainty associated with the toxicity of the surrogate compound.

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What is a Xyzal?

Xyzal is a drug with a pronounced antihistamine and antiallergic effect. The active component of the drug Xyzal – levocetirizine is the R-enantiomer of cetirizine. Levocetirizine competitively blocks the H1-histamine receptors, and the pharmacological activity of levocetirizine is almost 2 times higher than that of cetirizine.

Xyzal affects the histamine-dependent phase of the allergic reaction. In addition, levocetirizine reduces eosinophil migration and decreases vascular permeability. Xyzal also slightly slows down the release of cytokines and inflammatory mediators.

The drug has antipruritic and antiexudative action, facilitates the course and prevents the development of allergic reactions. Levocetirizine has almost no effect on cholinergic and serotonin receptors, and does not have a significant sedative effect.

After oral administration, levocetirizine is well absorbed in the intestinal tract. Taking the drug at the same time as eating does not change the bioavailability and rate of absorption of levocetirizine. The peak plasma concentration of the active substance is reached within 1 hour after ingestion. Equilibrium plasma concentrations are achieved on the second day of therapy with levocetirizine.

The degree of connection of levocetirizine with plasma proteins reaches 90%, oral bioavailability is 100%. Slightly metabolized in the body. Excreted mainly by the kidneys by tubular secretion and glomerular filtration. About 13% of levocetirizine is excreted by the intestines. The half-life varies from 6 to 10 hours depending on the individual characteristics of the patient. In children, the half-life of levocetirizine is shortened.

In patients with impaired renal function, an increased half-life is observed. During hemodialysis, levocetirizine is practically not excreted (during the 4-hour hemodialysis, no more than 10% of levocetirizine is excreted).