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Zyrtec (Cetirizine)

Cetirizine hydrochloride, an antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria. The structural similarity of cetirizine to hydroxyzine, and its derivation from piperazine, attribute similar adverse reactions and properties to other piperazine derivatives.

Formerly prescription-only in the US and Canada, cetirizine is now available over the counter in both countries as Zyrtec and Reactine respectively. Zyrtec was the top new non-food product of 2008 in the US, generating sales of $315.9 million. It is also available as a generic. In Australia Zyrtec is available over the counter in pharmacies and in the UK cetirizine can be sold in limited quantities off-the-shelf in any outlet and is often available in supermarkets.

Pharmacology

Cetirizine crosses the blood-brain barrier only slightly, eliminating the sedative side-effect common with older antihistamines; however it still causes mild drowsiness. It has also been shown to inhibit eosinophil chemotaxis and LTB4 release. At a dosage of 20 mg, Boone et al. found that it inhibited the expression of VCAM-1 in patients with atopic dermatitis.

Administration method and metabolisation

Chewable, non-chewable, and syrup forms of cetirizine are similarly absorbed rapidly and effectively, with absorbed food minutely affecting the absorption rate which yields a peak serum level one hour after administration; in a study of healthy volunteers prescribed 10 mg tablets, once daily for 10 days, a mean peak serum level of 311 ng/mL was observed. The metabolic effects of cetirizine are long acting; remaining in the system for a maximum of 21 hours before being excreted, the average elimination half-life is 8 hours. 70% of the drug is excreted or eliminated by kidney function within 72 hours, and 10% is removed through urine or excrement; of which half is observed as unchanged cetirizine compound. Like many other antihistamine medications, cetirizine is commonly prescribed in combination with pseudoephedrine hydrochloride, a decongestant. These combinations are marketed using the same brand name as the cetirizine with a “-D” suffix (Zyrtec-D, Virlix-D, etc.)

Additionally, cetirizine HCl not sold in combination with pseudoephedrine, is commonly known and marketed in the United States under the brand name, “Zyrtec.” Formerly only available by a prescription, both Zyrtec and Zyrtec-D are currently available over the counter in the United States. In the Philippines, a leading cetirizine is Aforvir.

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