Antihistamines for urticaria

The use of classical antihistamines is limited by their side effects, including sedation, anticholinergic properties and
paradoxical excitation in children. There may be carry-over effects of sedation in the morning and patients should be
warned of this. Hydroxyzine is the most potent of the classical antihistamines. Twenty fi ve
mg of hydroxyzine is equivalent to 10 mg of cetirizine.
The second generation of potent, specifi c, low-sedation H1 antihistamines
is now the treatment of choice [2]. Their main advantage
is low sedation at doses recommended by the manufacturer
and minimal anticholinergic side effects, although an occasional
individual may develop sedation with any of them. They are at
least as effective as hydroxyzine and generally as effective as each
other. There is no clear evidence that tolerance occurs after continued
use. Very rarely, antihistamines appear to make urticaria
worse. This has been reported anecdotally with cetirizine but clinical
experience suggests that most or all antihistamines may be
implicated in those who are affected.
Acrivastine (adult dose 8 mg three times a day) has a rapid
onset and duration of action and is excreted predominantly in the
urine.
Cetirizine (adult dose 10 mg/day) is poorly metabolized in the
liver and is excreted, predominantly in the urine, unchanged. It is
also rapidly absorbed. It is more sedative than placebo in some
studies and is best taken at night. Cetirizine reduces dermal eosinophil
cell accumulation in vitro and in vivo. However, the clinical
importance of this effect in the treatment of delayed pressure
urticaria and urticarial vasculitis, where eosinophils may be an
important component of the infl ammatory cell infi ltrate, is uncertain.
There are no studies to show that its active enantiomer,
levocetirizine, has an advantage in the treatment of chronic
urticaria.
Fexofenadine is the metabolite of terfenadine but appears to be
devoid of cardiotoxicity at clinically relevant doses and has
the widest therapeutic window of the second generation
antihistamines.
Loratadine (adult dose 10 mg daily) is a derivative of azatadine.
Although loratadine is also metabolized in the liver by cytochrome
P450 to some extent, so far no clinically proven, relevant drug
interactions have been reported. It is not yet clear whether its
metabolite, desloratadine, offers a clinical advantage in urticaria
or any subsets of it.
Low-sedation antihistamines are used to reduce urticarial activity,
with minimal side effects. Individual response is variable, but
adequate dose and timing in relationship to maximal urticarial
activity is important. Alternative low-sedation antihistamines can
be tried, and sedating ones added at night. A combination of an
H1 antihistamine with an H2 antagonist may be more effective
than H1 antihistamines alone in some patients. Use of ranitidine
(adults 150 mg twice a day) is preferable to cimetidine, which has
more antiandrogenic side effects and potential drug interactions.