Levocetirizine , an antihistamine indicated in the treatment of allergic rhinitis and chronic idiopathic urticaria.Levocetirizine (as levocetirizine dihydrochloride) is a third generation non-sedative antihistamine, developed from the second generation antihistamine cetirizine. Chemically, levocetirizine is the active enantiomer of cetirizine.
Chemically,
2-[2-[4-[(R)-(4-chlorophenyl)-phenyl-methyl] piperazin-1-yl]ethoxy]acetic acid
Biochemical basis of levocetirizine
Like cetirizine, levocetirizine inhibits eotaxin-induced eosinophil TEM through both dermal and lung microvascular endothelial cells, suggesting that it has potential anti-inflammatory effects. This anti-inflammatory effect is underlined by the ability of levocetirizine's ability to inhibit eosinophil chemotaxis. It has a very high affinity for the H1 receptor. The carboxylic function of cetirizine and levocetirizine is important in this regard.
Uses to treat allergy
In one study of 470 patients, individual symptom severity scores for sneezing, rhinorrhea, itchy nose, and itchy eyes were significantly decreased for all doses of levocetirizine, with 5mg once daily possessing an optimal benefit/risk ratio in the treatment of seasonal allergic rhinitis. Both levocetirizine and cetirizine significantly attenuated the histamine-induced increase in nasal airway resistance by nearly 50%. Both cetirizine and levocetirizine caused a marked inhibition of histamine-induced wheal and flare, while levocetirizine 2.5mg has comparable anti-histaminic activity to cetirizine 5mg. Levocetirizine relieves symptoms associated with house-dust mite allergy.
Several large European uncontrolled studies have also suggested that levocetirizine is an effective agent. In one study, oral levocetirizine 5mg once daily for 32 days was reported effective in the treatment of patients with seasonal and perennial allergic rhinitis with or without concurrent asthma (n=14,319). Alleviation or improvement of symptoms (e.g., rhinorrhea, sneezing, conjunctivitis, asthmatic symptoms) was observed in over 80% of patients at the end of treatment. Global assessments also indicated very good or good efficacy in over 80%. Adverse effects were minimal.
Of note to dermatologists, a similar study showed that levocetirizine decreased the severity of eczema. In a large uncontrolled study, oral levocetirizine 5mg once daily for 32 days was reported effective in the treatment of patients with chronic urticaria (n=2707) or other dermatologic conditions (i.e., atopic dermatitis) (n=961). Collectively, alleviation or improvement of symptoms (e.g., pruritus, wheal/flare, eczema) occurred in at least 80% of patients at the end of treatment. Global assessments also indicated very good or good efficacy in over 80%. Adverse effects were minimal.
Levocetirizine compared to other agents
Levocetirizine's potency compares favorably with other agents. It was more potent at suppressing weal and flare than ebastine, fexofenadine, mizolastine, and loratadine. Levocetirizine (5 mg) is a potent inhibitor of the effects of histamine in human skin with an efficacy that exceeded that of loratadine (10 mg) when single doses of the drugs were administered 4 hours before the test.
Side Effects, Absorption and Pharmacokinetics
The side effect profile of levocetirizine is mild. Levocetirizine does not produce any deleterious effect on cognitive and psychometric functions compared with placebo in healthy male volunteers. Whereas promethazine affects cognitive function and psychomotor performance, levocetirizine does not. Skin rash (rarely), headache, and fatigue have been reported as side effects.
Marketed Brands:
Laveta(Alembic Ltd.)
2007-01-07 00:52:52
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answer #2
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answered by Anonymous
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