2-(2-{4-[(R)-(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid
1. 成人及十二歲以上青少年:建議每日劑量為5mg。
2. 老年患者:具有中度到嚴重腎功能障礙的老年患者,需調整其劑量。
3. 六歲至十二歲孩童:建議每日劑量為5mg。
4. 六歲以下孩童尚不建議使用。
Absorption
Rapidly and extensively absorbed. T max is 0.9 h. C max is 270 and 308 ng/mL after single and repeated once-daily dosing, respectively. Steady state achieved after 2 days. Food delayed T max by approximately 1.25 h and decreased C max by approximately 36%.
Distribution
Plasma protein binding is approximately 92%. Vd is approximately 0.4 L/kg.
Metabolism
Metabolism is less than 14% and by aromatic oxidation, N- and O-dealkylation, and taurine conjugation.
Elimination
The half-life is about 8 to 9 h. Elimination is 85.4% and 12.9% via urine and feces, respectively. Excreted both by glomerular filtration and active tubular secretion.
No formal in vivo drug-drug interaction studies have been performed with levocetirizine. Drug interaction studies have been performed with racemic cetirizine.
Alcohol, CNS depressants
Additive CNS depressant effects; concurrent use should be avoided.
Food
Food had no effect on the extent of levocetirizine exposure; however, the half-life was delayed about 1.25 hours and the C max was decreased about 36% after administration with a high-fat meal. Levocetirizine may be taken without regard to food.
Ritonavir
Cetirizine AUC and half-life may be increased, while Cl may be decreased. The risk of adverse reactions may be increased.
Theophylline
May decrease cetirizine Cl.
2. 嚴重腎功能障礙者(creatinine clearance < 10 ml/min)禁用。
對於levocetirizine過量並無特殊的解毒劑。建議以徵狀治療。以可考慮洗胃(服用短期內)。血液透析對levocetirizine的排除無效。



