Lumiracoxib is a selective cyclooxygenase (COX)-2 inhibitor that possesses a carboxylic acid group that makes it weakly acidic. It has good oral bioavailability; maximum plasma concentrations are reached two hours after oral administration. Lumiracoxib has been found to be effective at doses of 100 - 400 mg once a day for chronic pain and 400 mg/day for acute pain. In comparison to NSAIDs (nonsteroidal anti-inflammatory drugs), patients taking lumiracoxib experience significantly fewer adverse events and greater tolerability[3]. In single- and multiple-dose well designed trials in patients with acute pain associated with primary dysmenorrhoea, dental or orthopaedic surgery or tension-type headache, lumiracoxib 100 - 800 mg once daily was more effective in relieving acute pain than placebo or controlled-release oxycodone 20 mg, and was at least as effective as selective COX-2 inhibitors or nonselective NSAIDs[4]. COX-2 selectivity of lumiracoxib is associated with a reduced incidence of gastroduodenal erosions compared with naproxen and a lack of effect on both small and large bowel permeability[5].
Lumiracoxib/罗美昔布 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Rats
Thermal hyperalgesia model
Oral
0, 1, 3, 10, 30 mg/kg
Single dose, lasting 10 hours (experiment I) or 24 hours (experiment II)
To evaluate the analgesic effects of Lumiracoxib and establish a pharmacokinetic/pharmacodynamic model. Results showed that Lumiracoxib significantly reversed carrageenan-induced hyperalgesia at doses of 10 and 30 mg/kg.
Br J Pharmacol. 2010 Jan;159(1):176-87
Mice
Chronic oral corticosterone-induced anxiety-like behavior model
Intraperitoneal injection
5 mg/kg
Acute: single dose; Repeated: once daily for 13 days
To investigate the effects of Lumiracoxib on chronic corticosterone-induced anxiety-like behavior and amygdala glutamatergic signaling. Results showed that both acute and repeated administration of Lumiracoxib reversed chronic corticosterone-induced anxiety-like behavior and normalized spontaneous excitatory glutamatergic currents in anterior basolateral amygdala neurons.
Neurobiol Stress. 2019 Aug 10;11:100190
Rats
5-day short-term tolerability model
Oral
2 mg/kg
Once daily for 4 consecutive days
Lumiracoxib substantially prevented roflumilast-mediated loss, spleen weight loss, leukocytosis, blood neutrophilia, and induction of serum CINC-1.
搜索
