COX-1/COX-2 inhibitor
CAS：70374-39-9
分子式：C13H10ClN3O4S2
分子量：371.82
纯度：98%
存储：Store at -20°C

Background:

IC50: A potent COX-1 and COX-2 inhibitor with IC50 values of 5 nM and 8 nM, respectively.

Lornoxicam, a new nonsteroidal anti-inflammatory drug (NSAID) belonging to the oxicam class. By intensively inhibit COX-1 and COX-2, this drug, both in oral and parenteral formulations, shows remarkable analgesic, anti-inflammatory and antipyretic properties. [1]

In vitro: Studies on intact human cells showed that lornoxicam intensively inhibit COX-1 and COX-2 with the lowest IC50 among a large panel of NSAIDs tested. Similar findings were obtained in the whole blood for COX-1/-2. In addition lornoxicam suppressed NO formation in a dose-dependently manner with an IC50 of 65 μM. [2]

In vivo: In vivo studies found that Lornoxicam was as effective as comparative NSAIDs and that 8 mg Lornoxicam was more effective than 10 mg morphine as a pain-reliever after oral surgery. Orally administration of lornoxicam at 16-24 mg daily was more effective than tramadol at 300 mg daily in pain-alleviating after knee surgery. Compared to naproxen, Lornoxicam showed higher therapeutic potency and lower gastrointestinal toxicity. This was probably due to the short half-life of lornoxicam as compared to the other oxicams. [3]

Clinical trials: A clinical study was performed to assess the efficacy and tolerability of intravenous lornoxicam in Indian patients with postoperative pain or other acute painful traumatic conditions. Patients were treated for 3 days with intravenous lornoxicam at a dosage of 8 mg twice or three times daily. Study demonstrated that intravenous lornoxicam is a powerful NSAID with an optimal efficacy/toxicity ratio and thus could be a reasonable therapeutic option for patients with painful traumatic conditions requiring parenteral NSAIDs. [4]

参考文献:
[1]Balfour JA, Fitton A and Barradell LB.  Lornoxicam, a review of its pharmacology and therapeutic potential in the management of painful and inflammatory conditions. Drugs. 1996 Apr; 51(4): 639-57.
[2]Berg J, Fellier H, Christoph T, Grarup J and Stimmeder D.  The analgesic NSAID lornoxicam inhibits cyclooxygenase (COX)-1/-2, inducible nitric oxide synthase (iNOS), and the formation of interleukin (IL)-6 in vitro. Inflamm Res. 1999 Jul; 48(7): 369-79.
[3]Radhofer-Welte S and Rabasseda X.  Lornoxicam, a new potent NSAID with an improved tolerability profile. Drugs Today (Barc). 2000 Jan; 36(1): 55-76.
[4]Sharma A, Pingle A, and Baliga VP.  Lornoxicam efficacy in acute pain (LEAP) trial. J Indian Med Assoc. 2008 Dec; 106(12): 811-3.