lornoxicam and nimesulide

Efficacy of different nonsteroid anti-inflammatory drugs (voltaren (diclofenac), movalis (meloxicam), nimesil (nimesulide) and xefocam (lornoxicam) in stopping the pain syndrome and normalization of motor activity was assessed in 140 patients with dorsalgia using the Visual Analogous Scale and the modified Waddel scale. Moreover, we suggest a method for calculating a treatment efficacy coefficient. The most effective drug in the treatment of back pain was xefocam (lornoxicam). Nimesil (nimesulide) was somewhat less effective. Other drugs did not reveal any significant effect. Xefocam was well-tolerated: adverse effects were rare compared to other drugs used in the study.

Topics: Adult; Aged; Anti-Inflammatory Agents, Non-Steroidal; Back Pain; Dose-Response Relationship, Drug; Drug Administration Schedule; Female; Humans; Injections, Intramuscular; Male; Middle Aged; Outpatients; Pain Measurement; Piroxicam; Sulfonamides; Treatment Outcome

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Cyclooxygenase 1; Cyclooxygenase 2; Disease Models, Animal; Female; Gastric Mucosa; Ligation; Male; Piroxicam; Rats; Stomach Ulcer; Sulfonamides

Hypochlorous acid (HOCl) is an oxygen-derived species involved in physiological processes related to the defence of the organism that may cause adverse effects when its production is insufficiently controlled. In order to examine its reactivity with potential scavenging molecules from the non steroidal anti-inflammatory drugs (NSAIDs) family, a competition assay based on para-aminobenzoic acid (PABA) chlorination was developed. The original optimised in vitro fluorimetric procedure offered the possibility to determine rate constants (ks) for the reaction with HOCl in physiologically relevant conditions. The specificity of the system was improved by a liquid chromatography (LC) which allows the separation of the drugs and their oxidation products. After determination of the rate constant for PABA chlorination by HOCl (mean +/- SD in M(-1) s(-1): 4.3 +/- 0.3 x 10(3)), the applied mathematical model for a chemical competition permits to obtain linear curves from competition studies between several NSAIDs and PABA. Their slopes provided the following rate constants for the different studied drugs: tenoxicam: 4.0 +/- 0.7 x 10(3), piroxicam: 3.6 +/- 0.7 x 10(3), lornoxicam: 4.3 +/- 0.7 x 10(3), meloxicam: 1.7 +/- 0.3 x 10(4), nimesulide: 2.3 +/- 0.6 x 10(2). Meloxicam therefore reacted significantly faster than the other oxicams and nimesulide, which is the weakest scavenger of the studied series. The identification of some of the oxidation products by NMR or MS permitted to explore the reaction mechanism and to examine some aspects of the structure/activity relationships for the molecules of the same chemical family.

Topics: 4-Aminobenzoic Acid; Anti-Inflammatory Agents, Non-Steroidal; Binding, Competitive; Hypochlorous Acid; Kinetics; Linear Models; Meloxicam; Molecular Structure; Oxidation-Reduction; Piroxicam; Sulfonamides; Thiazines; Thiazoles