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Ethnopharmacological Relevance: Mexican people employed infusion of leaves of Choisya ternata Kunth for their antispasmodic and "simulative properties"., Aim of the Study: In the present study the detailed GC and GC-MS analyses of the essential oil of Choisya ternata Kunth (Rutaceae) were performed. The presence of a minor constituent isopropyl N-methylanthranilate (1) was revealed among other identified volatiles. A synthesis of 1 was undertaken in order to corroborate this find and obtain gram quantities that would allow the testing of its biological activity (peripheral and central antinociceptive activity)., Materials and Methods: The oils were investigated by GC and GC-MS. Synthesized compounds were spectrally characterized (UV-Vis, IR, 1D and 2D NMR, MS). The obtained synthetic samples of compounds were assayed for peripheral and central antinociceptive activity in two models (effects on acetic acid induced writhing in mice and the hot plate test for nociception)., Results: Detailed GC and GC-MS analyses of the essential oil of Choisya ternata Kunth (Rutaceae) among 157 other identified volatiles revealed the presence of a minor constituent isopropyl N-methylanthranilate (1). Compound 1, named ternanthranin, is therefore detected as a natural product for the first time with a very restricted occurrence (samples of several citrus oils were screened for the presence of 1). The antinociceptive activities were assayed for ternanthranin, the two other synthetic analogs, methyl and propyl N-methylanthranilate, as well as the essential oil and the crude ethanol extract of the leaves. The results clearly demonstrate a very high (even significant at 0.3 mg/kg) dose dependent activity for the anthranilates (and the extracts). Isopropyl N-methylanthranilate showed the highest, while methyl N-methylanthranilate showed the lowest activity (with the methyl ester at 3 mg/kg still better than acetylsalicylic acid, at 200 mg/kg, in the first, or comparable with morphine, at 5mg/kg, in the second test)., Conclusion: This study once again revealed that detailed investigations of plant species with ethnopharmacologically documented activity may yield new natural compounds-a new alkaloid (ternanthranin), a volatile simple anthranilate that can be considered responsible for the antinociceptive activity of the crude plant extracts., (Copyright © 2011 Elsevier Ireland Ltd. All rights reserved.)

Aim: To assess the welfare impact of lameness on dairy cattle in New Zealand by measuring the duration of allodynia (decreased nociceptive threshold) and increased locomotion score, and to evaluate the influence of treatment on that duration., Methods: After lame cows were treated using corrective paring by a veterinarian, they were allocated to one of six treatment groups. If the veterinarian determined that additional elevation of the lesion was not required the cow was randomly allocated to receive one of four treatments, viz 2 mg/kg tolfenamic acid, a plastic shoe to elevate the lesion, both treatments, or no further treatment. Cows that required additional elevation were treated using a plastic shoe and then randomly allocated to two separate treatment groups, either 2 mg/kg tolfenamic acid or no further treatment. Assessments of locomotion score (based on posture and gait) and mechanical nociceptive threshold (using a pneumatically actuated blunt pin) were made prior to treatment, and 3, 8, 28 and 100 days later., Results: Data were collected from 149 lame cows from nine dairy farms. There were significant improvements in mean locomotion score and nociceptive threshold in all treatment groups. At all time-points after treatment, locomotion score and nociceptive threshold were significantly improved when compared with the previous time-point. Thus, in these cows, the deleterious effects of lameness persisted for longer than 28 days, despite treatment, as the mean locomotion scores and nociceptive threshold on Day 100 were better than those on Day 28. No significant long-term benefit of using tolfenamic acid at the time of treatment was observed on either locomotion score or nociceptive threshold, nor was there any benefit in using a plastic shoe in cases where it had been determined that such treatment was not necessary., Conclusions: This study demonstrated that the welfare impact of lameness on dairy cattle in New Zealand is of long duration even when treated effectively. In contrast to previous studies, no significant long-term benefit of using non-steroidal anti-inflammatory drugs (NSAID) at the time of treatment was observed, probably because unlike those previous studies the nociceptive threshold improved in the cattle which did not receive an NSAID, perhaps because treated cattle were kept on pasture rather than housed., Clinical Relevance: The long duration of increased allodynia after treatment demonstrates that prevention of lameness rather than therapeutic treatment is the key to reducing its impact on the welfare of dairy cows.

To test the hypothesis that the postoperative abdominal pain of tubal occlusion is mediated by prostaglandins, the effects of meclofenamate, a potent inhibitor of cyclooxygenase, on postoperative analgesia and incidence of abdominal pain were compared with those of acetaminophen, a weak inhibitor of prostaglandin activity. One hundred patients undergoing tubal occlusion under local anesthesia were studied. The patients were randomly divided into four equal groups: control; acetaminophen, 1300 mg; meclofenamate, 100 mg; meclofenamate, 200 mg. The fallopian tubes were occluded by electrocautery in 47 patients and by application of Falope rings in 53 patients. Both acetaminophen and meclofenamate provided substantial analgesia for 4 hours after the operation (p less than 0.05). Meclofenamate reduced the incidence of abdominal pain by one half (p less than 0.02), but acetaminophen did not. These results suggest that a portion of pain relief achieved by meclofenamate may be due to suppression of myosalpingian and/or myometrial contractions, a process mediated by prostaglandins.

Three hundred and twelve patients suffering from painful conditions were admitted to a multicentre, double-blind controlled trial, conducted in general practice in which five analgesics--floctafenine (Idarac), paracetamol, aspirin, dihydrocodeine and pentazocine--were compared. Overall ratings of analgesic effect placed floctafenine first in rank order. Floctafenine was statistically significantly superior in effect to pentazocine but not to the other three agents as far as doctor ratings were concerned; and superior to both pentazocine and dihydrocodeine in the opinion of patients. Fewer patients experienced side-effects on floctafenine than on the other four analgesics and this difference between floctafenine and pentazocine, and floctafenine and dihydrocodeine was statistically significant.

The efficacy of an anti-prostaglandin, tolfenamic acid (T.A.), in the prevention of side-effects after insertion of a copper-T200 intrauterine contraceptive device (I.U.D.) was evaluated in a double-blind trial in 160 women. T.A. relieved pain and reduced bleeding after insertion and during three subsequent menstruations without serious side-effects. A scoring system for the assessment of I.U.D. side-effects showed that the acceptability of I.U.D. was significantly better in women treated with T.A. than in those given placebo.

A double-blind study was carried out in 42 patients suffering from acute rheumatic pain to compare the analgesic effectiveness and tolerance of tiapride with that of glafenine, a widely used analgesic in Europe. Patients were allocated at random to receive either 100 mg tiapride or 200 mg glafenine 3-times daily over a period of 14 days. Pain intensity was rated daily by the patients using a visual analogue scale and an overall assessment of response to treatment was made by both patients and physician at the end of the study. The results showed that, whilst both treatments resulted in a marked reduction in mean pain scores, pain disappeared completely in 16 (76%) of the 21 patients treated with tiapride compared with 9 (43%) of the 21 receiving glafenine. There was also a significant difference in favour of tiapride in the physician's overall assessment of response which was considered as excellent in 71% of the patients on tiapride compared with 31% receiving glafenine. Both treatments were well tolerated and few side-effects were reported. Drowsiness occurred in 6 patients on tiapride but this was only mild in 5 and moderate in the other patient.