Analgesic Effects of 1st Generation Anti-histamines in Mice.

Pain is sensed, transmitted, and modified by a variety of mediators and receptors. Histamine is a well-known mediator of pain. In addition to their anti-histaminic effects, the classical, or 1st generation, anti-histamines (1st AHs) possess, to various degrees, anti-muscarinic, anti-serotonergic, anti-adrenergic, and other pharmacologic effects. Although there have been attempts to use 1st AHs as analgesics and/or analgesic adjuvants, the advent of non-steroidal anti-inflammatory drugs (NSAIDs) discouraged such trials. We previously reported that in patients with temporomandibular disorders, osteoporosis, and/or osteoarthritis, the analgesic effects of certain 1st AHs (chlorpheniramine and diphenhydramine) are superior to those of the NSAIDs flurbiprofen and indomethacin. Here, we compared analgesic effects among 1st AHs and NSAIDs against responses shown by mice to intraperitoneally injected 0.7% acetic acid. Since 1st AHs are water soluble, we selected water-soluble NSAIDs. For direct comparison, drugs were intravenously injected 30 min before the above tests. Histamine-H1-receptor-deficient (H1R-KO) mice were used for evaluating H1-receptor-independent effects. The tested 1st AHs (especially cyproheptadine) displayed or tended to display analgesic effects comparable to those of NSAIDs in normal and H1R-KO mice. Our data suggest that the anti-serotonergic and/or anti-adrenergic effects of 1st AHs make important contributions to their analgesic effects. Moreover, combination of a 1st AH with an NSAID (cyclooxygenase-1 inhibitor) produced remarkably potent analgesic effects. We propose that a 1st AH, by itself or in combination with a cyclooxygenase-1 inhibitor, should undergo testing to evaluate its usefulness in analgesia.

Examination of the relationship between masseter muscle activity during sleep and wakefulness measured by using a wearable electromyographic device.

Purpose This study aimed to measure masseter muscle activity throughout the day in outpatients suspected of having awake bruxism (AB) and/or sleep bruxism (SB) and examine the relationship between AB and SB by comparing muscle activity during daytime wakefulness and nighttime sleep.Methods Fifty outpatients with suspected SB and/or AB participated in this study. A single-channel wearable electromyogram (EMG) device was used for EMG recording. The selected EMG bursts were divided into bursts during sleep (S-bursts) and bursts during awake state (A-bursts). The number of bursts per hour, average burst duration, and ratio of burst peak value to maximum voluntary contraction were calculated for both the S- and A-bursts. These values of the S- and A-bursts were then compared, and the correlations between them were analyzed. Additionally, the ratios of phasic and tonic bursts in the S- and A-bursts were compared.Results The number of bursts per hour was significantly higher for A-bursts than for S-bursts. No significant correlation was found between the numbers of S- and A-bursts. The ratio of phasic bursts was large and that of tonic bursts was small in both the S- and A-bursts. A comparison of the S- and A-bursts showed that the S-bursts had a significantly lower ratio of phasic bursts and higher ratio of tonic bursts than the A-bursts.Conclusions The number of masseteric EMG bursts during wakefulness did not show any association with that during sleep. It became clear that sustained muscle activity was not dominant in AB.

Frequency distribution of the number and amplitude of electromyographic waveforms of the masseter muscle during sleep in patients with a clinical diagnosis of sleep bruxism.

OBJECTIVE: This study aimed to clarify frequency distribution of number and peak amplitude of electromyographic (EMG) waveforms of sleep bruxism (SB) in outpatients with clinical diagnosis of SB (probable bruxer: P-bruxer). METHODS: Subjects were 40 P-bruxers. Masseteric EMG during sleep was measured at home using a wearable EMG system. EMG waveforms with amplitude of more than two times the baseline and with duration of 0.25 s were extracted as SB bursts. Clusters of bursts, i.e. SB episodes, were also scored. RESULTS: There were large variations among the subjects in numbers of SB bursts and episodes and in burst peak amplitude. As for burst peak amplitude within a subject, a wide right-tailed frequency distribution was shown with the highest frequency at the class of 5-10% maximum voluntary contraction. CONCLUSION: The number and amplitude of SB waveforms for P-bruxers were distributed over a wide range, indicating the existence of large individual differences.

Comparison of the occurrence of sleep bruxism under accustomed conditions at home and under polysomnography conditions in a sleep laboratory.

PURPOSE: We aimed to clarify the relationship between the number of sleep bruxism (SB) bursts at home and in a laboratory equipped with polysomnography with audio-video recording (PSG-AV). We applied an identical single-channel wearable electromyography (EMG) device for both types of SB burst scorings. METHODS: The subjects were 20 healthy student volunteers (12 men and 8 women; mean age, 21.9 years) who were clinically diagnosed with bruxism based on the criteria set forth by the International Classification of Sleep Disorders (ICSD-2). We used a wearable EMG device attached to the masseteric area (the FLA-500-SD [FLA]), for scoring SB bursts at home and in the laboratory. PSG-AV was set within the laboratory environment as well. The mean interval for both sleep studies was 28.8 days. EMG bursts with amplitudes greater than twice the baseline amplitude and with durations of longer than 0.25 s were selected. EMG bursts with amplitudes ≥5% MVC (maximum voluntary contraction), ≥10% MVC, and ≥20% MVC were selected as well. A cluster of bursts was defined as an episode. RESULTS: In all the conditions for selecting EMG bursts specified above, the number of SB bursts and episodes recorded under laboratory conditions was statistically significantly smaller than that recorded at home. There were no statistically significant differences between the data obtained on the first and second recording days. CONCLUSION: The results of this study suggest that the unfamiliar environment of a sleep laboratory equipped with PSG-AV affects the emergence of SB as compared with home conditions.