[Metabolism of 3-cyanomethyl-4-methyl-DCK, a new anti-HIV candidate, in human intestinal microsomes].

The biotransformation, CYP reaction phenotyping, the impact of CYP inhibitors and enzyme kinetics of 3-cyanomethyl-4-methyl-DCK (CMDCK), a new anti-HIV preclinical candidate belonging to DCK analogs, were investigated in human intestinal microsomes and recombinant cytochrome P450 (CYP) enzymes. CMDCK (4 micromol L(-1)) was incubated with a panel of rCYP enzymes (CYP1A2, 2C9, 2C19, 2D6 and 3A4) in vitro. The remaining parent drug in incubates was quantitatively analyzed by a LC-MS method. CYP3A4 was identified as the principal CYP isoenzyme responsible for its metabolism in intestinal microsomes. The major metabolic pathway of CMDCK was oxidation and a number of oxidative metabolites were screened with LC-MS. The Km, Vmax, CLint and T1/2 of CMDCK obtained from human intestinal microsome were 45.6 micromol L(-1), 0.33 micromol L(-1) min(-1), 12.1 mL min(-1) kg(-1) and 25.7 min, respectively. Intestinal clearance of CMDCK was estimated from in vitro data to be 3.3 mL min(-1) kg(-1), and was almost equal to the intestinal blood flow rate (4.6 mL min(-1) kg(-1)). The selective CYP3A4 inhibitors, ketoconazole, troleandomycin and ritonavir demonstrated significant inhibitory effects on CMDCK intestinal metabolism, which suggested that co-administration of CMDCK with potent CYP3A inhibitors, such as ritonavir, might decrease its intestinal metabolic clearance and subsequently improve its bioavailability in body.

Ultrasonography in Acupuncture-Uses in Education and Research.

This study aims to explore the potential use of ultrasound in locating the second posterior sacral foramen acupuncture point, quantifying depth of insertion and describing surrounding anatomical structures. We performed acupuncture needle insertion on a study team member. There were four steps in our experiment. First, the acupuncturist located the acupuncture point by palpation. Second, we used an ultrasound machine to visualize the structures surrounding the location of the acupuncture point and measure the depth required for needle insertion. Third, the acupuncturist inserted the acupuncture needle into the acupuncture point at an angle of 30°. Fourth, we performed another ultrasound scan to ensure that the needle was in the desired location. Results suggested that ultrasound could be used to locate the acupuncture point and estimate the depth of needle insertion. The needle was inserted to a depth of 4.0 cm to reach the surface of the sacral foramen. Based on Pythagoras theorem, taking a needle insertion angle of 30° and a needle insertion depth of 4.0 cm, the estimated perpendicular depth is 1.8 cm. An ultrasound scan corroborated the depth of 1.85 cm. The use of an ultrasound-guided technique for needle insertion in acupuncture practice could help standardize the treatment. Clinicians and students would be able to visualize and measure the depth of the sacral foramen acupuncture point, to guide the depth of needle insertion. This methodological guide could also be used to create a standard treatment protocol for research. A similar mathematical guide could also be created for other acupuncture points in future.

Is Electroacupuncture Treatment More Effective in Somatic Tinnitus Than in Nonsomatic Tinnitus?

Background: In recent years, evidence has been accumulating linking subjective tinnitus to the somatosensory system. Somatic tinnitus is defined as tinnitus in which forceful contractions of jaw and neck muscles modulate the psychoacoustic attributes of tinnitus, such as pitch and loudness. Being a somatosensory-based treatment modality, needling might well be more effective for treating somatic than nonsomatic tinnitus. Objective: The aim of this study was to compare the outcomes of electroacupuncture (EA) treatment between patients with somatic and nonsomatic tinnitus. Materials and Methods: A single-blinded prospective study was carried wherein 27 patients with tinnitus were divided into either a somatic or a nonsomatic group, based on whether their tinnitus could be modulated by at least one of a series of forceful jaw and neck muscular contraction maneuvers. Tinnitus responses were evaluated after a single session of EA on selected acupoints for 30 minutes. Results: Seventeen of the 27 patients (63.0%) studied were found to have somatic tinnitus. Generalized estimating equation model analysis did not find any overall statistically significant difference in EA response between patients with somatic and nonsomatic tinnitus. However, patients with somatic tinnitus who were consistent in their responses to the muscular contraction maneuvers were more likely to improve with EA than variable responders to these maneuvers (62.5% versus 22.0%). Conclusions: EA did not provide increased benefits for patients with somatic tinnitus, compared to those with nonsomatic tinnitus overall. However, within the somatic tinnitus group, a subpopulation of patients appeared to be relatively more responsive to EA treatment.

[Standardized management of acupuncture-moxibustion clinic in Singapore General Hospital].

The standardized management of acupuncture-moxibustion in Singapore General Hospital is introduced. With gradual improvement of outpatient infrastructure, re-training of medical staff, strict disinfection of manipulation, periodical inspection of medical instruments, unified management of writing, saving and processing in medical records and public education of TCM knowledge, a standardized management system in accordance with modernized hospital is gradually established. As a result, efficiency and quality of clinical treatment is continuously increasing. From April of 1998 to December of 2012, a total of 74 654 times of treatment were performed, and treatment amount per day is gradually increased. The unusual condition of acupuncture is avoided. Periodical strict inspection of joint committee authenticated by domestic and overseas medical health organization is repeatedly passed and accepted. Additionally, three clinical researches funded by Singapore Health-care Company are still in progress in acupuncture-moxibustion department.

[Impacts on the skin temperature by the different distances of moxibustion: discussion on the safe distance of moxibusiton].

OBJECTIVE: To observe the impacts of the different distances of moxibustion on local skin temperature and provide a safy distance of moxibustion. METHODS: Three healthy adult volunteers were included. The pure moxa stick (without other herbs mixed together) was used. The moxa-stick moxibustion and the mild moxibustion (with moxa box) were applied to Zusanli (ST 36) on the right side and Guanyuan (CV 4) respectively. The distance from moxibustion to the local skin was 2 cm, 3 cm and 4 cm separately. The moxibustion time was limited by 3 cm stick burned out. The infrared thermography was adopted to record and store thermal images and made the systematic analysis. The same trial was repeated on the second day. The means of the skin temperature measured at each acupoint each time was taken as the results for the analysis. RESULTS: (1) Moxibustion with moxa box at Guanyuan (CV 4): at the distance of 4 cm, the local skin temperature at over 44 degrees C [(44.1 +/- 1.3)-(46.7 +/- 1.5) degrees C)] lasted 7 min; at the distance of 3 cm, the local skin temperature at over 44 degrees C [(44.1 +/- 1.3)-(49.3 +/- 2.0) degrees C] lasted about 10 min and that at over 49 degrees C [(49.0 +/- 2.1)-(49.3 +/- 2.0) degrees C)] lasted 2 min; at the distance of 2 cm, the observation could not be followed due to local burning pain. (2) Moxa-stick moxibustion at Zusanli (ST 36): at the distance of 4 cm, the skin temperature was ranged from (40.0 +/- 2.0) degrees C to (44.9 +/- 2.3) degrees C; at the distance of 3 cm, in 1 min of moxibustion, the skin temperature increased over 44 degrees C, sustaining in the range from (45.9 +/- 3.0) degrees C to (47.8 +/- 2.0) degrees C; at the distance of 2 cm, the observation could not be followed due to local burning pain. CONCLUSION: In moxibustion, the closer the moxa stick to the skin is, the higher the local skin temperature is. No matter with stick moxibustion or box moxibustion, the distance of moxa stick to the skin should be in the range from 3 to 4 cm.