1.Clinical analysis of opioid drug on treating 146 case moderate or severe cancer pain
Jiaqi LIU ; Xushi WANG ; Ling ZHANG ; Qin YUAN ; Shucai XU
Clinical Medicine of China 2014;30(5):475-478
Objective To investigate the distribution of moderate to severe cancer pain and administrated dose of opioid drugs in order to provide the reference for the treatment of moderate and severe cancer pain.Methods Retrospective analyzed the clinical data of 146 patients with moderate to severe cancer pain.The information were recorded including opioid use dose,cancer pain incidence,age,gender,height,weight,body surface area and type of tumor.Results There were no significant difference among patients with opioids drug administration in terms of gender,average daily oral dose(x2 =0.473,Z =-0.185,P > 0.05).Meanwhile cancer incidence rate was same in different age groups (x2 =2.280,P =0.684).The average daily opioid dose in patients with over 80 year old was the lowest among other age groups (Z =-2.745,-1.986,-2.141,-2.162;P <0.05).Cancer pain incidence in patients with hepatobiliary pancreatic tumors were 67.50% (27/40),highest than other different types cancer including metastatic tumor(62.50% (10/16)),urinary tumor (61.54% (8/13)),lung cancer (52.63% (50/95)),breast cancer and gynecological tumor (50.00% (17/34)),gastrointestinal tumor(41.94% (26/62)),other tumors 38.46% (5/13) and head and neck tumor(25.00% (3/12)),the difference was statistically significant (x2 =23.672,P < 0.05).The average day oral morphine dose of different types tumor were listed as followed from high to low in the order:160 (80,200) mg of metastatic tumors,120 (60,160) mg of breast and gynecological tumor,100 (40,125) mg of lung cancer,90(45,115) mg of urinary tract tumors,80(60,160) mg of other tumors,70(50,90) mg of hepatobiliary pancreatic tumor,60 (40,80) mg of gastrointestinal tumor,55 (40,70) mg of head and neck tumor.There were significant differences in terms of among oral morphine dose per day of different type tumors (H=14.280,P <0.05).No correlation was found between pain patients with height,body mass,body surface area and average daily dose of morphine (r =-0.045,-0.042,-0.046 ; P < 0.05).Conclusion No significant differences were found in terms of moderate to severe cancer pain among different type tumors at different and age groups.While there is significant difference in term of cancer pain incidence among different tumor types.The average daily amount of morphine in patients with cancer pain is not related to gender,height,body mass and body surface area.The average amount of morphine of patients with age over 80 years old is significantly lower than that of the other age groups,and the average amount of morphine t is related to cancer type.
2.Design and synthesis of deuterium-labeled vorapaxar
Yu HUANG ; Baomin LIU ; Xushi LIU ; Yinsheng ZHANG
Journal of China Pharmaceutical University 2018;49(3):295-300
Vorapaxar,a novel antagonist of the protease-activated receptor 1 (PAR-1 ),can inhibit the clotting process. Deuterium-labeled vorapaxar was required for the analysis of clinical sample as an internal stand-ard. Starting for unlabeled vorapaxar,four-step reactions including hydrolysis,condensation,transesterification and hydrogen-deuterium exchange were carried out to synthesize [D8]vorapaxar effectively for the first time. All intermediates and final products were confirmed by NMR and high resolution mass spectrometry (HRMS).Impor-tantly,the prepared [D8]vorapaxar could meet the requirements of sample analysis as the internal standard.