Preliminary screening of therapeutic drugs for phenylalanine hydroxylase deficiency / 中国基层医药

Objective:To screen new drugs for treatment of phenylalanine hydroxylase deficiency.Methods:From October 2019 to October 2020, virtual drug screening was performed in Center of Genetic Medicine, Nanjing Maternity and Child Health Care Hospital, Women's Hospital of Nanjing Medical University computer according to the characteristics of the binding ability of phenylalanine hydroxylase to drug spatial structure. Ten candidate drugs were screened from the FDA drug library (including 2 697 kinds of active pharmaceutical ingredients). A eukaryotic expression system was used to determine the effects of drugs on the activity of phenylalanine hydroxylase at the molecular level. Drug-sensitive mutants were screened.Results:Among the 10 candidate drugs, neoplasm hydrochloride, fluocinonide acetate and risperidone increased 23% [ t = 18.21, P < 0.001, vs. non-drug-treated phenylalanine hydroxylase group (i.e., only solvent and no drug added to the reaction system)], 21% ( t = 3.44, P < 0.05, vs. non-drug-treated phenylalanine hydroxylase group), 31% ( t = 19.57, P < 0.001, vs. non-drug-treated phenylalanine hydroxylase group) of the activity of phenylalanine hydroxylase. The remaining drugs exhibited weak even inhibitory effects on the activity of phenylalanine hydroxylase. 25% of p.D101N mutant could be activated by risperidone ( t = 15.86, P < 0.001, vs. non-drug-treated p.D101N mutant group). Conclusion:Neoplasm hydrochloride, fluocinonide acetate and risperidone can be used as potential therapeutic drugs for phenylalanine hydroxylase deficiency, and p.D101N mutant can be used as the drug-sensitive mutation site.

A clinical study of ropivacaine mesylate combined with nefopam hydrochloride in cesarean section postoperative patient-controlled epidural analgesia / 中国医师进修杂志

Objective To compare the effects of two patient-controlled epidural analgesia(PCEA) after cesarean section and the incidence of nausea vomiting, lethargy and urinary retention. Methods Sixty cesarean section patients were randomly divided into two groups, each group had 30 patients. Group Ⅰ: 0.15% bupivacaine hydrochloride plus tramadoL group Ⅱ: 0.179% ropivacaine mesylate plus nefopam hydrochloride. Postoperative 0-48 hours within the period pain (visual analog score, VAS)and the corresponding time motor block level(the Bromage scale), and incidence of nausea vomiting, lethargy and urinary retention were recorded. Results VAS difference was not statistically significant (P>0.05), Bromage scores in group Ⅱ was shorter than those in group Ⅰ(P<0.05), the incidence rates of nausea vomiting, lethargy and urinary retention in group Ⅱ were lower than those in group Ⅰ(P<0.01). Conclusion Ropivacaine mesylate combined with nefopam hydrochloride PCEA analgesic effect is certain, which shows a clear superiority in the motor function recovery and reducing the incidence of adverse reactions.

Nefopam Hydrochloride for Postoperative Subcutaneous Patient Controlled Analgesia / 中国药房

0.05).Neither pruritus nor respiratory depression was noted in both groups.CONCLUSION:At an equivalent dose,Nefopam Hydrochloride showed a similar PCSA efficacy to Fentanyl after surgery but less side effect,therefore,it can be applied in postoperative PCSA.

Pharmacokinetics and bioequivalence of sustained-released tablet of nefopam / 中国临床药理学与治疗学

AIM: To verify the bioequivalence between sustained released tablet of nepopam and normal one. METHODS: 18 volunteers were randomly devided into two groups. Double periodical crossed design was used, and poly dose of nefopam was administered to 18 volunteers following single dose after one week interval. The concentration of nefopam hydrochloride in serum was determinated by HPLC, and the related parameters came out through 3p97 programme. RESULTS: In the single dose test the drug concentration of sustained released tablet maitained 2040 mg?L -1 for 10 h ,c max was ( 45.8 ?15.7) mg?L -1 ,t peak was ( 3.4 ? 0.8) h , and the corresponding parameters of normal tablet were over 20 mg?L -1 for 7.5 h ,( 72.7 ?26.0) mg?L -1 ,and ( 1.6 ? 0.6) h . The AUC was ( 363.4 ? 107.1 ) and ( 374.8 ?125.7) mg?h?L -1 respectively, and F was ( 1.02 ? 0.25 ). In the poly dose test the c max of sustained released and normal one was ( 31.50 ? 12.65 ) and ( 33.68 ?10.51) mg?L -1 ,c min was ( 13.4 ? 4.4 ) and ( 10.9 ?5.4) mg?L -1 , t peak was ( 2.6 ? 0.6 ) and ( 1.22 ? 0.46) h , and FI was ( 0.77 ? 0.26 ) and ( 1.04 ? 0.18 ) respectively. CONCLUSION: The sustained released tablet is credible and the two types of tablet are equieffective in AUC.