A recently published systematic review and meta-analy-sis, incorporating all relevant studies on the association of acid suppressive medications and pneumonia identi-fied up to August 2009, revealed that for every 200...A recently published systematic review and meta-analy-sis, incorporating all relevant studies on the association of acid suppressive medications and pneumonia identi-fied up to August 2009, revealed that for every 200 patients, treated with acid suppressive medication, one will develop pneumonia. They showed the overall risk of pneumonia was higher among people using proton pump inhibitors （PPIs） [adjusted odds ratio （OR） = 1.27, 95% CI： 1.11-1.46, I2 = 90.5%] and Histamine-2 re-ceptor antagonists （H2RAs） （adjusted OR = 1.22, 95% CI： 1.09-1.36, I2 = 0.0%）. In the randomized controlled trials, use of H2RAs was associated with an elevated risk of hospital-acquired pneumonia （relative risk 1.22, 95% CI： 1.01-1.48, I2 = 30.6%）. Another meta-analysis of 11 studies published between 1997 and 2011 found that PPIs, which reduce stomach acid production, were associated with increased risk of fracture. The pooled OR for fracture was 1.29 （95% CI： 1.18-1.41） with use of PPIs and 1.10 （95% CI： 0.99-1.23） with use of H2RAs, when compared with non-use of the respective medications. Long-term use of PPIs increased the risk of any fracture （adjusted OR = 1.30, 95% CI： 1.15-1.48） and of hip fracture risk （adjusted OR = 1.34, 95% CI： 1.09-1.66）, whereas long-term H2RA use was not sig-nifcantly associated with fracture risk. Clinicians should carefully consider when deciding to prescribe acid-sup-pressive drugs, especially for patients who are already at risk for pneumonia and fracture. Since it is unneces-sary to achieve an achlorhydric state in order to resolve symptoms, we recommend using the only minimum effective dose of drug required to achieve the desired therapeutic goals.展开更多
Proceeding from natural amino acid L-asparagine and commercially available aldehydes a stereoselective synthesis was developed of (2S,4S)-2-alkyl(aryl)-3-(3-sulfanylpropanoyl)-6-oxohexahy- dropyrimidine-4-carboxylic a...Proceeding from natural amino acid L-asparagine and commercially available aldehydes a stereoselective synthesis was developed of (2S,4S)-2-alkyl(aryl)-3-(3-sulfanylpropanoyl)-6-oxohexahy- dropyrimidine-4-carboxylic acids, potential antihypertensive drugs, inhibitors of the angiotensin converting enzyme.展开更多
Recent pharmacokinetic studies have demonstrated that gastric acid suppression(AS)reduces exposure of gefitinib.However,the clinical significance of this drug-drug interaction(DDI)has not been determined.We,therefore,...Recent pharmacokinetic studies have demonstrated that gastric acid suppression(AS)reduces exposure of gefitinib.However,the clinical significance of this drug-drug interaction(DDI)has not been determined.We,therefore,evaluated it in this real-world study.A total of 200 NSCLC patients who received gefitinib from 2016 to 2018 at Fudan University Shanghai Cancer Center(FUSCC)were randomly selected.The patients were divided into two groups according to whether AS was used.The clinical characteristics of the patients were collected,and the efficacy and safety of gefitinib were compared between the two groups.We showed that 188 patients were considered eligible for this retrospective analysis,49 received AS(AS user group),while 139 patients did not(AS non-user group).Objective response rate(ORR)and disease control rate(DCR)in the AS user group versus AS non-user group were 69.4%versus 73.4%(P=0.591)and 89.8%versus 90.6%(P=0.486),respectively,while the progression-free survival(PFS)were 9.7 versus 12.2 months(P=0.0644).No significant difference in ORR,DCR or PFS was observed between the two groups.Further study showed that the PFS was related to the time of co-administration,and the patients receiving over 50%AS prescription overlap with gefitinib was significantly less compared with the other people(8.4 vs 12.6 months,P=0.0004).The frequencies of rash(8.2%vs 15.1%,P=0.281),diarrhea(4.1%vs 6.5%,P=0.539)and elevated ALT or AST level(6.1%vs 10.1%,P=0.407)were similar for both groups.Therefore,concomitant use of AS and gefitinib might affect the efficacy of gefitinib,which should be avoided if possible.展开更多
（S）-2-aminobutyric acid being initial raw material,（S）-2-hydroxybutyric acid methyl ester was synthesized by means of a three step reaction of hydroxylation, salification and esterification. The product had a yiel...（S）-2-aminobutyric acid being initial raw material,（S）-2-hydroxybutyric acid methyl ester was synthesized by means of a three step reaction of hydroxylation, salification and esterification. The product had a yield rate of 60.4%, purity of 99% and ee value higher than 99% by characterization of GC, HPLC and 1H NMR. This synthesis technique has advantages of high purity and ee value, low cost, short reaction time and mild reaction conditions so that it is suitable for production on industrial scale.展开更多
文摘A recently published systematic review and meta-analy-sis, incorporating all relevant studies on the association of acid suppressive medications and pneumonia identi-fied up to August 2009, revealed that for every 200 patients, treated with acid suppressive medication, one will develop pneumonia. They showed the overall risk of pneumonia was higher among people using proton pump inhibitors （PPIs） [adjusted odds ratio （OR） = 1.27, 95% CI： 1.11-1.46, I2 = 90.5%] and Histamine-2 re-ceptor antagonists （H2RAs） （adjusted OR = 1.22, 95% CI： 1.09-1.36, I2 = 0.0%）. In the randomized controlled trials, use of H2RAs was associated with an elevated risk of hospital-acquired pneumonia （relative risk 1.22, 95% CI： 1.01-1.48, I2 = 30.6%）. Another meta-analysis of 11 studies published between 1997 and 2011 found that PPIs, which reduce stomach acid production, were associated with increased risk of fracture. The pooled OR for fracture was 1.29 （95% CI： 1.18-1.41） with use of PPIs and 1.10 （95% CI： 0.99-1.23） with use of H2RAs, when compared with non-use of the respective medications. Long-term use of PPIs increased the risk of any fracture （adjusted OR = 1.30, 95% CI： 1.15-1.48） and of hip fracture risk （adjusted OR = 1.34, 95% CI： 1.09-1.66）, whereas long-term H2RA use was not sig-nifcantly associated with fracture risk. Clinicians should carefully consider when deciding to prescribe acid-sup-pressive drugs, especially for patients who are already at risk for pneumonia and fracture. Since it is unneces-sary to achieve an achlorhydric state in order to resolve symptoms, we recommend using the only minimum effective dose of drug required to achieve the desired therapeutic goals.
文摘Proceeding from natural amino acid L-asparagine and commercially available aldehydes a stereoselective synthesis was developed of (2S,4S)-2-alkyl(aryl)-3-(3-sulfanylpropanoyl)-6-oxohexahy- dropyrimidine-4-carboxylic acids, potential antihypertensive drugs, inhibitors of the angiotensin converting enzyme.
文摘Recent pharmacokinetic studies have demonstrated that gastric acid suppression(AS)reduces exposure of gefitinib.However,the clinical significance of this drug-drug interaction(DDI)has not been determined.We,therefore,evaluated it in this real-world study.A total of 200 NSCLC patients who received gefitinib from 2016 to 2018 at Fudan University Shanghai Cancer Center(FUSCC)were randomly selected.The patients were divided into two groups according to whether AS was used.The clinical characteristics of the patients were collected,and the efficacy and safety of gefitinib were compared between the two groups.We showed that 188 patients were considered eligible for this retrospective analysis,49 received AS(AS user group),while 139 patients did not(AS non-user group).Objective response rate(ORR)and disease control rate(DCR)in the AS user group versus AS non-user group were 69.4%versus 73.4%(P=0.591)and 89.8%versus 90.6%(P=0.486),respectively,while the progression-free survival(PFS)were 9.7 versus 12.2 months(P=0.0644).No significant difference in ORR,DCR or PFS was observed between the two groups.Further study showed that the PFS was related to the time of co-administration,and the patients receiving over 50%AS prescription overlap with gefitinib was significantly less compared with the other people(8.4 vs 12.6 months,P=0.0004).The frequencies of rash(8.2%vs 15.1%,P=0.281),diarrhea(4.1%vs 6.5%,P=0.539)and elevated ALT or AST level(6.1%vs 10.1%,P=0.407)were similar for both groups.Therefore,concomitant use of AS and gefitinib might affect the efficacy of gefitinib,which should be avoided if possible.
文摘（S）-2-aminobutyric acid being initial raw material,（S）-2-hydroxybutyric acid methyl ester was synthesized by means of a three step reaction of hydroxylation, salification and esterification. The product had a yield rate of 60.4%, purity of 99% and ee value higher than 99% by characterization of GC, HPLC and 1H NMR. This synthesis technique has advantages of high purity and ee value, low cost, short reaction time and mild reaction conditions so that it is suitable for production on industrial scale.
