Hypertension plays a major role in the development and progression of micro-and macrovascular disease.Moreover,increased blood pressure often coexists with additional cardiovascular risk factors such as insulin resist...Hypertension plays a major role in the development and progression of micro-and macrovascular disease.Moreover,increased blood pressure often coexists with additional cardiovascular risk factors such as insulin resistance.As a result the need for a comprehensive management of hypertensive patients is critical.However,the various antihypertensive drug categories have different effects on glucose metabolism.Indeed,angiotensin receptor blockers as well as angiotensin converting enzyme inhibitors have been associated with beneficial effects on glucose homeostasis.Calcium channel blockers(CCBs)have an overall neutral effect on glucose metabolism.However,some members of the CCBs class such as azelnidipine and manidipine have been shown to have advantageous effects on glucose homeostasis.On the other hand,diuretics andβ-blockers have an overall disadvantageous effect on glucose metabolism.Of note,carvedilol as well as nebivolol seem to differentiate themselves from the rest of theβ-blockers class,being more attractive options regarding their effect on glucose homeostasis.The adverse effects of some blood pressure lowering drugs on glucose metabolism may,to an extent,compromise their cardiovascular protective role.As a result the effects on glucose homeostasis of the various blood pressure lowering drugs should be taken into account when selecting an antihypertensive treatment,especially in patients which are at high risk for developing diabetes.展开更多
Background: Stroke is a worldwide health problem, the world’s second-leading cause of death and third-leading cause of disability. Currently, the majority of stroke patients are ischemic stroke patients. It is necess...Background: Stroke is a worldwide health problem, the world’s second-leading cause of death and third-leading cause of disability. Currently, the majority of stroke patients are ischemic stroke patients. It is necessary to evaluate risk factors to prevent ischemic stroke. Data and Methods: The risk factors for stroke in the previous fiscal year were analyzed. They were divided into nonmodifiable and modifiable factors. The probit and ordered probit models were used in the study, with 59341 and 50542 observations used in the estimation of the models, respectively. Results: Among the nonmodifiable factors, age, gender and cerebrovascular disease history are important risk factors. The history of cerebrovascular diseases is considered to be an especially important factor. Among the modifiable factors, taking antihypertensive drugs and recent large weight change are negative risk factors;however, sleeping well significantly reduces the probability of ischemic stroke. Conclusion: It is very important to ensure that medical personnel know a patient’s history of cerebrovascular diseases for proper treatments. Ischemic stroke might be considered an important side effect of antihypertensive drugs. Limitations: The dataset was observatory. There are various types of antihypertension drugs, and their effects are not analyzed.展开更多
A new rapid and sensitive high performance liquid chromatography (HPLC) method has been developed for the simultaneous determination of atorvastatin—an antihyperlipidemic drug along with most commonly prescribed drug...A new rapid and sensitive high performance liquid chromatography (HPLC) method has been developed for the simultaneous determination of atorvastatin—an antihyperlipidemic drug along with most commonly prescribed drugs (antihyperlipidemic, antihypertensive, antidiabetic, antithrombotic) in bulk and marketed combined formulations. The chromatographic separation was carried out by gradient elution mode with acetonitrile as organic modifier and 0.1% triethylamine acetate (TEAA) buffer pH 5 at a flow rate of 1 mL/min and a diode array detector at wavelength 230 nm was employed for detection of the analytes. Calibration curves were linear in the range of 5-150 mg/mL for all the drugs with correlation coefficients of determination (r 2 values)Z0.999. Limits of detection (LODs) and Limits of quantification (LOQs) ranged from 0.1 to 0.27 mg/mL and 0.3 to 0.89 mg/mL respectively. Intra-day and inter-day precision was studied at three concentration levels (20, 60 and 100 mg/mL). The intra-day and inter-day RSD for all compounds was less than 2.0%. The accuracy for all compounds was found to be between 98% and 102%. Thus, the performance of the method described allows its use in quantification of atorvastatin along with 9 most commonly prescribed drugs available in market as atorvastatin combined dosage forms.展开更多
Background: The American College of Cardiology (ACC), American Heart Association (AHA) and other organizations announced a new hypertension guideline (2017 ACA/AHA Guideline) in November 2017. However, other organizat...Background: The American College of Cardiology (ACC), American Heart Association (AHA) and other organizations announced a new hypertension guideline (2017 ACA/AHA Guideline) in November 2017. However, other organizations such as the European Society of Cardiology and European Society of Hypertension maintained their diagnostic thresholds. It is necessary to evaluate the effects of blood pressure (BP) and antihypertensive drugs on the probability of having heart disease (HD). Data and Methods: The effects of BP, antihypertensive drugs and other factors on the probability of undergoing HD treatment were analyzed. We used a dataset containing 83,287 medical check-up and treatment records obtained from 35,504 individuals in 5 fiscal years. The probit models were used in the study. Considering the possibility of endogeneity problems, different types of models were used. Results: We could not find evidence that a higher systolic BP increased the probability of undergoing HD treatment. However, diastolic BP increased the probability in most of the models. Taking antihypertensive drugs also increased the probability of undergoing HD treatment. Diabetes was another important risk factor. Conclusion: The results of this study did not support the new 2017 ACC/AHA Guideline. It is necessary to choose proper drugs and methods to reduce the risks of side effects. Limitations: The dataset was observatory, the data were obtained from just one medical society, and sample selection bias might exist.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
Objective To find out several patented technologies of antihypertensive drugs with the most market value through analysis,and provide a reference for the research and development of enterprises.Methods The most valuab...Objective To find out several patented technologies of antihypertensive drugs with the most market value through analysis,and provide a reference for the research and development of enterprises.Methods The most valuable patented technologies of antihypertensive drugs from 2009 to 2019 were analyzed to explore the patent layout and technical characteristics of the main patent applicants,and then the key directions of their research and development were gotten.Results and Conclusion Based on the method of patent analysis,five patents with the most market value are extracted to provide important technical support and market value reference for the research and development of generic drugs or new drugs.展开更多
Objective To evaluate the differences in 24-hour ambulatory blood pressure (BP) in older patients with hypertension treated with the five major classes of antihypertensive drugs,as monotherapy or dual combination ther...Objective To evaluate the differences in 24-hour ambulatory blood pressure (BP) in older patients with hypertension treated with the five major classes of antihypertensive drugs,as monotherapy or dual combination therapy,to improve daytime and nighttime BP control. Methods We enrolled 1920 Chinese community-dwelling outpatients aged ≥ 60 years and compared ambulatory BP values and ambulatory BP control (24-hour BP < 130/80 mmHg;daytime mean BP < 135/85 mmHg;and nighttime mean BP < 120/70 mmHg),as well as nighttime BP dip patterns for monotherapy and dual combination therapy groups. Results Patients’ mean age was 71 years,and 59.5% of patients were women. Calcium channel blockers (CCBs) constituted the most common (60.3% of patients) monotherapy,and renin–angiotensin system (RAS) blockers combined with CCBs was the most common (56.5% of patients) dual combination therapy. Monotherapy with beta-blockers (BB) provided the best daytime BP control. The probabilities of having a nighttime dip pattern and nighttime BP control were higher in patients receiving diuretics compared with CCBs (OR = 0.52,P = 0.05 and OR = 0.41,P = 0.007,respectively). Patients receiving RAS/diuretic combination therapy had a higher probability of having controlled nighttime BP compared with those receiving RAS/CCB (OR = 0.45,P = 0.004). Compared with RAS/diuretic therapy,BB/CCB therapy had a higher probability of achieving daytime BP control (OR = 1.27,P = 0.45). Conclusions Antihypertensive monotherapy and dual combination drug therapy provided different ambulatory BP control and nighttime BP dip patterns. BB-based regimens provided lower daytime BP,whereas diuretic-based therapies provided lower nighttime BP,compared with other antihypertensive regimens.展开更多
High blood pressure (HBP) is a health problem world—wide. In Togo, that affection constitutes a more and more pre-occupying cause of morbidity and mortality. This study is a prospective one which intended to identify...High blood pressure (HBP) is a health problem world—wide. In Togo, that affection constitutes a more and more pre-occupying cause of morbidity and mortality. This study is a prospective one which intended to identify the antihypertensive regimens prescribed and evaluate their effect on patients’ blood pressure (BP) control. Out of the 204 patients enrolled (mean: 55.01 ± 12.55 years;sex ratio: 1.3), 112/176 placed on antihypertensive therapy have controlled their BP (38.39% outpatients vs 61.61% inpatients). Related to the sex factor, we didn’t observe any significant difference in the BP control. Whereas, the mean median value of BP reduction of outpatients (30.00/15.00 mmHg) (p = 0.001) was half lower than that of inpatients (60.00/30.00 mmHg (p = 0.004)). Thirty five outpatients (81.40%) vs 64 inpatients (92.75%) were placed on combination therapy. The bitherapy was prescribed to 23 outpatients (53.49%) against 27 inpatients (39.13%) while the quadritherapy and more than 4 drugs combination were prescribed exclusively to inpatients (20.29%, n = 14). That quadritherapy induced a significant mean reduction of inpatients’ SBP compared to monotherapy (p = 0.043) and to bitherapy (p = 0.004). The favorite combinations were D + CCA, D + ACEI, D + CCA + ACEI and D + CCA + ACEI + CAAD of which the quadruple therapy showed a significant inpatients’ DBP control (p = 0.015) compared to D + CCA combination. The combinations including at least one diuretic induced a significant difference between outpatients (median value: 30.000/10.000 mmHg) (p < 0.001) and inpatients (median value: 60.000 mmHg/30 mmHg) (p < 0.001). The first-line molecules and fixe combinations prescribed in decreasing frequency were among others: hydrochlorothiazide + captopril, nicardipine, α methyldopa for outpatients;furosemide, nicardipine, captopril, α methyldopa, hydrochlorothiazide + captopril for inpatients. Diuretics, CCAs and ACEIs were the 3 favorite pharmacological groups for essential hypertension management in our African resource limited context. Combined to CAAD, they represented the best quadruple combination among inpatients having showed a significant difference in DBP control compared to D + CCA combination.展开更多
文摘Hypertension plays a major role in the development and progression of micro-and macrovascular disease.Moreover,increased blood pressure often coexists with additional cardiovascular risk factors such as insulin resistance.As a result the need for a comprehensive management of hypertensive patients is critical.However,the various antihypertensive drug categories have different effects on glucose metabolism.Indeed,angiotensin receptor blockers as well as angiotensin converting enzyme inhibitors have been associated with beneficial effects on glucose homeostasis.Calcium channel blockers(CCBs)have an overall neutral effect on glucose metabolism.However,some members of the CCBs class such as azelnidipine and manidipine have been shown to have advantageous effects on glucose homeostasis.On the other hand,diuretics andβ-blockers have an overall disadvantageous effect on glucose metabolism.Of note,carvedilol as well as nebivolol seem to differentiate themselves from the rest of theβ-blockers class,being more attractive options regarding their effect on glucose homeostasis.The adverse effects of some blood pressure lowering drugs on glucose metabolism may,to an extent,compromise their cardiovascular protective role.As a result the effects on glucose homeostasis of the various blood pressure lowering drugs should be taken into account when selecting an antihypertensive treatment,especially in patients which are at high risk for developing diabetes.
文摘Background: Stroke is a worldwide health problem, the world’s second-leading cause of death and third-leading cause of disability. Currently, the majority of stroke patients are ischemic stroke patients. It is necessary to evaluate risk factors to prevent ischemic stroke. Data and Methods: The risk factors for stroke in the previous fiscal year were analyzed. They were divided into nonmodifiable and modifiable factors. The probit and ordered probit models were used in the study, with 59341 and 50542 observations used in the estimation of the models, respectively. Results: Among the nonmodifiable factors, age, gender and cerebrovascular disease history are important risk factors. The history of cerebrovascular diseases is considered to be an especially important factor. Among the modifiable factors, taking antihypertensive drugs and recent large weight change are negative risk factors;however, sleeping well significantly reduces the probability of ischemic stroke. Conclusion: It is very important to ensure that medical personnel know a patient’s history of cerebrovascular diseases for proper treatments. Ischemic stroke might be considered an important side effect of antihypertensive drugs. Limitations: The dataset was observatory. There are various types of antihypertension drugs, and their effects are not analyzed.
基金the Department of Pharmaceuticals (Ministry of Chemicals and Fertilizers),New Delhi,for grant of a MS(Pharm.) fellowship
文摘A new rapid and sensitive high performance liquid chromatography (HPLC) method has been developed for the simultaneous determination of atorvastatin—an antihyperlipidemic drug along with most commonly prescribed drugs (antihyperlipidemic, antihypertensive, antidiabetic, antithrombotic) in bulk and marketed combined formulations. The chromatographic separation was carried out by gradient elution mode with acetonitrile as organic modifier and 0.1% triethylamine acetate (TEAA) buffer pH 5 at a flow rate of 1 mL/min and a diode array detector at wavelength 230 nm was employed for detection of the analytes. Calibration curves were linear in the range of 5-150 mg/mL for all the drugs with correlation coefficients of determination (r 2 values)Z0.999. Limits of detection (LODs) and Limits of quantification (LOQs) ranged from 0.1 to 0.27 mg/mL and 0.3 to 0.89 mg/mL respectively. Intra-day and inter-day precision was studied at three concentration levels (20, 60 and 100 mg/mL). The intra-day and inter-day RSD for all compounds was less than 2.0%. The accuracy for all compounds was found to be between 98% and 102%. Thus, the performance of the method described allows its use in quantification of atorvastatin along with 9 most commonly prescribed drugs available in market as atorvastatin combined dosage forms.
文摘Background: The American College of Cardiology (ACC), American Heart Association (AHA) and other organizations announced a new hypertension guideline (2017 ACA/AHA Guideline) in November 2017. However, other organizations such as the European Society of Cardiology and European Society of Hypertension maintained their diagnostic thresholds. It is necessary to evaluate the effects of blood pressure (BP) and antihypertensive drugs on the probability of having heart disease (HD). Data and Methods: The effects of BP, antihypertensive drugs and other factors on the probability of undergoing HD treatment were analyzed. We used a dataset containing 83,287 medical check-up and treatment records obtained from 35,504 individuals in 5 fiscal years. The probit models were used in the study. Considering the possibility of endogeneity problems, different types of models were used. Results: We could not find evidence that a higher systolic BP increased the probability of undergoing HD treatment. However, diastolic BP increased the probability in most of the models. Taking antihypertensive drugs also increased the probability of undergoing HD treatment. Diabetes was another important risk factor. Conclusion: The results of this study did not support the new 2017 ACC/AHA Guideline. It is necessary to choose proper drugs and methods to reduce the risks of side effects. Limitations: The dataset was observatory, the data were obtained from just one medical society, and sample selection bias might exist.
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Objective To find out several patented technologies of antihypertensive drugs with the most market value through analysis,and provide a reference for the research and development of enterprises.Methods The most valuable patented technologies of antihypertensive drugs from 2009 to 2019 were analyzed to explore the patent layout and technical characteristics of the main patent applicants,and then the key directions of their research and development were gotten.Results and Conclusion Based on the method of patent analysis,five patents with the most market value are extracted to provide important technical support and market value reference for the research and development of generic drugs or new drugs.
基金supported by a grant from the Chinese Ministry of Sciences and Technology (2016YFC1300100)
文摘Objective To evaluate the differences in 24-hour ambulatory blood pressure (BP) in older patients with hypertension treated with the five major classes of antihypertensive drugs,as monotherapy or dual combination therapy,to improve daytime and nighttime BP control. Methods We enrolled 1920 Chinese community-dwelling outpatients aged ≥ 60 years and compared ambulatory BP values and ambulatory BP control (24-hour BP < 130/80 mmHg;daytime mean BP < 135/85 mmHg;and nighttime mean BP < 120/70 mmHg),as well as nighttime BP dip patterns for monotherapy and dual combination therapy groups. Results Patients’ mean age was 71 years,and 59.5% of patients were women. Calcium channel blockers (CCBs) constituted the most common (60.3% of patients) monotherapy,and renin–angiotensin system (RAS) blockers combined with CCBs was the most common (56.5% of patients) dual combination therapy. Monotherapy with beta-blockers (BB) provided the best daytime BP control. The probabilities of having a nighttime dip pattern and nighttime BP control were higher in patients receiving diuretics compared with CCBs (OR = 0.52,P = 0.05 and OR = 0.41,P = 0.007,respectively). Patients receiving RAS/diuretic combination therapy had a higher probability of having controlled nighttime BP compared with those receiving RAS/CCB (OR = 0.45,P = 0.004). Compared with RAS/diuretic therapy,BB/CCB therapy had a higher probability of achieving daytime BP control (OR = 1.27,P = 0.45). Conclusions Antihypertensive monotherapy and dual combination drug therapy provided different ambulatory BP control and nighttime BP dip patterns. BB-based regimens provided lower daytime BP,whereas diuretic-based therapies provided lower nighttime BP,compared with other antihypertensive regimens.
文摘High blood pressure (HBP) is a health problem world—wide. In Togo, that affection constitutes a more and more pre-occupying cause of morbidity and mortality. This study is a prospective one which intended to identify the antihypertensive regimens prescribed and evaluate their effect on patients’ blood pressure (BP) control. Out of the 204 patients enrolled (mean: 55.01 ± 12.55 years;sex ratio: 1.3), 112/176 placed on antihypertensive therapy have controlled their BP (38.39% outpatients vs 61.61% inpatients). Related to the sex factor, we didn’t observe any significant difference in the BP control. Whereas, the mean median value of BP reduction of outpatients (30.00/15.00 mmHg) (p = 0.001) was half lower than that of inpatients (60.00/30.00 mmHg (p = 0.004)). Thirty five outpatients (81.40%) vs 64 inpatients (92.75%) were placed on combination therapy. The bitherapy was prescribed to 23 outpatients (53.49%) against 27 inpatients (39.13%) while the quadritherapy and more than 4 drugs combination were prescribed exclusively to inpatients (20.29%, n = 14). That quadritherapy induced a significant mean reduction of inpatients’ SBP compared to monotherapy (p = 0.043) and to bitherapy (p = 0.004). The favorite combinations were D + CCA, D + ACEI, D + CCA + ACEI and D + CCA + ACEI + CAAD of which the quadruple therapy showed a significant inpatients’ DBP control (p = 0.015) compared to D + CCA combination. The combinations including at least one diuretic induced a significant difference between outpatients (median value: 30.000/10.000 mmHg) (p < 0.001) and inpatients (median value: 60.000 mmHg/30 mmHg) (p < 0.001). The first-line molecules and fixe combinations prescribed in decreasing frequency were among others: hydrochlorothiazide + captopril, nicardipine, α methyldopa for outpatients;furosemide, nicardipine, captopril, α methyldopa, hydrochlorothiazide + captopril for inpatients. Diuretics, CCAs and ACEIs were the 3 favorite pharmacological groups for essential hypertension management in our African resource limited context. Combined to CAAD, they represented the best quadruple combination among inpatients having showed a significant difference in DBP control compared to D + CCA combination.
