hypertensive drug
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2022 ◽  
Vol 13 (1) ◽  
Author(s):  
Soumyaparna Das ◽  
Valerie Popp ◽  
Michael Power ◽  
Kathrin Groeneveld ◽  
Jie Yan ◽  
...  

AbstractHereditary degeneration of photoreceptors has been linked to over-activation of Ca2+-permeable channels, excessive Ca2+-influx, and downstream activation of Ca2+-dependent calpain-type proteases. Unfortunately, after more than 20 years of pertinent research, unequivocal evidence proving significant and reproducible photoreceptor protection with Ca2+-channel blockers is still lacking. Here, we show that both D- and L-cis enantiomers of the anti-hypertensive drug diltiazem were very effective at blocking photoreceptor Ca2+-influx, most probably by blocking the pore of Ca2+-permeable channels. Yet, unexpectedly, this block neither reduced the activity of calpain-type proteases, nor did it result in photoreceptor protection. Remarkably, application of the L-cis enantiomer of diltiazem even led to a strong increase in photoreceptor cell death. These findings shed doubt on the previously proposed links between Ca2+ and retinal degeneration and are highly relevant for future therapy development as they may serve to refocus research efforts towards alternative, Ca2+-independent degenerative mechanisms.


2021 ◽  
Vol 9 (10) ◽  
pp. 1277-1286
Author(s):  
Sarvesh Patel ◽  
◽  
Jai Narayan Mishra ◽  
Dhaneswar Kumar Vishwakarma ◽  
◽  
...  

Finally in the project work Atenolol is an anti-hypertensive drug. It has been formulated into fast dissolving tablets by direct compression method by using the Excipients like lactose, sucrose magnesium stearate, sodium lauryl and sulphate and many type super disintegrates such as crosscarmellose and sodium starch glycolate and the prepared by the tablets were evaluated for the pre-compression parameter such as angle of repose, bulk density, tapped density, % index, Hausners ratio, partition coefficients, melting points, UV spectroscopy, % assay, TLC, loss on drying and post compression parameter such as thickness, hardness, friability, drugs contents, weight variation, water absorbance ratio, Invitro disintegrating time , Invitro dissolution studies. All the parameter shows good results. FDTs are prepared by direct compression method are results found to be that the among of nine formulation as the F9 to be best as its shows 87.10% (direct compression method) maximum drug release respectively. The stability testing of manufactured tablets have being at 400 c having 75% relativity humidity for 1month and found to be stable. Prepared fast dissolving tablets of Atenolol 10 mg was found to be under fasting federal condition.


Author(s):  
Anshul Kumar ◽  
Rajnish Kumar ◽  
Avijit Mazumdar

Terazosin hydrochloride is an anti-hypertensive drug which is used to treat the diseases of hypertension. The literature survey shows the proposed synthesis of Terazosin hydrochloride derived from the starting material of 2-chloro-6, 7-dimethoxy–quinazoline-4-amine in the presence of 2-methoxy ethanol with n- benzyl piperazine to form the product. The Terazosin derivatives were prepared with the help of literature survey were 1, 4-bis-(furan-2-yl-carbonl) piperazine, 1, 4-bis-(tertrahydrofuran-2-yl) carbonyl piperazine, and 1-(4-amino-6, 7-dimethoxy- quinazoline-2-yl)- 4-formyl- piperazine were prepared by maintaining environmental condition. The characterization done for prepared derivative was done through 1H-NMR, MASS and IR Spectroscopy. The antibacterial activity of prepared derivatives was performed on the various bacteria like E. coli, Pseudomonas aeruginosa, Shigella sonneii, Klebsiella pneumonia, Staphylococcus aureus, Shigella flexneri, Vibrio cholera, Bacillus subtilis, Pseudomonas fluorescens, Pseudomonas aeruginosa, Staphylococcus aureus. The desired derivatives shown maximum zone of inhibition using concentration prepared 100µg and 200µg using standard drug. The derivatives that shows maximum inhibition 6, 7-dimethoxy-2-piperazine-1-yl-quinazoline -4-amine and minimum was shown by 1, 4-bis-(furan-2-yl-carbonl) piperazine, 1,4-bis-(tertrahydrofuran- 2-yl) carbonyl piperazine. The result should that prepared Terazosin derivatives shows potent actively when compared with standard ciprofloxacin.


2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Jill Hardin ◽  
Jenna M. Reps

Abstract Background The goal of our study is to examine the impact of the lookback length when engineering features to use in developing predictive models using observational healthcare data. Using a longer lookback for feature engineering gives more insight about patients but increases the issue of left-censoring. Methods We used five US observational databases to develop patient-level prediction models. A target cohort of subjects with hypertensive drug exposures and outcome cohorts of subjects with acute (stroke and gastrointestinal bleeding) and chronic outcomes (diabetes and chronic kidney disease) were developed. Candidate predictors that exist on or prior to the target index date were derived within the following lookback periods: 14, 30, 90, 180, 365, 730, and all days prior to index were evaluated. We predicted the risk of outcomes occurring 1 day until 365 days after index. Ten lasso logistic models for each lookback period were generated to create a distribution of area under the curve (AUC) metrics to evaluate the discriminative performance of the models. Calibration intercept and slope were also calculated. Impact on external validation performance was investigated across five databases. Results The maximum differences in AUCs for the models developed using different lookback periods within a database was < 0.04 for diabetes (in MDCR AUC of 0.593 with 14-day lookback vs. AUC of 0.631 with all-time lookback) and 0.012 for renal impairment (in MDCR AUC of 0.675 with 30-day lookback vs. AUC of 0.687 with 365-day lookback ). For the acute outcomes, the max difference in AUC across lookbacks within a database was 0.015 (in MDCD AUC of 0.767 with 14-day lookback vs. AUC 0.782 with 365-day lookback) for stroke and < 0.03 for gastrointestinal bleeding (in CCAE AUC of 0.631 with 14-day lookback vs. AUC of 0.660 with 730-day lookback). Conclusions In general the choice of covariate lookback had only a small impact on discrimination and calibration, with a short lookback (< 180 days) occasionally decreasing discrimination. Based on the results, if training a logistic regression model for prediction then using covariates with a 365 day lookback appear to be a good tradeoff between performance and interpretation.


Author(s):  
Dibya Das ◽  
Dhiman Halder ◽  
Himangshu Sekhar Maji ◽  
Pintu Kumar De ◽  
Tapan Kumar Pal

The aim of this study is to develop and validate an accurate, sensitive, rapid, precise, and simple bioanalytical method for the estimation of Azelnidipine (calcium channel blocker, used in hypertension) in the human plasma by using LC-ESI-MS/MS. The method was developed by gradient conditions using 0.1% Formic Acid in Acetonitrile and Milli-Q water with 10mM Ammonium acetate as a mobile phase with a flow rate of 0.5 mL/min. The Analyte and IS (Metoprolol) were separated by using a C18 Phenomenex Kinetex (50x3mm, 5µ) column. 7.0 minutes was the chromatographic run time. The analyte and IS extracted from plasma by simple protein precipitation technique (PPT). The LOD and LLOQ were found to be 0.53125ng/mL and 1.0625ng/mL, respectively. The extraction recovery of the drug from plasma was high. The other validation parameters were found within the range, as mentioned by USFDA and EMA guidelines.


2021 ◽  
Vol 8 (3) ◽  
Author(s):  
Achintya Kumar Mandal ◽  
Thatipelli Sujith ◽  
Allu Rajesh ◽  
Kallingil Gopi Divya ◽  
Koppala Narayana Sunilkumar ◽  
...  

The present work aims to study powder microscopy, physicochemical and high-performance thin-layer chromatography photo documentation and fingerprint profiles of a Siddha drug, Rattha Piththathirku Kudinir Chooranam (RPK). The raw drugs were collected, authenticated and the RPK was prepared. Then the drug was investigated for powder microscopic characters, physicochemical parameters, Thin Layer Chromatographic photo documentation (TLC), High-Performance Thin-Layer Chromatographic (HPTLC) fingerprint profiles of successive n-hexane, successive chloroform, successive ethanol and hydro alcohol (1:1) extracts. The successive and hydro alcohol extracts of the drug displayed distinct TLC spots and HPTLC peaks which are distinct to this drug.


Biomolecules ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 706
Author(s):  
Xiuman Zhou ◽  
Ling Jiao ◽  
Yuzhen Qian ◽  
Qingyu Dong ◽  
Yixuan Sun ◽  
...  

Strategies boosting both innate and adaptive immunity have great application prospects in cancer immunotherapy. Antibodies dual blocking the innate checkpoint CD47 and adaptive checkpoint PD-L1 or TIGIT could achieve durable anti-tumor effects. However, a small molecule dual blockade of CD47/SIRPα and TIGIT/PVR pathways has not been investigated. Here, an elevated expression of CD47 and PVR was observed in tumor tissues and cell lines analyzed with the GEO datasets and by flow cytometry, respectively. Compounds approved by the FDA were screened with the software MOE by docking to the potential binding pockets of SIRPα and PVR identified with the corresponding structural analysis. The candidate compounds were screened by blocking and MST binding assays. Azelnidipine was found to dual block CD47/SIRPα and TIGIT/PVR pathways by co-targeting SIRPα and PVR. In vitro, azelnidipine could enhance the macrophage phagocytosis when co-cultured with tumor cells. In vivo, azelnidipine alone or combined with irradiation could significantly inhibit the growth of MC38 tumors. Azelnidipine also significantly inhibits the growth of CT26 tumors, by enhancing the infiltration and function of CD8+ T cell in tumor and systematic immune response in the tumor-draining lymph node and spleen in a CD8+ T cell dependent manner. Our research suggests that the anti-hypertensive drug azelnidipine could be repositioned for cancer immunotherapy.


2021 ◽  
Vol 20 (1) ◽  
Author(s):  
Annayya R. Aroor ◽  
Srinivas Mummidi ◽  
Juan Carlos Lopez-Alvarenga ◽  
Nitin Das ◽  
Javad Habibi ◽  
...  

Abstract Objective Cardiac diastolic dysfunction (DD) and arterial stiffness are early manifestations of obesity-associated prediabetes, and both serve as risk factors for the development of heart failure with preserved ejection fraction (HFpEF). Since the incidence of DD and arterial stiffness are increasing worldwide due to exponential growth in obesity, an effective treatment is urgently needed to blunt their development and progression. Here we investigated whether the combination of an inhibitor of neprilysin (sacubitril), a natriuretic peptide-degrading enzyme, and an angiotensin II type 1 receptor blocker (valsartan), suppresses DD and arterial stiffness in an animal model of prediabetes more effectively than valsartan monotherapy. Methods Sixteen-week-old male Zucker Obese rats (ZO; n = 64) were assigned randomly to 4 different groups: Group 1: saline control (ZOC); Group 2: sacubitril/valsartan (sac/val; 68 mg•kg−1•day−1; ZOSV); Group 3: valsartan (31 mg•kg−1•day−1; ZOV) and Group 4: hydralazine, an anti-hypertensive drug (30 mg•kg−1•day−1; ZOH). Six Zucker Lean (ZL) rats that received saline only (Group 5) served as lean controls (ZLC). Drugs were administered daily for 10 weeks by oral gavage. Results Sac/val improved echocardiographic parameters of impaired left ventricular (LV) stiffness in untreated ZO rats, without altering the amount of food consumed or body weight gained. In addition to improving DD, sac/val decreased aortic stiffness and reversed impairment in nitric oxide-induced vascular relaxation in ZO rats. However, sac/val had no impact on LV hypertrophy. Notably, sac/val was more effective than val in ameliorating DD. Although, hydralazine was as effective as sac/val in improving these parameters, it adversely affected LV mass index. Further, cytokine array revealed distinct effects of sac/val, including marked suppression of Notch-1 by both valsartan and sac/val, suggesting that cardiovascular protection afforded by both share some common mechanisms; however, sac/val, but not val, increased IL-4, which is increasingly recognized for its cardiovascular protection, possibly contributing, in part, to more favorable effects of sac/val over val alone in improving obesity-associated DD. Conclusions These studies suggest that sac/val is superior to val in reversing obesity-associated DD. It is an effective drug combination to blunt progression of asymptomatic DD and vascular stiffness to HFpEF development in a preclinical model of obesity-associated prediabetes.


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