- Long-term mortality and cardiovascular events of seven angiotensin receptor blockers in hypertensive patients: Analysis of a national real-world database: A retrospective cohort study. [Journal Article]Health Sci Rep. 2023 Feb; 6(2):e1056.HS
- CONCLUSIONS: In a Korean population of patients with hypertension without CVD, six different ARBs showed similar efficacy to losartan in terms of long-term mortality and MACEs. Further well-designed prospective studies are required to confirm our findings.
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- Utility of a Systematic Approach to Selecting Candidate Prodrugs: A Case Study Using Candesartan Ester Analogues. [Journal Article]J Pharm Sci. 2023 Feb 01 [Online ahead of print]JP
- Development of prodrugs is a useful strategy to overcome some disadvantages of candidate drugs. Recently, we established a systematic approach to selecting appropriate prodrugs, and validated the utility of this approach using oseltamivir analogues. In this study, the utility of the approach was further examined using candesartan cilexetil and 20 kinds of its analogues having various types of sid…
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- Chemometric Methods for Simultaneous Determination of Candesartan Cilexetil and Hydrochlorothiazide in Binary Combinations. [Journal Article]
- Simple, accurate, precise, and cost-effective chemometric techniques for the measurement of candesartan cilexetil and hydrochlorothiazide in synthetic mixtures were improved and validated. H-point standard addition, Q-absorption ratio, and correction absorbance spectrophotometric techniques were utilized for the simultaneous determination of both medicines in real pharmaceutical formulations. A n…
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- Investigation of Carcinogenic Impurities of N-Nitrosamines in Sartan Pharmaceutical Products Marketed in Brazil: Development and Validation of Method Based on High-Performance Liquid Chromatography-Tandem Mass Spectrometry. [Journal Article]J Pharm Sci. 2023 Jan 16 [Online ahead of print]JP
- N-nitrosamines (NA) impurities have unexpectedly been found in sartan products, angiotensin II receptor antagonists that are used to control hypertension, representing an urgent concern for industry, global regulators and for the patients. In this study, an HPLC-MS/MS method was developed and validated for the quantification of six NA (N-nitrosodimethylamine, N-Nitroso-N-methyl-4-aminobutyric aci…
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- Role of angiotensin receptor blockers in the context of Alzheimer's disease. [Review]Fundam Clin Pharmacol. 2023 Jan 18 [Online ahead of print]FC
- As the world's population ages, the prevalence of age-related neurological disorders such as Alzheimer's disease (AD) is increasing. There is currently no treatment for Alzheimer's disease, and the few approved medications have a low success rate in lowering symptoms. As a result, several attempts are underway worldwide to identify new targets for the therapy of Alzheimer's disease. In preclinica…
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- Medium-term real-world data for erenumab in 177 treatment resistant or difficult to treat chronic migraine patients: persistence and patient reported outcome measures after 17-30 months. [Journal Article]
- CONCLUSIONS: Approximately 55% of treatment resistant or difficult to treat CM patients who trialled erenumab in our clinics reported a subjective benefit and were still on treatment after 17-30 months.
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- Effects of candesartan on cerebral microvascular function in mild cognitive impairment: Results of two clinical trials. [Journal Article]Int J Stroke. 2023 Jan 30 [Online ahead of print]IJ
- CONCLUSIONS: This study suggests that candesartan is associated with improved microvascular function in MCI, and these findings are independent of its blood pressure effect in these VCI and prodromal AD populations.
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- Effect of candesartan treatment on echocardiographic indices of cardiac remodeling in post-myocardial infarction patients. [Journal Article]Rev Assoc Med Bras (1992). 2023 Jan 09 [Online ahead of print]RA
- CONCLUSIONS: Our results suggest that candesartan treatment following myocardial infarction may potentially be useful in terms of improving post-myocardial infarction cardiac remodeling.
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- [Role of polypills in cardiovascular risk reduction in primary prevention]. [Review]Medicina (B Aires). 2022; 82(6):904-913.M
- Unlike medications that contain fixed-dose combinations, such as those recommended by clinical guidelines for treating high blood pressure, the so-called polypills contain several drugs that simultaneously treat two or more cardiovascular conditions or risk factors. They were proposed 2 decades ago, both for primary and secondary prevention with the hypothesis that they could have wide disseminat…
- Evaluation of Ameliorative Effect of Quercetin and Candesartan in Doxorubicin-Induced Cardiotoxicity. [Journal Article]
- CONCLUSIONS: The overall result depicts more beneficial and cardioprotective effect of quercetin and candesartan combination as compared to their individual effects in doxorubicin treated animals. Therefore, this combination might be a suitable option to treat the cardiotoxic effect of doxorubicin.
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- Thymol-Based Hydrophobic Deep Eutectic Solvents as a Green Approach for Screening Polar Nitrosamines in Sartans Pharmaceutical Products by Ultrasound-Assisted Dispersive Liquid-Liquid Microextraction Combined with HPLC-DAD. [Journal Article]J Pharm Sci. 2022 Dec 05 [Online ahead of print]JP
- Nitrosamines are carcinogens substances firstly detected in sartans drugs in 2018, leading to new regulations and monitoring programmes that raised the costs and challenges to the pharmaceutical industry. Therefore, reliable and cost-effective methods for screening nitrosamines in medicines are highly desirable. Hydrophobic deep eutectic solvents (HDES), a novel "eco-friendly" alternative to solv…
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- Candesartan-the next anti-amyloid drug? [Journal Article]
- This scientific commentary refers to 'Safety and biomarker effects of candesartan in non-hypertensive adults with prodromal Alzheimer's disease' by Hajjar et al. (https://doi.org/10.1093/braincomms/fcac270).
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- Safety and biomarker effects of candesartan in non-hypertensive adults with prodromal Alzheimer's disease. [Journal Article]
- Observational studies suggest that angiotensin receptor blockers in hypertensive adults are associated with lower post-mortem indicators of Alzheimer's disease pathology. Candesartan, an angiotensin receptor blocker, has a positive cognitive effect in mild cognitive impairment with hypertension. However, its safety and effects in non-hypertensive individuals with Alzheimer's disease are unclear. …
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- Sustained AT1R stimulation induces upregulation of growth factors in human cardiac fibroblasts via Gαq/TGF-β/ERK signaling that influences myocyte hypertrophy. [Journal Article]Eur J Pharmacol. 2022 Dec 15; 937:175384.EJ
- Stimulation of angiotensin II receptor (ATR) with angiotensin II (Ang II) accelerates cardiac fibroblast activation, resulting in upregulation of cytokines and growth factors. Growth factors were strongly upregulated in animal models of myocardial fibrosis and hypertrophy as well as patients with heart failure. Nevertheless, the signal transduction of ATR for upregulation of growth factors in hum…
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- Histomorphometry Changes and Decreased Reactivity to Angiotensin II in the Ileum and Colon of Streptozotocin-Induced Diabetic Rats. [Journal Article]
- Diabetes mellitus (DM) is a chronic progressive metabolic disorder associated with several gastrointestinal complications, affecting up to 75% of patients. Knowing that Angiotensin II (AngII) also regulates intestinal contraction, we decided to evaluate changes in ileum and colon histomorphometry and AngII reactivity in a rat model of DM. Streptozotocin (STZ, 55 mg/kg) was administered to induce …
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- Assessment of Urinary Exosomal NHE3 as a Biomarker of Acute Kidney Injury. [Journal Article]
- The diagnosis of acute kidney injury (AKI) traditionally depends on the serum creatinine (Scr) and urine output, which lack sufficient sensitivity and specificity. Using urinary exosomes as a biomarker has unique advantages. To assess whether urinary exosomal Na+/H+ exchanger isoform 3 (NHE3) protein could serve as a biomarker of AKI, we constructed four AKI rat models: cisplatin (7.5 mg/kg) inje…
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- Treatment of Hypertension: A Review. [Review]
- CONCLUSIONS: Hypertension affects approximately 116 million adults in the US and more than 1 billion adults worldwide and is a leading cause of CVD morbidity and mortality. First-line therapy for hypertension is lifestyle modification, consisting of weight loss, dietary sodium reduction and potassium supplementation, healthy dietary pattern, physical activity, and limited alcohol consumption. When drug therapy is required, first-line therapies are thiazide or thiazidelike diuretics, angiotensin-converting enzyme inhibitor or angiotensin receptor blockers, and calcium channel blockers.
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- Candesartan Attenuates Cisplatin-Induced Lung Injury by Modulating Oxidative Stress, Inflammation, and TLR-4/NF-κB, JAK1/STAT3, and Nrf2/HO-1 Signaling. [Journal Article]
- Cisplatin (CIS) is an effective chemotherapeutic agent against different cancers. The use of CIS is associated with acute lung injury (ALI) and other adverse effects, and oxidative stress and inflammation were implicated in its toxic effects. Candesartan (CAN), an angiotensin II (Ang II) receptor blocker, showed beneficial effects against oxidative stress and inflammation. Therefore, this study i…
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- Candesartan Does Not Activate PPARγ and Its Target Genes in Early Gestation Trophoblasts. [Journal Article]
- Angiotensin II receptor 1 blockers are commonly used to treat hypertension in women of childbearing age. While the fetotoxic effects of these drugs in the second and third trimesters of pregnancy are well documented, their possible impacts on placenta development in early gestation are unknown. Candesartan, a member of this group, also acts as a peroxisome proliferator-activated receptor gamma (P…
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- In Silico Identification of New Anti-SARS-CoV-2 Main Protease (Mpro) Molecules with Pharmacokinetic Properties from Natural Sources Using Molecular Dynamics (MD) Simulations and Hierarchical Virtual Screening. [Journal Article]
- Infectious agents such as SARS-CoV, MERS-CoV, and SARS-CoV-2 have emerged in recent years causing epidemics with high mortality rates. The quick development of novel therapeutic compounds is required in the fight against such pathogenic agents. Unfortunately, the traditional drug development methods are time-consuming and expensive. In this study, computational algorithms were utilized for virtua…
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- Consensus of the Brazilian Headache Society (SBCe) for prophylactic treatment of episodic migraine: part II. [Journal Article]Arq Neuropsiquiatr. 2022 09; 80(9):953-969.AN
- CONCLUSIONS: Despite an effort by the scientific community to find really effective drugs in the treatment of migraine, given the large number of drugs tested for this purpose, we still have few therapeutic options.
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- Medicine-Induced Acute Kidney Injury Findings from Spontaneous Reporting Systems, Sequence Symmetry Analysis and a Case-Control Study with a Focus on Medicines Used in Primary Care. [Journal Article]
- CONCLUSIONS: This research highlights a number of medicines that may contribute to acute injury; however, we had an insufficient sample to confirm associations of some medicines. Spironolactone, furosemide, and trimethoprim with sulfamethoxazole are medicines that, in particular, need to be used carefully and monitored closely in patients in the community at risk of acute kidney injury.
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- Candesartan Reduces Neuronal Apoptosis Caused by Ischemic Stroke via Regulating the FFAR1/ITGA4 Pathway. [Journal Article]
- Ischemic stroke (IS) is a general term for necrosis of brain tissue caused by stenosis, occlusion of arteries supplying blood to the brain (carotid artery and vertebral artery), and insufficient blood supply to the brain. Cerebral ischemia is the main kind of IS causing cell damage. However, the underlying mechanism still needs to be clarified further. In this study, it was demonstrated that FFAR…
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- Study of possible sex features of ramipril and candesartan treatment under experimental arterial hypertension in rats. [Journal Article]Ceska Slov Farm. 2022 Summer; 71(3):116-120.CS
- The article presents the results of a preclinical study of ramipril and candesartan in an experimental group of hypertensive rats of different sexes. Antihypertensive therapy was performed for 21 days. The drugs were administered daily in moderate therapeutic doses calculated for rats using the coefficient of species sensitivity. It was found that the course of experimental hypertension has gende…
- Pharmacodynamic model of slow reversible binding and its applications in pharmacokinetic/pharmacodynamic modeling: review and tutorial. [Review]
- Therapeutic responses of most drugs are initiated by the rate and degree of binding to their receptors or targets. The law of mass action describes the rate of drug-receptor complex association (kon) and dissociation (koff) where the ratio koff/kon is the equilibrium dissociation constant (Kd). Drugs with slow reversible binding (SRB) often demonstrate delayed onset and prolonged pharmacodynamic …
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- Virtual Screening for FDA-Approved Drugs That Selectively Inhibit Arginase Type 1 and 2. [Journal Article]
- Arginases are often overexpressed in human diseases, and they are an important target for developing anti-aging and antineoplastic drugs. Arginase type 1 (ARG1) is a cytosolic enzyme, and arginase type 2 (ARG2) is a mitochondrial one. In this study, a dataset containing 2115-FDA-approved drug molecules is virtually screened for potential arginase binding using molecular docking against several AR…
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- TMAO Suppresses Megalin Expression and Albumin Uptake in Human Proximal Tubular Cells Via PI3K and ERK Signaling. [Journal Article]
- Trimethylamine-N-oxide (TMAO) is a uremic toxin, which has been associated with chronic kidney disease (CKD). Renal tubular epithelial cells play a central role in the pathophysiology of CKD. Megalin is an albumin-binding surface receptor on tubular epithelial cells, which is indispensable for urine protein reabsorption. To date, no studies have investigated the effect of TMAO on megalin expressi…
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- Angiotensin II receptor type 1 blocker candesartan improves morphine tolerance by reducing morphine‑induced inflammatory response and cellular activation of BV2 cells via the PPARγ/AMPK signaling pathway. [Journal Article]
- Morphine is the most common drug of choice in clinical pain management; however, morphine tolerance presents a significant clinical challenge. The pathogenesis of morphine tolerance is known to be closely associated with angiotensin II receptor type 1 (AT1R) in microglia. As an AT1R antagonist, candesartan may serve an important role in regulating morphine tolerance. Therefore, the present study …
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- Incidence and Pattern of Aminotransferase Elevation During Anti-Hypertensive Therapy With Angiotensin-II Receptor Blockers. [Journal Article]
- CONCLUSIONS: Approximately 2% of patients receiving ARB therapy had significant ALT elevation (4.24/106 cumulative defined daily doses [cDDDs]), which was associated with probable ARB-related liver injury in 0.07% of patients (0.15/106 cDDDs). Elevation of ALT was more commonly associated with fimasartan than the other ARBs. Clinicians should be aware of the possibility of ARB-related ALT elevation in patients with unexplained chronic abnormal ALT.
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- Sustainable spectrophotometric determination of antihypertensive medicines reducing COVID-19 risk via paired wavelength data processing technique - Assessment of purity, greenness and whiteness. [Journal Article]
- Recent studies have reported that using certain antihypertensive therapies such as angiotensin II receptor blockers (ARBs) is associated with mitigation of fatal outcomes and enhancing clinical features of patients having hypertension during coronavirus pandemic. Thus, in the current work an innovative, effective, white and sustainable spectrophotometric technique called paired wavelength data pr…
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