Valsartan

Ardiana, Febry; Suciati, Suciati; Indrayanto, Gunawan

doi:10.1016/bs.podrm.2015.01.004

Cited by 21 publications

(10 citation statements)

References 62 publications

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“…The chemical name of valsartan is N-(1-Oxophentyl)-N-[[20-(1H-tetrazole-5-yl)[1,10-biphenyl]-4-yl] methyl]-L-valine and with highly lipid solubility. The pKa of valsartan is 4.9 and practically insoluble in water ( Ardiana et al, 2015 ). It is difficult dissociated and easily absorbed under physiological pH conditions.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics and safety of highly variable valsartan in single-pill combination with amlodipine versus its generic formulation: a randomized, three-cycle, three-sequence, partially replicated crossover phase I bioequivalence clinical trial

Qiu,

Song,

Ding

et al. 2023

Front. Pharmacol.

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Valsartan/amlodipine (I) is a single-pill combination (SPC) of an angiotensin II receptor blocker (ARB) and a calcium channel blocker (CCB) for treating hypertension. A clinical trial was performed to demonstrate that the test and reference valsartan/amlodipine formulations were bioequivalent under fasting and postprandial conditions. Participants were randomly divided into three sequences at a ratio of 1:1:1 for three-cycle, reference formulation replicated, crossover administration. The average bioequivalence (ABE) and reference-scaled average bioequivalence (RSABE) methods were used to evaluate BE using the main pharmacokinetic (PK) parameters. Overall, 45 eligible participants were enrolled in the postprandial trial, which was consistent with the fasting trial. For valsartan, the RSABE method was used to evaluate the BE of Cmax, while the ABE method was applied to evaluate the BE of AUC0–t and AUC0–∞. Both point estimates and 95% upper confidence bound met the BE criteria. For amlodipine, the ABE method was performed, and the 90% confidence intervals of the geometric mean ratios (GMR) for Cmax and AUC0–72 h were all within 80%–125%, with the BE criteria being met. Therefore, the two formulations are bioequivalent and have similar safety profiles in healthy Chinese subjects.Clinical trial registration: [http://www.chinadrugtrials.org.cn/index.html], identifier [CTR20210214].

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Section: Discussionmentioning

confidence: 99%

Pharmacokinetics and safety of highly variable valsartan in single-pill combination with amlodipine versus its generic formulation: a randomized, three-cycle, three-sequence, partially replicated crossover phase I bioequivalence clinical trial

Qiu,

Song,

Ding

et al. 2023

Front. Pharmacol.

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“…As the first dual-effect compound preparation of an enkephalinase inhibitor and ARB, sacubitril and valsartan have been reported to exert a dual role in neuroendocrine system activity ( 24 ). Valsartan not only exerts its effects by blocking angiotensin receptors to relax blood vessels, but also acts as an antagonist of aldosterone, producing diuresis and sodium excretion, resulting in a net reduction of water and sodium retention ( 25 ). As an enkephalinase inhibitor, sacubitril can block enkephalinase activity and reduce the degradation of BNP ( 26 ).…”

Section: Discussionmentioning

confidence: 99%

Protective effect of sacubitril/valsartan in patients with acute myocardial infarction: A meta‑analysis

Liu

Yin

et al. 2022

Exp Ther Med

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To evaluate the effects and safety of sacubitril/valsartan in patients with acute myocardial infarction (AMI), a total of four databases, including PubMed, Cochrane Library, Embase and Web of Science, and the ClinicalTrials.gov website were searched. Using a combination of medical subject headings and entry terms, the final search was performed in July 2021. A manual search of cross-references from the original articles was also conducted. The meta-analysis was subsequently performed with Revman 5.3 software and a total of four studies comprising 586 patients were included. The results disclosed a significant reduction in major adverse cardiovascular and cerebrovascular events (MACCEs) [odds ratio (OR), 0.47; 95% confidence interval (CI), 0.30-0.73; P=0.0007], readmission (OR, 0.45; 95% CI, 0.29-0.71; P=0.0006), incidence of acute heart failure (AHF) (OR, 0.45; 95% CI, 0.28-0.71; P=0.0007) and N-terminal pro B-type natriuretic peptide [standardized mean difference (SMD), -0.88; 95% CI, -1.55-(-0.21); P=0.01] in the sacubitril/valsartan group compared with that in the control group, and a random effects model was used to pool these data. No significant differences were identified in the incidence of hypotension (OR, 2.91; 95% CI, 0.55-15.51; P=0.21), adverse events (OR, 2.19; 95% CI, 0.42-11.37; P=0.35), left ventricular ejection fraction (mean difference, 1.96; 95% CI, -0.84-4.76; P=0.17) or soluble suppression of tumorigenesis-2 (SMD, -0.45; 95% CI, -1.62-0.71; P=0.45) according to the random effects model. In conclusion, the present meta-analysis revealed that sacubitril/valsartan was able to effectively reduce the incidence of MACCEs, readmission and AHF in patients with AMI after revascularization without any obvious adverse events.

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“…and the LabScribe3.0 software (iWorx Systems, Inc.). A selective AT 1 antagonist valsartan (≥98%, Sigma) was used as a reference drug (Ardiana & Suciati Indrayanto, 2015).…”

Section: At1-receptor Assaymentioning

confidence: 99%

Discovery and evaluation of biphenyl derivatives of 2‐iminobenzimidazoles as prototype dual PTP1B inhibitors and AMPK activators with in vivo antidiabetic activity

et al. 2023

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This work describes the synthesis of series hydrobromides of N-(4-biphenyl) methyl-N′-dialkylaminoethyl-2-iminobenzimidazoles, which, due to the presence of two privileged structural fragments (benzimidazole and biphenyl moieties), can be considered as bi-privileged structures. Compound 7a proved to activate AMP-activated kinase (AMPK) and simultaneously inhibit protein tyrosine phosphatase 1B (PTP1B) with similar potency. This renders it an interesting prototype of potential antidiabetic agents with a dual-target mechanism of action.Using prove of concept in vivo study, we show that dual-targeting compound 7a has a disease-modifying effect in a rat model of type 2 diabetes mellitus via improving insulin sensitivity and lipid metabolism.

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Valsartan

Cited by 21 publications

References 62 publications

Pharmacokinetics and safety of highly variable valsartan in single-pill combination with amlodipine versus its generic formulation: a randomized, three-cycle, three-sequence, partially replicated crossover phase I bioequivalence clinical trial

Pharmacokinetics and safety of highly variable valsartan in single-pill combination with amlodipine versus its generic formulation: a randomized, three-cycle, three-sequence, partially replicated crossover phase I bioequivalence clinical trial

Protective effect of sacubitril/valsartan in patients with acute myocardial infarction: A meta‑analysis

Discovery and evaluation of biphenyl derivatives of 2‐iminobenzimidazoles as prototype dual PTP1B inhibitors and AMPK activators with in vivo antidiabetic activity

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