Mathematical simulation of the structure of pulsed arterial pressure relations with vascular damage factors in patients with arterial hypertension
Waldemar Wójcik, Sergii Pavlov, Maksat Kalimoldayev in Information Technology in Medical Diagnostics II, 2019
The patients were examined in the dynamics of combined antihypertensive and hypolipidemic therapy before treatment and 1 year after it. A combination of an angiotensin II receptor antagonist, Olmesartan in a daily dose of 20–40 mg and third generation calcium antagonist of prolonged action Lercanidipine in a daily dose of 10–20 mg with addition (if the target arterial pressure levels (AP) less than 140 and 90 mmHg were not reached) of the third drug – a highly selective beta-adrenoblocker with vasodilating activity Nebivolol in a daily dose of 5 mg, was used as antihypertensive therapy. Hypolipidemic therapy was performed with Atorvastatin at a daily dose of 20 mg. Drug therapy was administered against a background of recommendations on hypocaloric diet with restriction of easily digestible carbohydrates, as well as saturated fats and purines.
Women's health—hormone replacement treatment
H. Gavras in The Year in Hypertension 2004, 2004
BACKGROUND. Congenic mRen(2).Lewis rats overexpress renin and exhibit gender differences (male > female) in BP. The effects of oestrogen and the A^ receptor antagonist olmesartan on the congenic mRen(2).Lewis rat were assessed in this study. Ovariectomized rats demonstrated a progressive increase in BP that was attenuated by oestrogen treatment. BP in ovariectomized rats was similar to that of male mRen(2).Lewis rats. Olmesartan essentially normalized BP, an effect that persisted for weeks after withdrawal of treatment. In addition, plasma angiotensin II, ACE activity, renin concentration, and urinary excretion of angiotensin II, 8-isoprostane F2ol, and endothelin-1 were elevated, while renal endothelial nitric oxide synthase (eNOS) mRNA levels were suppressed after ovariectomy. Oestrogen treatment reversed these changes.
Renal system
Pankaj Desai in Pre-eclampsia, 2020
It has been postulated that angiotensin-II may play an essential role in the pathogenesis of pre-eclampsia. In a transgenic mouse model, the mice developed pregnancy-associated hypertension (PAH) by the overproduction of angiotensin-II in maternal circulation during late pregnancy. The Mice with PAH exhibited maternal and foetal abnormalities, such as proteinuria, cardiac hypertrophy, placental morphological changes and IUGR. In one study, to attenuate the activity of redundant renin-angiotensin system during the advanced stages of PAH, olmesartan an angiotensin receptor blocker, was administered, as was captopril, an angiotensin-converting enzyme inhibitor, from 17 to 19 days of gestation, and evaluated for their effects on cardiac and placental abnormalities and foetal growth. Olmesartan and captopril administration lowered the blood pressure of mice with PAH, and placental histological change and severe IUGR were markedly ameliorated in both groups. On the contrary, both treatments had little effect on cardiac remodelling during the advanced stages of PAH. These findings highlight a variety of therapeutic actions of the renin-angiotensin system repression on the progressive pathology of PAH in mice.22
QbD-driven development and evaluation of nanostructured lipid carriers (NLCs) of Olmesartan medoxomil employing multivariate statistical techniques
Published in Drug Development and Industrial Pharmacy, 2018
Sarwar Beg, Sumant Saini, Shantanu Bandopadhyay, O. P. Katare, Bhupinder Singh
Olmesartan medoxomil (OLM) is primarily used as an antihypertensive drug for the treatment of high blood pressure like conditions. It acts blocks vasoconstrictor effect of angiotensin II by selectively blocking its binding with AT1 receptor present on vascular smooth muscles [9]. It is usually prescribed in the dose of 40 mg for management of hypertension in adults. Being a BCS class II drug, OLM exhibits low oral bioavailability (i.e. 28%) as a function of poor aqueous solubility, extensive first-pass effect and P-gp efflux [10,11]. Several drug delivery systems have been explored for improving oral bioavailability of OLM, yet the available formulation lacks potential for holistically addressing its biopharmaceutical challenges. In this regard, we focused on developing NLCs of the selected drug candidate, as lipidic formulations can easily overcome multiple challenges associated with oral bioavailability.
Low-dose Bevacizumab Decreases Ocular Hypotensive Effect of Angiotensin II in Sprague Dawley Rats
Published in Current Eye Research, 2021
J. Skrzypecki, K. Ciepiaszuk, M. Gawryś-Kopczyńska
In contrast to our findings, some researchers postulate that inhibition of angiotensin II receptors, rather than stimulation, lowers IOP. However, studies involving angiotensin II receptor blockers (ARBs) are inconclusive,15,26-28 and industry-sponsored clinical trial investigating topical olmesartan was terminated due to insufficient IOP-lowering effect.29 Nevertheless, it is possible that intake of ARBs has IOP-lowering effect due to decreased production of the aqueous humor in selected patients.12 Notably, these observations are in line with hypothesis that angiotensin II could increase IOP by stimulation of aqueous humor production12 and decrease IOP due to vasoconstriction and reduction of blood supply to the ciliary body.11 Our data does not show any effect of low-dose bevacizumab on BP in rats. These results are in line with majority of clinical studies dealing with low-dose intravitreal injection of bevacizumab. Although both animal and human studies have shown that systemic high-dose anti-VEGF agents have an impact on endothelium, decrease nitric oxide production and lead to hypertension,30 majority of clinical trials on low-dose intravitreal anti-VEGF therapy did not find any interference with BP in a long-term observation.31–33
Development of olmesartan medoxomil lipid-based nanoparticles and nanosuspension: preparation, characterization and comparative pharmacokinetic evaluation
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2018
Arun B., Narendar D., Kishan Veerabrahma
In this study, OM-loaded SLN and NS were developed and characterized. A comparison was made by including different quantities of GMS and stearic acid in SLN preparation. Formulation with very low SA level yielded better SLNs over all, with less size, ZP and EE. The solid-state characterization revealed the transformation of crystalline state of the drug to amorphous form in SLNs. Controlled release and enhanced dissolution were accomplished by incorporating OM into the SLN and NS. The SLN (F10) was rather not stable at RT and 4 °C. The PK studies in rats of optimized SLN and NS showed 7.21- and 3.52-folds improvement in oral bioavailability when compared with coarse suspension, respectively. Hence, these results confirmed the potential of SLN and NS as suitable delivery system for oral delivery of olmesartan in improving the oral bioavailability. In this study, the OM-SLNs were found to be superior in performance than OM-NS.
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