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Štefan Farský, Andrea Strišková, Marián Borčin
We have analysed the database of 1,595 consecutive patients visiting our department of cardiology and internal medicine clinic in 2005-2014. The analysis included 13,990 visit records, and the average number of visits per patient was 8.5 ± 7.0. Our goals were to evaluate the effectivity of hypertension treatment as for drug choice, decrease of sBP and dBP associated with a certain drug, a drug combination, and therapeutic inertia in patients with metabolic syndrome and/or diabetes mellitus. The final number of patients for analysis who fulfilled the inclusion criteria for interpenetration of both diagnostic circles was 570...
2018: Cardiology Research and Practice
Nesreen M I M Elkomy, Islam A A E-H Ibrahim, Shimaa M Elshazly, Hassan M El-Fayoumi
Chronic alcoholism is a risk factor for kidney injury. Clonidine is an α2 -adrenergic receptor/imidazoline-1 receptor agonist that can reduce blood pressure and maintain renal functions. This study aims to investigate the possible ameliorative effects of clonidine on ethanol induced kidney injury and its mechanism of action. Kidney injury was induced in rats by adding ethanol to drinking water for eight weeks. Clonidine effects on kidney functions and histopathology were measured. Moreover, phentolamine (α-adrenergic receptor antagonist), efaroxan (imidazoline-1 receptor antagonist) and rilmenidine (imidazoline-1 receptor agonist) were used to clarify the role of imidazoline-1 receptor in mediating renal ameliorative effects...
April 5, 2018: European Journal of Pharmacology
Benjamin R Underwood, Zeyn W Green-Thompson, Peter J Pugh, Stanley E Lazic, Sarah L Mason, Jules Griffin, P Simon Jones, James B Rowe, David C Rubinsztein, Roger A Barker
Preclinical data have shown that rilmenidine can regulate autophagy in models of Huntington's disease (HD), providing a potential route to alter the disease course in patients. Consequently, a 2-year open-label study examining the tolerability and feasibility of rilmenidine in mild-moderate HD was undertaken. 18 non-demented patients with mild to moderate HD took daily doses of 1 mg Rilmenidine for 6 months and 2 mg for a further 18 months followed by a 3-month washout period. The primary outcome was the number of withdrawals and serious adverse events...
December 2017: Journal of Neurology
Nirma D Perera, Rebecca K Sheean, Chew L Lau, Yea Seul Shin, Philip M Beart, Malcolm K Horne, Bradley J Turner
Macroautophagy/autophagy is the main intracellular catabolic pathway in neurons that eliminates misfolded proteins, aggregates and damaged organelles associated with ageing and neurodegeneration. Autophagy is regulated by both MTOR-dependent and -independent pathways. There is increasing evidence that autophagy is compromised in neurodegenerative disorders, which may contribute to cytoplasmic sequestration of aggregation-prone and toxic proteins in neurons. Genetic or pharmacological modulation of autophagy to promote clearance of misfolded proteins may be a promising therapeutic avenue for these disorders...
2018: Autophagy
Linda D Mercer, Gavin C Higgins, Chew L Lau, Andrew J Lawrence, Philip M Beart
Toxicity of 3,4-methylenedioxymethamphetamine (MDMA) towards biogenic amine neurons is well documented and in primate brain predominantly affects serotonin (5-HT) neurons. MDMA induces damage of 5-HT axons and nerve fibres and intracytoplasmic inclusions. Whilst its pathobiology involves mitochondrially-mediated oxidative stress, we hypothesised MDMA possessed the capacity to activate autophagy, a proteostatic mechanism for degradation of cellular debris. We established a culture of ventral pons from embryonic murine brain enriched in 5-HT neurons to explore mechanisms of MDMA neurotoxicity and recruitment of autophagy, and evaluated possible neuroprotective actions of the clinically approved agent rilmenidine...
May 2017: Neurochemistry International
Kyungjoon Lim, Kristy L Jackson, Sandra L Burke, Geoffrey A Head
The surge in arterial pressure during arousal in the waking period is thought to be largely due to activation of the sympathetic nervous system. In this study we compared in SHR the effects of chronic administration of the centrally acting sympatholytic agent rilmenidine with an angiotensin converting enzyme inhibitor perindopril on the rate of rise and power of the surge in mean arterial pressure (MAP) that occurs with arousal associated with the onset of night. Recordings were made using radiotelemetry in 17 adult SHR before and after treatment with rilmenidine (2mg/kg/day), perindopril (1mg/kg/day) or vehicle in the drinking water for 2 weeks...
2016: PloS One
Monique L Parkin, Kyungjoon Lim, Sandra L Burke, Geoffrey A Head
We investigated the effects of chronic subcutaneous treatment with centrally-acting antihypertensive agents moxonidine, rilmenidine, and clonidine on the baroreflex control of heart rate (HR) in conscious normotensive rabbits over 3 weeks. Infusions of phenylephrine and nitroprusside were performed at week 0 and at weeks 1 and 3 of treatment to determine mean arterial pressure (MAP)-HR baroreflex relationships. A second curve was performed after intravenous methscopolamine to determine the sympathetic baroreflex relationship...
2016: Frontiers in Physiology
Ágnes Fehér, Viktória E Tóth, Mahmoud Al-Khrasani, Mihály Balogh, Bernadette Lázár, Zsuzsanna Helyes, Klára Gyires, Zoltán S Zádori
Imidazoline receptors (IRs) have been recognized as promising targets in the treatment of numerous diseases; and moxonidine and rilmenidine, agonists of I1-IRs, are widely used as antihypertensive agents. Some evidence suggests that IR ligands may induce anti-inflammatory effects acting on I1-IRs or other molecular targets, which could be beneficial in patients with inflammatory bowel disease (IBD). On the other hand, several IR ligands may stimulate also alpha2-adrenoceptors, which were earlier shown to inhibit, but in more recent studies to rather aggravate colitis...
February 2017: Inflammopharmacology
Renan B Ferreira, Mariana G de Oliveira, Edson Antunes, Wanda P Almeida, Badr M Ibrahim, Abdel A Abdel-Rahman
2-Aminothiazolines share an isosteric relationship with imidazolines and oxazolines with antihypertensive activity mainly mediated by the imidazoline I1-receptor. In the present work, we have prepared five aminothiazolines, following a previously described synthetic pathway. Aminothiazolines derived from dicyclopropylmethylamine (ATZ1) and cyclohexylamine (3) are unprecedented in the literature. Competitive radioligand assay was carried out with all synthetic compounds, and the I1 receptor affinity in comparison to rilmenidine in PC12 cells was determined...
November 15, 2016: European Journal of Pharmacology
Michel Azizi, Helena Pereira, Idir Hamdidouche, Philippe Gosse, Matthieu Monge, Guillaume Bobrie, Pascal Delsart, Claire Mounier-Véhier, Pierre-Yves Courand, Pierre Lantelme, Thierry Denolle, Caroline Dourmap-Collas, Xavier Girerd, Jean Michel Halimi, Faiez Zannad, Olivier Ormezzano, Bernard Vaïsse, Daniel Herpin, Jean Ribstein, Bernard Chamontin, Jean-Jacques Mourad, Emile Ferrari, Pierre-François Plouin, Vincent Jullien, Marc Sapoval, Gilles Chatellier
BACKGROUND: The DENERHTN trial (Renal Denervation for Hypertension) confirmed the blood pressure-lowering efficacy of renal denervation added to a standardized stepped-care antihypertensive treatment for resistant hypertension at 6 months. We report the influence of adherence to antihypertensive treatment on blood pressure control. METHODS: One hundred six patients with hypertension resistant to 4 weeks of treatment with indapamide 1.5 mg/d, ramipril 10 mg/d (or irbesartan 300 mg/d), and amlodipine 10 mg/d were randomly assigned to renal denervation plus standardized stepped-care antihypertensive treatment, or the same antihypertensive treatment alone...
September 20, 2016: Circulation
Jelica Vucicevic, Tatjana Srdic-Rajic, Marco Pieroni, Jonne M M Laurila, Vladimir Perovic, Sabrina Tassini, Elisa Azzali, Gabriele Costantino, Sanja Glisic, Danica Agbaba, Mika Scheinin, Katarina Nikolic, Marco Radi, Nevena Veljkovic
The clonidine-like central antihypertensive agent rilmenidine, which has high affinity for I1-type imidazoline receptors (I1-IR) was recently found to have cytotoxic effects on cultured cancer cell lines. However, due to its pharmacological effects resulting also from α2-adrenoceptor activation, rilmenidine cannot be considered a suitable anticancer drug candidate. Here, we report the identification of novel rilmenidine-derived compounds with anticancer potential and devoid of α2-adrenoceptor effects by means of ligand- and structure-based drug design approaches...
July 15, 2016: Bioorganic & Medicinal Chemistry
Alessandro R Nascimento, Marcus V Machado, Fabiana Gomes, Aline B Vieira, Cassiano F Gonçalves-de-Albuquerque, Marcos A Lessa, Pascal Bousquet, Eduardo Tibiriçá
OBJECTIVES: The objective of this study was to investigate the role of the SNS on hemodynamic, metabolic, and microvascular alterations in a rat model of HFD-induced MS with salt supplementation. METHODS: In total, 40 adult male Wistar rats were fed normal chow (n = 10) or a HFD (n = 30) for 20 weeks. Thereafter, the HFD group received the centrally acting sympatho-modulatory drugs clonidine (0.1 mg/kg) or rilmenidine (1 mg/kg) or vehicle (n = 10/group) orally by gavage...
May 2016: Microcirculation: the Official Journal of the Microcirculatory Society, Inc
Tatjana Srdic-Rajic, Katarina Nikolic, Milena Cavic, Ivana Djokic, Branislava Gemovic, Vladimir Perovic, Nevena Veljkovic
Imidazoline I1 receptor signaling is associated with pathways that regulate cell viability leading to varied cell-type specific phenotypes. We demonstrated that the antihypertensive drug rilmenidine, a selective imidazoline I1 receptor agonist, modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells. Rilmenidine acts through a mechanism which involves deactivation of Ras/MAP kinases ERK, p38 and JNK...
January 1, 2016: European Journal of Pharmaceutical Sciences
V Forni Ogna, E Pereira, M Sapoval, M Azizi
OBJECTIVE: The French DENERHTN trial has shown that renal denervation (RDN, Symplicity Catheter) in addition to standardized optimal medical treatment (SOMT) decreases ambulatory BP more (6 mmHg) than the same SOMT alone at 6 months in patients (pts) with resistant hypertension (RH). However, some pts did not respond to RDN or SOMT at 6 months. The aim of the study was to determine the prevalence and characteristics of refractory hypertension (RFH) to more than 5 antihypertensive treatments at 6 months in the 2 groups...
June 2015: Journal of Hypertension
Michel Azizi, Marc Sapoval, Philippe Gosse, Matthieu Monge, Guillaume Bobrie, Pascal Delsart, Marco Midulla, Claire Mounier-Véhier, Pierre-Yves Courand, Pierre Lantelme, Thierry Denolle, Caroline Dourmap-Collas, Hervé Trillaud, Helena Pereira, Pierre-François Plouin, Gilles Chatellier
BACKGROUND: Conflicting blood pressure-lowering effects of catheter-based renal artery denervation have been reported in patients with resistant hypertension. We compared the ambulatory blood pressure-lowering efficacy and safety of radiofrequency-based renal denervation added to a standardised stepped-care antihypertensive treatment (SSAHT) with the same SSAHT alone in patients with resistant hypertension. METHODS: The Renal Denervation for Hypertension (DENERHTN) trial was a prospective, open-label randomised controlled trial with blinded endpoint evaluation in patients with resistant hypertension, done in 15 French tertiary care centres specialised in hypertension management...
May 16, 2015: Lancet
Haya Abu Ghazaleh, Maggie D Lalies, David J Nutt, Alan L Hudson
Harmane is an active component of clonidine displacing substance and a candidate endogenous ligand for imidazoline binding sites. The neurochemistry of tritiated harmane was investigated in the present study examining its uptake and release properties in the rat brain central nervous system (CNS) in vitro. At physiological temperature, [(3)H]harmane was shown to be taken up in rat brain cortex. Further investigations demonstrated that treatment with monoamine uptake blockers (citalopram, nomifensine and nisoxetine) did not alter [(3)H]harmane uptake implicating that the route of [(3)H]harmane transport was distinct from the monoamine uptake systems...
March 17, 2015: Neuroscience Letters
Suleyman Salman, Serkan Kumbasar, Nesrin Gursan, Yakup Kumtepe, Bunyamin Borekci, Beyzagul Polat, Hamit Hakan Alp, Mustafa Talip Sener, Halis Suleyman
BACKGROUND: In this study, we investigated the effects of treatment with chronic antihypertensive drugs (clonidine, methyldopa, amlodipine, ramipril and rilmenidine) on oxidant-antioxidant parameters and toxic effects on DNA in rat uterus tissue. In addition, uterus tissues were examined histopathologically. MATERIALS AND METHODS: A total of 36 albino Wistar rats were divided into the following six groups: 0.075 mg/kg clonidine group; 100 mg/kg methyldopa group; 2 mg/kg amlodipine group; 2...
July 2011: International Journal of Fertility & Sterility
Kristy L Jackson, Kesia Palma-Rigo, Thu-Phuc Nguyen-Huu, Pamela J Davern, Geoffrey A Head
OBJECTIVE: BPH/2J hypertensive mice have an exaggerated sympathetic contribution to blood pressure (BP). Premotor sympathetic neurons within the rostroventrolateral medulla (RVLM) are a major source of sympathetic vasomotor tone and major site of action of the centrally acting sympatholytic agent, rilmenidine. The relative cardiovascular effect of rilmenidine in BPH/2J versus normotensive BPN/3J mice was used as an indicator of the involvement of the RVLM in the sympathetic contribution to hypertension in BPH/2J mice...
March 2014: Journal of Hypertension
H H Chung, J- T Cheng
Imidazoline I1-receptor (I1R) is known to regulate the blood pressure, and rilmenidine, as the agonist, is used to treat hypertension in clinics. However, the role of I1R in obesity is still unclear. In the present study, we investigated the changes of obesity by activation of I1R in high fat diet (HFD)-fed mice. Chronic administration of rilmenidine into HFD-fed mice for 8 weeks significantly reduced body weight, which was reversed by efaroxan at the dose sufficient to block I1R. Also, rilmenidine significantly decreased the energy intake of HFD-fed mice...
August 2013: Hormone and Metabolic Research, Hormon- und Stoffwechselforschung, Hormones et Métabolisme
Zoltán S Zádori, Ágnes Fehér, Mahmoud Al-Khrasani, Erzsébet Lackó, Viktória E Tóth, Serena B Brancati, Lutz Hein, Péter Mátyus, Klára Gyires
Several lines of evidence suggest that imidazoline receptors mediate various physiological processes. It is rather difficult, however, to distinguish the imidazoline receptor-mediated effects from the alpha₂-adrenoceptor-mediated ones due to the reasonable affinity of most imidazoline ligands for the alpha₂-adrenoceptors. In the present study the effects of different imidazoline ligands were tested on the electrical field stimulation (EFS)-induced gastric contractions in wild-type (WT), alpha₂A-, alpha₂B- and alpha₂C-adrenoceptor knockout (KO) mice in order to analyze, whether imidazoline I₁ and I₂ receptors take part in the regulation of gastric motor activity...
April 5, 2013: European Journal of Pharmacology
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