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Interventional Therapies for Essential Hypertension
Published in Giuseppe Mancia, Guido Grassi, Konstantinos P. Tsioufis, Anna F. Dominiczak, Enrico Agabiti Rosei, Manual of Hypertension of the European Society of Hypertension, 2019
Konstantinos P. Tsioufis, Kyriakos Dimitriadis, Alex Kasiakogias, Vassilios Papademetriou
In the Renal Denervation in Hypertension (DENER-HTN) study, 106 patients with resistant hypertension were randomised to either standard stepwise therapy with predetermined doses of certain drugs (indapamide 1.5 mg, remipril 10 mg or irbesartan 300 mg) and amlodipine 10 mg daily for 4 weeks plus spironolactone 25 mg, bisoprolol 10 mg, prazosine 5 mg and rilmenidine 1 mg (53). There was a −5.9 mmHg difference in the daytime ambulatory BP in the RDN group compared to drug therapy at 6 months. In this well-designed trial, the severity of hypertensive disease was less and baseline BP lower than in the Symplicity HTN-2 study population (43,53).
Adrenoceptors: Classification and Distribution
Published in Kenneth J. Broadley, Autonomic Pharmacology, 2017
Further roles for imidazoline receptors are now emerging. Imidazolines, such as efaroxan (see Table 5.2), enhance the rate of insulin secretion from the islets of Langerhans, possibly through I2 receptors (Chan et al. 1994). Clonidine and the selective I1 imidazoline agonist, moxonidine (see Table 4.3), inhibit gastric acid secretion and reduce ethanol-induced gastric mucosal injury (Glavin & Smyth 1995). Moxonidine also induces sodium and water excretion when given centrally (Penner & Smyth 1994). However, peripheral administration of the α2-agonists, rilmenidine (I1) and guanabenz (I2), increased blood pressure and urine excretion via α2-adrenoceptors (Evans & Anderson 1995).
Physiology
Published in Stephen W. Carmichael, Susan L. Stoddard, The Adrenal Medulla 1986 - 1988, 2017
Stephen W. Carmichael, Susan L. Stoddard
Valet, Tran, Damase-Michel et al. (1988) reported that rilmenidine, a new α-adrenoreceptor agonist, decreased sympathetic tone primarily through action on the adrenal medulla. In anesthetized normotensive dogs, this drug decreased heart rate, blood pressure, and catecholamine release from the adrenal medulla. In conscious, sino-aortic denervated dogs, an experimental model of hypertension, the drug significantly decreased cardiovascular parameters and plasma epinephrine and norepinephrine levels.
Recent advances in the combination delivery of drug for leukemia and other cancers
Published in Expert Opinion on Drug Delivery, 2020
Thikrayat Al-Attar, Sundararajan V. Madihally
Some of the available treatment options for CML, apart from chemotherapy, are molecular inhibitors of BCR-ABL pathway and tyrosine kinases such as imatinib mesylate (sold under the trade name Gleevec), nilotinib (Tasigna) and dasatinib (Sprycel). Imatinib (or STI-571) is a BCR-ABL tyrosine kinase inhibitor that is used in CML chemotherapy (3 µM lowers cell metabolism to around 20%) [12]. Reported side effects in 10% of CML patients include mild to moderate nausea, myalgias, edema, fatigue, dyspepsia, diarrhea, and skin reaction [13]. Ocular-related side effects such as abnormal vision and intraocular pressure could occur with 400 mg/day – 800 mg/day Imatinib dosage administration [13]. Skin reactions include superficial edema in 48-65% of cases, and maculopapular eruption ~67% of cases [14]. ABL drug-related mutation has also been reported [15]. Rilmenidine, a selective imidazoline I1 receptor agonist, effect on suppressing cell proliferation has also been studied. Rilmenidine downregulates the BCR-ABL pathway upon binding. With rilmenidine alone, the apoptotic cells percentage was 20%, reaching 42% when used in combination with doxorubicin [16].
Pharmacotherapeutic strategies for treating hypertension in patients with obesity
Published in Expert Opinion on Pharmacotherapy, 2018
Revathy Carnagarin, Vance Matthews, Cynthia Gregory, Markus P. Schlaich
Given the important role of increased sympathetic outflow in the pathogenesis of OHT, it is perhaps surprising that central sympatholytic blockade with imidazoline I1-receptor agonists is not used more frequently in the management of OHT. Some misconceptions may exist relating to the adverse effects of older central sympatholytic agents such as clonidine or α-methyldopa, which were commonly associated with tiredness, sedation, and rebound hypertension when ceased (clonidine). The newer imidazoline I1-receptor agonists such as moxonidine and rilmenidine have been demonstrated to be well tolerated and effective in lowering BP. In contrast to clonidine which binds to central α2 receptors, the newer agents bind to the Imidazoline I1-receptor thereby largely avoiding the clonidine like side effects [66,67]. However, a dry mouth sensation can occur in up to 10% of patients on moxonidine due to its inhibitory effect on salivary flow [68]. From a metabolic perspective, moxonidine has been demonstrated to enhance insulin sensitivity, as shown with an insulin clamp technique in obese spontaneously hypertensive rats [69]. In addition to BP lowering, moxonidine treatment improves insulin sensitivity in patients with obesity hypertension [70]. The BP-lowering effect of moxonidine was comparable to amlodipine, but with additional effects such as the improvement of insulin resistance, reduction of plasma leptin levels and attenuation of sympathetic overdrive [71].
Responsiveness of α2-adrenoceptor/I1-imidazoline receptor in the rostral ventrolateral medulla to cardiovascular regulation is enhanced in conscious spontaneously hypertensive rat
Published in Clinical and Experimental Hypertension, 2019
Masanobu Yamazato, Minori Nakamoto, Atsushi Sakima, Yoriko Yamazato, Shuichi Takishita, Yusuke Ohya
Cardiovascular and sympathetic responses to various drugs are influenced by anesthetics. Urethane attenuates the cardiovascular responses to central α2-adrenoceptor stimulation (10) and the sympathetic responses to stimulation or inhibition of RVLM neurons by injection of amino acids into the RVLM (11). Anesthesia with sodium pentobarbital and propofol was shown to enhance the cardiovascular effects of rilmenidine and clonidine in rats (9,12). Thus, there is a need to characterize the effects of clonidine in a conscious state. We previously reported that clonidine injected into the RVLM of conscious normotensive rats decreased the blood pressure, heart rate (HR), and renal sympathetic nerve activity (RSNA) and induced sedation via the α2-adrenoceptor mechanisms (9).