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Drugs Affecting Storage and Release from Sympathetic Neurones
Published in Kenneth J. Broadley, Autonomic Pharmacology, 2017
Guanabenz undergoes extensive first-pass metabolism in the liver and has a half-life of <12 hr. The side-effects are similar to those of clonidine, with dry mouth and sedation being sufficiently troublesome to necessitate discontinuation of therapy. It is therefore of little advantage over other newer antihypertensive agents (Holmes et al. 1983).
Diagnosis and Management of Hypertension in Pediatrics
Published in Sam Kacew, Drug Toxicity and Metabolism in Pediatrics, 1990
Clonidine is rapidly absorbed from the GI tract. Nearly one half of an oral dose of clonidine is metabolized in the liver and the other half is excreted unchanged in the urine.70 The usual starting dosage of clonidine is 0.005 to 0.01 mg/kg/d in a twice-a-day dosage format. The drug can be increased to a maximum of 0.9 mg/d. Falkner and co-workers71 have also demonstrated the effectiveness of transdermally administered clonidine in normalizing blood pressure in 22 adolescents. The advantage of transdermal clonidine is that the clonidine transdermal patch needs to be placed only once a week.72 Guanabenz and guanfacine are other centrally acting antihypertensive agents that are used in adults, but there is limited information on their use in the child.
Targeting the integrated stress response in ophthalmology
Published in Current Eye Research, 2021
Hsiao-Sang Chu, Cornelia Peterson, Albert Jun, James Foster
Dephosphorylation of eIF2α is the key step of ISR termination and restoration of protein synthesis for normal cellular functions. As shown in Figures 1 and 3, in mammals, two phosphatases are responsible for the dephosphorylation of peIF2α, the CReP63 and GADD34.145 As the name suggested, CReP normally operates in unstressed cells for maintaining low level of peIF2α. While GADD34 expression is induced by ATF4 and CHOP, and acts as a negative feedback loop to resume protein synthesis once the stress is relieved.64 Salubrinal and its analogue SAL003, are inhibitors of both GADD34 and CReP.123,146 Guanabenz and its derivative, Sephin 1 are known to inhibit GADD34.146 Nelfinavir, a HIV protease inhibitor downregulates CReP and increases peIF2α.147 Among these peIF2α phosphatase inhibitors, salubrinal has been shown to result in high levels of peIF2α. It has also been demonstrated that salubrinal blocked the replication of HSV in cell culture models.148,149 In vitro, Salubrinal treatment protects trabecular meshwork cells against ER stress150 and RPE cells against toxins.151,152 However, we found SAL003 stimulates the ISR and leads to apoptosis of normal fibroblasts cultivated from donor corneas.123
Recent advances in cellular models for discovering prion disease therapeutics
Published in Expert Opinion on Drug Discovery, 2022
Lea Nikolić, Chiara Ferracin, Giuseppe Legname
Importantly, guanabenz, an agonist of α2-adrenergic receptors, was for the first time discovered as an anti-prion agent through a yeast-based assay. The anti-prion activity of guanabenz was further substantiated in ovine PrPSc- infected immortalized cells. More importantly, in vivo treatment of scrapie-infected transgenic mice (Tg338) resulted in decreased PrPres levels. This indicates that some biochemical pathways controlling prion formation and/or degradation may be conserved between mammals and yeasts [115].
Serum catestatin level is increased in women with preeclampsia
Published in Journal of Obstetrics and Gynaecology, 2022
Nevin Tüten, Onur Güralp, Koray Gök, Kübra Hamzaoglu, Yahya Ozgün Oner, Melike Makul, Huri Bulut, Kübra Irmak, Abdullah Tüten, Eduard Malik
CgA is known as a neuroendocrine tumour marker. However, increased CgA levels have also been associated with cardiovascular diseases (Goetze et al. 2014). O’Connor first found that CgA levels were elevated in both primary and secondary hypertensive patients (O'Connor 1984). The blockade of the sympathetic nervous system with guanabenz led to a decrease in the level of circulating CgA. This finding indicates that increased sympathoadrenal activity in primary hypertension is closely associated with CgA levels (O’Connor 1985).