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Adrenoceptor Antagonists
Published in Kenneth J. Broadley, Autonomic Pharmacology, 2017
Celiprolol (CelectolR) has been refered to as a ‘third generation’ β1-selective antagonist, in that it has additional vasodilator properties. The vasodilator activity appears to be due to β2-adrenoceptor partial agonist activity, making it a novel compound if it selectively blocks atβ1-adrenoceptors yet selectively stimulates at β2-adrenoceptors (Dhein et al. 1992). It effectively lowers blood pressure but there is some doubt as to whether the ISA is truly selective for β2-adrenoceptors in man (Wheeldon et al. 1992).
Role of hesperidin and fresh orange juice in altering the bioavailability of beta-blocker, metoprolol tartrate. An in vivo model
Published in Xenobiotica, 2022
Rabiha Salam, Syeda Nayyab Batool Rizvi, Naqi Hussain, Shama Firdous, Muhammad Zaheer, Muhammad Naeem
Results showed that hesperidin significantly increased the AUC of MT by 68.3% in comparison to the control group (p < 0.01), which is in agreement with Piao and Choi (2008) in which hesperidin increased the oral bioavailability of verapamil in rats (Piao and Choi 2008). Similar to MT, verapamil is also a substrate of the cytochrome p450 enzyme system and undergoes extensive first-pass metabolism. A study conducted in 2008 showed a marked decrease in the bio-absorption of celiprolol when injected along with hesperidin into the rat duodenum (Uesawa and Mohri 2008). Celiprolol is a substrate of intestinally expressed OATP subtypes (OATP1A2 and OATP2B1) and hesperidin was found to significantly inhibit OATP1A2 activity, however, the inhibition caused by hesperidin is less than that of naringin (Bailey et al. 2007). MT being extensively metabolised, the lipophilic drug may have a reduced vulnerability to OATP-mediated interactions. The increased bioavailability of MT with hesperidin administration may probably be the result of decreased intestinal CYP2D6 metabolism (Figure 3).
Pharmacological resources, diagnostic approach and coordination of care in joint hypermobility-related disorders
Published in Expert Review of Clinical Pharmacology, 2018
Studies on EDS reveal a wider array of CV manifestations in hereditary soft connective tissue disorders. Vascular EDS is dominated with a restricted quantity of life due to an increased risk of sudden death for ruptures of the middle arteries [69]. A single multicenter, randomized, open trial on 53 vascular EDS adults suggests that celiprolol (a specific β-blocker) reduces the risk of adverse vascular events in these patients. Celiprolol was administered twice daily and uptritated by 100 mg steps every 6 months up to 400 mg/day [70]. A similar approach seems reasonable also in other EDS variants with increased vascular fragility.
Diverse pharmacological properties, trial results, comorbidity prescribing and neural pathophysiology suggest European hypertension guideline downgrading of beta-blockers is not justified
Published in Blood Pressure, 2022
Murray Esler, Sverre E. Kjeldsen, Atul Pathak, Guido Grassi, Reinhold Kreutz, Giuseppe Mancia
Some beta-blockers (acebutolol, celiprolol, labetalol, oxprenolol and pindolol) cause beta-adrenoceptor stimulation (variously β-1 or β-2), in parallel with β-receptor blockade. Beta-blockers with intrinsic agonist activity lower heart rate less than other beta-blockers and exhibit direct vasodilator actions [31,32,37].