Disease relevance of Selectol

• Accordingly, a randomized, double-blind, cross-over placebo-controlled study was performed to assess the efficacy of celiprolol, a new cardioselective beta-blocker with partial intrinsic sympathomimetic activity, on exercise performance in nine men with chronic atrial fibrillation [1].
• Effects of celiprolol on cardiovascular reactivity to laboratory stressors in patients with hypertension [2].
• Acute haemodynamic profile of celiprolol in patients with coronary heart disease and hypertension: a double-blind comparison with metoprolol [3].
• Celiprolol. A preliminary review of its pharmacodynamic and pharmacokinetic properties and its therapeutic use in hypertension and angina pectoris [4].
• Significant inhibition of exercise tachycardia occurs 24 hours after a single oral dose of celiprolol [4].

Psychiatry related information on Selectol

• Our data suggest that in the majority of treated patients celiprolol is effective in reducing blood pressure not only at rest but also during a variety of stressful events, thereby ameliorating the impact of recurring stress-induced increases of blood pressure on the cardiovascular system [2].
• The apnea-hypopnea index was similar under celiprolol and placebo (48 +/- 7.4 vs 53 +/- 7.8, respectively), as were the total sleep time and percent of duration of the different sleep stages [5].
• Propranolol, celiprolol and atenolol also increased duration of wakefulness [6].
• Also patient compliance was better for celiprolol than for atenolol [7].
• Celiprolol, a beta-adrenoceptor antagonist with vasodilator effect, improves hemodynamic response to catecholamine, spontaneous locomotor activity, and survival in cardiomyopathic hamsters with advanced heart failure [8].

High impact information on Selectol

• These results indicate that chronic treatment with high D-glucose concentrations leads to an impairment of calcium signaling, which might be ameliorated by celiprolol [9].
• Heart rate, blood pressure and gas exchange variables were measured at rest and during treadmill exercise testing while the patients were receiving maintenance celiprolol or placebo [1].
• Significant reductions in heart rate and systolic blood pressure compared with control values were observed at submaximal exercise, at the gas exchange anaerobic threshold and at maximal exertion while the patients were taking celiprolol [1].
• However, oxygen uptake at the gas exchange anaerobic threshold during celiprolol therapy was 12.3 versus 14.0 ml oxygen/kg per min during placebo administration (a 12% difference, p less than 0.01) [1].
• Our objective was to investigate the effect of orange juice on the pharmacokinetics of celiprolol in healthy subjects [10].

Chemical compound and disease context of Selectol

• In preliminary therapeutic trials celiprolol 200 to 600mg once daily was similar in efficacy to propranolol 40mg to 80mg twice daily or atenolol 100mg once daily in patients with mild to moderate hypertension or angina pectoris [4].
• Similar doses of celiprolol are as efficacious as propranolol and atenolol in improving exercise tolerance and reducing the frequency of anginal attacks in patients with angina pectoris [11].
• Comparison of celiprolol and propranolol in stable angina pectoris. Celiprolol International Angina Study Group [12].
• In contrast, prostaglandin E1 and forskolin exposure lead to a similar increase in pertussis toxin-catalyzed ADP-ribosylation of about 40 kDa G-proteins as isoproterenol exposure whereas treatment with propranolol, celiprolol and xamoterol had no or only a very small effect on pertussis toxin substrates [13].
• Effects of celiprolol on plasma renin, aldosterone, norepinephrine and epinephrine in primary hypertension [14].

Biological context of Selectol

• Celiprolol is a 'third generation' beta-blocking agent which is claimed to avoid problems associated with simpler beta-blockers, such as vasoconstriction, bronchoconstriction and myocardial depression [3].
• Orange juice substantially reduces the bioavailability of the beta-adrenergic-blocking agent celiprolol [10].
• Celiprolol increased cardiac and stroke volume indices and the EF; the PAOP was reduced without change in other measured variables [15].
• The metabolic effects of celiprolol, a new beta-adrenoceptor blocking agent with intrinsic sympathomimetic activity and alpha 2-blocking properties, were evaluated in a series of patients with hypertension, both with and without hyperlipidemia [16].
• Some studies suggest that celiprolol, because of vasodilation, may be less likely to reduce blood flow to the peripheries than other beta-adrenoceptor blocking drugs and hence cause fewer peripheral vascular side effects [4].

Anatomical context of Selectol

• CONCLUSIONS: Unlike other beta receptor blockers (or any other agent studied in the SHR), celiprolol was effective in reducing mass of right and left ventricles and of aorta; decreasing mean arterial pressure through a fall in total peripheral resistance; and improving left ventricular function and aortic distensibility in the SHR [17].
• 1. The transepithelial transport of the beta-adrenoceptor blocking drug, celiprolol, was investigated in monolayers of the well differentiated human intestinal epithelial cell line, Caco-2 [18].
• Transport of celiprolol across human intestinal epithelial (Caco-2) cells: mediation of secretion by multiple transporters including P-glycoprotein [18].
• Release of endothelial nitric oxide in coronary arteries by celiprolol, a beta(1)-adrenoceptor antagonist: possible clinical relevance [19].
• Vasodilatation results from the reduction in vascular resistance of skeletal muscle tissues, but celiprolol also produces dilatation of vascular areas such as the kidney [20].

Associations of Selectol with other chemical compounds

• Both drugs exerted a similar hypotensive effect after gradual dose adjustment; however, propranolol reduced heart rate to a higher extent (-20.5%) than celiprolol (-7.7%) [16].
• OBJECTIVES: Our objective was to evaluate the effects of itraconazole and grapefruit juice on the pharmacokinetics of the beta-adrenergic receptor-blocking agent celiprolol in healthy volunteers [21].
• Six weeks of treatment with carvedilol, N-696, celiprolol, dilevalol, acebutolol, urapidil, doxazosin and altiopril reduced blood pressure with various changes in heart rate [22].
• The effects on sleep of six beta-adrenergic blockers (propranolol, dilevalol, pindolol, metoprolol, celiprolol and atenolol) which differ in their pharmacological characteristics were studied in spontaneously hypertensive rats [6].
• 8. Plasma concentrations for celiprolol and bisoprolol usually achieved in vivo were below the IC50 value obtained in vitro [23].

Gene context of Selectol

• Only minor changes in P-glycoprotein activity were observed when the metabolically stable P-glycoprotein substrate celiprolol was used [24].
• Upregulated preproendothelin-1, endothelin ET(A) receptor, TGF-beta(1), c-fos, and type I collagen expression and extracellular signal-regulated kinase activities were suppressed by celiprolol [25].
• Celiprolol inhibits mitogen-activated protein kinase and endothelin-1 and transforming growth factor-beta(1) gene in rats [25].
• However, the changes after 12 weeks treatment were different (p less than 0.05) between the groups, leading to lower levels of plasma esterified cholesterol, low-density lipoprotein (LDL) cholesterol and apoprotein AI, AII, and B in the celiprolol group [26].
• We examined the effects of long-term treatment with celiprolol, a specific beta1-antagonist with a weak beta2-agonist action, on eNOS expression in the left ventricle and evaluated its relationship to myocardial remodeling in the left ventricle of deoxycorticosterone acetate (DOCA)-salt hypertensive rats [27].

Analytical, diagnostic and therapeutic context of Selectol

• To test whether this criterion is fulfilled by celiprolol, a new beta 1-selective adrenergic blocker drug with peripheral vasodilating activity, we examined the effects of its oral administration on cardiovascular reactivity to laboratory stressors in 18 patients with essential hypertension, according to a placebo-controlled crossover design [2].
• If the apparent pharmacodynamic advantages of celiprolol translate into clinical benefits and are confirmed in well designed long term clinical trials, then celiprolol should represent a definite advance in beta-blocker therapy [11].
• The effects of a beta-blocker, celiprolol, on sleep and arterial blood pressure (BP) were evaluated during a single-blind study in seven hypertensive patients with sleep apnea [5].
• Diurnal ambulatory BP measurements with an automatic cuff-inflation device and polysomnography with simultaneous Finapres BP recording were performed separately on consecutive days at the end of two 21-day treatment periods involving placebo followed by celiprolol (200 mg/day) [5].
• Experimental design for enantioselective separation of celiprolol by capillary electrophoresis using sulfated beta-cyclodextrin [28].

References