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Adrenergic Agonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
These are compounds with a catechol nucleus (benzene ring containing two hydroxy groups in the third and fourth position) and an amine containing side chain attached to it (Katzung et al., 2014). The natural or endogenous catecholamines are adrenaline, noradrenaline, and dopamine (Brunton et al., 2011). The synthetic catecholamines available are isoprenaline (Rang et al., 2007), dobutamine, dopexamine, dipivefrine.
Dopaminergic Prodrugs
Published in M.D. Francesco Amenta, Peripheral Dopamine Pathophysiology, 2019
Cesare Casagrande, Francesco Santangelo
There are only two examples of adrenergic prodrugs which have demonstrated clinical usefulness; both have been developed for topical application. Dipivefrine (Figure 1), the dipivaloyl ester of dl-epinephrine is instilled in the eyes for the treatment of glaucoma;5 bitolterol (Figure 1), the di-p-toluyl ester of colterol (N-t-butyl-dl-norepinephrine), has recently been introduced as a long-lasting bronchodilator when administered by inhalation.6 On the other hand, levodopa (Figure 1), a milestone in the therapy of Parkinson’s disease,7 has to be considered, when administered exogenously, a DA prodrug, activated by the same enzyme, i.e., l-dopa decarboxylase, or aromatic l-aminoacid decarboxylase, which acts on the endogenous precursor in the sequence of events converting phenylalanine into the catecholamines; its delivery through the blood-brain barrier is dependent upon the facilitated transport system of large neutral amino acids. A degree of central nervous system (CNS) selectivity is achieved by the coadministration of a peripheral inhibitor of the decarboxylase, such as carbidopa or benserazide.
Adrenergic agonists and antagonists as antiglaucoma agents: a literature and patent review (2013–2019)
Published in Expert Opinion on Therapeutic Patents, 2019
Alessio Nocentini, Claudiu T. Supuran
The combination of a β-blocker with epinephrine did not result in a clinical useful additional effect on IOP reduction [49]. The combination of levobunolol with dipivefrine showed only a modest additional IOP reduction. In contrast, combining β1-selective betaxolol with dipivefrine or epinephrine resulted in a significant additional reduction of IOP, because of an increase of conventional outflow facility [49,50].