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Metoprolol was synthesized and its activity discovered in 1969. [12] The specific agent in on-market formulations of metoprolol is either metoprolol tartrate or metoprolol succinate, where tartrate is an immediate-release formulation and the succinate is an extended-release formulation (with 100 mg metoprolol tartrate corresponding to 95 mg ...
Nebivolol is a beta blocker used to treat high blood pressure and heart failure. [5] As with other β-blockers, it is generally a less preferred treatment for high blood pressure. [ 6 ] It may be used by itself or with other blood pressure medication. [ 6 ]
metoprolol tartrate 319. metrizamide 320. metronidazole 321. mexiletine hydrochloride ... nebivolol 351. nebumetone 352. nelfinavir mesilate 353. netilmicin sulphate ...
[14] [15] [16] Bisoprolol, carvedilol, and sustained-release metoprolol are specifically indicated as adjuncts to standard ACE inhibitor and diuretic therapy in congestive heart failure, although at doses typically much lower than those indicated for other conditions. Beta blockers are only indicated in cases of compensated, stable congestive ...
Metoprolol; Nebivolol; β 2-selective agents Butaxamine (weak α-adrenergic agonist activity) - No common clinical applications, but used in experiments. ICI-118,551 Highly selective β 2-adrenergic receptor antagonist - No known clinical applications, but used in experiments due to its strong receptor specificity.
The β-blockers are an immensely important class of drugs due to their high prevalence of use. The discovery of β-blockers reaches back to more than 100 years ago, when early investigators came up with the idea that catecholamines were binding selectively to receptor-like structures and that this was the cause of their pharmacological actions. [3]
[113] [114] Interactions with other CYP2D6 substrates, such as metoprolol, imipramine, nortriptyline, [114] venlafaxine, [109] and nebivolol [2] have also been reported. However, in a notable exception, bupropion does not seem to affect the concentrations of CYP2D6 substrates fluoxetine and paroxetine.
Betaxolol also shows greater affinity for beta 1 receptors than metoprolol. In addition to its effect on the heart, betaxolol reduces the pressure within the eye (intraocular pressure). This effect is thought to be caused by reducing the production of the liquid (which is called the aqueous humor) within the eye. The precise mechanism of this ...