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Metoprolol is a beta blocker, or an antagonist of the β-adrenergic receptors. It is specifically a selective antagonist of the β 1-adrenergic receptor and has no intrinsic sympathomimetic activity. [37] Metoprolol exerts its effects by blocking the action of certain neurotransmitters, specifically adrenaline and noradrenaline.
The drug is highly cardioselective at 5 mg. [19] In addition, at doses above 10 mg, nebivolol loses its cardioselectivity and blocks both β1 and β2 receptors, [18] while the recommended starting dose of nebivolol is 5 mg, sufficient control of blood pressure may require doses up to 40 mg. [18] Furthermore, nebivolol is also not ...
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 ...
Bisoprolol is eliminated from the body in two ways - 50% of the substance is converted in the liver to inactive metabolites, which are then excreted in the kidneys. The remaining 50% is eliminated unchanged via the kidneys. [49] Since elimination is equal in liver and kidney, no dose adjustment is required in patients with hepatic or renal ...
Atenolol is available in the form of 25, 50, and 100 mg oral tablets. [21] [4] It is also available in the form of oral tablets containing a combination of 50 or 100 mg atenolol and 50 mg chlortalidone. [21] Atenolol was previously available in a 0.5 mg/mL solution for injection as well, but this formulation was discontinued. [21]
The duration of action of a single oral dose is longer than the half-life and may be up to 12 hours if the single dose is high enough (e.g., 80 mg). [72] Effective plasma concentrations are between 10 and 100 mg/L. [citation needed] Toxic levels are associated with plasma concentrations above 2000 mg/L. [citation needed]
However, there are short-term escape and long-term drift effects in some people. That is, tolerance develops. It may reduce the extent of the daytime IOP curve up to 50%. The IOP is higher during sleep. Efficacy of timolol in lowering IOP during the sleep period may be limited. [16] [17] [18] It is a 5–10× more potent beta blocker than ...
Over the last 40 years, a variety of drugs have been developed from non-selective alpha-1 receptor antagonists to selective alpha-1 antagonists and alpha-1 receptor inverse agonists. [ 2 ] [ 3 ] The first drug that was used was a non-selective alpha blocker, named phenoxybenzamine and was used to treat BPH. [ 2 ]