Betaxolol: A comprehensive profile

Alwadei, Majed; Bakheit, Ahmed H.; Abdel‐Aziz, Alaa A.‐M.; Wani, Tanveer A.

doi:10.1016/bs.podrm.2020.07.002

Cited by 4 publications

(13 citation statements)

References 43 publications

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“…BET, as a selective β-adrenergic receptor antagonist, was once the first-line treatment for open-angle glaucoma [18,19]. It can also be used to treat high blood pressure [20][21][22].…”

Section: Discussionmentioning

confidence: 99%

Betaxolol as a Potent Inhibitor of NDM-1-Positive E. coli That Synergistically Enhances the Anti-Inflammatory Effect in Combination with Meropenem

Sun,

Ren,

Yang

et al. 2023

IJMS

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With significant human and economic losses, increasing bacterial resistance is a serious global threat to human life. Due to their high efficacy, broad spectrum, and cost-effectiveness, beta-lactams are widely used in the clinical management of bacterial infection. The emergence and wide spread of New Delhi metallo-β-lactamase (NDM-1), which can effectively inactivate β-lactams, has posed a challenge in the design of effective new antimicrobial treatments. Medicine repurposing is now an important tool in the development of new alternative medicines. We present a known glaucoma therapeutic, betaxolol (BET), which with a 50% inhibitory concentration (IC50) of 19.3 ± 0.9 μM significantly inhibits the hydrolytic activity of the NDM-1 enzyme and may represent a potential NDM-1 enzyme inhibitor. BET combined with meropenem (MEM) showed bactericidal synergism in vitro. The efficacy of BET was further evaluated against systemic bacterial infections in BALB/c mice. The results showed that BET+MEM decreased the numbers of leukocytes and inflammatory factors in peripheral blood, as well as the organ bacterial load and pathological damage. Molecular docking and kinetic simulations showed that BET can form hydrogen bonds and hydrophobic interactions directly with key amino acid residues in the NDM-1 active site. Thus, we demonstrated that BET inhibited NDM-1 by competitively binding to it and that it can be developed in combination with MEM as a new therapy for the management of infections caused by medicine-resistant bacteria.

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“…BET, as a selective β-adrenergic receptor antagonist, was once the first-line treatment for open-angle glaucoma [18,19]. It can also be used to treat high blood pressure [20][21][22].…”

Section: Discussionmentioning

confidence: 99%

Betaxolol as a Potent Inhibitor of NDM-1-Positive E. coli That Synergistically Enhances the Anti-Inflammatory Effect in Combination with Meropenem

Sun,

Ren,

Yang

et al. 2023

IJMS

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“…Betaxolol is a selective beta-1-adrenoceptor antagonist [ 82 ]. The use of this eyedrop in NTG is controversial.…”

Section: The Pharmacological Approaches In Ntg Therapymentioning

confidence: 99%

“…Studies have shown that similar to timolol, betaxolol can induce hypotensive dipping of blood pressure during nighttime, with detrimental effects on the VF damage progression [ 83 ]. Comparative clinical trials investigating the use of local beta-blocker for managing NTG have shown a greater reduction in IOP with timolol, however, better VF preservation using betaxolol [ 82 ], suggesting that the decrease in blood pressure due to the systemic effect of nonselective beta-blockers could have a negative effect on the preservation of visual function.…”

Section: The Pharmacological Approaches In Ntg Therapymentioning

confidence: 99%

“…Betaxolol, carteolol and levobunolol eye drops have been associated with increased ONH blood flow in glaucoma patients [ 78 , 80 , 81 , 82 ]. Carvedilol has shown the ability to improve ocular microcirculation in animal models after topical or oral administration by blocking the alfa-adrenergic receptors [ 85 ].…”

Section: The Pharmacological Approaches In Ntg Therapymentioning

confidence: 99%

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Pharmaceutical Approaches to Normal Tension Glaucoma

Salvetat,

Pellegrini,

Spadea

et al. 2023

Pharmaceuticals

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Normal tension glaucoma (NTG) is defined as a subtype of primary open-angle glaucoma (POAG) in which the intraocular pressure (IOP) values are constantly within the statistically normal range without treatment and represents approximately the 30–40% of all glaucomatous cases. The pathophysiology of this condition is multifactorial and is still not completely well known. Several theories have been proposed to explain the onset and progression of this disease, which can be divided into IOP-dependent and IOP-independent factors, suggesting different therapeutic strategies. The current literature strongly supports the fundamental role of IOP in NTG. The gold standard treatment for NTG tends to be based on the lowering IOP even if “statistically normal”. Numerous studies have shown, however, that the IOP reduction alone is not enough to slow down or stop the disease progression in all cases, suggesting that other IOP-independent risk factors may contribute to the NTG pathogenesis. In addition to IOP-lowering strategies, several different therapeutic approaches for NTG have been proposed, based on vaso-active, antioxidant, anti-inflammatory and/or neuroprotective substances. To date, unfortunately, there are no standardized or proven treatment alternatives for NTG when compared to traditional IOP reduction treatment regimes. The efficacy of the IOP-independent strategies in decreasing the risk or treating NTG still remains inconclusive. The aim of this review is to highlight strategies reported in the current literature to treat NTG. The paper also describes the challenges in finding appropriate and pertinent treatments for this potentially vision-threatening disease. Further comprehension of NTG pathophysiology can help clinicians determine when to use IOP-lowering treatments alone and when to consider additional or alternatively individualized therapies focused on particular risk factors, on a case-by-case basis.

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“…Betaxolol (brand names Kerlone and Optipres-S) is a selective β1-receptor antagonist which may be used to treat hypertension, though it is more commonly used topically as an anti-glaucoma agent [1]. Glaucoma is a dysfunction or damage affecting the optic nerve, leading to gradual loss of eyesight, which is often caused by high intraocular pressure [2].…”

Section: Introductionmentioning

confidence: 99%

Chemo-Enzymatic Synthesis of Enantiopure β-Antagonist (S)-Betaxolol

Troøyen

Jacobsen

2022

Catalysts

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The β-blocker (S)-betaxolol has been synthesized in 99% enantiomeric excess (ee) from the commercially available precursor 4-(2-hydroxyethyl)phenol. The racemic chlorohydrin 1-chloro-3-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)propan-2-ol was esterified with vinyl acetate catalyzed by lipase B from Candida antarctica, which gave the R-chlorhydrin (R)-1-chloro-3-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)propan-2-ol in 99% ee with 38% yield. The enantiomeric excess of the R-chlorohydrin was retained in an amination reaction with isopropylamine in methanol to yield (S)-betaxolol in 99% ee and with 9% overall yield. We are under way to improve the yield.

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Betaxolol: A comprehensive profile

Cited by 4 publications

References 43 publications

Betaxolol as a Potent Inhibitor of NDM-1-Positive E. coli That Synergistically Enhances the Anti-Inflammatory Effect in Combination with Meropenem

Betaxolol as a Potent Inhibitor of NDM-1-Positive E. coli That Synergistically Enhances the Anti-Inflammatory Effect in Combination with Meropenem

Pharmaceutical Approaches to Normal Tension Glaucoma

Chemo-Enzymatic Synthesis of Enantiopure β-Antagonist (S)-Betaxolol

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