Oral acetazolamide for intraocular pressure lowering: balancing efficacy and safety in ophthalmic practice

Gulati, Shawn; Aref, Ahmad A.

doi:10.1080/17512433.2021.1931123

Cited by 13 publications

(10 citation statements)

References 48 publications

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“…SmaBCA and EhiCA are both well-inhibited with many anion and sulfonamide derivatives. (59)(60)(61)(62). With low micromolar range are sulfamide and phenylarsonic acid with K I s of 28-38 μM and 8-20 μM, for EhiCA and SmaBCA respectively.…”

Section: Discussionmentioning

confidence: 99%

Cloning, Characterization, and Inhibition of the Novel β-Carbonic Anhydrase from Parasitic Blood Fluke, Schistosoma mansoni

Haapanen

Angeli

Tolvanen

et al. 2023

Preprint

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Schistosoma mansoni is an intestinal parasite with one β-class carbonic anhydrase, SmaBCA. We report the sequence enhancing, production, catalytic activity, and inhibition results of the recombinant SmaBCA. It showed significant catalytic activity on CO hydration in vitro with k 1.38 x 10 s and k /K 2.33 x 10 M s . Several sulfonamide inhibitors, from which many are clinically used, showed submicromolar or nanomolar inhibitory effects on SmaBCA. The most efficient inhibitor with a K of 43.8 nM was 4-(2-amino-pyrimidine-4-yl)-benzenesulfonamide. Other effective inhibitors with K s in the range of 79.4 nM-95.9 nM were benzolamide, brinzolamide, topiramate, dorzolamide, saccharin, epacadostat, celecoxib, and famotidine. The other tested compounds showed at least micromolar range inhibition against SmaBCA. Our results introduce SmaBCA as a novel target for drug development against schistosomiasis, a highly prevalent parasitic disease.

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Section: Discussionmentioning

confidence: 99%

Cloning, Characterization, and Inhibition of the Novel β-Carbonic Anhydrase from Parasitic Blood Fluke, Schistosoma mansoni

Haapanen

Angeli

Tolvanen

et al. 2023

Preprint

View full text Add to dashboard Cite

show abstract

“…Other nanomolar range inhibitors are 4-(2-aminoethyl)benzenesulfonamide (compound 6), 4-((2-amino-4-pyrimidinyl)amino)benzenesulfonamide (compound 19), and acetazolamide (AAZ) with K I s of 509–798 nM for EhiCA and K I s of 44–286 nM for SmaBCA, from which acetazolamide is already in clinical use. 73–76 With low micromolar range are sulfamide and phenylarsonic acid with K I s of 28–38 and 8–20 µM, for EhiCA and SmaBCA, respectively. The many agents with good inhibitory activity demonstrate the possibilities for developing CA inhibitors as anti-parasitic drugs against both enzymes of these parasites.…”

Section: Discussionmentioning

confidence: 99%

Cloning, characterization, and inhibition of the novel β-carbonic anhydrase from parasitic blood fluke, Schistosoma mansoni

Haapanen

Angeli

Tolvanen

et al. 2023

Journal of Enzyme Inhibition and Medicinal Chemistry

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Schistosoma mansoni is an intestinal parasite with one β-class carbonic anhydrase, SmaBCA. We report the sequence enhancing, production, catalytic activity, and inhibition results of the recombinant SmaBCA. It showed significant catalytic activity on CO 2 hydration in vitro with k cat 1.38 × 10 5 s −1 and k cat / K m 2.33 × 10 7 M −1 s −1 . Several sulphonamide inhibitors, from which many are clinically used, showed submicromolar or nanomolar inhibitory effects on SmaBCA. The most efficient inhibitor with a K I of 43.8 nM was 4-(2-amino-pyrimidine-4-yl)-benzenesulfonamide. Other effective inhibitors with K I s in the range of 79.4–95.9 nM were benzolamide, brinzolamide, topiramate, dorzolamide, saccharin, epacadostat, celecoxib, and famotidine. The other tested compounds showed at least micromolar range inhibition against SmaBCA. Our results introduce SmaBCA as a novel target for drug development against schistosomiasis, a highly prevalent parasitic disease.

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“…- Carbonic anhydrase inhibitors (CAIs) (dorzolamide, brinzolamide and acetazolamide): They inhibit the carbonic anhydrase isoenzyme 2, reducing the IOP production, with a baseline IOP reduction of approximately 15–20% for topical and 20–30% for oral administration [ 90 , 91 ]. The CAIs have been demonstrated to lower IOP for 24 h, also during the nocturnal/sleep period [ 74 , 90 , 91 ].…”

Section: The Pharmacological Approaches In Ntg Therapymentioning

confidence: 99%

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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Oral acetazolamide for intraocular pressure lowering: balancing efficacy and safety in ophthalmic practice

Cited by 13 publications

References 48 publications

Cloning, Characterization, and Inhibition of the Novel β-Carbonic Anhydrase from Parasitic Blood Fluke, Schistosoma mansoni

Cloning, Characterization, and Inhibition of the Novel β-Carbonic Anhydrase from Parasitic Blood Fluke, Schistosoma mansoni

Cloning, characterization, and inhibition of the novel β-carbonic anhydrase from parasitic blood fluke, Schistosoma mansoni

Pharmaceutical Approaches to Normal Tension Glaucoma

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