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Brymonidyna na twarz - Tajemnicze Piękno Naturalnej Pielęgnacji
Identification
Brinzolamide is a carbonic anhydrase inhibitor used for the reduction of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.
Brinzolamide is a highly specific, non-competitive, reversible carbonic anhydrase II (CA-II) inhibitor indicated to reduce ocular pressure in patients with ocular hypertension or open-angle glaucoma. 5 Although the exact pathophysiology of glaucoma is still unknown, one of the main hallmarks of this disease is vascular dysregulation and abnormalities. 1,2 The resulting vascular resistance increases intraocular pressure, thus impairing ocular perfusion. 1,2 Although systemic anti-carbonic anhydrase (CA) therapy has been used for almost 50 years with varying degrees of success, systemic administration results in an increase in incidences of adverse effects. 1,2
Brinzolamide was developed as a topical solution to the systemic side effects and dorzolamide, the first-ever approved topical CA inhibitor with contrasting results and evidence. 2 Unlike dorzolamide, brinzolamide has a higher lipophilicity to facilitate diffusion across the blood-retinal barrier. 2 Brinzolamide was approved by the FDA in 1998 as a standalone product and in 2013 as a combination product with brimonidine tartrate. 5,6 In Europe, it was also approved as a combination product with timolol in 2008. 7
Type Small Molecule Groups Approved Structure
Structure for Brinzolamide (DB01194)
Weight Average: 383.507Monoisotopic: 383.064332867 Chemical Formula C12H21N3O5S3 Synonyms Poor quality drug data slowing you down?
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RESULTS
Representative pictures of a mouse from each group. (A) Group 1: 1% brimonidine cream before UVR. (B) Group 2: 0.33% brimonidine gel before UVR. C) Group 3: 1% brimonidine cream after UVR. (D) Group 4: UVR, no drug treatment (UVR control). (E) Group 5: 1% brimonidine cream without UVR. (F) The mice from Group 1 and 5 developed erythema after the application of 1% brimonidine cream.
(a) Representative SCC on the back of a UVR control mouse. (b) Overview histology picture (H&E staining) (c). Close up of SCC keratin pearls.
Kaplan–Meier plot showing the probability of survival without a tumor of at least 1 mm in diameter for the groups treated with 1% brimonidine cream before UVR (Group 1), 0.33% brimonidine gel before UVR (Group 2), 1% brimonidine cream after UVR (Group 3) and UVR alone (Group 4). No tumors developed in the nonirradiated Group 5. Panels: (a) first tumor, (b) second tumor, and (c) third tumor.
MATERIALS AND METHODS
Animals
Hairless female C3.Cg/TifBomTac immunocompetent mice (n = 125), aged 14–22 weeks at the beginning of the experiment, purchased from Taconic (Ry, Denmark) were used in this study. Mice were anesthetized with 0.05 mL of HypDorm (0.158 mg/mL fentanyl citrate, 5 mg/mL fluanisone, 2.5 mg/mL midazolam), tattooed with consecutive numbers on the abdomen and randomized into five groups. Each group was housed in an individual cage with access to water and a standard diet (Table 1 ) and maintained at 23–24°C under a 12‐h light‐dark cycle. This study followed recommendations described by national guidelines. All protocols were approved by national (permit number 2014‐15‐0201‐00096) and institutional ethical committees.
TABLE 1
Treatment schedule and median number of days until 50% of the mice had a first, second, and third tumor.
| Group | Treatment | Irradiation dose (SEDs) | Median days to first tumor (Q3–Q1) † | Median days to second tumor (Q3–Q1) † | Median days to third tumor (Q3–Q1) † |
|---|---|---|---|---|---|
| 1 | 1% brimonidine cream before UVR | 3 | 295 (302–288) | 302 (309–302) | 309 (316–302) |
| P‐value ‡ | 0.000006 | 0.000004 | 0.000001 | ||
| 2 | 0.33% brimonidine gel before UVR | 3 | 267 (295–254) | 281 (295–267) | 288 (295–274) |
| P‐value ‡ | 0.313 | 0.447 | 0.372 | ||
| 3 | 1% brimonidine cream after UVR | 3 | 274 (281–261) | 288 (295–274) | 295 (295–288) |
| P‐value ‡ | 0.252 | 0.172 | 0.080 | ||
| 4 | UVR, no drug treatment (UVR control) | 3 | 267 (274–254) | 274 (281–267) | 274 (288–267) |
| 5 | 1% brimonidine cream | NA | No tumor | No tumor | No tumor |
Brimonidine Eye Drops within the Reach of Children: A Possible Foe
3 Department of Innovative Technologies in Medicine and Dentistry, “Gabriele d’Annunzio” University of Chieti-Pescara, 66100 Chieti, Italy
Carmela Salladini
Patrizia Ballerini
3 Department of Innovative Technologies in Medicine and Dentistry, “Gabriele d’Annunzio” University of Chieti-Pescara, 66100 Chieti, Italy
Claudia Rossi
3 Department of Innovative Technologies in Medicine and Dentistry, “Gabriele d’Annunzio” University of Chieti-Pescara, 66100 Chieti, Italy
Maurizio Aricò
3 Department of Innovative Technologies in Medicine and Dentistry, “Gabriele d’Annunzio” University of Chieti-Pescara, 66100 Chieti, Italy
Received 2024 Jan 29, Revised 2024 Feb 26, Accepted 2024 Mar 5.Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
Pharmacology
Brinzolamide, either as a standalone agent or in combination with brimonidine, is approved by the FDA for the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. 8,5 Brinzolamide is also approved in Europe to be used in combination with timolol to treat the same conditions. 7
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Avoid life-threatening adverse drug events with our Clinical APIInhibition of carbonic anhydrase II (CA-II) in the ciliary process of the eye slows the formation of bicarbonate and thus fluid flow, lowering intraocular pressure (IOP). 3,4
The IOP-reducing effect of brinzolamide as adjunctive therapy to the prostaglandin analog travoprost was studied. Following a 4-week run-in with travoprost, patients with an IOP ≥19 mmHg were randomized to receive added treatment with brinzolamide or timolol. An additional decrease in mean diurnal IOP of 3.2 to 3.4 mmHg for the brinzolamide group and 3.2 to 4.2 mmHg for the timolol group were observed. There was an overall higher incidence of non-serious ocular adverse reactions, mainly related to signs of local irritation, in the brinzolamide/travoprost groups. The events were mild and did not affect the overall discontinuation rates in the studies. 11
A clinical trial was conducted with brinzolamide in 32 pediatric patients less than 6 years of age, diagnosed with glaucoma or ocular hypertension. Some patients were naive to IOP therapy whilst others were on other IOP-lowering medicinal product(s). Those who had been on previous IOP medicinal products were not required to discontinue their IOP medicinal product(s) until the initiation of monotherapy with brinzolamide. 11