Preclinical Overview of Brinzolamide1

DeSantis, Louis

doi:10.1016/s0039-6257(99)00108-3

Cited by 104 publications

(63 citation statements)

References 33 publications

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“…However, the blood level is not high enough to cause adverse reactions 4 . Yet, topical CAIs have the potential to induce SJS-TEN in patients, as they are sulfonamide derivatives that behave similarly to systemic sulfonamide 3 .…”

Section: Discussionmentioning

confidence: 99%

Toxic Epidermal Necrolysis Induced by the Topical Carbonic Anhydrase Inhibitors Brinzolamide and Dorzolamide

et al. 2008

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Section: Discussionmentioning

confidence: 99%

Toxic Epidermal Necrolysis Induced by the Topical Carbonic Anhydrase Inhibitors Brinzolamide and Dorzolamide

et al. 2008

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“…Brinzolamide is used as a CA inhibitor and an ocular hypotensive agent. 27) Therefore, latanoprost free acid is a weak inhibitor of both HCA I and II.…”

Section: Discussionmentioning

confidence: 99%

The Mechanisms by Which Latanoprost Free Acid Inhibits Human Carbonic Anhydrase I and II

Sugimoto

Ikeda

Tsukamoto³

et al. 2008

Biological & Pharmaceutical Bulletin

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In the treatment of glaucoma several types of agents such as beta-adrenoceptor blockers, carbonic anhydrase inhibitors and prostaglandin F2alpha analogues are clinically used at present.1) These agents are given alone and/or in combination.2) Beta-adrenoceptor blockers such as timolol have been used most commonly and reduce intraocular pressure (IOP) through the reduction of aqueous humor formation by blocking beta-adrenergic receptors in the ciliary body.3) The inhibition of carbonic anhydrase (CA) in the ciliary body decreases aqueous humor secretion presumably by slowing the formation of bicarbonate ions with a subsequent reduction in sodium and fluid transport. Thus, the inhibition of CA results in a reduction of IOP through the reduction of aqueous humor production and dorzolamide, a CA inhibitor, is used clinically to treat glaucoma. 4)Monotherapy patients treated with dorzolamide, a CA inhibitor, show a smaller intraocular pressure (IOP) reduction than those treated with timolol, a beta-adrenergic blocker. 5)This suggests that beta-adrenergic blockers have stronger effect for IOP reduction than CA inhibitors. Latanoprost is the only available prostaglandin F2alpha analogue and has been shown to be an effective ocular hypotensive agent when used for the treatment of ocular-hypertensive or open-angle glaucoma patients. 6,7) In spite of the weaker IOP reduction activity of dorzolamide compared to timolol in monotharapy, the combination treatment of dorzolamide with latanoprost showed a comparable IOP reduction activity with the combination use of timolol and latanoprost.8) Puscas and Coltau have shown that prostaglandin F2alpha, enhances CA activity, resulting in an elevation of blood pressure.9) Therefore, latanoprost is supposed to have some influence on CA activity in the eyes. CA is an enzyme found in many tissues of the body.10) It catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid. There exist a number of isoenzymes of CA, and the most active one is CA II (CA-II) in humans, found primarily in red blood cells but also in other tissues. In eye tissue, types I and II of CA exist. 10)Latanoprost is an isopropyl ester of latanoprost free acid, a form of pro-drug, which is enzymatically converted to latanoprost free acid by endogenous esterase. The free acid is a 200 times more potent ligand than latanoprost for the human recombinant prostaglandin F (FP) receptor. The free acid acts as a selective prostanoid FP receptor agonist which reduces IOP by increasing the outflow of aqueous humour.12) On the other hand, it has been shown that the aqueous inflow is not affected. 13)The structure of latanoprost free acid, which is an effective ocular hypotensive agent, is very similar to that of prostaglandin F2alpha. The purpose of this report is to clarify the effect and mechanism of latanoprost free acid on the hydration activity of HCA I or II in an in vitro study. In our previous paper, we showed that docking-simulation of the ligand molecule with the e...

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“…8 The onset of IOP lowering of brinzolamide in the laser-treated monkey model was seen by 1 h, peak IOP lowering occurred by 3 h after dosing. 9 Although the time of onset of action and peak IOP-lowering effect of two drugs did not coincide with each other, we administered both drugs immediately after surgery in order to keep the variables to a minimum when comparing their effect on IOP.…”

Section: Discussionmentioning

confidence: 99%

“…It has high affinity and inhibitory potency against human carbonic anhydrase inhibitor-II, an isozyme found in the ciliary epithelia, which are involved with aqueous humour secretion. 9 Several antiglaucomatous agents have been used to control IOP after cataract surgery. 4,7,[10][11][12][13][14][15][16] In this prospective, randomized, doublemasked, controlled study, we evaluated the IOP-lowering effect of travoprost and brinzolamide within the first 24 h after phacoemulsification cataract surgery.…”

Section: Introductionmentioning

confidence: 99%

Comparing the effects of travoprost and brinzolamide on intraocular pressure after phacoemulsification

Ermiş

Öztürk

İnan

2004

Eye

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Purpose To evaluate the intraocular pressure (IOP) lowering effect of travoprost and brinzolamide within the first 24 h after phacoemulsification cataract surgery. Methods This prospective, randomized, double-masked, controlled study comprised 90 eyes of 90 consecutive patients with senile cataract who had uneventful phacoemulsification surgery. Eyes in the first group received travoprost 0.0015%, second group received brinzolamide 1%. Eyes in the third group received balanced salt solution and were used as control. One drop was instilled immediately after surgery. IOP was measured 24 h preoperatively, 6 and 24 h postoperatively. Analysis of variance, Student's-t and w 2 -tests were used for statistical analyses. Results Preoperatively IOP was not significantly different among the three groups (P ¼ 0.653). At 6 and 24 h postoperatively IOP was lower in both travoprost and brinzolamide group when compared to control group (P ¼ 0.018 and 0.015 at 6 h, P ¼ 0.010 and 0.012 at 24 h, respectively). The difference between travoprost and brinzolamide group was not significant (P ¼ 0.859 at 6 h and P ¼ 0.581 at 24 h). Both travoprost and brinzolamide significantly reduced IOP increases when compared to control eyes at 6 and 24 h (P ¼ 0.036 and 0.029 at 6 h, P ¼ 0.010 and 0.007 at 24 h, respectively). The difference in IOP increase at 6 and 24 h between travoprost and brinzolamide group was not significant (P ¼ 0.744 at 6 h and P ¼ 0.672 at 24 h). Conclusion Both travoprost and brinzolamide significantly lowered IOP after small incision phacoemulsification cataract surgery within the first 24 h without any side effect.

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Preclinical Overview of Brinzolamide1

Cited by 104 publications

References 33 publications

Toxic Epidermal Necrolysis Induced by the Topical Carbonic Anhydrase Inhibitors Brinzolamide and Dorzolamide

Toxic Epidermal Necrolysis Induced by the Topical Carbonic Anhydrase Inhibitors Brinzolamide and Dorzolamide

The Mechanisms by Which Latanoprost Free Acid Inhibits Human Carbonic Anhydrase I and II

Comparing the effects of travoprost and brinzolamide on intraocular pressure after phacoemulsification

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