Betaxolol is an effective ocular antihypertensive agent, pharmacologically classified as a cardioselective beta-blocker. Its mode of action in reducing intraocular pressure is similar to that of non-selective blockers, suppressing the flow of aqueous humor. The extent of occupation, in the systemic circulation, of the beta 1-adrenoceptor of betaxolol when applied topically is smaller than that of non-selective blockers and the occupation of the beta 2 receptor is insignificant, providing a better safety profile in patients with cardiopulmonary disease . Experimental studies have revealed that this drug targets the retina after topical administration and exhibits L-type dependent calcium channel blocking activity, which likely allows betaxolol to improve retinal perfusion and serve as a recommended neuroprotective agent in various forms of glaucoma . The most frequent adverse reaction to betaxolol is burning after administration, which is minimized by an ocular suspension with a reduced concentration of similar efficacy (Betoptic S, 0.25%). A double-blind multicenter clinical study, with 352 patients with primary open-angle glaucoma or ocular hypertension, compared the effects on intraocular pressure and ocular comfort of a 0.5% betaxolol ophthalmic solution, in contrast to the suspension of betaxolol with 0.25%. With twice-daily doses, baseline intraocular pressure was significantly reduced (P = 0.0005), with no significant difference between the two groups, at Week 2 and at Months 1, 2, and 3. In addition, the prevalence of ocular discomfort topical application was significantly lower for the 0.25% betaxolol suspension than for the 0.5% betaxolol solution (P = 0.0005). Discuss the pharmacotechnical aspects that may be related to the results obtained in the studies mentioned above, specifically: - Dosage reduction versus maintenance of activity, in case of suspension. - The reduction of discomfort during application observed for suspension over solution.
Betaxolol is an effective ocular antihypertensive agent, pharmacologically classified as a cardioselective beta-blocker.
Its mode of action in reducing intraocular pressure is similar to that of non-selective blockers, suppressing the flow of aqueous humor. The extent of occupation, in the systemic circulation, of the beta 1-adrenoceptor of betaxolol when applied topically is smaller than that of non-selective blockers and the occupation of the beta 2 receptor is insignificant, providing a better safety profile in patients with cardiopulmonary disease .
Experimental studies have revealed that this drug targets the retina after topical administration and exhibits L-type dependent calcium channel blocking activity, which likely allows betaxolol to improve retinal perfusion and serve as a recommended neuroprotective agent in various forms of glaucoma .
The most frequent adverse reaction to betaxolol is burning after administration, which is minimized by an ocular suspension with a reduced concentration of similar efficacy (Betoptic S, 0.25%).
A double-blind multicenter clinical study, with 352 patients with primary open-angle glaucoma or ocular hypertension, compared the effects on intraocular pressure and ocular comfort of a 0.5% betaxolol ophthalmic solution, in contrast to the suspension of betaxolol with 0.25%. With twice-daily doses, baseline intraocular pressure was significantly reduced (P = 0.0005), with no significant difference between the two groups, at Week 2 and at Months 1, 2, and 3. In addition, the prevalence of ocular discomfort topical application was significantly lower for the 0.25% betaxolol suspension than for the 0.5% betaxolol solution (P = 0.0005).
Discuss the pharmacotechnical aspects that may be related to the results obtained in the studies mentioned above, specifically:
- Dosage reduction versus maintenance of activity, in case of suspension.
- The reduction of discomfort during application observed for suspension over solution.
Betaxolol is a drug given for the treatment of glaucoma, hypertension and angina. This drug blocks the beta-adreno-I receptors. There are two modes of delivery. In one form there is application of 0.5% solution of Betaxolol and in another method there is application of 0.25% drug betaxolol suspension.
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