Bupranolol, A β<sub>1</sub>- and β<sub>2</sub>-Blocker, Causes Constriction of the Pupil in Men

Tsukahara, Shigeo; Sasaki, Takaya; Yamabayashi, Shigeki; Shimizu, Yukio

doi:10.1159/000265407

Cited by 2 publications

(2 citation statements)

References 8 publications

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“…BPL is a potent nonselective β-blocking agent (Tsukahara et al, 1986). BPL was quickly and completely absorbed from the gut with less than 10% oral bioavailability.…”

Section: Nonselective β-Blockers (β1 and β2)mentioning

confidence: 99%

Systemic delivery of β-blockers via transdermal route for hypertension

Ahad

Al-Jenoobi

Al-Mohizea

et al. 2015

Saudi Pharmaceutical Journal

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Hypertension is the most common cardiovascular disease worldwide. Moreover, management of hypertension requires long-term treatment that may result in poor patient compliance with conventional dosage forms due to greater frequency of drug administration. Although there is availability of a plethora of therapeutically effective antihypertensive molecules, inadequate patient welfare is observed; this arguably presents an opportunity to deliver antihypertensive agents through a different route. Ever since the transdermal drug delivery came into existence, it has offered great advantages including non-invasiveness, prolonged therapeutic effect, reduced side effects, improved bioavailability, better patient compliance and easy termination of drug therapy. Attempts were made to develop the transdermal therapeutic system for various antihypertensive agents, including β-blockers, an important antihypertensive class. β-blockers are potent, highly effective in the management of hypertension and other heart ailments by blocking the effects of normal amounts of adrenaline in the heart and blood vessels. The shortcomings associated with β-blockers such as more frequent dose administration, extensive first pass metabolism and variable bioavailability, make them an ideal candidate for transdermal therapeutic systems. The present article gives a brief view of different β-blockers formulated as transdermal therapeutic system in detail to enhance the bioavailability as well as to improve patient compliance. Constant improvement in this field holds promise for the long-term success in technologically advanced transdermal dosage forms being commercialized sooner rather than later.

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“…BPL is a potent nonselective β-blocking agent (Tsukahara et al, 1986). BPL was quickly and completely absorbed from the gut with less than 10% oral bioavailability.…”

Section: Nonselective β-Blockers (β1 and β2)mentioning

confidence: 99%

Systemic delivery of β-blockers via transdermal route for hypertension

Ahad

Al-Jenoobi

Al-Mohizea

et al. 2015

Saudi Pharmaceutical Journal

View full text Add to dashboard Cite

show abstract

“…Bupranolol is a potent nonselective beta-blocking agent, without intrinsic sympathomimetic activity (Tsukahara et al, 1986). Upon oral administration it undergoes an extra-ordinary first-pass metabolism (N 90% in humans) and is rapidly eliminated with a biological half-life of 1.5-2.0 h (Waller et al, 1982;Wellstein et al, 1986).…”

Section: Introductionmentioning

confidence: 99%