Respiratory Difficulties With Betaxolol

Harris, Laurence S.; Greenstein, Scott H.; Bloom, Alan F.

doi:10.1016/0002-9394(86)90157-1

Cited by 77 publications

(14 citation statements)

References 2 publications

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“…Experimental studies with cardioselective ocular ,-adrenoceptor blockers in healthy volunteers (Cervantes et al, 1986;LeJeunne et al, 1990) as well as clinical studies in asthmatics (Brooks et al, 1987;Cervantes et al, 1986;Dunn et al, 1986;Ofner & Smith, 1987;Schoene et al, 1984;Spiritus & Casciari, 1985;Van Buskirk et al, 1986) demonstrated a lack of measurable changes in airway calibre. On the other hand, systemic adverse effects have been occasionally reported with betaxolol (Bauer et al, 1991;Harris et al, 1986;LeJeunne et al, 1990;Nelson & Kuitsky, 1987;Weinreb et al, 1988;Zabel & MacDonald, 1987). Different methods applied to investigate ophthalmic ,3-adrenoceptor blockers may explain the controversial findings.…”

Section: Discussionmentioning

confidence: 99%

Assessment of bronchial effects following topical administration of butylamino‐phenoxy‐propanol‐acetate, an oculoselective beta‐ adrenoceptor blocker in asthmatic subjects.

Bauer¹,

Brunner-Ferber²,

Distlerath³

et al. 1992

Brit J Clinical Pharma

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Section: Discussionmentioning

confidence: 99%

Assessment of bronchial effects following topical administration of butylamino‐phenoxy‐propanol‐acetate, an oculoselective beta‐ adrenoceptor blocker in asthmatic subjects.

Bauer¹,

Brunner-Ferber²,

Distlerath³

et al. 1992

Brit J Clinical Pharma

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“…46 Betaxolol is the drug of choice in patients with compromised respiratory or cardiac functions if a ␤ -blocker has to be used. However, betaxolol is more expensive than most ophthalmic ␤ -blockers, 37 and it has been associated with more ocular burning and stinging.…”

Section: E823mentioning

confidence: 99%

Ophthalmic drug design based on the metabolic activity of the eye: Soft drugs and chemical delivery systems

Bodor

Buchwald²

2005

AAPS J

104

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A BSTRACTDespite its apparent easy accessibility, the eye is, in fact, well protected against the absorption of foreign materials, including therapeutic agents, by the eyelids, by the tearfl ow, and by the permeability barriers imposed by the cornea on one side and the blood-retinal barrier on the other. Most existing ophthalmic drugs were adapted from other therapeutic applications and were not specifi cally developed for the treatment of eye diseases; hence, they are not well suited to provide eye-specifi c effects without causing systemic side effects. A real breakthrough in the area of ophthalmic therapeutics can be achieved only by specifi cally designing new drugs for ophthalmic applications to incorporate the possibility of eye targeting into their chemical structure. Possibilities provided along these lines by designing chemical delivery systems (CDSs) and soft drugs within the framework of retrometabolic drug design are reviewed here. Both are general concept applicable in almost any therapeutic area. This review will concentrate on ␤ -adrenergic agonists and anti-infl ammatory corticosteroids, where clinical results obtained with new chemical entities, such as betaxoxime, adaprolol, loteprednol etabonate, and etiprednol dicloacetate, exist to support the advantages of such metabolism-focused, ophthalmic-specifi c drug design approaches.K EYWORDS: beta-blockers , corticosteroids , eye-targeted delivery , glaucoma , intraocular pressure , oxime OCULAR DRUG DESIGN AND DELIVERY: CHALLENGESFor the therapeutic treatment of most ocular problems, topical administration clearly seems the preferred route, because for systemically administered drugs, only a very small fraction of their total dose will reach the eye from the general circulatory system. Even for this fraction, distribution to the inside of the eye is further hindered by the blood-retinal barrier (BRB), which is almost as effective as the blood-brain barrier (BBB) in restricting the passage of xenobiotics from the blood stream. 1 At fi rst sight, the eye seems an ideal, easily accessible target organ for topical treatment. However, the eye is, in fact, well protected against absorption of foreign materials, fi rst by the eyelids and tear-fl ow and then by the cornea, which forms the physical-biological barrier. When any foreign material or medication is introduced on the surface of the eye, the tear-fl ow immediately increases and washes it away in a relatively short time. Under normal conditions, the eye can accommodate only a very small volume without overfl owing. Commercial eyedrops have a volume of ~30 L, which is about the volume of the conjunctival sac in humans; however, after a single blink, only an estimated 10 L remains. 2 Consequently, there is a window of only ~5 to 7 minutes for any topically introduced drug to be absorbed, and in many cases, no more than 2% of the medication introduced to the eye will actually be absorbed. 2-4 The rest will be washed away and absorbed through the nasolacrimal duct and the mucosal membranes of the nasa...

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“…Cardio-selective beta-blockers (e.g., betaxolol) preferentially inhibit b1 adrenoceptors [21]. Betaxolol, which has a 70-fold higher affinity for b1 receptors, may be better tolerated than nonselective beta-blockers in patients with pulmonary disease, but may still pose significant risk of serious complications [34]. A recent report has suggested that betaxolol, as a result of calciumchannel-blocking activity, may prevent neuronal cell death when given at micromolar concentrations (concentrations unattainable with clinical dosing) [35].…”

Section: Beta-blockers As Ocular Hypotensive Agents: a Historymentioning

confidence: 99%

Evolving Paradigms in the Medical Treatment of Glaucoma

2004

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In the last 5 years, numerous novel ocular hypotensive agents have been introduced for the control of intraocular pressure (IOP). Clinicians now have more options than ever in medical therapy for the treatment of glaucoma and ocular hypertension. When selecting an ocular hypotensive medication for their patients, clinicians should consider not only the IOP-lowering efficacy of an agent but also the ability of the drug to achieve target levels of IOP that are low enough to stop the progression of glaucomatous damage. Other considerations should include how well the drug controls diurnal IOP, the likelihood of serious adverse events, the versatility of the medication for use as an adjunctive agent, as well as other potential attributes (e.g., neuroprotection).

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Respiratory Difficulties With Betaxolol

Cited by 77 publications

References 2 publications

Assessment of bronchial effects following topical administration of butylamino‐phenoxy‐propanol‐acetate, an oculoselective beta‐ adrenoceptor blocker in asthmatic subjects.

Assessment of bronchial effects following topical administration of butylamino‐phenoxy‐propanol‐acetate, an oculoselective beta‐ adrenoceptor blocker in asthmatic subjects.

Ophthalmic drug design based on the metabolic activity of the eye: Soft drugs and chemical delivery systems

Evolving Paradigms in the Medical Treatment of Glaucoma

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