Pilot Study of Bendazac for Treatment of Cataract

Testa, M.; Iuliano, Giuseppe; Silvestrini, Bruno

doi:10.1016/s0140-6736(82)91893-1

Cited by 20 publications

(11 citation statements)

References 9 publications

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“…This incon venience could be easily circumvented by using eye drops with appropriate drug con centration. Good eye penetration after topi cal application has demonstrated that this compound is strongly recommended for a topical therapy [6], To date, several clinical studies have con firmed that bendazac-L-lysine salt possessed a significant anticataract activity [7,12,13] exerted through its protective effect against lens protein dénaturation both in vitro and in vivo in some forms of cataract. Our find ings seem to extend the curative effects of bendazac to diabetic cataract, achieved through the inhibition of aldose reductase activity.…”

Section: Resultsmentioning

confidence: 99%

Inhibition of Rat Lens Aldose Reductase by Bendazac-L-Lysine Salt

Iuliano¹,

Menzione²,

Apponi-Battini³

et al. 1989

Enzyme

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Section: Resultsmentioning

confidence: 99%

Inhibition of Rat Lens Aldose Reductase by Bendazac-L-Lysine Salt

Iuliano¹,

Menzione²,

Apponi-Battini³

et al. 1989

Enzyme

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“…The usual dosage has been 500mg orally 3 times daily. Testa et al (1982) claimed an improvement in visual acuity in 22 of 29 eyes of 17 patients, in only 1 to 4 months in the first such trial. An improvement in visual acuity implying decreased opacity is not expected as the cataractogenic process in man is thought to be largely irreversible.…”

Section: Bendazacmentioning

confidence: 99%

Pharmacological Treatment Strategies in Age-Related Cataracts

Harding

1992

Drugs & Aging

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Cataract is the major cause of blindness worldwide and at present the only approved treatment in many countries including the UK and USA is surgical removal of the lens. In other countries various anti-cataract drugs are available without proof of their efficacy. Research is continuing into the possible benefits of several groups of drugs and some vitamins. The first to be studied were sorbitol-lowering agents (aldose reductase inhibitors) based on the sorbitol hypothesis for diabetic cataract. Sorbitol-lowering agents have distinct effects in vitro and many of them delay the development of cataract in galactose-fed rats. A few delay cataract in diabetic rats but none have been proved effective in clinical trials, although these continue. Aspirin, paracetamol (acetaminophen) and ibuprofen delay diabetic cataract in rats, and have been shown to delay other experimental cataracts. Case-control studies from 3 continents indicate that these drugs, or at least aspirin, protect against cataract. Results of studies on all 3 drugs indicate a benefit even at low doses. Population-based studies did not identify any protection against early lens opacities but tiny opacities that do not impair vision are not a problem. Bendazac protects lens proteins in vitro and delays cataractogenesis in x-irradiated rats. In humans, it reached the clinical trial stage but most trials have been small and with subjective criteria of opacification. One objectively monitored trial suffered from a high drop-out rate. Other preparations studied less extensively include vitamins, aminoguanidine to prevent protein cross-linking in diabetes and agents designed to boost glutathione levels. It is probable that some agents which may delay or prevent cataract will be proved effective soon, and in the end there may be different drugs to delay cataract in different high risk groups. This is what might be expected of a multifactorial disease, although compounds that intervene in the final common pathways to cataract could have a broad efficacy.

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“…Limitations of the model are the lack of precision relating the position of a carbonyl moiety with respect to the aromatic plane and the failure to focus on the position of 1 79 an inhibitor acidic moiety with respect to the aromatic plane. The problem with carbonyl moiety orientation is well illustrated by the fact that the sorbinil hydantoin carbonyls lie in a plane orthogonal to the aromatic plane, whereas the carbonyl in antiallergy AR inhibitors lie in the aromatic plane.…”

Section: Ar Inhibitor Site Modelmentioning

confidence: 99%