Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0086543 (cataract)
 29,165 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

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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PMID:Pharmacological treatment strategies in age-related cataracts. 150 43

Bendazac is a drug which protects proteins from denaturation induced by different agents. It is also effective in protecting rabbits from X-ray-induced cataract. This study deals with the effects of bendazac on the intense light-induced retinal damage in rats. Four groups of animals received orally 0, 50, 100 or 200 mg/kg of bendazac L-lysine salt three times a day for 3 days and once the fourth day, before 1 h exposure to intense-green filtered light. Fourteen days after housing in a dark room, the rats were sacrificed and the retinae were examined by light microscopy. Retinal damage was graded according to a score severity from 0 to 5. The mean score for control animals was 2.23, whereas a dose-related and statistically significant reduction of retinal damage was detected in bendazac treated rats, i.e. 1.72, 1.54 and 1.40. A protective activity in the distribution of the severity score, i.e. a higher incidence of no damaged retinae and a lower frequency in the most severely affected ones, was also observed in treated versus control rats. These results suggest a potential therapeutic value of bendazac in the treatment of those conditions, such as retinitis pigmentosa and senile macular degeneration, in which the light exposure plays a role as a co-factor.
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PMID:Pretreatment with bendazac attenuates retinal damage induced by intense light in rats. 194 39

In connection with the clinical trial of an anti-cataract drug (Bendazac lysine) a number of examination methods were used to assess the progress of the cataract: slitlamp examination, visual acuity determination, and the measurement of the contrast sensitivity, light scatter in the eye and the autofluorescence and transmission of the lens. In this article the measurements of 43 patients (43 eyes) are presented, taken at the time that medication was started. In this way we can get an impression of the value of these measurements for the study of cataractous lenses. The contrast sensitivity of the cataractous eye is lowered for all spatial frequencies as compared with the normal population. Light scatter is greatly increased. The autofluorescent profile of the lens with nuclear cataract differs markedly from that of the lens with cortical cataract.
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PMID:Clinical and physical measurements of the cataractous lens. 209 Mar 99

Bendazac is an oxyacetic acid with anti-inflammatory, antinecrotic, choleretic and antilipidaemic properties, but its principal effect is to inhibit the denaturation of proteins. The lysine salt, which is better absorbed than the parent compound after oral administration, has been evaluated as a treatment for cataract, a condition which appears to result mainly from the denaturation, aggregation and precipitation of proteins within the lens. Results from a very small number of preliminary studies using objective photographic and densitometric methods have suggested that oral bendazac lysine, usually at a dosage of 500 mg 3 times daily, can stabilise the progression of lens opacification in patients with cataract. Significant improvements in individual and mean visual acuities in treated patients have been reported by several studies, but this parameter is not universally accepted as a reliable index of lens status. Preliminary studies evaluating bendazac lysine 0.5% eyedrops have reported comparable results to those obtained with oral treatment. Overall, tolerability of the drug has been good in studies to date. A dose-related laxative effect and other gastrointestinal disturbances are the most common adverse effects associated with oral therapy, and a transient burning sensation is the most commonly reported symptom occurring with eyedrop application. Bendazac lysine is one of a number of agents which have been introduced for the management of cataract. Although the results of preliminary studies have suggested that the drug may be useful for delaying the progression of cataract, further clinical studies using proven objective methods are required to fully establish its value in the management of this condition and its long term tolerability.
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PMID:Bendazac lysine. A review of its pharmacological properties and therapeutic potential in the management of cataracts. 219 Jul 95

Bendazac is a drug previously reported to prevent protein denaturation produced by various agents, including free radicals. Results of these experiments show that bendazac also prevents the photosensitized haemolysis of intact red blood cells which is related to damage of membrane proteins and/or lipids induced by reactive species originating from oxygen. Based on results of a previous study, it is proposed that the antioxidant activity of bendazac is due to interaction with protein molecules rather than free radicals. The protective activity of bendazac against photo-oxidative damage might have therapeutic implications in conditions such as cataract and haemolytic anaemias.
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PMID:Photosensitized haemolysis of human erythrocytes is reduced by bendazac. 279 73

The reaction of lens proteins with cyanate (carbamylation) causes many changes seen in human cataract including disruption of the protein conformations. Bendazac, a putative anti-cataract drug, decreases the binding of cyanate to lens proteins and prevents the cyanate-induced elevation of the phase separation temperature in incubated rat lenses. Its major metabolite, 5-hydroxybendazac, also inhibits the binding of cyanate to lens proteins even when it is present only during a pre-incubation period. The metabolite is more effective than the parent compound.
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PMID:Bendazac prevents cyanate binding to soluble lens proteins and cyanate-induced phase-separation opacities in vitro: a possible mechanism by which bendazac could delay cataract. 381 34

Bendazac, as such or in the form of its l-lysine salt, has a protective effect against lens protein denaturation both in vitro and in vivo. In vitro this effect has been documented on the lens proteins of rats, rabbits and pigs by using nephelometry, electrophoresis and electron microscopy. In vivo the protective effect has been observed after treatments ranging in duration from 3 to 14 days depending on the dosage used; the minimal effective dose produced a serum level of 35 micrograms/ml of bendazac. The penetration of the drug into the lens has been shown by both radioassay and HPLC; the lens concentration of bendazac increases with the duration of treatment. The mechanism of the protective action of bendazac against lens protein denaturation is discussed together with the implications of such protective action in the treatment of cataract.
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PMID:Basic data supporting the use of the l-lysine salt of bendazac in cataract. 661 87

Bendazac has been used as an anti-cataractogenic drug. It has been reported that this acts by preventing protein denaturation. In this study the ability of bendazac to inhibit in vitro glycation of human lens crystallins was evaluated. Possible effects of bendazac were detected by incubation of WS crystallins with the reducing sugars glucose and fructose. The efficiency of bendazac was evaluated by means of selected parameters including: browning, glycation (measured as tyrosine content) and specific NTP-fluorescence. The results showed clearly that bendazac (bendazac L-lysine and sodium) inhibits the early stages of protein glycation, as well as the formation of fluorescent advanced glycation products. Bendazac lysine (20 mM) proved to be more effective in inhibiting fluorescence development (67% inhibition) that the corresponding sodium salt (35% inhibition). No significant differences were found with respect to furosine levels; about 40% inhibition was produced with either bendazac lysine or sodium salt bendazac clearly inhibits glycation of human lens crystallins, as can be efficiently monitored by following specific changes in lens protein fluorescence. These results may constitute a new and relevant therapeutic approach to monitoring cataract development.
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PMID:Bendazac decreases in vitro glycation of human lens crystallins. Decrease of in vitro protein glycation by bendazac. 862 Aug 22

Oxidative damage to lens components is associated with cataract formation and reactive oxygen species (ROS) overproduction at inflammation sites is thought to lead to the development of inflammatory disorders. Bendazac is a non-steroidal anti-inflammatory drug able to delay the cataractogenic process. Aim of the present study is to characterize, both chemically and biologically, the activity of this anticataract agent as a radical scavenger. Bendazac has been shown to be a strong reacting substrate in a chemical oxidizing system, which mimics a physiological pathway of hydroxy radical generation. In the Fenton-Cier reaction the drug rapidly forms a mixture of hydroxylated derivatives, among which 5-hydroxybendazac, bendazac's main metabolite, being a hydroxy radical scavenger itself. Moreover, by means of a rapid and sensitive flow cytometric method able to determine reactive oxygen intermediate production, bendazac and its 5-hydroxy derivative were shown to inhibit oxidative burst activation in polymorphonuclear neutrophil leukocytes (PMNLs).
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PMID:Radical scavenger activity of bendazac, an anticataract non-steroidal anti-inflammatory agent. 873 88

1. Diabetic neuropathy is a many faceted complication of both type I and II diabetes. The aim of the present study was to investigate the effects of bendazac lysine (BDL), an anticataract drug, on experimental diabetic peripheral neuropathy (DPN) in rats. 2. Diabetes was induced in rats by intraperitoneal injection of 75 mg/kg streptozotocin (STZ) dissolved in 0.1 mol/L citrate buffer (pH 4.4). Bendazac lysine was administered to rats at doses of 50, 100 and 200 mg/kg twice a day for 12 weeks. 3. Diabetic rats without treatment showed hypopraxia, polydipsia, polyuria, slow weight gain, cataract, increased tail-flick threshold temperature, decreased motor nerve conduction velocity (nd induced pathological morphological changes of myelinated nerve fibres. All these symptoms were ameliorated in diabetic rats treated with BDL. Bendazac lysine ameliorated the blood glucose concentration, glycosylated haemoglobin levels and insulin levels in the plasma of diabetic rats, reduced aldose reductase activity in erythrocytes and advanced glycation end-products in both nerves and serum and increase the activity of glutathione peroxidase in the nerves and Na(+)/K(+)-ATPase in the nerves and erythrocytes. 4. Bendazac lysine exerts its protective effects against the progression of diabetic peripheral neuropathy in STZ-diabetic rats through multiple mechanisms and is a potential drug for the prevention of deterioration in DPN.
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PMID:Protective effects of bendazac lysine on diabetic peripheral neuropathy in streptozotocin-induced diabetic rats. 1718 6


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