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PubMedDate not supplied

Randomised double-masked trial of lodoxamide and sodium cromoglycate in allergic eye disease. A multicentre study.

135 patients were entered into a 28-day randomized double-masked multicentre study comparing the efficacy and short-term safety of lodoxamide 0.1% ophthalmic solution (Alomide--Alcon Laboratories), a mast cell stabilizer, with sodium cromoglycate 2% ophthalmic solution (Opticrom--Fisons Pharmaceuticals) in the treatment of allergic eye disease. Patients given lodoxamide 0.1% showed a significantly more rapid and greater improvement in their signs and symptoms of allergic eye disease than patients given sodium cromoglycate 2%. Both treatments were found to be safe, and side-effect profiles were comparable between the two treatment groups, although the overall incidence of side-effects in this study was found to be less frequent in the lodoxamide-treated group.

Adolescent↗
PubMedDate not supplied

Tear histamine and histaminase during the early (EPR) and late (LPR) phases of the allergic reaction and the effects of lodoxamide.

The objectives of this study were two-fold: to identify tear histamine content and its relationship to changes in tear histaminase activity during the early (EPR) and late phases (LPR) of the allergic reaction induced by a conjunctival provocation test (CPT) and to evaluate the effects of lodoxamide on histamine release and allergic signs and symptoms during EPR and LPR. A baseline CPT was administered to 20 allergic patients with no baseline signs or symptoms of allergy. Clinical signs and symptoms were evaluated after 20 minutes and 6 hours. Tear samples were taken after 5-10 minutes and after 6 hours for subsequent analyses of cytology and histamine content (ELISA). Patients were then randomly assigned to receive lodoxamide or placebo four times daily for one week in a double-masked fashion. A second CPT was done after this therapy and the same parameters were re-evaluated. During EPR, tear histamine increased significantly with respect to baseline values (p < 0.05). During LPR, tear histamine increased significantly (p < 0.05) only in histamine inactivated samples. Histaminase enzymes were also significantly less active during the EPR (5.5 +/- 0.7) than the LPR (9.9 +/- 2.3) and at baseline. Histamine levels significantly correlated with allergic signs and symptoms (p < 0.05) only during the EPR. Lodoxamide significantly reduced histamine release during EPR (p < 0.05), allergic signs and symptoms during both EPR (p < 0.001) and LPR (p < 0.005), and tear cytology counts during LPR. In conclusion, greater histaminase activity may account for the smaller amount of tear histamine generally found during LPR, while these enzymes seem to play less of a role during the surge of histamine release and activity in the EPR. Lodoxamide was shown to ideally inhibit various aspects of the allergic reaction: clinical signs and symptoms in both the early and late phases, the primarily EPR-related peak of histamine release, and the primarily LPR-related changes in tear cytology.

Administration, Topical↗
PubMedDate not supplied

Comparison of topical 0.05% levocabastine and 0.1% lodoxamide in patients with allergic conjunctivitis. Study Group.

PURPOSE: The aim of the study was to assess the efficacy and safety of 0.05% levocabastine eyedrops (H1 receptor blocker given BID + vehicle BID) compared with 0.1% lodoxamide ophthalmic solution (mast-cell stabilizer instilled QID) in reducing ocular signs and symptoms of allergic conjunctivitis. METHODS: A randomized, double-masked, parallel-group study was conducted in seven centres in France, in which 93 patients suffering from seasonal or perennial allergic conjunctivitis were randomly allocated to either 0.05% levocabastine (n = 47) or 0.1% lodoxamide (n = 46) in both eyes for a 14-day period. Efficacy was evaluated by subjective (prickling, burning, photophobia, itching) and objective (redness, chemosis, eyelid edema, tearing) sign scores at visits on days 7 and 14, and from data noted daily by the patient in a self-evaluation form. Safety was assessed as tolerance upon instillation and adverse event reports. RESULTS: The ocular allergy symptom and sign scores were comparable in the two treatment groups at baseline. With time, statistically and clinically significant reductions (p < 0.001) from baseline were observed for the subjective and objective scores, with no difference between the treatment groups. After the first instillation, signs were alleviated more rapidly in levocabastine-treated patients than in the lodoxamide group (p < 0.001). Overall assessments by the patient and investigator were similar in both groups. No serious adverse events were reported. CONCLUSIONS: Levocabastine ophthalmic suspension 0.05% (BID) appears to be as effective and safe as lodoxamide 0.1% (QID) in the management of allergic conjunctivitis.

Adolescent↗
PubMed1979

Properties and substrate specificities of two neuraminidases from Trichomonas fetus.

Trichomonas fetus, a protozoon belonging to the class of flagellates causes vaginal infections in cows, leading to sterility or abortion in early stage of pregnancy. Two neuraminidases were isolated from the culture medium and purified by various procedures of gel chromatography, ion exchange chromatography, and by affinity chromatography on N-(4-nitrophenyl)-oxamic acid-Sepharose 4B. The molecular weights of the two neuraminidases were determined as 320 000 (enzyme I) and 38 000 (enzyme II) respectively. However, enzyme I seems to consist of two isoenzymes containing four subunits of almost equal molecular weight. The pH optima of both enzymes depend on the substrates and range from pH 4.7 to 5.5. Due to the type of substrate, the Michaelis constants (Km) vary between 5.0 x 10(-2)M and 6.6 x 10(-3)M for enzyme I and between 1.4 x 10(-2)M and 4.9 x 10(-3)M for enzyme II. Among the different groups of NeuAc-containing substrates, i.e. glycoproteins, glycolipids, oligosaccharides and synthetic ketosides, enzyme I preferably cleaves high molecular weight glycoprotein type substrates whereas enzyme II shows higher affinities to low-molecular weight oligosaccharides. The ganglioside II3NeuAcGgOse4Cer is susceptible to both enzymes only after removal of the lipophilic ceramide residue. Both enzymes show differences in the specificity towards alpha 2 leads 3 to 3, alpha 2 leads to 6, and alpha 2 leads to 8 glycosidic linkages of NeuAc. Taking the rate of cleavage of the alpha 2 leads to linkage in II3NeuAc-Lac as 100, enzyme I reveals 65 for the alpha 2 leads to 6 linkage in II6NeuAc-Lac, and 15 for the alpha 2 leads to 8 linkage in II3(comes from 2 alpha NeuAc8)2-Lac, whereas enzyme II exhibits values around 50 for both the alpha 2 leads to 6- and the alpha 2 leads to 8-linked substrates. The activity of neuraminidase I and II is not influenced by Ca2 but is inhibited by Cu2, Hg2, ann 4-hydroxymercurisulfonic acid. The inhibition by Hg2 and by the latter is reversible with enzyme I by addition of dithioerythritol.

Animals↗
PubMed2005

Trypanosoma cruzi: inhibition of alpha-hydroxyacid dehydrogenase isozyme II by N-allyl and N-propyl oxamates and their effects on intact epimastigotes.

N-allyl (NAOx) and N-propyl (NPOx) oxamates were designed as inhibitors of alpha-hydroxyacid dehydrogenase (HADH) isozyme II from Trypanosoma cruzi. The kinetic studies showed that NAOx and NPOx were competitive inhibitors of HADH-isozyme II (Ki = 72 microM, IC50 = 0.33 mM and 70 microM, IC50 = 0.32 mM, respectively). The attachment of the allylic and propylic chains to nitrogen of the competitive inhibitor oxamate (Ki = 0.91 mM, IC50 = 4.25 mM), increased 12.6 and 13-folds respectively, the affinity for T. cruzi HADH-isozyme II. NAOx and NPOx were selective inhibitors of HADH-isozyme II, because other T. cruzi dehydrogenases were not inhibited by these substances. Since HADH-isozyme II participates in the energy metabolism of T. cruzi, a trypanocidal effect can be expected with these inhibitors. However, we were not able to detect any trypanocidal activity with these oxamates. When the corresponding ethyl esters of N-allyl (Et-NAOx) and N-propyl (Et-NPOx) oxamates were tested as a possible trypanocidal prodrugs, in comparison with nifurtimox and benznidazole, the expected trypanocidal effects were obtained.

Alcohol Oxidoreductases↗
PubMed1999

Efficacy of lodoxamide eye drops on tear fluid cytology of patients with vernal conjunctivitis.

A double-masked, randomized, placebo-controlled study was conducted to evaluate the effectiveness of lodoxamide tromethamine 0.1% eyedrops in preventing inflammatory cell accumulation in the tear fluid of patients with vernal conjunctivitis. A 1-week baseline period was followed by 4 weeks of treatment with either lodoxamide tromethamine 0.1% ophthalmic solution or placebo in 30 symptomatic subjects with vernal conjunctivitis. Cytological evaluation of tear fluid was performed before and after the treatment. In the lodoxamide-treated group, but not in the placebo-treated group, the number of neutrophils (P = 0.051) and eosinophils (P = 0.020) in the tears significantly decreased at the end of 4 weeks when compared with baseline (Wilcoxon-signed rank test). It was concluded that lodoxamide treatment was significantly more effective than the placebo in terms of reducing inflammatory cells in the tear fluid in vernal conjunctivitis. This objective inhibition of inflammatory cells may be associated with clinical relief.

Adolescent↗
PubMedDate not supplied

Effect of lactate on the recovery of CHO-KI cells from gamma radiation damage.

The effect of pre-exposure of CHO-KI cells to lactate on their capacity to recover from or repair radiation damage was examined. Prolonged pre-exposure to lactate and a number of inhibitors of glycolysis has previously been shown to reduce the cell survival after irradiation. Following a split dose of irradiation, cells pre-treated with lactate for 18 hours had a higher relative recovery factor than controls even though survival following a single dose was reduced. Where lactate was added just before irradiation it had a radiation protective effect on the single dose survival curve and no effect on recovery. To investigate a possible involvement of NADH generation via lactate dehydrogenase in the mechanism, oxamate, a non-metabolisable analogue of lactate, was investigated. It reduced the survival of irradiated CHO-KI cells following prolonged and short pre-exposure and did not significantly affect the recovery factor. It is suggested that since lactate and oxamate both inhibit glucose breakdown, their radiobiologic effects may be due to depletion of cellular energy substrates necessary for repair. In contrast, the increased recovery and short term radiation protective effect seen with lactate only may involve LDH activity.

Animals↗
PubMed1995

Modification of tumour glucose metabolism for therapeutic benefit.

Tumours have a much greater dependence than normal tissues on anaerobic glycolysis for energy generation. We have studied the effects of glycolysis inhibition on tumour cells in vitro. Cellular ATP fell during exposure of cells in air to 2-deoxy glucose or to the lactate dehydrogenase inhibitor oxamate. Glycolysis inhibition alone did not alter clonogenic cell survival over 6 h, but a 6-h exposure to oxamate combined with doxorubicin (Dox) gave greater than additive cell killing. This effect was greatest when oxamate was dosed after Dox, suggesting that oxamate inhibited repair of Dox-induced damage. Oxamate also gave greater than additive cell killing in multicellular spheroids when combined with Dox and there was a greater than additive growth delay in spheroids dosed with Dox plus oxamate. These data demonstrate that inhibition of anaerobic glycolysis might be used to obtain a significant therapeutic gain in combination treatments with cytotoxic drugs or radiotherapy.

Adenosine Triphosphate↗
PubMed1996

Transvascular and interstitial migration of neutrophils in rat mesentery.

OBJECTIVE: The consequential implications of the leukocyte-endothelial cell adhesion reaction, as well as the subsequent migratory activity of the leukocytes within the interstitium proper, are currently known only in general phenomenological terms. Our objective was to carry out a detailed quantitative analysis of transendothelial and interstitial migration. METHOD: We incorporated several new features, such as the video recording of time-lapse photography in conjunction with the time history of individual leukocytes under the influence of representative stimulators and inhibitors. The mesentery was suffused with the chemical activator N-formyl-met-leu-phe (fMLP, 5 x 10(-8) M) and histamine (10(-6) M) for periods up to 3 h. This leads to an attachment of neutrophils preferentially to the walls of small postcapillary venules followed by migration into the adjacent interstitium. RESULTS: The time interval between the initial neutrophil adhesion to the luminal side of the venules and their first appearance on the abluminal side of the venule wall was about 25 min. The time interval for the actual physical migration across the endothelium was only about 1-2 min. There was an initial increase in the number of neutrophils migrating across the wall per unit time after the application of fMLP. However, this effect then gradually decreased over the course of 1 h. In the extravascular tissue, the neutrophils appeared to migrate along random pathways with an average trajectory away from the venular wall. When histamine (1 microM) was applied topically in conjunction with fMLP, the overall migratory flux across the venular wall increased, although the cells migrated comparatively short distances into the interstitium. After pretreatment with phalloidin (25 micrograms/kg), an actin cross-linking agent, neutrophil adhesion and migration in response to fMLP stimulation was reduced. The mast cell stimulator 48/80 (25 mg/ml) resulted in rapid degranulation, which was accompanied by an insignificant increase in neutrophil diapedesis. After fMLP stimulation there was reduced neutrophil emigration in the presence of mast cell inhibitors, such as lodoxamide (1 microgram/kg) and ketotifin (microgram/kg). CONCLUSIONS: Our results demonstrate that both the endothelial cells and interstitial mast cells are involved in the rate of transvascular migration of leukocytes across postcapillary venules and into the interstitium.

Animals↗
PubMed1986

Elevated blood glucose after compound 48/80 treatment is not related to hepatic mast cell degranulation in rats.

Blood glucose, hepatic glycogen, and the histological integrity of hepatic mast cells, were evaluated in anesthetized rats receiving iv injections of 0.125 mg/kg body weight compound 48/80 (a mast cell degranulator) and/or of 0.001 to 10.0 mg/kg body weight lodoxamide tromethamine (an inhibitor of mast cell degranulation). A nonglucogenic dose of lodoxamide, 0.001 mg/kg body weight, prevented dissipation of histochemically demonstrable fluorescence in mast cells (degranulation) without inhibiting compound 48/80-induced hyperglycemia and hepatic glycogenolysis. These results suggest that this glucotropic response is independent of compound 48/80-evoked release of mediators such as serotonin from mast cells.

Animals↗
PubMed2000

[An efficacy study of lodoxamide treatment in allergic eye lesions].

Lodoxamid is an antiallergic drug, which stabilizes the mast cells' membrane blocking the release of the type I hypersensitivity reaction chemical mediators. A number of 25 patients with ocular allergic diseases (allergic conjunctivitis, vernal and atopic keratoconjunctivitis, giant papillary conjunctivitis), were included in this study. Lodoxamid, solution 0.1% (Alomide), was given 4 times daily for 6 weeks. The study's aim was to assess the lodoxamid's efficiency, on the ocular signs and symptoms. The study's results showed a significant improvement, or the disappearance of the ocular allergic disease. It is debated upon the lodoxamid's way and place of action, in blocking the type I hypersensitivity reaction. The lodoxamid's efficiency is due to its pharmacological features, by means of which it is effective on many links of the pathogenic chain: mast cells, eosinophils, lymphocytes, neutrophils, antigen presenting cells. Due to its action lodoxamid stabilizes the mast cell's membrane, and inhibits the release of histamine, prostaglandins, leukotrienes, triptase, interleukines -4, -8 and TNF-. During therapy with lodoxamid recruitment and activation of eosinophils is decreased, causing a significant reduction of the basic major protein, cationic eosinophilic protein, eosinophilic derived neurotoxin, eosinophilic peroxidase. Lodoxamid reduces the expression of ICAM-1 on the surface of the antigen presenting cells, and decreases the number of the TH2 cells, from the tears of the allergic patients.

Adolescent↗
PubMed2001

[Evaluation of efficacy and safety of sterile solution of lodoxamide in patients with ocular allergy].

PURPOSE: Evaluating the efficiency and safety of Alomide (lodoxamide 01.%) in the treatment of allergic conjunctivitis. MATERIAL, METHOD: 12 patients have been selected during may-august 1998, in order to be treated with Alomide 4 times daily. The clinical exam of the patient included: general information, history, ocular examination. The ocular status of each patient has been evaluated with a score: the intensity of each symptom and sign has been graded between 1-3. RESULTS: In all cases, the use of Alomide induced the improvement of the typical symptoms and signs of the allergic conjunctivitis. No side effect related to the use of the drug has been noted. CONCLUSION: Due to its dual action (inhibition of both mast cells and eosinophils), Alomide covers most of the allergic response.

Administration, Topical↗
PubMed2001

Lodoxamide as adjuvant therapy in patients with dry eye.

Dry eye, due to its impaired function of tear film becomes more susceptible to all kinds of airborne allergens. Due to air pollution this is more marked in urban areas, and is compounded by the modern way of life. There are various standard topical medications which alleviate allergic reaction of the eye, but many of them must be administered with caution and only on short term due to their potentially hazardous side effects. The purpose of this work is to assess the efficacy of lodoxamide, a new antiallergic medication for topical use, whose advantage is low or absent risk of adverse side effects, in alleviating local allergic reactions of the eye in patients with dry eye. Research has shown that, compared to treatment with eye lubricants alone (artificial tears), treatment with artificial tears combined with lodoxamide has resulted in more marked decrease in the signs of inflammation, and to the lesser extent to the reduction of the symptoms as well.

Administration, Topical↗
PubMed2000

Contrast of the effect of alomide and sodium cromoglycate in the treatment of allergic eye diseases.

PURPOSE: To observe the clinical effect of alomide and sodium cromoglycate eyedrops in the treatment of atopic conjunctivitis, vernal conjunctivitis and giant papillary conjunctivitis. METHODS: Randomized control study was used. Alomide and sodium cromoglycate eyedrops used to treat two groups of patients for two weeks. The effects of the two groups were compared. RESULTS: With respect of comprehensive therapeutic effect, the effectiveness rate was 83.6% in alomide group, and 63.3% in sodium cromoglycate group, which was not significantly different statistically. With respect of itching alleviation, alomide is more effective than sodium cromoglycate. No adverse effects were found in both groups. CONCLUSION: Our study suggests that alomide is a safe and effective drug in the treatment of allergic conjunctivitis.

Adolescent↗
PubMed2002

[Evaluation of the efficacy and safety of lodoxamide in patients with allergic eye diseases].

PURPOSE: To evaluate the effectiveness of lodoxamide in the therapy and prophylaxis of the ocular allergies. PATIENTS AND METHODS: This prospective study included 64 patients divided in 2 groups. In the first group there were 47 symptomatic patients suffering from seasonal allergic conjunctivitis (n = 27), perennial allergic conjunctivitis (n = 16) and giant papillary conjunctivitis (n = 4). The symptomatic patients were examined upon arrival and every 2 weeks until the symptoms were reduced. During the period, lodoxamide drops were administered 4 times a day. In the second group there were 17 patients who had a history of seasonal ocular allergies during previous years but were still not symptomatic upon arrival. In the group of 17 patients who were very likely to develop ocular allergy but up to inclusion into the study had no ocular symptoms, 12 (70%) presented with allergic rhinitis while 5 (30%) had asthma. The symptoms intensity (itching, discomfort, foreign body sensation, pain, tearing) was graded on a 0-3 scale. The clinical signs (follicles, papillae, hyperemia, conjunctival edema, Trantas dots, stromal infiltrates) were detected on a slit lamp examination and graded on a 0-3 scale. RESULTS: In the group of 47 symptomatic patients 2-4 weeks after lodoxamide administration, 70-80% of symptomatic patients examined clinically had less or no follicles, 60-70% had reduced or no edema, the secretion was stopped or greatly reduced in 50-70% of patients. All of the patients reported reduced or no itching, 60% of patients reported less discomfort, photophobia and reduced tearing. In the asymptomatic group two weeks after the initiation of the prophylaxis 88% of patients were still with no ocular signs of allergy while 12% of patients had a conjunctival hyperemia and follicles. After 4 weeks of the prophylaxis 76% of patients patients were still asympthomatic while only 4 developed a mild form of allergic conjunctivitis (conjunctival hyperemia and papillae), but less severe than during previous episodes. CONCLUSION: Lodoxamide was effective in reduction of symptoms and clinical signs of the ocular allergies. The best results were obtained if the drug was administered as a prophylaxis or very early in the course of the disease.

Anti-Allergic Agents↗