Topical Levocabastine Research Articles

The Early Efficacy of Topical Levocabastine in Patients with Allergic Conjunctivitis

We investigated the early efficacy of topical levocabastine, an H(1) histamine-receptor antagonist, in improving the clinical symptoms of allergic conjunctivitis. Thirty-six patients with allergic conjunctivitis were enrolled. One drop of levocabastine was instilled in one eye and one drop of artificial tears in the contralateral eye. Clinical examinations were performed before, and 15 and 30 minutes after instillation. Symptoms of itching and signs of injection were assessed at each time point. Both levocabastine and artificial tears resulted in a statistically significant reduction in ocular itching. However, levocabastine was significantly more effective. Although artificial tears had a positive effect in reducing symptoms of allergic conjunctivitis, by the washing out of allergens, levocabastine was more effective than artificial tears in controlling acute symptoms of allergic conjunctivitis, demonstrating that the selective H1 histamine-receptor antagonist action of levocabastine is rapidly effective in a clinical setting.

Treatment options for seasonal allergic rhinitis

Background:Seasonal Allergic Rhinitis (SAR) or ‘hay fever’ is a common, complex disorder resulting in nasal and ocular symptoms. Treatments for SAR aim to minimise symptoms, improve quality of life and reduce the risk of developing any co-existent disease. Improving the evidence-base for treatment decisions in primary care is now a priority for the NHS.Methods:We used standard systematic review methods to conduct a systematic review of all randomised control studies (1990-2002) evaluating the effectiveness of treatments for SAR. For a study to be included all patients had to be at least 12 years with a physician confirmed diagnosis of hay fever. The minimum length of follow-up was stipulated as being 2 weeks. The interventions and comparisons analysed were those including topical or systemic antihistamines, decongestants, leukotriene antagonists and ipratropium bromide. Steroids were not included as they are preventative rather than curative. Our primary outcome measure was rhinitis quality of life using the validated Juniper Rhinitis Quality of Life Questionnaire. Secondary parameters of effectiveness included visual analogue rhinitis symptom score completed by the doctor and/or patient, medication usage and medication usage scores, days off school or work and adverse events.Results:We found 68 trials satisfying our inclusion criteria, although only four of these had used formally validated outcome measures (Juniper-RQLQ) to assess clinical effectiveness. Because of the heterogeneous nature of the studies identified, we used a narrative overview to summarise data. Three trials have shown that oral fexofenadine significantly improves disease specific quality of life and evidence from one trial indicates that a combination of oral monteleukast and loratadine is also clinically effective. Numerous trials indicate that a number of oral antihistamines with/without oral decongestants improve rhinitis symptoms. Topical levocabastine is also of benefit in reducing rhinitis symptoms but there is at present confliciting evidence on the usefulness of other topical treatments (azelastine and ipratropium bromide).Conclusions:Fexofenadine and a combination of oral monteleukast/loratadine should be regarded as first line interventions for the medical treatment of SAR. There is evidence to suggest that other oral antihistamines and intranasal levocabastine are also likely to be of clinical benefit.

From IgE to anti-IgE: where do we stand?

From IgE to anti-IgE: where do we stand?

Comparison of effects of topical levocabastine and nedocromil sodium on the early response in a conjunctival provocation test with allergen

BACKGROUND:Multiple ocular challenges or seasonal trials have demonstrated the efficacy of levocabastine and nedocromil sodium in the treatment of allergic conjunctivitis. OBJECTIVE: This study was designed to compare the protective effect of levocabastine eye drops with that of nedocromil in a conjunctival provocation test with allergen. METHODS: Twenty-four patients with allergic conjunctivitis to grass pollen were recruited. After a preliminary provocation to determine conjunctival reaction threshold (erythema of at least 50% of the conjunctiva with ocular itching), patients were randomized to receive either topical levocabastine (0.05%) or nedocromil (2%) 15 minutes before provocation. Erythema and pruritus intensity were recorded at each concentration of allergen up to the reaction threshold. RESULTS: The allergen concentration level necessary to reach reaction threshold was increased ( p < 0.001) after treatment with both drugs. Comparison between screening and each treatment indicated that the shift in allergen concentration was significantly greater after levocabastine treatment than after nedocromil treatment ( p = 0.019). Conjunctival itching (symptom score) and erythema (percent conjunctival surface) were also better controlled by levocabastine than by nedocromil during provocation ( p < 0.05). CONCLUSION: In a provocation test with allergen, levocabastine and nedocromil were both effective in increasing the conjunctival tolerance to allergen, with better protection provided by levocabastine. (J Allergy Clin Immunol 1996;98:1045-50.)

Topical ocular levocabastine reduces ICAM-1 expression on epithelial cells both in vivo and in vitro

Topical ocular levocabastine reduces ICAM-1 expression on epithelial cells both in vivo and in vitro

Levocabastine

Levocabastine is a potent and selective histamine H1-receptor antagonist which has been evaluated as a topical treatment (nasal spray and/or eyedrops) for allergic rhinitis and/or conjunctivitis. Data available at the time of the previous review in Drugs, together with more recent results, have clearly demonstrated that levocabastine nasal spray and eyedrops are clinically effective, have a rapid onset of action and are well tolerated in patients with nasal and/or ocular allergic conditions. Previous evidence indicating that topical levocabastine has efficacy similar to or better than that of topical sodium cromoglycate (cromolyn sodium) has been confirmed in more recent studies. Furthermore, results from a number of controlled clinical trials have also shown that topical levocabastine is at least as effective as oral terfenadine for the treatment of allergic rhinoconjunctivitis. Notably, topical levocabastine appears to be more effective than oral terfenadine in improving the severity of selected symptoms. Limited data indicating efficacy equivalent to that of oral loratadine, oral cetirizine or azelastine nasal spray will need to be confirmed. Data from several studies have shown that topical levocabastine has a tolerability profile similar to that of placebo, topical sodium cromoglycate or oral terfenadine. The main adverse events seen in patients treated with topical levocabastine are ocular irritation after application of eyedrops, and headache, nasal irritation, somnolence and fatigue after administration of the nasal spray. Administered doses of topical levocabastine, and subsequent plasma concentrations, are low, and the risk of systemic adverse events is therefore expected to be minimal. Thus, topical administration of levocabastine rapid and effective symptom relief with no apparent serious adverse events in patients with allergic rhinitis and/or conjunctivitis. Topical levocabastine is a useful alternative to topical sodium cromoglycate or oral terfenadine. Additional data supporting current evidence that topical levocabastine can provide more effective symptom relief than oral terfenadine, together with clarification of the relative efficacies of these agents in relation to varying pollen exposure, would help to further confirm its clinical potential. However, the results available to date suggest that the topical formulations of levocabastine are a valuable treatment option in patients with allergic rhinitis and/or conjunctivitis.

Topical levocabastine—a review of therapeutic efficacy compared with topical sodium cromoglycate and oral terfenadine on days with high pollen counts

Levocabastine is a new H1-receptor antagonist specifically developed for the topical treatment of seasonal allergic rhinoconjunctivitis. Clinical experience to date clearly demonstrates that levocabastine eye drops and nasal spray are effective and well tolerated for the treatment of this allergic disorder. Analysis of data from a number of comparative trials reveals that topical levocabastine is at least as effective as sodium cromoglycate and the oral antihistamine terfenadine, even on days with high pollen counts (≥ 50 pollen particles/m3 ) when symptoms are severe. Coupled with a rapid onset of action and twice daily dosing, these findings make topical levocabastine an attractive alternative to other therapeutic approaches as a first-line therapy for the treatment, of this common condition.

Treatment of allergic rhinoconjunctivitis: a review of the role of topical levocabastine

Lcocabastine is an extremely potent and highly selective H1-receptor antagonist which has been specifically developed as eye drops and nasal spray for the treatment of allergic rhinoconjunctivitis. Clinical experience to date suggests that this topical antihistamine is at least as effective as other current first-line therapeutic approaches for the treatment of this condition, including oral H1-receptor antagonists and sodium cromoglycate. Onset of action is rapid, with clinical effects apparent within minutes of instillation. Moreover, duration of action is sufficiently long to permit a convenient twice-daily dosing regimen. Topical levocabastine is well tolerated with an adverse-effect profile comparable with that of placebo and sodium cromoglycate. As might be expected from the route of drug administration, application site reactions are the most frequent adverse effect associated with levocabastine eye drops and nasal spray with an incidence comparable with that seen in placebotreated controls. The availability of effective and well-tolerated topical antihistamines, such as levocabastine, is an important advance which broadens the range of therapeutic approaches available for the clinical management of allergic rhinoconjunctivitis. Levocabastine appears to be an attractive alternative to oral antihistamines as a first-line therapeutic option for the treatment of this atopic condition.

Faster onset of action with topical levocabastine than with oral cetirizine

This international multicentre, open-label, parallel-group trial was undertaken to compare the therapeutic efficacy and tolerability of topical levocabastine and oral cetirizine in patients with perennial allergic rhinoconjunctivitis, with particular reference to the comparative onset of action of the two drugs. A total of 207 patients were randomized to receive either levocabastine nasal spray (0.5 mg/ml, two sprays in each nostril twice daily) plus levocabastine eye drops as required (0.5 mg/ml, one drop in each eye twice daily p.r.n.) or cetirizine orally (10 mg once daily) with a treatment duration of 2 weeks. Onset of action was found to be significantly more rapid with levocabastine than with cetirizine for both nasal and ocular symptoms (p < 0.001). Within 15 min of study drug administration, 36% of levocabastine-treated patients reported relief from nasal symptoms and 32% relief from ocular symptoms compared with 10% and 17% of patients on cetirizine, respectively. At 1 h, the percentages of patients reporting relief were 76% and 38% for nasal symptoms, and 81% and 48% for ocular symptoms in the levocabastine and cetirizine treatment groups, respectively. At 8 h there were no differences between the two treatments. Overall therapeutic efficacy was found to be comparable in the two treatment groups over the 2-week study period with no significant intergroup differences in symptom severity or global therapeutic efficacy. Both drugs were well tolerated with no significant differences in the incidence or type of adverse reactions between the two groups. In conclusion, levocabastine eye drops and nasal spray are as effective and well tolerated as oral cetirizine for the treatment of perennial allergic rhinoconjunctivitis with the advantage of a significantly faster onset of action for both nasal and ocular symptoms.

Comparison of the efficacy and tolerability of topical levocabastine and sodium cromoglycate in the treatment of seasonal allergic rhinoconjunctivitis in children

Children (n = 110) with seasonal allergic rhinoconjunctivitis were randomized to receive either twice daily 0.05% levocabastine eye drops and nasal spray plus twice daily topical placebos or 2% sodium cromoglycate eye drops and nasal spray four times daily for a period of 4 weeks. Patients were required to use the nasal sprays as directed and the eye drops only when required. The results obtained suggest that topical levocabastine is at least as effective as sodium cromoglycate for the treatment of this condition. After 2 weeks treatment the effect of therapy on nasal symptoms was considered to be excellent or good in 72% of levocabastine-treated patients and 54% of patients on sodium cromoglycate (p = 0.009), with corresponding values for ocular symptoms of 81% and 57% in the two groups, respectively (p < 0.05). Investigator assessments also revealed that the severity of sneezing and lacrimation were significantly lower in the levocabastine group at this time (p < 0.05). After 4 weeks of treatment, patient diary data revealed that levocabastine was at least as effective as sodium cromoglycate with intergroup differences attaining statistical significance in favor of the topical antihistamine for nasal congestion (p < 0.05). Both agents were well-tolerated with no significant differences in the incidence or type of adverse reactions in the two treatment groups.

THE ROLE OF LEVOCABASTINE IN THE TREATMENT OF ALLERGIC RHINOCONJUNCTIVITIS

SUMMARY Allergic rhinoconjunctivitis is a common atopic condition frequently encountered in clinical practice, with prevalence figures as high as 20% reported. The socioeconomic impact of this condition is considerable — not only in terms of medical costs but lost work and schooldays and quality of life. A wide range of therapeutic approaches is available, including levocabastine, an extremely potent and highly specific H1‐receptor antagonist which has been developed for topical application as eyedrops and nasal spray. The available clinical data demonstrate that this agent is well tolerated, with an adverse effect profile comparable to sodium cromoglycate and placebo. Onset of action is rapid, with maximum therapeutic effects typically being observed within minutes of application. Results of comparative clinical trials suggest that topical levocabastine is as at least as effective as oral antihistamines and sodium cromoglycate for the treatment of allergic rhinoconjunctivitis, and it is suggested as an attractive alternative to oral antihistamines as first‐line therapeutic option.

Topical levocabastine is more effective than sodium cromoglycate for the prophylaxis and treatment of seasonal allergic conjunctivitis

The efficacy, tolerability, and adverse-effect profile of the recently developed, topical antihistamine levocabastine were compared with those of sodium cromoglycate in a 4-week double-blind, placebo-controlled trial in 95 patients with seasonal allergic conjunctivitis. At the end of the trial, global therapeutic efficacy was considered to be excellent or good in 87% of levocabastine-treated patients, as compared with 68% of sodium cromoglycate-treated patients (P = 0.006) and 63% of those who received placebo (P = 0.05). After 4 weeks of treatment, levocabastine patients had experienced significantly greater relief from their most severe ocular symptom than patients in the sodium cromoglycate group (P < 0.05). Furthermore, 37% of levocabastine-treated patients were virtually symptom-free for at least 75% of the treatment period, as compared with only 6% of patients in the sodium cromoglycate group (P < 0.01) and 4% of those who received placebo (P < 0.01). Moreover, this trend was maintained on days when the pollen count was high, when the corresponding figures were 33%, 6% (P = 0.02), and 4% (P = 0.02), respectively. Levocabastine was well tolerated. Indeed, the incidence of adverse reactions was no greater in the levocabastine group than in the placebo group. Topical levocabastine is an effective and well-tolerated drug for the prophylaxis and treatment of seasonal allergic conjunctivitis.

Topical levocabastine compared with orally administered terfenadine for the prophylaxis and treatment of seasonal rhinoconjunctivitis

Background: This study was designed to compare the efficacy and tolerability of a new topical (nasal spray and eye drops) H 1-receptor antagonist, levocabastine, with that of orally administered terfenadine for the prophylaxis and treatment of seasonal allergic rhinoconjunctivitis. Methods: A total of 115 patients with documented birch pollen allergy were enrolled in this randomized, double-blind, double-dummy, parallel-group trial. Treatment was initiated immediately before the birch pollen season started and continued for a total of 8 weeks. Xylometrazoline (Otrivin) nasal spray was permitted as rescue medication. Results: The investigator's evaluation of symptoms showed similar effects for levocabastine and terfenadine. Both the patients' and the investigator's global evaluations of ocular and nasal symptoms disclosed a somewhat higher percentage of good or excellent results for levocabastine, but the differences were not statistically significant. Visual analog scale ratings from the patients' diaries showed better results for levocabastine. Levocabastine was significantly more effective than terfenadine in relieving sneezing, rhinorrhea, lacrimation, itch, and burning sensation ( p < 0.05). For some symptoms, levocabastine was significantly more effective than terfenadine on days when the pollen count was high. There were no statistically significant differences in the use of rescue medication or in the incidence of adverse reactions reported in each treatment group. Conclusions: In the present study topical levocabastine was frequently more effective than orally administered terfenadine for the treatment of seasonal allergic rhinoconjunctivitis. Both drugs were well-tolerated.

The Dose and Duration of Effect of Levocabastine, A New Topical H1 Antagonist, on Nasal Provocation Reaction to Allergen

This study investigated the dose and duration of effect of topical levocabastine (LC) in patients with perennial allergic rhinitis as evaluated by the effect on nasal provocation test with house dust antigen. Three different doses (0.05, 0.1, and 0.2 mg) of LC were independently administered to evaluate the dose response and duration of effect. Reaction to nasal provocation was evaluated by a scoring system based on a combination of symptoms, such as number of sneezes, degree of nasal discharge, and nasal obstruction. The mean scores at 30 minutes postadministration of each of the three different doses of LC showed a significant decrease as compared with those of preadministration. The effect persisted for 4 hours with a dose of 0.05 mg and 0.1 mg of LC and for 12 hours with 0.2 mg of LC. In a comparison of the three doses potency of effect of LC, the highest dose (0.2 mg) demonstrated the strongest effect in the interval from 4 hours to 10 hours postadministration. These results indicate that LC has an immediate effect and its effect is dose dependent. The present study suggests that nasal symptoms in perennial allergic rhinitis could be relieved by topical application of 0.2 mg of LC, twice a day.

Topical levocabastine compares well with sodium cromoglycate in allergic rhinitis

Topical levocabastine compares well with sodium cromoglycate in allergic rhinitis

Levocabastine

Levocabastine is a long acting, highly potent and selective histamine H1-receptor antagonist, which has been developed for nasal and ocular administration. In controlled trials performed to date levocabastine was effective and well tolerated in the treatment of allergic rhinitis and allergic conjunctivitis. Comparative studies have demonstrated that levocabastine is superior to placebo and at least as effective as sodium cromoglycate (cromolyn sodium) in alleviating symptoms associated with seasonal allergic conditions. Although levocabastine appears to be less effective than the topical corticosteroid beclomethasone with regard to relieving runny and blocked nose, further comparative trials between these 2 agents would be desirable. Similar to other antihistamines, levocabastine provides minimal relief of nasal blockage, but this symptom is believed to be mediated by receptors other than histamine H1. The prompt onset of antiallergic activity after application differentiates levocabastine from the reference topical antiallergic, sodium cromoglycate, which has an onset of efficacy characterised by a lag period, thereby necessitating maintenance treatment. The incidence of adverse effects associated with levocabastine therapy is low and is similar to that observed with placebo and sodium cromoglycate. Levocabastine provides prophylactic protection as well as acute relief from nasal and ocular symptoms in patients with seasonal allergic disorders. With the ever increasing trend towards topical therapy for the treatment of allergic rhinitis and allergic conjunctivitis, levocabastine is a useful addition to the range of drugs currently available. Possible avenues for additional research should include determining whether the antiallergic efficacy of topical levocabastine is superior to that of oral agents such as astemizole and terfenadine, and whether topical therapy is indeed preferred, considering the relative ease of administration of effective oral antiallergic agents.

Topical levocabastine versus sodium cromoglycate in allergic conjunctivitis

The aim of this study was to evaluate the effect of levocabastine, a new H1-blocking antihistamine for topical use, in comparison with sodium cromoglycate on conjunctival symptoms of birch pollinosis. The two drugs were compared in a randomized double-blind comparative study over 5 weeks in 37 children and adolescents (6-19 years of age) with birch pollen conjunctivitis. Nasal symptoms occurred in 31 of the children and were treated with beclomethasone dipropionate nasal spray. An oral antihistamine was offered as rescue medication for eye symptoms. Initially, the patients received placebo four times a day for a 7-day run-in period. Conjunctival symptoms were recorded daily on diary cards on a 100 mm visual analogue scale. The pollen counts indicated a short but intensive birch pollen season. There was no statistically significant difference between the two treatment groups with regard to eye symptom scores before and during active treatment. However, the patients' evaluation of the efficacy of the therapy was in favour of levocabastine (P less than 0.01). Topical levocabastine, an H1-blocker, applied twice daily, seems to protect from symptoms of allergic conjunctivities as favourably as sodium cromoglycate applied four times a day. There was no difference in number or character of reported adverse reactions between the two treatment groups.

Effect of topical levocabastine on allergic and non‐allergic perennial rhinitis

Forty-four patients, with symptoms of nasal obstruction, sneezing, itching and/or rhinorrhea, were entered into a placebo-controlled, double-blind study to evaluate the clinical efficacy of a topical antihistamine drug, levocabastine, applied 4 times a day for 14 days. At the end of the treatment the placebo patients were treated with levocabastine and the levocabastine patients were treated with beclomethasone dipropionate in a single-blind design for another 14 days. This study showed that levocabastine is significantly more active than placebo with reference to nasal discharge and sneezing. Placebo application improved the symptom score. Levocabastine could not be proved to be more effective against nasal obstruction than placebo in the double-blind trial. In the single-blind set-up, levocabastine resulted in an additional improvement in the score for obstruction, after the placebo period. Although the allergic group tended to respond better, no statistically significant difference could be detected between allergic and non-allergic patients. After treatment with levocabastine, beclomethasone dipropionate administration could not improve the results for nasal discharge and sneezing. For nasal congestion, beclomethasone dipropionate proved to be superior to levocabastine.

Topical levocabastine, a selective H1 antagonist, in seasonal allergic rhinoconjunctivitis

Sixty-six patients with seasonal allergic rhinitis due to birch pollens, participated in an efficacy evaluation of topically applied, nasal and ocular, levocabastine, a highly selective H1 antagonist. A single blind comparison was performed between nasal levocabastine and flunisolide, a topical glucocorticoid preparation. Ocular levocabastine was compared with topical naphazoline/antazoline eye drops. Nasal and ocular symptom scores were recorded during a 31-day period. Pollen counts of birch pollens were done simultaneously. A global assessment of treatment efficacy was also made. In the comparison between the ocular treatments a significantly higher number of patients cited levocabastine excellent--it also had the advantage of fewer daily administrations. For nasal symptom scores the topical glucocorticosteroid therapy was in favour by number of sneezes. As for side effects, 44% of the patients complained of local irritation from naphazoline/antazoline eye drops or flunisolide nasal spray, but none with the levocabastine preparations. Topical levocabastine may provide an interesting alternative in the treatment of allergic rhinoconjunctivitis.