Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UMLS:C0033774 (
pruritus
)
14,546
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Levocabastine
is a new topical histamine H1 antagonist. The antihistaminic and antiallergic effects of levocabastine eye drops have been evaluated in eight conjuctival provocation studies (n = 238). Two studies used a histamine challenge; five studies used allergen challenge; one study used both and in one study allergic provocation was with compound 48/80. In all but one study, only one single dose of levocabastine (one or two drops) was given. Six studies were against placebo only; one was against cromoglycate and one study used both placebo and cromoglycate as reference drugs. Single instillation of levocabastine eye drops protected against histamine and allergen-induced ocular symptoms within a period of 10 minutes.
Levocabastine
eye drops significantly alleviated conjunctival
itching
, redness, chemosis, eyelid swelling and tearing induced by histamine or allergen challenge (p < or = 0.05). Four hours after administration levocabastine was still active. With levocabastine, but not with cromoglycate, a significant increase was observed in the allergen threshold. Even when compared to cromoglycate given as a pre-treatment four times daily for two weeks before the allergen challenge, a single dose of levocabastine was significantly more effective in inhibiting hyperaemia, eyelid swelling, chemosis and tearing (all p < 0.05). In conclusion, conjunctival provocation studies have established that levocabastine has a rapid and long-lasting effect in protecting against histamine or allergen-induced conjunctival symptoms.
...
PMID:Efficacy of levocabastine in conjunctival provocation studies. 136 80
Histamine is the key mediator producing
itching
, redness and chemosis in allergic conjunctivitis. Histamine levels in tears are increased ten-fold in patients with this allergic condition.
Levocabastine
is a newly synthesized histamine H1 antagonist which has been formulated as both eye drops and nasal spray. In well established assays of antihistamine activity, levocabastine was found to be the most potent antihistamine compound available, being 15,000 times more potent than chlorpheniramine. Ocular provocation studies in man have shown that levocabastine protects against the symptoms of allergen-induced conjunctivitis. Ophthalmological examinations, including slit lamp and ophthalmoscopy showed no adverse effects. Data from therapeutic studies are available for more than 1700 patients with allergic conjunctivitis treated for 2-16 weeks. One drop of levocabastine (0.5 mg/ml) per eye given two to four times daily provided significantly better symptom control than placebo, with good to excellent results in 71% of patients on levocabastine compared to 55% on placebo (p < 0.001).
Levocabastine
has a fast onset of action. In one study 94% of patients experienced symptom relief within 15 minutes after the first instillation. The effects observed with levocabastine were at least as good as those with ocular cromoglycate or oral terfenadine. The incidence of adverse experiences was not different from placebo.
Levocabastine
promises to be a valuable treatment for patients with allergic conjunctivitis.
...
PMID:New trends in the treatment of allergic conjunctivitis. 136 81
Levocabastine
is a new H1 receptor blocking antihistamine which is intended for topical use in the treatment of allergic conjunctivitis. The protective effect of the drug in conjunctival provocation test (CPT) was evaluated in a double blind study of 25 children aged 9-17 years with confirmed pollen allergy. One drop of levocabastine, cromoglycate or placebo was instilled into the conjunctival sac of both eyes. After 15 min CPT was performed, starting with 320 BU of pollen extract. The allergen dose was increased every 10 min in half 10-log steps in the right eye until a positive reaction occurred, or the top dose 320,000 BU was reached. The lowest dose resulting in a positive CPT reaction, i.e. at least 50% of the conjunctiva with erythema, was defined as the allergenic threshold dose (ATD). Pretreatment with levocabastine resulted in a median ATD of 32,000 BU, compared with 10,000 after cromoglycate (P less than 0.001) or placebo (P less than 0.01).
Levocabastine
was also superior in reducing subjective
itch
in the eyes. Determination of the ATD can be used as a relatively quick assessment of drugs intended for the treatment of allergic conjunctivitis.
...
PMID:Topical levocabastine protects better than sodium cromoglycate and placebo in conjunctival provocation tests. 196 26
Levocabastine
is a new, highly potent, and specific H1 antagonist. The effects of this drug, administered topically, were evaluated in a conjunctival provocation test (CPT) with allergens. CPT was performed by the instillation of one drop of allergen at increasing concentrations in the inferior conjunctival sac of each eye, alternatively, and stopped when both
itching
and redness of the conjunctiva were present. The concentration of allergen at this step was considered as the reaction threshold. Eleven patients, allergic to grass pollen, underwent, in winter, a first CPT without pretreatment (screening test); the CPT was then repeated twice after a 24-hour treatment, once, with a placebo, and once, with levocabastine (one drop twice a day, 0.5 mg/ml), administered in a double-blind fashion and in random order. The minimal interval between the two tests was 1 week. There was no significant difference between the thresholds determined in the two CPTs performed without medication (screening test and placebo), whereas the threshold was significantly increased (p less than 0.001) after pretreatment with levocabastine. Individually, the threshold increased in 10/11 patients (p less than 0.01).
Levocabastine
prevented both redness and
itching
. A late allergic reaction was observed by the patient in 6/11 CPTs performed after placebo treatment and 8/11 after levocabastine treatment. We conclude that, in this model of allergic conjunctivitis, levocabastine increased the conjunctival tolerance to an allergen. Further studies should help to determine the true place of this H1 antagonist in the treatment of allergic conjunctivitis.
...
PMID:Effect of levocabastine, a new H1 antagonist, in a conjunctival provocation test with allergens. 290 14
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.
...
PMID:Effect of topical levocabastine on allergic and non-allergic perennial rhinitis. A double-blind study, levocabastine vs. placebo, followed by an open, prospective, single-blind study on beclomethasone. 304 8
The efficacy of a new antihistamine, levocabastine, in alleviating the ocular allergic reactions induced by both histamine and 48/80 was evaluated in humans.
Levocabastine
(0.5%) was instilled in one eye of 30 volunteers, and vehicle in the contralateral eye. After 15 minutes, half of the subjects received histamine (25 mg/ml) and half, 48/80 (7.5 mg/ml). The signs and symptoms of allergy were graded clinically after 30 minutes. Compared with a buffer control, levocabastine significantly alleviated
itching
(P = 0.01), redness (P = 0.0156), and chemosis (P = 0.005) induced by histamine, and
itching
(P = 0.032) and redness (P = 0.029) induced by 48/80. The results from these pharmacologic models support the clinical use of levocabastine for the treatment of allergic conjunctivitis.
...
PMID:Levocabastine. Evaluation in the histamine and compound 48/80 models of ocular allergy in humans. 321 58
This double-blind, parallel-group study compared topical levocabastine (eye drops and nasal spray) and oral terfenadine in 27 patients with seasonal allergic rhinoconjunctivitis over a period of 8 weeks. The main aim of this trial was to assess the ocular tolerability of levocabastine eye drops. Comparison of therapeutic efficacy was a secondary study objective. Use of oral and ocular medication was mandatory, however the nasal spray was only to be used when required. The use of nasal spray was 46% in the levocabastine group and 56% in the terfenadine group. Ophthalmologic examinations indicated that levocabastine eye drops were well tolerated. The incidence of adverse reactions was 31% in the levocabastine group and 43% in the terfenadine group. At the end of the trial, a total of 88% of levocabastine-treated patients rated the effect of therapy on ocular symptoms to be excellent or good compared with 75% of those who received terfenadine, while 75% of patients in each group were satisfied with the effect of therapy on nasal symptoms. The investigator's evaluation of symptom severity revealed consistently better results with levocabastine.
Levocabastine
was significantly more effective than terfenadine in relieving ocular
itching
(p = .02). The patients' visual analogue scale ratings also showed significantly better results for levocabastine, particularly with respect to nasal symptoms.
Levocabastine
was significantly better than terfenadine for a number of symptoms on days when the pollen count was high. In conclusion, topical levocabastine appears to be a well-tolerated and effective alternative to oral terfenadine for the treatment of seasonal allergic rhinoconjunctivitis.
...
PMID:Safety and efficacy of topical levocabastine compared with oral terfenadine. 790 99
The term ocular allergy encompasses a group of diseases in which there is a high frequency of atopy, ocular
itching
, stringy discharge and a papillary conjunctival reaction. Conditions confined to the lids and conjunctiva (e.g. seasonal allergic conjunctivitis) have a good prognosis but those involving the cornea may result in visual impairment (e.g. atopic keratoconjunctivitis). Mast cell and eosinophil mechanisms are important in al the ocular allergies, but T cell inflammation is prominent only in vernal keratoconjunctivitis, atopic keratoconjunctivitis and giant papillary conjunctivitis. Therapy involves the use of antigen avoidance (where possible), nonspecific medical therapy (e.g. cold compresses, artificial tears), specific medical therapy and, in certain situations, immunotherapy and surgery. Topical antihistamines (often in combination with a vasoconstrictor) and oral antihistamines are widely used in perennial and seasonal conjunctivitis.
Levocabastine
is a new preparation which is more rapid and potent. Mast cell inhibitors [e.g. sodium cromoglycate (cromolyn sodium)] have a proven track record as safe and effective therapy for all ocular allergic diseases and the newer, more potent nedocromil and lodoxamide are now available. Topical steroids are only indicated in sight-threatening disease due to their serious adverse effects and other therapy should be continued to minimise the dose required. There is a lack of intermediate potency and high potency but safe topical preparations. A number of future possibilities exist, some of which have been partially explored. Cyclo-oxygenase inhibitors have proved of limited use, but inhibitors of lipoxygenase and kinin pathways are awaited. Although results with HEPP have been disappointing, other modulators of mast cell function (e.g. picumast, beta-agonists and phosphodiesterase inhibitors) may prove useful in the future. So far, results with topical cyclosporin in serious disease are very encouraging. Future developments in the manipulation of eosinophilic products, cytokines and adhesion molecules may also be relevant. However, the current situation for those with serious ocular allergy remains a disturbing dependence upon topical steroids, with all the attendant risks.
...
PMID:Therapeutic options in ocular allergic disease. 852 55
A total of 22 asymptomatic patients with a documented history of allergic rhinitis participated in this single-centre, double-blind, randomized, placebo-controlled, cross-over trial undertaken to assess the efficacy and tolerability of levocabastine nasal spray (0.5 mg/ml) in the prevention of allergen-induced nasal symptoms. Objective assessment of nasal symptoms revealed that the severity of sneezing was significantly lower following treatment with levocabastine (p < 0.001), with rhinorrhoea also tending to be less severe in the levocabastine-treated group (0.05 < p < 0.1). Rhinomanometry and acoustic rhinometry failed to reveal any significant intergroup differences, and there were no differences in nasal albumin concentrations between the two treatment groups. Patients' VAS ratings revealed significant differences in favour of levocabastine for sneezing (p < 0.001) and
itching
(p < 0.05), with the severity of rhinorrhoea also tending to be lower during treatment with this topical antihistamine (0.05 < p < 0.1). The mean total symptom score was also significantly lower in levocabastine-treated patients (p < 0.05).
Levocabastine
was well tolerated. Only two adverse events were reported: fatigue in one patient, and vesicular rash with facial oedema and urticaria in another. In conclusion, intranasal levocabastine provided effective protection from nasal allergen challenge and would appear to be a valuable therapeutic approach in patients with allergic rhinitis.
...
PMID:Intranasal levocabastine provides fast and effective protection from nasal allergen challenge. 893 80