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

Azevedo, M.

doi:10.1155/s0962935195000809

Cited by 4 publications

(3 citation statements)

References 3 publications

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“…Terfenadine, a selective histamine H1 receptor antagonist [1][2][3][4][5][6][7][8], is clinically used against allergic disorders such as hay fever, allergic rhinitis, and other histamine-mediated disorders [6,[8][9][10]. The substance does not impair psychomotor performance to a similar extent as traditional antihistamines [4,[6][7][8].…”

Section: Introductionmentioning

confidence: 99%

Stimulating Effect of Terfenadine on Erythrocyte Cell Membrane Scrambling

Signoretto

Castagna²,

Bhuyan³

et al. 2016

Cell Physiol Biochem

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Background/Aims: The antihistaminic drug Terfenadine may trigger apoptosis of tumor cells, an effect unrelated to its effect on histamine receptors. Similar to apoptosis of nucleated cells, erythrocytes may enter eryptosis, the suicidal death of erythrocytes characterized by cell shrinkage and cell membrane scrambling with phosphatidylserine translocation to the erythrocyte surface. Signaling triggering eryptosis include increase of cytosolic Ca²⁺ activity ([Ca²⁺]_i), oxidative stress, and ceramide. The present study explored, whether Terfenadine is capable to trigger eryptosis. Methods: Flow cytometry was employed to estimate phosphatidylserine abundance at the erythrocyte surface from annexin-V-binding, cell volume from forward scatter, [Ca²⁺]_i from Fluo3-fluorescence, abundance of reactive oxygen species (ROS) from 2′,7′-dichlorodihydrofluorescein (DCF) diacetate dependent fluorescence, and ceramide abundance at the human erythrocyte surface utilizing specific antibodies. Hemolysis was quantified from haemoglobin concentration in the supernatant. Results: A 48 hours exposure of human erythrocytes to Terfenadine (≥ 5 µM) significantly increased the percentage of annexin-V-binding cells and triggered hemolysis without significantly modifying the average forward scatter. Terfenadine (7.5 µM) significantly increased Fluo3-fluorescence, but did not significantly modify DCF fluorescence or ceramide abundance. The effect of Terfenadine on annexin-V-binding was significantly blunted but not abolished by removal of extracellular Ca²⁺. Exposure of human erythrocytes to Ca²⁺ ionophore ionomycin (1 µM, 15 min) triggered annexin-V-binding, an effect augmented by Terfenadine pretreatment (10 µM, 48 hours). Conclusions: Terfenadine triggers phospholipid scrambling of the human erythrocyte cell membrane, an effect in part due to entry of extracellular Ca²⁺ and in part due to sensitizing human erythrocyte cell membrane scrambling to Ca²⁺.

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Section: Introductionmentioning

confidence: 99%

Stimulating Effect of Terfenadine on Erythrocyte Cell Membrane Scrambling

Signoretto

Castagna²,

Bhuyan³

et al. 2016

Cell Physiol Biochem

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“…Topical levocabastine appears to be at least as effective as oral antihistamines for the treatment of allergic rhinoconjunctivitis, with the advantage of a significantly more rapid onset of action 8 and, in particular, may provide greater relief from symptoms on days with high pollen counts. 56 Furthermore, topical levocabastine is at least as effective as azelastine nasal spray, with the advantage of a more favourable tolerability profile and the availability of eye dro9Ps for the relief of concurrent ocular symptoms.…”

Section: Allergen Avoidancementioning

confidence: 99%

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

1995

Mediators of Inflammation

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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.

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“…Levocabastine hydrochloride ( 1 ), a selective second-generation H 1 receptor antagonist, was discovered in 1979 by Janssen. Since then, it has been used in clinical formulations such as eye drops and nasal sprays for the treatment of allergic conjunctivitis and rhinitis [ 13 , 14 , 15 ]. Despite its clinical importance, only two synthetic methods for the preparation of levocabastine have been reported [ 16 , 17 ].…”

Section: Introductionmentioning

confidence: 99%

Practical and Sustainable Synthesis of Optically Pure Levocabastine, a H1 Receptor Antagonist

et al. 2017

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A practical and sustainable method for the synthesis of levocabastine hydrochloride (1), a H1 receptor antagonist for the treatment of allergic conjunctivitis, that can be applied to the industrial production of the compound has been developed. Substantial improvements over the previously reported procedure are achieved via efficient preparation of an optically active key intermediate (5) without chiral resolution and with a more effective detosylation, which complements the previous procedure. Notably, our process requires no chromatographic purification and provides levocabastine hydrochloride in greater than 99.5% purity in a 14.2% overall yield.

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

Cited by 4 publications

References 3 publications

Stimulating Effect of Terfenadine on Erythrocyte Cell Membrane Scrambling

Stimulating Effect of Terfenadine on Erythrocyte Cell Membrane Scrambling

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

Practical and Sustainable Synthesis of Optically Pure Levocabastine, a H1 Receptor Antagonist

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