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Monographs of Topical Drugs that Have Caused Contact Allergy/Allergic Contact Dermatitis
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Levocabastine is a synthetic piperidine derivative with antihistamine properties. It is a second generation histamine- 1 receptor antagonist. When applied locally into the eye as a topical solution, this agent reduces itching, rhinorrhea and symptoms of allergic rhinitis or conjunctivitis. Levocabastine can also reduce symptoms of allergic rhinitis by preventing an increase in vascular permeability of nasal mucosa. In pharmaceutical products, it is employed as levo- cabastine hydrochloride (CAS number 79547-78-7, EC number not available, molecular formula C26H30ClFN2O2) (1).
Receptors for Neuropeptides: Ligand Binding Studies
Published in Edwin E. Daniel, Neuropeptide Function in the Gastrointestinal Tract, 2019
Sultan Ahmad, Hans-Dieter Allescher, Chiu-Yin Kwan
The antihistamine levocabastine is reported to inhibit NT binding to rat24 and mouse brain membranes.25 Levocabastine selectively inhibited neurotensin binding to low-affinity sites without affecting high-affinity sites.25 We found no effect of levocabastine on NT binding to canine small intestine circular smooth muscle plasma membranes or to neuronal membranes from deep muscular plexus or submucous plexus.153 Several other nonmurine tissues are also known to be insensitive to levocabastine.26 More extensive screening of several tissues from different species with regard to the action of levocabastine would provide interesting information about the biological evolution of the levocabastine-sensitive sites of NT receptors.
Pharmacokinetic-Pharmacodynamic Correlations of Antihistamines
Published in Hartmut Derendorf, Günther Hochhaus, Handbook of Pharmacokinetic/Pharmacodynamic Correlation, 2019
Eric Snoeck, Achiel Van Peer, Jos Heykants
All first-generation H1-receptor antagonists were usually administered three or four times daily. However, the development of the second-generation H1-receptor antagonists was focused on a more convenient once or twice daily dosing. Most second-generation H1-receptor antagonists are to be administered orally in the treatment of rhinoconjunctivitis and urticaria.1.However, intranasally applied levocabastine provides significant protection against allergen-triggered allergic rhinitis symptoms.63,64 In addition, levocabastine applied to the conjunctivae also provides relief of allergic conjunctivitis symptoms.65
Efficacy and Tolerability of Ketotifen in the Treatment Of Seasonal Allergic Conjunctivitis: Comparison between Ketotifen 0.025% and 0.05% Eye Drops
Published in Ocular Immunology and Inflammation, 2019
Andrea Leonardi, Decio Capobianco, Nicola Benedetti, Antonio Capobianco, Fabiano Cavarzeran, Tania Scalora, Rocco Modugno, Oren Mark Feuerman
First generation antihistamines are still used in combination with vasoconstrictors for the treatment of OA because of their rapid onset of action and easy over the counter accessibility. However, due to the short duration of effects, usually 2 hours, dosing may be necessary up to four times per day. In addition, the vasoconstrictor causes stinging upon instillation, can lead to rebound congestion and local toxicity, and are contraindicated in the presence of narrow angles. The second-generation of topical antihistamines levocabastine and emedastine eye drops share several benefits including longer duration of action, lasting 4 hours, and less stinging upon instillation.
Current therapeutical strategies for allergic rhinitis
Published in Expert Opinion on Pharmacotherapy, 2019
Ludger Klimek, Annette Sperl, Sven Becker, Ralph Mösges, Peter Valentin Tomazic
H1 antihistamines are available for both systemic and topical administration [9,10]. Nasal obstruction is probably more effectively treated via the topical route [9]. Topical antihistamines such as azelastine, levocabastine, and olopatadine show rapid effects (within approximately 15 min) and are therefore particularly useful in cases of acute onset of symptoms [9,11]. In the direct comparison of their efficacy with that of nasal GCS, no clear recommendations can be made [12]. While some studies attribute better efficacy to nasal GCSs [13], other studies have shown equal efficacy for both therapeutic approaches [14].
Therapeutic approaches targeting the neurotensin receptors
Published in Expert Opinion on Therapeutic Patents, 2021
Meclinertant (SR48692, 3) was discovered as the first selective, non-peptide antagonist of NTSR1 [29,30]. It was in phase II/III clinical trials by Sanofi for the treatment of psychiatric disorders, anorexia nervosa, colorectal cancer, small cell lung cancer, and prostate cancer. However, no recent development has been reported. It is used extensively as a research tool to explore the interaction between neurotensin and other neurotransmitters and their roles in physiological and pathological processes. SR142948A (4), another compound described by the Sanofi group blocked both NTSR1 and NTSR2 was found to be more potent than SR48692 [31]. The antihistamine levocabastine (5) was subsequently found to act as a potent and selective antagonist for NTSR2 and was the first drug used to characterize the different subtypes of neurotensin receptors [22]. There is still discrepancy in the pharmacological properties of NTSR2. In particular, it is known that NT can act as an agonist, inverse agonist, or antagonist at this receptor. Depending on the species from which the NTSR2 was isolated and the cell system used to evaluate signaling, the assays have yielded different results [24], and the pharmacological profile of the known compounds have also varied [32]. Using FLIPR assays in a CHO cell line stably expressing NTSR2, this receptor mediated calcium release, and the compounds SR48692 and SR142948A, which are known NTSR1 antagonists in vivo, were full agonists at NTSR2 [33]. It was also found that the NTSR2-selective compound levocabastine, an analgesic in vivo, was found to be a partial agonist in vitro. In contrast, although NT behaves as an analgesic in vivo, it acted as an NTSR2 antagonist in the FLIPR assay. β-Lactotensin (His-Ile-Arg-Leu) derived from residues 146–149 of bovine β-lactoglobulin was reported to be a first natural ligand selective for NTSR2 over NTSR1 (Figure 2) [34].