Alesion (epinastine) / Boehringer Ingelheim - LARVOL DELTA

One-Pot Synthesis of Hantzsch Reaction for Fluorometric Quantification of Epinastine in Aqueous Humor Samples. (PubMed, Luminescence) - "The dynamic range for EPS detection in the pure state is 0.1-1.0 μg/mL (LOQ = 79.23 ng/mL and LOD = 26.15 ng/mL). The approach exhibits favorable percentage recoveries in spiked aqueous humor (95.80 ± 1.57% to 100.80 ± 1.89%)."

Journal • Conjunctivitis • Ocular Infections • Ocular Inflammation • Ophthalmology

Direct comparison of the effects of first- and second-generation H1 -receptor blockers on motor functions in mice. (PubMed, Pharmazie) - "This study investigated the impact of first-generation (diphenhydramine and d -chlorpheniramine) and second-generation (epinastine, ketotifen, bepotastine, and levocetirizine) H1R antagonists on motor functions in mice using activity wheel, balance beam, inclined screen, and rotarod tests. These findings provide valuable insights into the differential effects of first- and second-generation H1R antagonists on motor functions. These results highlight the importance of understanding individual profiles of H1R antagonists to minimize adverse effects, ensure patient safety, and improve quality of life."

Clinical • Journal • Preclinical • Allergy

Successful Transition From Topical Ophthalmic Drops to Cream Formulation in the Management of Mild Allergic Conjunctivitis: A Case Report. (PubMed, Cureus) - "This case suggests that epinastine eyelid cream may serve as an effective once-daily alternative to conventional eye drops in mild allergic conjunctivitis. While this represents the first documented successful transition between delivery methods, larger clinical trials are warranted to confirm these findings and explore applications across various presentations and severities of allergic ocular disease."

Journal • Allergy • Conjunctivitis • Immunology • Ocular Infections • Ocular Inflammation • Ophthalmology

Abating a micropollutant epinastine by UV-based advanced oxidation processes: Comparison for UV/hydrogen peroxide, UV/persulfate, and UV/chlorine, impacts of bromide contents, and formation of DBPs during post-chlorination. (PubMed, Chemosphere) - "By comparing estimated DBP formations at a constant degradation rate of epinastine, UV/chlorine formed smaller concentrations of DBPs. Consequently, this study experimentally revealed that UV/chlorine is superior to UV/hydrogen peroxide and UV/persulfate for degrading epinastine at the possible pH and bromide content in the environment and controlling toxicological risks caused by disinfection DBPs formation by optimising chlorine dosage and UV fluence."

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Identification of Epinastine as CD96/PVR inhibitor for cancer immunotherapy. (PubMed, BMC Biol) - "Our results demonstrated that the development of small molecule inhibitor Epinastine targeting CD96/PVR pathway, which proposed a promising strategy and drug candidate for cancer immunotherapy."

Journal • Oncology • CD96 • IFNG • IL2 • TIGIT

Efficacy of Epinastine Eyelid Cream in Pediatric Vernal Keratoconjunctivitis: A Case Report. (PubMed, Cureus) - "Further studies are needed to evaluate the long-term efficacy and safety of epinastine eyelid cream. However, once-daily application of eyelid cream may serve as a viable treatment and management option for pediatric patients with VKC."

Journal • Atopic Dermatitis • Conjunctivitis • Dermatitis • Dermatology • Dry Eye Disease • Immunology • Inflammation • Ocular Infections • Ocular Inflammation • Ophthalmology • Pediatrics

Safety and efficacy of a novel 0.5% epinastine topical eyelid cream in allergic conjunctivitis: a phase 3 trial. (PubMed, Jpn J Ophthalmol) - "With its novel route of administration, 0.5% epinastine topical eyelid cream may be considered a unique, easy-to-use, once-daily treatment option to prevent the onset of seasonal allergic conjunctivitis."

Journal • P3 data • Conjunctivitis • Ocular Infections • Ocular Inflammation • Ophthalmology

Effects of natural environments on drug contents in nails: comparison of drug residual rates between nails and hair to determine the drug-use history of corpses in unnatural death cases using micro-segmental analysis. (PubMed, Forensic Toxicol) - "In comparison with hair data obtained under the same environmental conditions, light affected drugs in the hair rather than in nails, whereas water and soil greatly affected drugs in the nails rather than in hair. Although the disposition of drugs incorporated in the tissues differed between nails and hair, the analytes were detected in nails and hair strands left in severe natural environments. MSA could be useful for estimating drug-use histories and personal profiles using the nails and hair of a corpse."

Journal • Allergic Rhinitis • Immunology

Cost-effectiveness Analysis of Second-Generation Antihistamine 1 Receptor Blockers and Japanese Kampo Shoseiryuto for Treating Perennial Allergic Rhinitis in Outpatient Settings in Japan. (PubMed, Hosp Pharm) - " The most cost- and clinically effective SGAs were determined from a list of 6 SGAs (bepotastine, 10 mg; cetirizine, 10 mg; ebastine, 10 mg; epinastine, 20 mg; loratadine, 10 mg; and olopatadine, 5 mg) together with shoseiryuto, using the overall improvement rate through a model-based analysis. Ebastine (10 mg) was the most cost-effective treatment strategy for PAR among the agents evaluated in this study. This insight could aid in establishing an appropriate formulary for treating PAR in hospitals and communities."

Cost effectiveness • HEOR • Journal • Allergic Rhinitis • Immunology • Inflammation

Anti-edematous effects of epinastine, cetirizine and its enantiomers in λ-carrageenan-induced edema in rat hind paw. (PubMed, Pharmazie) - "Urticaria is induced by the histamine released from mast cells which develops wheals (edema) as a visual feature. In summary, second-generation histamine H1 -receptor blockers, at least those examined in this study, may be able to reduce the clinical symptoms of urticaria associated with edema. Levocetirizine hydrochloride is also anticipated to have stronger anti-edematous effects than cetirizine hydrochloride because levocetirizine is responsible for cetirizine's anti-edematous activity."

Journal • Preclinical • Dermatology • Immunology • Urticaria

Trans-eyelid distribution of epinastine to the conjunctiva following eyelid application in rabbits. (PubMed, Jpn J Ophthalmol) - "After the application of epinastine cream to the eyelid skin, epinastine gradually permeated the eyelid. The compound was retained in the conjunctiva for 8-24 h post-administration, indicating that epinastine cream is a promising long-acting formulation for treating allergic conjunctivitis."

Journal • Preclinical • Conjunctivitis • Ocular Infections • Ocular Inflammation • Ophthalmology

Microliquid/Liquid Interfacial Sensors: Biomimetic Investigation of Transmembrane Mechanisms and Real-Time Determinations of Clemastine, Cyproheptadine, Epinastine, Cetirizine, and Desloratadine. (PubMed, Anal Chem) - "Real-time determinations of these antihistamines have been achieved through potentiostatic chronoamperometry (I-t), exhibiting good selectivity with the addition of nine common organic or inorganic compounds in living organisms and revealing the potential for in vivo pharmacokinetics. Besides providing a satisfactory surrogate for studying the transmembrane mechanism of antihistamines, this work also sheds light on micro- and nano L/L interfacial sensors for in vivo analysis of pharmacokinetics at a single-cell or single-organelle level."

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Monoaminergic Systems in Flight-Induced Potentiation of Phonotactic Behavior in Female Crickets Gryllus bimaculatus. (PubMed, Insects) - "Octopamine is known to be released into the hemolymph during flight in insects; however, the octopamine receptor antagonist epinastine did not abolish the effects of flight in our study...Our results suggest that the serotoninergic system may contribute to the facilitation of female phonotactic behavior by flying. We suggest that both flying and serotonin enhance sexual motivation in females and, by these means, impact their behavioral response to the male calling song."

Journal

A Study to Evaluate the Efficacy and Safety of Epinastine Hydrochloride Eye Drops in the Treatment of Chinese Seasonal Allergic Conjunctivitis Patients (clinicaltrials.gov) - P3 | N=266 | Completed | Sponsor: Zhaoke (Guangzhou) Ophthalmology Pharmaceutical Ltd.

New P3 trial • Conjunctivitis • Ocular Infections • Ocular Inflammation • Ophthalmology

Epinastine Cream: A Novel Once-Daily Therapeutic Agent for Allergic Conjunctivitis. (PubMed, J Ocul Pharmacol Ther) - " The results suggest that epinastine cream is a strong, long-lasting, and skin-penetrating inhibitor of type I allergic reactions. The 0.5% epinastine cream applied once daily could be a promising, potent, and long-acting therapeutic agent for allergic conjunctivitis."

Journal • Allergy • Conjunctivitis • Ocular Infections • Ocular Inflammation • Ophthalmology

Effects of temperature, humidity, light, and soil on drug stability in hair: a preliminary study for estimating personal profiles using micro-segmental analysis of corpse hair. (PubMed, Forensic Toxicol) - "Although the exposure to sunlight and storage in soil for long times made drug-distribution analysis difficult, MSA could be applied even to hair strands collected from corpses left in severe environments."

Journal • Allergic Rhinitis • Immunology

Bite force, body size, and octopamine mediate mating interactions in the house cricket (Acheta domesticus). (PubMed, J Evol Biol) - "Our results show that male bite capacity, in combination with body size, influences both the likelihood and the outcomes of mating interactions, whereas treatment of males with epinastine eliminates motivation to mate. Our results suggest a functional role for bite force in affecting both sexual conflict and sexual selection and expand our knowledge of the influence of biogenic amines on reproductive behaviour."

Journal

Roles of octopamine neurons in the vertical lobe of the mushroom body for the execution of a conditioned response in cockroaches. (PubMed, Neurobiol Learn Mem) - "We showed that injection of epinastine (an OA receptor antagonist) into the head hemolymph impaired both conditioning and execution of the CR, in accordance with findings in crickets...We propose that OANs in the MB vertical lobes play critical roles in the execution of the CR in cockroaches. This is analogous to the fact that midbrain dopamine neurons govern execution of learned actions in mammals."

Journal

Evaluation of applicability of micro-segmental analysis to hair treated with heat and haircare products. (PubMed, Forensic Toxicol) - "The analytes used in this study were minimally affected by ordinary haircare and could be detected even in bleached hair. Therefore, MSA can be applicable regardless of haircare history."

Journal • Allergic Rhinitis • Immunology

Visual learning in tethered bees modifies flight orientation and is impaired by epinastine. (PubMed, J Comp Physiol A Neuroethol Sens Neural Behav Phys) - "Because the total orienting time was not altered by conditioning, conditioning did not enhance orientation activity itself but increased the relative time for orientation to CS. When 0.4 or 4 mM epinastine (an antagonist of octopamine receptors) was injected into the bee's head 30 min prior to the experiment, both short- and long-term memory formation were significantly impaired, suggesting that octopamine, which is crucial for appetitive olfactory learning in insects, is also involved in visual orientation learning."

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Diaminoanthraquinone Enhances Alkaloid Ionization in MALDI-MS. (PubMed, Mass Spectrom (Tokyo)) - "The alkaloids epinastine, 3-methylxanthine and camptothecin were analyzed by matrix-assisted laser desorption/ionization mass spectrometry (MALDI-MS)...In addition, the DAAQ ion peak was very weak relative to those of the analytes due to the low absorbance efficiency. These properties of DAAQ are advantageous for the DAAQ-MALDI-MS analysis of alkaloids."

Journal

Molecular and Pharmacological Characterization of β-Adrenergic-like Octopamine Receptors in the Endoparasitoid Cotesia chilonis (Hymenoptera: Braconidae). (PubMed, Int J Mol Sci) - "Their activities were inhibited by potential antagonists and were most efficiently blocked by epinastine. Our study offers important information about the molecular and pharmacological properties of β-adrenergic-like OARs from C. chilonis that will provide the basis to reveal the contribution of individual receptors to the physiological processes and behaviors in parasitoids."

Journal

Re-evaluation of over-the-counter histamine H1-receptor antagonists based on their effects on murine models of allergen-induced nasal hyperresponsiveness. (PubMed, J Pharmacol Sci) - "Intragastric epinastine, fexofenadine, and loratadine administration suppressed allergen-induced immediate nasal response but not NHR in immunized mice. Regardless of the alleviation of stimulation-induced Th2 cytokine expression by loratadine and desloratadine in vitro, allergen-induced NHR and nasal eosinophil infiltration in Th2 cell-transferred mice were unaffected by loratadine in vivo. This influence on T cell-mediated NHR was excluded from the pharmacological effects of antihistamines."

Journal • Preclinical • Allergic Rhinitis • Immunology • Inflammation

Possibility of drug-distribution measurement in the hair of drowned bodies: evaluation of drug stability in water-soaked hair using micro-segmental analysis. (PubMed, Int J Legal Med) - "The participants ingested 4 hay-fever medicines (fexofenadine, epinastine, cetirizine, and loratadine) every day for approximately 4 months before hair collection. As natural river and sea waters contain divalent ions, the drugs in hair were hardly washed out even when the hair was soaked for 2 months. Thus, it was concluded that drug-distribution measurements using micro-segmental analysis can also be applied to the hairs of drowned bodies."

Journal • Allergic Rhinitis • Immunology

Octopamine affects courtship call structure in male Acheta domesticus crickets. (PubMed, Horm Behav) - "Males treated with epinastine exhibited clear differences in call structure compared to untreated controls, such that epinastine-treated males were more likely to produce simpler calls and to exhibit their carrier frequencies as ticks rather than chirps. Thus, we were able to directly modify male courtship calling performance during mating interactions by altering the neuropharmacological milieu, demonstrating the potential role of biogenic amines in contributing to the diversity of call types in nature."

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