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Last update 16 May 2025
Epinastine Hydrochloride
Last update 16 May 2025
Overview
Basic Info
Drug Type Small molecule drug |
Synonyms Epinastine, Epinastine hydrochloride (JAN), エピナスチン + [13] |
Target |
Action antagonists |
Mechanism H1 receptor antagonists(Histamine H1 receptor antagonists) |
Therapeutic Areas |
Active Indication |
Inactive Indication |
Originator Organization |
Inactive Organization |
License Organization |
Drug Highest PhaseApproved |
First Approval Date Japan (01 Apr 1994), |
Regulation- |
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Structure/Sequence
Molecular FormulaC16H16ClN3 |
InChIKeyVKXSGUIOOQPGAF-UHFFFAOYSA-N |
CAS Registry108929-04-0 |
Related
51
Clinical Trials associated with Epinastine HydrochlorideCTR20243732
盐酸依匹斯汀片在健康受试者中的单中心、随机、开放、单次给药、两制剂、两序列、两周期、双交叉、空腹及餐后状态下的生物等效性研究
[Translation] A single-center, randomized, open-label, single-dose, two-formulation, two-sequence, two-period, double-crossover, fasting and fed bioequivalence study of epinastine hydrochloride tablets in healthy subjects
CTR20234212
0.1%STN1011403滴眼液治疗过敏性结膜炎的多中心随机评价者盲态阳性对照试验
[Translation] A multicenter randomized evaluator-blind positive controlled trial of 0.1% STN1011403 eye drops in the treatment of allergic conjunctivitis
CTR20231572
0.05%盐酸依匹斯汀滴眼液治疗中国过敏性结膜炎患者的有效性和安全性的随机、双盲、阳性药平行对照、多中心临床研究
[Translation] A randomized, double-blind, positive-drug parallel-controlled, multicenter clinical study on the efficacy and safety of 0.05% epinastine hydrochloride eye drops in the treatment of allergic conjunctivitis in Chinese patients
100 Clinical Results associated with Epinastine Hydrochloride
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100 Translational Medicine associated with Epinastine Hydrochloride
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100 Patents (Medical) associated with Epinastine Hydrochloride
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310
Literatures (Medical) associated with Epinastine Hydrochloride01 Apr 2025CHEMOSPHERE
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
Article
Author: Murata, Yuichiro ; Sakai, Hiroshi
Anthropogenic organic compounds, such as pharmaceuticals and personal care products, contaminate water, posing toxicological risks caused by either their parent compounds or transformation products. This study compares ultraviolet (UV)-based advanced oxidation processes (UV/hydrogen peroxide, UV/persulfate, and UV/chlorine) for the abatement of an antihistamine drug epinastine. UV light at 254 nm was irradiated upon solutions containing 10 μM epinastine and 100 μM oxidant. UV/chlorine degraded epinastine most effectively at pH 6.0-8.0; considerable contributions by reactive chlorine species and hydroxyl radicals were quantified using probe compounds. Furthermore, the degradation efficiency of the UV/chlorine treatment persisted with a halved chlorine dosage. Additionally, the types and concentrations of disinfection byproducts (DBPs) produced during UV/chlorine treatment with or without post-chlorination varied depending on the concentrations of chlorine or bromide. 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.
31 Mar 2025PHARMAZIE
Direct comparison of the effects of first- and second-generation H1 -receptor blockers on motor functions in mice.
Article
Author: Hori, S ; Tenjin, K ; Shimada, A ; Kizu, J ; Sakamoto, Y ; Iketani, O ; Hara, R ; Matsumoto, K ; Okamoto, Y ; Enoki, Y ; Taguchi, K
Histamine H1 receptor (H1R) antagonists are widely used to treat allergic reactions; however, their effects on the central nervous system can impair motor functions. 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. First-generation H1R antagonists significantly impaired motor functions, with diphenhydramine exerting stronger effects than those of d -chlorpheniramine. Among the second-generation agents, bepotastine and levocetirizine had minimal effects on all motor functions, whereas epinastine and ketotifen suppressed spontaneous movement, similar to first-generation H1R antagonists but had little effects on balance, postural stability, and coordinated movement. 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.
01 Jan 2025Forensic Toxicology
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
Article
Author: Kanamori, Tatsuyuki ; Okada, Yuki ; Yamamuro, Tadashi ; Tsujikawa, Kenji ; Iwata, Yuko T ; Miyaguchi, Hajime ; Segawa, Hiroki ; Kuwayama, Kenji
PURPOSE:
We previously developed evaluation methods using micro-segmental analysis (MSA) to examine the effects of external environments on drug content in hair and nails. In this study, the effects of the natural environmental factors (water, temperature, humidity, light, and soil) on drug contents in nails were examined and compared with our previous experimental data on hair.
METHODS:
Four hay-fever medicines were used as model drugs (fexofenadine, epinastine, cetirizine, and desloratadine) to evaluate drug stability in the nails. Reference nails containing the four medicines were collected from patients with hay fever who ingested the medicines daily for four months. The nails were exposed to various natural environments for up to four months.
RESULTS:
The effects of temperature, humidity, and light on drug contents in the nails were comparatively small. Soil significantly decomposed the nail surfaces and decreased the drug content of the nails (up to 17 %). Water also decreased the drug content (up to 12 %), although no apparent changes in nail surfaces were observed.
CONCLUSIONS:
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.
100 Deals associated with Epinastine Hydrochloride
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External Link
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| D01713 | Epinastine Hydrochloride |
R&D Status
Approved
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| Indication | Country/Location | Organization | Date |
|---|---|---|---|
| Conjunctivitis, Allergic | Japan | 20 Sep 2013 | |
| Seasonal allergic conjunctivitis | Austria | 04 Mar 2003 | |
| Seasonal allergic conjunctivitis | Belgium | 04 Mar 2003 | |
| Seasonal allergic conjunctivitis | Czechia | 04 Mar 2003 | |
| Seasonal allergic conjunctivitis | Denmark | 04 Mar 2003 | |
| Seasonal allergic conjunctivitis | France | 04 Mar 2003 | |
| Seasonal allergic conjunctivitis | Germany | 04 Mar 2003 | |
| Seasonal allergic conjunctivitis | Greece | 04 Mar 2003 | |
| Seasonal allergic conjunctivitis | Hungary | 04 Mar 2003 | |
| Seasonal allergic conjunctivitis | Ireland | 04 Mar 2003 | |
| Seasonal allergic conjunctivitis | Italy | 04 Mar 2003 | |
| Seasonal allergic conjunctivitis | Luxembourg | 04 Mar 2003 | |
| Seasonal allergic conjunctivitis | Netherlands | 04 Mar 2003 | |
| Seasonal allergic conjunctivitis | Poland | 04 Mar 2003 | |
| Seasonal allergic conjunctivitis | Portugal | 04 Mar 2003 | |
| Seasonal allergic conjunctivitis | Slovakia | 04 Mar 2003 | |
| Seasonal allergic conjunctivitis | Spain | 04 Mar 2003 | |
| Seasonal allergic conjunctivitis | Sweden | 04 Mar 2003 | |
| Seasonal allergic conjunctivitis | United Kingdom | 04 Mar 2003 | |
| Psoriasis | China | 16 Jun 2000 |
Developing
10 top R&D records. to view more data
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| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| Rhinitis, Allergic, Seasonal | Phase 3 | - | 18 Dec 2007 | |
| Dermatitis, Atopic | Phase 3 | - | 01 Jun 2001 | |
| Rhinitis, Allergic, Perennial | Phase 3 | - | 01 May 2000 |
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Clinical Result
Clinical Result
Indication
Phase
Evaluation
View All Results
Phase 3 | 87 | (Epinastine (DE-114) Ophthalmic Solution) | gravpkrtqd(cnhfcsjreq) = squlzjzzjo nfakmejgik (rwidzubxbd, 0.1) View more | - | 05 Nov 2014 | ||
Placebo (Placebo Ophthalmic Solution) | gravpkrtqd(cnhfcsjreq) = nhohjnrkdo nfakmejgik (rwidzubxbd, 0.1) View more | ||||||
Phase 3 | 130 | wqcwmzjwuv(ighigdhltr) = lcmnxmcxmg zfghwolckl (plpcuwbkwl, 0.1) View more | - | 23 Sep 2014 | |||
Phase 4 | 79 | (Elestat) | romtyqqtgc(rnjisescur) = bmoeagrcgy ajobvlpezc (seigvuowsb, 1.36) View more | - | 27 May 2009 | ||
(Pataday) | romtyqqtgc(rnjisescur) = ehntjxpjgy ajobvlpezc (seigvuowsb, 1.07) View more | ||||||
Not Applicable | 99 | Epinastine HCl 0.05% | lotzjemals(banlfngvwt) = Three (5.9%) epinastine patients and 7 (14.6%) ketotifen patients experienced adverse events. Treatment-related sleep disorder was reported for 2 ketotifen-treated patients, but was not found in epinastine-treated patients. pzcijhlptu (jvkcrwyquh ) | - | 01 May 2004 | ||
Not Applicable | - | Epinastine HCl 0.05% | naysqksufn(eajwyxpwgj) = zxiztecivv ijuzbsjhaf (fvxwpcodbh ) | Positive | 01 May 2003 | ||
naysqksufn(eajwyxpwgj) = ntzdsnqvzz ijuzbsjhaf (fvxwpcodbh ) | |||||||
Not Applicable | 14 | rjphijwfoz(zudwmnfmmb) = No adverse events nor any clinically relevant changes in visual acuity, biomicroscopy, ophthalmoscopy, vital signs, physical examination, or laboratory parameters were observed during the study yxzjinkdij (vsfwskwqci ) | Positive | 01 May 2003 | |||
Not Applicable | - | - | Epinastine HCl 0.05% | xdsxffsiwx(gkzeoouasq) = primarily colds/URI, was the most frequent AE reported in 5.0% of epinastine subjects and 8.3% of vehicle subjects wvbbwhwgkj (djxwlybgds ) | Positive | 01 May 2003 | |
Vehicle |
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