| Stereochemistry | RACEMIC |
| Molecular Formula | C16H15N3.ClH |
| Molecular Weight | 285.771 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.NC1=NCC2N1C3=C(CC4=C2C=CC=C4)C=CC=C3
InChI
InChIKey=VKXSGUIOOQPGAF-UHFFFAOYSA-N
InChI=1S/C16H15N3.ClH/c17-16-18-10-15-13-7-3-1-5-11(13)9-12-6-2-4-8-14(12)19(15)16;/h1-8,15H,9-10H2,(H2,17,18);1H
Epinastine (brand names Alesion, Elestat, Purivist, Relestat) is a second-generation antihistamine and mast cell stabilizer. Epinastine is a topically active, direct H1-receptor antagonist and an inhibitor of the release of
histamine from the mast cell. Epinastine is selective for the histamine H1-receptor and has affinity for
the histamine H2 receptor. Epinastine also possesses affinity for the α1-, α2-, and 5-HT2 –receptors.
Epinastine does not penetrate the blood/brain barrier and, therefore, is not expected to induce side effects of the central nervous system. Elestat ophthalmic solution is indicated for the prevention of itching associated with
allergic conjunctivitis.
CNS Activity
Originator
Approval Year
Cmax
AUC
T1/2
Doses
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as victim
Tox targets
Sourcing
PubMed
Sample Use Guides
The recommended dosage is one drop in each eye twice a day.
Treatment should be continued throughout the period of exposure (i.e., until the pollen season is
over or until exposure to the offending allergen is terminated), even when symptoms are absent.
Route of Administration:
Topical
Nasal epithelial cells (NECs) were stimulated with 25 ng/ml TNF-alpha in the presence of Epinastine (10 to 30 ng/ml). The minimum concentration of Epinastine (EP) that caused a significant decrease in eosinophil survival was 25 ng/ml. The addition of EP into eosinophil cultures did not cause inhibition of eosinophil survival, which was prolonged by stimulation with granulocyte-macrophage colony-stimulating factor (GM-CSF), even when 40 ng/ml EP was added to cell cultures.
ACTIVE MOIETY
SUBSTANCE RECORD
