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Pair of enantiomers
Epinastine
Trade names Alesion, Elestat, Purivist, Relestat
AHFS /
Drugs.com
Monograph
MedlinePlus
a604011
Pregnancy category
Routes of administration
Eye drops
ATC code
Protein binding 64%
Elimination half-life 12 hours
(RS )-3-amino-9,13b-dihydro-1H -dibenz(c,f)imidazo(1,5-a)azepine
CAS Number
PubChem
CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (
EPA )
ECHA InfoCard
100.120.187
Formula C 16 H 15 N 3
Molar mass 249.317 g·mol−1 3D model (
JSmol )
N\4=C(\N3c1c(cccc1)Cc2c(cccc2)C3C/4)N
InChI=1S/C16H15N3/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)
Y Key:WHWZLSFABNNENI-UHFFFAOYSA-N
Y
(verify)
Epinastine (brand names Alesion , Elestat , Purivist , Relestat ) is a second-generation
antihistamine and
mast cell stabilizer that is used in
eye drops to treat
allergic conjunctivitis . It is produced by
Allergan and marketed by
Inspire in the United States.
[1] It is highly
selective for the
H1 receptor and does not cross the
blood-brain-barrier .
[2]
It was patented in 1980 and came into medical use in 1994.
[3]
References
^ Pradhan S, Abhishek K, Mah F (September 2009). "Epinastine: topical ophthalmic second generation antihistamine without significant systemic side effects". Expert Opinion on Drug Metabolism & Toxicology . 5 (9): 1135–1140.
doi :
10.1517/17425250903117284 .
PMID
19630694 .
S2CID
207490591 .
^ Walther G, Daniel H, Bechtel WD, Brandt K (April 1990). "New tetracyclic guanidine derivatives with H1-antihistaminic properties. Chemistry of epinastine". Arzneimittel-Forschung . 40 (4): 440–446.
PMID
1972625 .
^ Fischer J, Ganellin CR (2006).
Analogue-based Drug Discovery . John Wiley & Sons. p. 549.
ISBN
9783527607495 .
H1
Agonists Antagonists
Others:
Atypical antipsychotics (e.g.,
aripiprazole ,
asenapine ,
brexpiprazole ,
brilaroxazine ,
clozapine ,
iloperidone ,
olanzapine ,
paliperidone ,
quetiapine ,
risperidone ,
ziprasidone ,
zotepine )
Phenylpiperazine
antidepressants (e.g.,
hydroxynefazodone ,
nefazodone ,
trazodone ,
triazoledione )
Tetracyclic antidepressants (e.g.,
amoxapine ,
loxapine ,
maprotiline ,
mianserin ,
mirtazapine ,
oxaprotiline )
Tricyclic antidepressants (e.g.,
amitriptyline ,
butriptyline ,
clomipramine ,
desipramine ,
dosulepin (dothiepin) ,
doxepin ,
imipramine ,
iprindole ,
lofepramine ,
nortriptyline ,
protriptyline ,
trimipramine )
Typical antipsychotics (e.g.,
chlorpromazine ,
flupenthixol ,
fluphenazine ,
loxapine ,
perphenazine ,
prochlorperazine ,
thioridazine ,
thiothixene )
H2
H3
H4