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Anti-convulsant medicine used to treat seizures in dogs
Imepitoin (
INN Tooltip International Nonproprietary Name ), sold under the brand name Pexion , is an
anticonvulsant which is used in
veterinary medicine in
Europe to treat
epilepsy in dogs.
[1]
[2]
[3]
[4] It was recently[
when? ] approved in the
United States .
[2]
[3]
[4] The drug also has
anxiolytic effects.
[1]
[2] It was originally developed to treat epilepsy in humans, but
clinical trials were terminated upon findings of unfavorable
metabolic differences in
smokers and non-smokers.
[1]
[2]
Imepitoin acts as a low-
affinity (4,350–5,140 nM; relative to Ki = 6.8 nM for
diazepam and Ki = 1.7 nM for
clonazepam )
partial agonist of the
benzodiazepine site of the
GABAA receptor (up to 12–21% of the maximal potentiation of diazepam, a
full agonist of this site).
[1] It is the first
partial agonist to be approved for the treatment of epilepsy.
[1] The drug also dose-dependently
blocks
voltage-gated calcium channels .
[3] It is
not a benzodiazepine ; instead, it is an
imidazolone , and bears some
structural
similarities to
hydantoin anticonvulsants like
ethotoin and
phenytoin .
[1]
See also
References
Alcohols
Barbiturates
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Carbamates
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AA-29504
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Org 25,435
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Calcium
VDCCs Tooltip Voltage-dependent calcium channels
Potassium
VGKCs Tooltip Voltage-gated potassium channels
IRKs Tooltip Inwardly rectifying potassium channel
KCa Tooltip Calcium-activated potassium channel
K2Ps Tooltip Tandem pore domain potassium channel
Sodium
VGSCs Tooltip Voltage-gated sodium channels
ENaC Tooltip Epithelial sodium channel
ASICs Tooltip Acid-sensing ion channel
Chloride
CaCCs Tooltip Calcium-activated chloride channel
CFTR Tooltip Cystic fibrosis transmembrane conductance regulator
Unsorted
Others
TRPs Tooltip Transient receptor potential channels
LGICs Tooltip Ligand gated ion channels