EPERISONE

Possibly Marketed Outside US

Details

Stereochemistry	RACEMIC
Molecular Formula	C17H25NO
Molecular Weight	259.3865
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CCC1=CC=C(C=C1)C(=O)C(C)CN2CCCCC2

InChI

InChIKey=SQUNAWUMZGQQJD-UHFFFAOYSA-N

InChI=1S/C17H25NO/c1-3-15-7-9-16(10-8-15)17(19)14(2)13-18-11-5-4-6-12-18/h7-10,14H,3-6,11-13H2,1-2H3

HIDE SMILES / InChI

Molecular Formula	C17H25NO
Molecular Weight	259.3865
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description

Eperisone is an antispasmodic drug approved in Japan for the treatment of of diseases characterized by muscle stiffness and pain. It is believed that eperisone exerts its effect through inhibition of sodium channels. The drug is still being marketed in Asia under the name Myonal (Square Pharmaceuticals).

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
skeletal muscle contraction 3	Inhibitor 8,297

Conditions

Condition	Modality	Highest Phase	Product
Low back pain 22	Palliative	Approved 8,429	MYONAL
Spastic paralysis 3	Palliative	Approved 8,429	MYONAL
Neck-shoulder-arm syndrome 2	Palliative	Approved 8,429	MYONAL
Scapulohumeral periarthritis 3	Palliative	Approved 8,429	MYONAL

C_max

Value	Dose	Analyte	Population
7.5 ng/mL	150 mg 1 times / day multiple, oral	EPERISONE plasma	Homo sapiens
7.8 ng/mL	150 mg 1 times / day multiple, oral	EPERISONE plasma	Homo sapiens
7.9 ng/mL	150 mg 1 times / day multiple, oral	EPERISONE plasma	Homo sapiens
2 ng/mL	50 mg single, oral	EPERISONE plasma	Homo sapiens
4.21 ng/mL	100 mg single, oral	EPERISONE plasma	Homo sapiens
7.18 ng/mL	150 mg single, oral	EPERISONE plasma	Homo sapiens
7.65 ng/mL	150 mg single, oral	EPERISONE plasma	Homo sapiens
3.46 ng/mL	150 mg single, oral	EPERISONE plasma	Homo sapiens

AUC

Value	Dose	Analyte	Population
19.68 ng × h/mL	150 mg 1 times / day multiple, oral	EPERISONE plasma	Homo sapiens
20.29 ng × h/mL	150 mg 1 times / day multiple, oral	EPERISONE plasma	Homo sapiens
21.08 ng × h/mL	150 mg 1 times / day multiple, oral	EPERISONE plasma	Homo sapiens
8.86 ng × h/mL	50 mg single, oral	EPERISONE plasma	Homo sapiens
13.2 ng × h/mL	100 mg single, oral	EPERISONE plasma	Homo sapiens
20.27 ng × h/mL	150 mg single, oral	EPERISONE plasma	Homo sapiens
20.88 ng × h/mL	150 mg single, oral	EPERISONE plasma	Homo sapiens
22.91 ng × h/mL	150 mg single, oral	EPERISONE plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
1.6 h	150 mg 1 times / day multiple, oral	EPERISONE plasma	Homo sapiens
1.68 h	150 mg 1 times / day multiple, oral	EPERISONE plasma	Homo sapiens
1.75 h	150 mg 1 times / day multiple, oral	EPERISONE plasma	Homo sapiens
3.37 h	50 mg single, oral	EPERISONE plasma	Homo sapiens
2.55 h	100 mg single, oral	EPERISONE plasma	Homo sapiens
2.93 h	150 mg single, oral	EPERISONE plasma	Homo sapiens
1.81 h	150 mg single, oral	EPERISONE plasma	Homo sapiens
1.99 h	150 mg single, oral	EPERISONE plasma	Homo sapiens