Itopride

JFDA label: Ganaton 50mg Tablet

Mechanism of Action

Antagonist of D(2) dopamine receptor — Dopamine D2 receptor antagonist; Inhibitor of Acetylcholinesterase — Acetylcholinesterase inhibitor

Target	Action	Gene / class
Acetylcholinesterase efficacy	INHIBITOR	ACHE
D(2) dopamine receptor efficacy	ANTAGONIST	DRD2

Indications

Off-label

• Constipation
• Digestive System Diseases
• Dyspepsia
• Irritable Bowel Syndrome
• Peritonitis

Pregnancy & Lactation

Chemistry & Properties

Formula	C20H26N2O4
Molecular weight	358.44 g/mol
IUPAC name	N-[[4-[2-(dimethylamino)ethoxy]phenyl]methyl]-3,4-dimethoxybenzamide
CAS	122898-67-3
PubChem CID	3792
InChIKey	QQQIECGTIMUVDS-UHFFFAOYSA-N
logP	2.57 (XLogP 2.3)
Polar surface area	60.03 Ų
H-bond acceptors / donors	5 / 1
Drug-likeness (QED)	0.75
Lipinski violations	0

SMILES

COc1ccc(C(=O)NCc2ccc(OCCN(C)C)cc2)cc1OC

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability	10.0%
Half-life	2.168 h
Volume of distribution	2.618 L/kg
Protein binding	86.3%
BBB penetrant	Yes

Enzyme interactions

Enzyme	Role	Detail
CYP1A2	Substrate	—
CYP2C19	Substrate	—
CYP2C8	Inhibitor	—
CYP2D6	Substrate	—
CYP3A4	Substrate	—

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (6)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
TOPRISAN 50 mg Film Coated Tablet	Film-Coated Tablet Itopride Hcl 50 mg	30 tab	Khoury Drug Store	3.050
Itolon	Tablet 50 mg	30 tab pack varies	Savvy Pharma	3.150
Gastrolon	Tablet 50 mg	30 tab	Hayat pharmaceutical industries	3.310
Ganaton	Tablet 50 mg	30 tab pack varies	Sukhtian Group	3.480
Itolon	Tablet 50 mg	100 tab pack varies	Savvy Pharma	9.850
Ganaton	Tablet 50 mg	100 tab pack varies	Sukhtian Group	10.940