Nefopam

JFDA label: Acupan 20mg /2ml Amp

Indications

Approved

• Fever — Fever
• Pain — pain

Off-label

• Burns
• Stomach Neoplasms

Adverse Reactions

Cardiac disorders (2)

Not Known Angina pectoris · Tachycardia

Nervous system disorders (3)

Not Known Dizziness · Headache · Somnolence

Renal and urinary disorders (1)

Not Known Urinary retention

Immune system disorders (1)

Not Known Hypersensitivity

Gastrointestinal disorders (3)

Not Known Dry mouth · Nausea · Vomiting

Skin and subcutaneous tissue disorders (2)

Not Known Erythema multiforme · Hyperhidrosis

Psychiatric disorders (3)

Not Known Confusional state · Hallucination · Insomnia

Eye disorders (1)

Not Known Vision blurred

Investigations (1)

Not Known Feeling abnormal

General disorders and administration site conditions (2)

Not Known Nervousness · Tension

Pregnancy & Lactation

Chemistry & Properties

Formula	C17H19NO
Molecular weight	253.35 g/mol
IUPAC name	5-methyl-1-phenyl-1,3,4,6-tetrahydro-2,5-benzoxazocine
CAS	13669-70-0
PubChem CID	4450
InChIKey	RGPDEAGGEXEMMM-UHFFFAOYSA-N
logP	3.24 (XLogP 2.9)
Polar surface area	12.47 Ų
H-bond acceptors / donors	2 / 0
Drug-likeness (QED)	0.77
Lipinski violations	0

SMILES

CN1CCOC(c2ccccc2)c2ccccc2C1

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrant	Yes

Enzyme interactions

Enzyme	Role	Detail
CYP1A2	Substrate	—
CYP2B6	Substrate	—
CYP2C19	Substrate	—
CYP2D6	Inhibitor	—
CYP2D6	Substrate	—
CYP3A4	Substrate	—

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (2)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Nefomed	Ampoule 20 mg/2 ml	5 amp	Land Of Medicine Drug Store	1.640
Acupan 20mg /2ml Amp	Ampoule 20 mg	5 amp	THE ARAB DRUG STORE P.S.C	2.660