LOPRAZOLAM

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C23H21ClN6O3
Molecular Weight	464.904
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

SMILES

CN1CCN(CC1)\C=C2/N=C3CN=C(C4=CC=CC=C4Cl)C5=C(C=CC(=C5)[N+]([O-])=O)N3C2=O

InChI

InChIKey=UTEFBSAVJNEPTR-RGEXLXHISA-N

InChI=1S/C23H21ClN6O3/c1-27-8-10-28(11-9-27)14-19-23(31)29-20-7-6-15(30(32)33)12-17(20)22(25-13-21(29)26-19)16-4-2-3-5-18(16)24/h2-7,12,14H,8-11,13H2,1H3/b19-14-

HIDE SMILES / InChI

Description

Loprazolam is a hypnotic drug which stimulates GABA-A receptors. Due to its hypnotic activity the drug is used to treat short-term sleep disordes.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
GABA-A receptor; benzodiazepine site	Agonist

Conditions

Condition	Modality	Targets	Highest Phase	Product
Short term slep problems	Primary		Approved	DORMONOCT

C_max

Value	Dose	Analyte	Population
4.3 ng/mL	1 mg single, oral	LOPRAZOLAM plasma	Homo sapiens
4.2 ng/mL	1 mg single, oral	LOPRAZOLAM plasma	Homo sapiens
4.1 ng/mL	1 mg 1 times / day multiple, oral	LOPRAZOLAM serum	Homo sapiens
4.6 ng/mL	1 mg 1 times / day multiple, oral	LOPRAZOLAM serum	Homo sapiens

AUC

Value	Dose	Analyte	Population
46.6 ng × h/mL	1 mg single, oral	LOPRAZOLAM plasma	Homo sapiens
74.5 ng × h/mL	1 mg single, oral	LOPRAZOLAM plasma	Homo sapiens
35.5 ng × h/mL	1 mg 1 times / day multiple, oral	LOPRAZOLAM serum	Homo sapiens
50 ng × h/mL	1 mg 1 times / day multiple, oral	LOPRAZOLAM serum	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
11.22 h	1 mg single, oral	LOPRAZOLAM plasma	Homo sapiens
19.77 h	1 mg single, oral	LOPRAZOLAM plasma	Homo sapiens
8 h	1 mg 1 times / day multiple, oral	LOPRAZOLAM serum	Homo sapiens
3.3 h	1 mg 1 times / day multiple, oral	LOPRAZOLAM serum	Homo sapiens

F_unbound

Value	Dose	Co-administered	Analyte	Population
15%			LOPRAZOLAM plasma	Homo sapiens

Doses

Show entries

Dose	Population	Adverse events
1 mg 7 times / day multiple, oral Recommended	unhealthy, ADULT
2 mg single, oral Recommended	unhealthy, ADULT	Other AEs: Lethargy, Dizziness...

Showing 1 to 2 of 2 entries

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AEs

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AE	Significance	Dose	Population
Lethargy		2 mg single, oral Recommended	unhealthy, ADULT
Ataxia	20%	2 mg single, oral Recommended	unhealthy, ADULT
Dizziness	20%	2 mg single, oral Recommended	unhealthy, ADULT

Showing 1 to 3 of 3 entries

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PubMed

Show entries

Title	Date	PubMed
A comparison of the hypnotic activity of loprazolam, temazepam and placebo in general practice.	1984	6141114

Showing 1 to 1 of 1 entries

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Patents

Sample Use Guides

In Vivo Use Guide

The usual adult dose is 1 - 2 mg at bedtime.

Route of Administration: Oral

In Vitro Use Guide

Unknown

Show entries

Name

Type

Language

LOPRAZOLAM

Official Name

English

loprazolam [INN]

Common Name

English

(Z)-6-(O-CHLOROPHENYL)-2,4-DIHYDRO-2-((4-METHYL-1-PIPERAZINYL)METHYLENE)-8-NITRO-1H-IMIDAZO(1,2-A)(1,4)BENZODIAZEPIN-1-ONE

Common Name

English

(2Z)-6-(2-CHLOROPHENYL)-2,4-DIHYDRO-2-((4-METHYL-1-PIPERAZINYL)METHYLENE)-8-NITRO-1H-IMIDAZO(1,2-A)(1,4)BENZODIAZEPIN-1-ONE

Systematic Name

English

TRIAZULENONE, (Z)-

Common Name

English

Showing 1 to 5 of 11 entries

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Classification Tree

Code System

Code

Sec. 1308.11 Schedule IV.

DEA NO.

2773

Benzodiazepine derivatives

WHO-VATC

QN05CD11

Antianxiety Agent

NCI_THESAURUS

C1012

Benzodiazepine derivatives

WHO-ATC

N05CD11

Showing 1 to 4 of 4 entries

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Code System

Code

Type

Description

FDA UNII

759N8462G8

PRIMARY

EPA CompTox

DTXSID30894873

PRIMARY

NCI_THESAURUS

C66032

PRIMARY

PUBCHEM

3033860

PRIMARY

INN

4884

PRIMARY

Showing 1 to 5 of 15 entries

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ACTIVE MOIETY


					759N8462G8

LOPRAZOLAM

SALT/SOLVATE (PARENT)


					VKF8383J65

LOPRAZOLAM MESILATE

SMILES

InChI

CNS Activity

Originator

Approval Year

Targets

Conditions

Cmax

AUC

T1/2

Funbound

Doses

AEs

PubMed

Patents

Sample Use Guides

C_max

T_1/2

F_unbound