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Details

Stereochemistry ACHIRAL
Molecular Formula C17H12ClF3N2O
Molecular Weight 352.738
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of HALAZEPAM

SMILES

FC(F)(F)CN1C2=C(C=C(Cl)C=C2)C(=NCC1=O)C3=CC=CC=C3

InChI

InChIKey=WYCLKVQLVUQKNZ-UHFFFAOYSA-N
InChI=1S/C17H12ClF3N2O/c18-12-6-7-14-13(8-12)16(11-4-2-1-3-5-11)22-9-15(24)23(14)10-17(19,20)21/h1-8H,9-10H2

HIDE SMILES / InChI

Molecular Formula C17H12ClF3N2O
Molecular Weight 352.738
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Halazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Halazepam is used to relieve anxiety, nervousness, and tension associated with anxiety disorders. Halazepam (Paxipam) is no longer commercially available in the United States. Common adverse effects are: hypotension, nausea, xerostomia, confusion, headache. Alcohol should be avoided while taking Paxipam as it causes drowsiness as well. Medications that also cause drowsiness should not be taken along with Paxipam. These include: Antidepressants, Pain relievers, Seizure medications, Muscle relaxants, Antihistamines, Sleeping pills and sedatives.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
29.0 nM [Ki]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
PAXIPAM
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
93 ng/mL
40 mg single, oral
HALAZEPAM plasma
Homo sapiens
147 ng/mL
40 mg single, oral
NORDAZEPAM plasma
Homo sapiens
137 ng/mL
40 mg 3 times / day steady-state, oral
HALAZEPAM plasma
Homo sapiens
916 ng/mL
40 mg 3 times / day steady-state, oral
NORDAZEPAM plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
347 ng × h/mL
40 mg single, oral
HALAZEPAM plasma
Homo sapiens
796 ng × h/mL
40 mg single, oral
NORDAZEPAM plasma
Homo sapiens
640 ng × h/mL
40 mg 3 times / day steady-state, oral
HALAZEPAM plasma
Homo sapiens
5863 ng × h/mL
40 mg 3 times / day steady-state, oral
NORDAZEPAM plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
1.9 h
40 mg 3 times / day steady-state, oral
HALAZEPAM plasma
Homo sapiens

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
20-40 mg 3-4 times a day; optimal doses range from 80-160 mg/day
Route of Administration: Oral
In Vitro Use Guide
Competition curves generated by displacing [3H]-flunitrazepam binding, in sections of the forebrain, with halazepam showed IC50 values of 124.45 nM.
Substance Class Chemical
Record UNII
320YC168LF
Record Status Validated (UNII)
Record Version