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Details

Stereochemistry ACHIRAL
Molecular Formula C16H15ClN2
Molecular Weight 270.757
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of MEDAZEPAM

SMILES

CN1CCN=C(C2=CC=CC=C2)C3=CC(Cl)=CC=C13

InChI

InChIKey=YLCXGBZIZBEVPZ-UHFFFAOYSA-N
InChI=1S/C16H15ClN2/c1-19-10-9-18-16(12-5-3-2-4-6-12)14-11-13(17)7-8-15(14)19/h2-8,11H,9-10H2,1H3

HIDE SMILES / InChI

Description

Medazepam is a benzodiazepine drug with anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is known by the following brand names: Azepamid, Nobrium, Tranquirax (mixed with bevonium), Rudotel, Raporan, Ansilan and Mezapam. Marketed in Russia. Indicated for the treatment of neurotic disorders and states, accompanied with sense of fear, anxiety, intension, raised irritability, insomnia, vegetative lability.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
170.0 µM [IC50]
528.0 nM [Ki]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Nobrium
Primary
Nobrium
Primary
Nobrium

Cmax

ValueDoseCo-administeredAnalytePopulation
0.21 μg/mL
10 mg single, oral
MEDAZEPAM plasma
Homo sapiens
0.98 μg/mL
50 mg single, oral
MEDAZEPAM blood
Homo sapiens
0.37 μg/mL
50 mg single, oral
MEDAZEPAM blood
Homo sapiens
0.58 μg/mL
50 mg 1 times / day multiple, oral
MEDAZEPAM blood
Homo sapiens
0.08 μg/mL
50 mg single, oral
DIAZEPAM blood
Homo sapiens
0.13 μg/mL
50 mg single, oral
NORDAZEPAM blood
Homo sapiens
0.07 μg/mL
50 mg 1 times / day multiple, oral
DIAZEPAM blood
Homo sapiens
0.45 μg/mL
50 mg 1 times / day multiple, oral
NORDAZEPAM blood
Homo sapiens

Doses

AEs

PubMed

Sample Use Guides

In Vivo Use Guide
The average dose for adults: single - 10-20 mg, the average daily - 20-30 mg, the maximum - 60-70 mg / day. At the beginning of treatment - for 5 mg 2-3 times a day, then gradually increase the dose to 30-40 mg per day. In outpatient settings recommended by 5 mg in the morning and in the afternoon, and 10 mg in the evening. Elderly patients, teenagers, as well as kidney function - 5-10 mg 1-2 times a day, or 10 mg at night. Babies dose depends on the age and body weight. Treatment duration should be as short as possible (about 2 Sun) and should not exceed 2 Months (including the period of gradual reduction of the dose).
Route of Administration: Oral
In Vitro Use Guide
Medazepam (10 (-5) M) inhibited the contractile response of circular muscle strips from the isolated guinea-pig gallbladder to sulfated cholecystokinin octapeptide (CCK8) in the presence of atropine.