MEDAZEPAM

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 Search

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

Molecular Formula	C16H15ClN2
Molecular Weight	270.757
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.sopharma.com/medazepam.php | http://omedicine.info/en/medazepam.html | http://www.druginfosys.com/drug.aspx?drugcode=441&type=1

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 Target	Pharmacology	Potency
nitric oxide synthase 1 (neuronal) 2 Target ID: 1.00520936E8 Gene Symbol: NOS1 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11731013	Inhibitor 8504	170.0 µM [IC50]
GABA-A receptor; anion channel 203 Target ID: CHEMBL2093872 Sources: http://www.genome.jp/dbget-bin/www_bget?D01292 \| https://wiki.tripsit.me/wiki/GABA_Receptors_and_Subunits_Info	Agonist 2752
GABA-A receptor; anion channel 203 Target ID: CHEMBL1907607 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2993620	Agonist 2752	528.0 nM [Ki]

Conditions

Condition	Modality	Highest Phase	Product
Anxiety 275 Sources: https://www.jstage.jst.go.jp/article/iryo1946/26/8/26_8_657/_article https://www.ncbi.nlm.nih.gov/pubmed/1078	Primary	Approved 8583	Nobrium Approved Use This medication is used in the treatment of anxiety disorders, alcohol withdrawal, tremor, muscle spasms and to control seizures. It may also be used before surgery or procedures to reduce apprehension and anxiety.
Tremor 2 Sources: http://premiersupplier.net/MEDAZEPAM-Nobrium-Ansilan-Rudotel-10mg-100-tabs-13.htm	Primary	Approved 8583	Nobrium Approved Use This medication is used in the treatment of anxiety disorders, alcohol withdrawal, tremor, muscle spasms and to control seizures. It may also be used before surgery or procedures to reduce apprehension and anxiety.
Muscle spasm 41 Sources: http://premiersupplier.net/MEDAZEPAM-Nobrium-Ansilan-Rudotel-10mg-100-tabs-13.htm	Primary	Approved 8583	Nobrium Approved Use This medication is used in the treatment of anxiety disorders, alcohol withdrawal, tremor, muscle spasms and to control seizures. It may also be used before surgery or procedures to reduce apprehension and anxiety.

C_max

Value	Dose	Analyte	Population
0.21 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37864/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	MEDAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
0.98 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/5487421/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	MEDAZEPAM blood	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
0.37 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/5487421/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	MEDAZEPAM blood	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
0.58 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/5487421/	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	MEDAZEPAM blood	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
0.08 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/5487421/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	DIAZEPAM blood	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
0.13 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/5487421/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	NORDAZEPAM blood	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
0.07 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/5487421/	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DIAZEPAM blood	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
0.45 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/5487421/	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	NORDAZEPAM blood	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
276 mg single, oral Overdose Dose: 276 mg Route: oral Route: single Dose: 276 mg Sources: https://pubmed.ncbi.nlm.nih.gov/18818182/	pregnant, ADULT Health Status: pregnant Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/18818182/	Disc. AE: Death fetal... AEs leading to discontinuation/dose reduction: Death fetal (521 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/18818182/
10 mg 3 times / day steady-state, oral Studied dose Dose: 10 mg, 3 times / day Route: oral Route: steady-state Dose: 10 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/4923930/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/4923930/	Other AEs: Drowsiness... Other AEs: Drowsiness (3 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/4923930/

AEs

AE	Significance	Dose	Population
Death fetal	521 patient Disc. AE	276 mg single, oral Overdose Dose: 276 mg Route: oral Route: single Dose: 276 mg Sources: https://pubmed.ncbi.nlm.nih.gov/18818182/	pregnant, ADULT Health Status: pregnant Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/18818182/
Drowsiness	3 patients	10 mg 3 times / day steady-state, oral Studied dose Dose: 10 mg, 3 times / day Route: oral Route: steady-state Dose: 10 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/4923930/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/4923930/

PubMed

Title	Date	PubMed
[Oxygen consumption by resting humans at different Elbrus altitudes].	2010-11-02	21033404
Effectiveness of additional supervised exercises compared with conventional treatment alone in patients with acute lateral ankle sprains: systematic review.	2010-10-26	20978065
A new method for the simultaneous determination of 1,4-benzodiazepines and amfepramone as adulterants in phytotherapeutic formulations by voltammetry.	2010-10-10	20472377
1-(1-Phenyl-ethyl-idene)carbonohydrazide.	2010-09-30	21587659
Daily functioning and self-management in patients with chronic low back pain after an intensive cognitive behavioral programme for pain management.	2010-09	20506027
From their own perspective - constraints in the Polio Eradication Initiative: perceptions of health workers and managers in a district of Pakistan's Punjab province.	2010-08-23	20731832
Development and validation of an EI-GC-MS method for the determination of benzodiazepine drugs and their metabolites in blood: applications in clinical and forensic toxicology.	2010-08-01	20172681
Cytokinin-binding protein (70 kDa) from etioplasts and amyloplasts of etiolated maize seedlings and chloroplasts of green plants and its putative function.	2010-07	20584787
Barriers to treatment adherence in physiotherapy outpatient clinics: a systematic review.	2010-06	20163979
Randomised controlled trial of integrated care to reduce disability from chronic low back pain in working and private life.	2010-03-16	20234040
Benzodiazepines medazepam and midazolam are activators of pregnane X receptor and weak inducers of CYP3A4: investigation in primary cultures of human hepatocytes and hepatocarcinoma cell lines.	2010-03-15	20080160
Framing access to medicines in developing countries: an analysis of media coverage of Canada's Access to Medicines Regime.	2010-01-04	20044940
Evaluation of an hPXR reporter gene assay for the detection of aquatic emerging pollutants: screening of chemicals and application to water samples.	2010-01	20024649
Adverse drug effects in hospitalized elderly: data from the healthcare cost and utilization project.	2010	22291486
Benzodiazepine prescription and length of hospital stay at a Japanese university hospital.	2009-10-09	19818119
OSBPL10, a novel candidate gene for high triglyceride trait in dyslipidemic Finnish subjects, regulates cellular lipid metabolism.	2009-08	19554302
A study of the effects of large doses of medazepam used for self-poisoning in 10 pregnant women on fetal development.	2008-09-27	18818182
Randomised controlled trial of Alexander technique lessons, exercise, and massage (ATEAM) for chronic and recurrent back pain.	2008-08-19	18713809
The educational background and qualifications of UK medical students from ethnic minorities.	2008-04-16	18416818
[Efficacy and possible mechanisms of action of a new peptide anxiolytic selank in the therapy of generalized anxiety disorders and neurasthenia].	2008	18454096
Human resource management in the Georgian National Immunization Program: a baseline assessment.	2007-07-31	17672907
Separation of 1,4-benzodiazepines by micellar elektrokinetic capillary chromatography.	2007-01-10	16563516
[The nitric oxide system in patients with arterial hypertension living in high mountains].	2007	18220026
Cytokinin-binding protein (70 kDa): localization in tissues and cells of etiolated maize seedlings and its putative function.	2007	17584953
Application of surface ionization methods for highly sensitive and selective analysis of benzodiazepine derivatives.	2005-04-29	15862696
Diagnostic imaging in Canada.	2005	16288163
Risk and benefit of drug use during pregnancy.	2005	16007261
Determination of diazepam in cream biscuits by liquid chromatography.	2004-08-04	15287652
Screening, library-assisted identification and validated quantification of 23 benzodiazepines, flumazenil, zaleplone, zolpidem and zopiclone in plasma by liquid chromatography/mass spectrometry with atmospheric pressure chemical ionization.	2004-08	15329838
Determination of clofazimine in leprosy patients by high-performance liquid chromatography.	2003-09	14516492
A study into the rate of incorporation of eight benzodiazepines into rat hair.	2003-04-23	12742689
Selective and potent inhibitors of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1) that metabolizes neurosteroids derived from progesterone.	2003-02-01	12604236
Pharmacological activity of phenazepam and flunitrazepam in ultralow doses.	2003-01	12949644
[Determination of diazepine derivatives: alprazolam, medazepam, chlordiazepoxid mixture by high performance liquid chromatography].	2003	14617856
[Comprehensive medical and ecological studies in Pryel'brussi].	2003	12918248
Mountain sports and total hip arthroplasty: a case report and review of mountaineering with total hip arthroplasty.	2003	12825885
Direct injection micellar liquid chromatographic determination of benzodiazepines in serum.	2002-11-25	12401349
Square-wave voltammetric techniques for determination of psychoactive 1,4-benzodiazepine drugs.	2002-11	12458422
Quantitation using GC-TOF-MS: example of bromazepam.	2002-08-14	12208027
Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines.	2002-04	11995921
A population-based case-control teratologic study of nitrazepam, medazepam, tofisopam, alprazolum and clonazepam treatment during pregnancy.	2002-03-10	11858890
Oesophageal motility disorders.	2002-01-12	11809295
[Analysis of benzodiazepine derivative mixture by gas-liquid chromatography].	2002	12474705
Structural requirements of benzodiazepines for the inhibition of pig brain nitric oxide synthase.	2001-11-30	11731013
Bromazepam, medazepam, chlordiazepoxide in treatment of neurotic anxiety.	1974-05	4836379
Medazepam compared with amylobarbitone in treatment of anxiety.	1971-01-16	4923930

Patents

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.

Substance Class	Chemical Created by `admin` on `Wed Apr 02 08:20:12 GMT 2025` Edited by `admin` on `Wed Apr 02 08:20:12 GMT 2025`
Record UNII	P0J3387W3S
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

MEDAZEPAM

Official Name

English

PAMNACE

Preferred Name

English

medazepam [INN]

Common Name

English

MEDAZEPAM [MI]

Common Name

English

Medazepam [WHO-DD]

Common Name

English

MEDAZEPAM [JAN]

Common Name

English

MEDAZEPAM [MART.]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1012