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=C1C=CC(Cl)=C3

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
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 8297	170.0 µM [IC50]
GABA-A receptor; anion channel 202 Target ID: CHEMBL2093872 Sources: http://www.genome.jp/dbget-bin/www_bget?D01292 \| https://wiki.tripsit.me/wiki/GABA_Receptors_and_Subunits_Info	Agonist 2678
GABA-A receptor; anion channel 202 Target ID: CHEMBL1907607 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2993620	Agonist 2678	528.0 nM [Ki]

Conditions

Condition	Modality	Highest Phase	Product
Anxiety 267 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 8429	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 8429	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 40 Sources: http://premiersupplier.net/MEDAZEPAM-Nobrium-Ansilan-Rudotel-10mg-100-tabs-13.htm	Primary	Approved 8429	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.

PubMed

Title	Date	PubMed
Medazepam compared with amylobarbitone in treatment of anxiety.	1971 Jan 16	4923930
Bromazepam, medazepam, chlordiazepoxide in treatment of neurotic anxiety.	1974 May	4836379
[Analysis of benzodiazepine derivative mixture by gas-liquid chromatography].	2002	12474705
Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines.	2002 Apr	11995921
A population-based case-control teratologic study of nitrazepam, medazepam, tofisopam, alprazolum and clonazepam treatment during pregnancy.	2002 Mar 10	11858890
Direct injection micellar liquid chromatographic determination of benzodiazepines in serum.	2002 Nov 25	12401349
[Determination of diazepine derivatives: alprazolam, medazepam, chlordiazepoxid mixture by high performance liquid chromatography].	2003	14617856
Selective and potent inhibitors of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1) that metabolizes neurosteroids derived from progesterone.	2003 Feb 1	12604236
Determination of clofazimine in leprosy patients by high-performance liquid chromatography.	2003 Sep	14516492
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 Aug	15329838
Determination of diazepam in cream biscuits by liquid chromatography.	2004 May-Jun	15287652
The educational background and qualifications of UK medical students from ethnic minorities.	2008 Apr 16	18416818
Adverse drug effects in hospitalized elderly: data from the healthcare cost and utilization project.	2010	22291486
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 Aug 1	20172681
Evaluation of an hPXR reporter gene assay for the detection of aquatic emerging pollutants: screening of chemicals and application to water samples.	2010 Jan	20024649
Framing access to medicines in developing countries: an analysis of media coverage of Canada's Access to Medicines Regime.	2010 Jan 4	20044940
Barriers to treatment adherence in physiotherapy outpatient clinics: a systematic review.	2010 Jun	20163979
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 Mar 15	20080160
Effectiveness of additional supervised exercises compared with conventional treatment alone in patients with acute lateral ankle sprains: systematic review.	2010 Oct 26	20978065

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.

Name

Type

Language

MEDAZEPAM

Official 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

PAMNACE

Brand Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1012