Medazepam

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Summary

Medazepam is a long-acting benzodiazepine used for its sedative and anxiolytic properties.

Generic Name
Medazepam
DrugBank Accession Number
DB13437
Background

Not Available

Type
Small Molecule
Groups
Experimental
Structure
Thumb
Weight
Average: 270.757
Monoisotopic: 270.092376197
Chemical Formula
C16H15ClN2
Synonyms
  • Medazepam

Pharmacology

Indication

Not Available

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Not Available

Mechanism of action
TargetActionsOrganism
AGABA(A) Receptor
positive allosteric modulator
Humans
AGABA(A) Receptor Benzodiazepine Binding Site
ligand
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
Adverseeffects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
1,2-BenzodiazepineThe risk or severity of adverse effects can be increased when 1,2-Benzodiazepine is combined with Medazepam.
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with Medazepam.
AcetophenazineThe risk or severity of adverse effects can be increased when Acetophenazine is combined with Medazepam.
AclidiniumMedazepam may increase the central nervous system depressant (CNS depressant) activities of Aclidinium.
AgomelatineThe risk or severity of adverse effects can be increased when Agomelatine is combined with Medazepam.
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Medazepam.
AlimemazineThe risk or severity of adverse effects can be increased when Alimemazine is combined with Medazepam.
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Medazepam.
AlosetronThe risk or severity of adverse effects can be increased when Alosetron is combined with Medazepam.
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Medazepam.
Interactions
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Food Interactions
Not Available

Products

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
TRANKO-BUSKAS DRAJE, 20 ADETMedazepam (10 mg) + Butylscopolamine (10 mg)Tablet, coatedOralTEVA İLAÇLARI SAN.VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
TRANKO-BUSKAS DRAJE, 40 ADETMedazepam (10 mg) + Butylscopolamine (10 mg)Tablet, coatedOralTEVA İLAÇLARI SAN.VE TİC. A.Ş.2020-08-14Not applicableTurkey flag

Categories

ATC Codes
N05BA03 — Medazepam
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as 1,4-benzodiazepines. These are organic compounds containing a benzene ring fused to a 1,4-azepine.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzodiazepines
Sub Class
1,4-benzodiazepines
Direct Parent
1,4-benzodiazepines
Alternative Parents
Dialkylarylamines / Benzene and substituted derivatives / Aryl chlorides / Ketimines / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds / Organopnictogen compounds / Organochlorides / Hydrocarbon derivatives
Substituents
1,4-benzodiazepine / Amine / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid / Dialkylarylamine / Hydrocarbon derivative / Imine
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
P0J3387W3S
CAS number
2898-12-6
InChI Key
YLCXGBZIZBEVPZ-UHFFFAOYSA-N
InChI
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
IUPAC Name
7-chloro-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepine
SMILES
CN1CCN=C(C2=CC=CC=C2)C2=C1C=CC(Cl)=C2

References

General References
  1. DIMDI Drug Product Information: Rudotel (medazepam) oral tablets [Link]
  2. FDA Thailand Product Information: Tranko-Buskas (hyoscine-N-butyl bromide/medazepam) oral dragee [Link]
ChemSpider
3901
BindingDB
50021058
RxNav
6680
ChEBI
31807
ChEMBL
CHEMBL28333
ZINC
ZINC000000001659
Wikipedia
Medazepam

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3Unknown StatusPreventionNausea / Vomiting1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
CapsuleOral
Capsule
Solution / dropsOral
Tablet10 mg
Tablet, coatedOral
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0126 mg/mLALOGPS
logP4.08ALOGPS
logP4.21ChemAxon
logS-4.3ALOGPS
pKa (Strongest Basic)9.57ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area15.6 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity80.85 m3·mol-1ChemAxon
Polarizability29.19 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00di-0090000000-9c4f6c5ef00f4df7ab04
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00di-0090000000-af47b18edb6dcbeff94a
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00dl-2290000000-0349047f44d1a9dd2a0d
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-052f-4490000000-8a5840db631279c0ef3a
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-052f-6790000000-57420afc127df9edd674
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-052f-6960000000-b6b4afe40a9a7223b2dc

Targets

Drugtargets2
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Kind
Protein group
Organism
Humans
Pharmacological action
Yes
Actions
Positive allosteric modulator
Curator comments
The GABA(A) receptor is pentameric (i.e. comprising 5 subunit proteins) and therefore has a multitude of potential isoforms. The above target is a collection of all possible GABA(A) subunits that may participate in the formation of the pentameric receptor and is not meant to imply direct a drug-protein interaction for each individual subunit.
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...

Components:
References
  1. Sigel E, Steinmann ME: Structure, function, and modulation of GABA(A) receptors. J Biol Chem. 2012 Nov 23;287(48):40224-31. doi: 10.1074/jbc.R112.386664. Epub 2012 Oct 4. [Article]
  2. Zhu S, Noviello CM, Teng J, Walsh RM Jr, Kim JJ, Hibbs RE: Structure of a human synaptic GABAA receptor. Nature. 2018 Jul;559(7712):67-72. doi: 10.1038/s41586-018-0255-3. Epub 2018 Jun 27. [Article]
Kind
Protein group
Organism
Humans
Pharmacological action
Yes
Actions
Ligand
Curator comments
Benzodiazepines modulate GABA(A) function by binding at the interface between alpha (α) and gamma (γ) subunits. Of the 6 α-subunits, only 4 (α-1, -2, -3, and -5) participate in the formation of this binding site. The above target is a collection of all α- and γ-subunits that are known to participate in the formation of the benzodiazepine binding site.
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...

Components:
References
  1. Sigel E, Steinmann ME: Structure, function, and modulation of GABA(A) receptors. J Biol Chem. 2012 Nov 23;287(48):40224-31. doi: 10.1074/jbc.R112.386664. Epub 2012 Oct 4. [Article]
  2. Zhu S, Noviello CM, Teng J, Walsh RM Jr, Kim JJ, Hibbs RE: Structure of a human synaptic GABAA receptor. Nature. 2018 Jul;559(7712):67-72. doi: 10.1038/s41586-018-0255-3. Epub 2018 Jun 27. [Article]

Drug created on June 23, 2017 20:42 / Updated on May 05, 2021 20:31