<?xml version="1.0" encoding="UTF-8"?>
<compound>
  <id type="integer">3091</id>
  <title>T3D3049</title>
  <common-name>Clotiazepam</common-name>
  <description>Clotiazepam is only found in individuals that have used or taken this drug. It is a benzodiazepine derivative, not approved for sale in the U.S. or Canada, but has been approved in the U.K. It is a schedule IV drug in Canada.Clotiazepam acts at the benzodiazepine receptors (BZD). This agonizes the action of GABA, increasing the frequency of opening of the channel chlorinates and penetration of the ions chlorinates through the ionophore. Increase in membrane polarization decreases the probability of discharge of neurons.</description>
  <cas>33671-46-4</cas>
  <pubchem-id>2811</pubchem-id>
  <chemical-formula>C16H15ClN2OS</chemical-formula>
  <weight>318.059360</weight>
  <appearance>White powder.</appearance>
  <melting-point>105-106°C</melting-point>
  <boiling-point nil="true"/>
  <density nil="true"/>
  <solubility>5.37e-03 g/L</solubility>
  <specific-gravity nil="true"/>
  <flash-point nil="true"/>
  <vapour-pressure nil="true"/>
  <route-of-exposure>Oral</route-of-exposure>
  <target nil="true"/>
  <mechanism-of-toxicity>Clotiazepam acts at the benzodiazepine receptors (BZD). This agonizes the action of GABA, increasing the frequency of opening of the channel chlorinates and penetration of the ions chlorinates through the ionophore. Increase in membrane polarization decreases the probability of discharge of neurons.</mechanism-of-toxicity>
  <metabolism>Hepatic.Half Life: 4 hours</metabolism>
  <toxicity nil="true"/>
  <lethaldose nil="true"/>
  <carcinogenicity>No indication of carcinogenicity to humans (not listed by IARC).</carcinogenicity>
  <use-source>For the treatment of anxiety disorders. Used as an anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant.</use-source>
  <min-risk-level nil="true"/>
  <health-effects>They cause slurred speech, disorientation and "drunken" behavior. They are physically and psychologically addictive. May cause a potentially dangerous rash that may develop into Stevens Johnson syndrome, an extremely rare but potentially fatal skin disease.</health-effects>
  <symptoms nil="true"/>
  <treatment>General supportive measures should be employed, along with intravenous fluids, and an adequate airway maintained. Hypotension may be combated by the use of norepinephrine or metaraminol. Dialysis is of limited value. Flumazenil (Anexate) is a competitive benzodiazepine receptor antagonist that can be used as an antidote for benzodiazepine overdose. In particular, flumazenil is very effective at reversing the CNS depression associated with benzodiazepines but is less effective at reversing respiratory depression. Its use, however, is controversial as it has numerous contraindications. It is contraindicated in patients who are on long-term benzodiazepines, those who have ingested a substance that lowers the seizure threshold, or in patients who have tachycardia or a history of seizures. As a general rule, medical observation and supportive care are the mainstay of treatment of benzodiazepine overdose. Although benzodiazepines are absorbed by activated charcoal, gastric decontamination with activated charcoal is not beneficial in pure benzodiazepine overdose as the risk of adverse effects often outweigh any potential benefit from the procedure. It is recommended only if benzodiazepines have been taken in combination with other drugs that may benefit from decontamination. Gastric lavage (stomach pumping) or whole bowel irrigation are also not recommended.</treatment>
  <created-at type="dateTime">2009-07-21T20:28:51Z</created-at>
  <updated-at type="dateTime">2014-12-24T20:25:56Z</updated-at>
  <interacting-proteins nil="true"/>
  <wikipedia>Clotiazepam</wikipedia>
  <uniprot-id></uniprot-id>
  <kegg-compound-id></kegg-compound-id>
  <omim-id></omim-id>
  <chebi-id>1178501</chebi-id>
  <biocyc-id></biocyc-id>
  <ctd-id nil="true"/>
  <stitch-id>Clotiazepam</stitch-id>
  <drugbank-id>DB01559</drugbank-id>
  <pdb-id></pdb-id>
  <actor-id nil="true"/>
  <organism nil="true"/>
  <export type="boolean">true</export>
  <metabolizing-proteins nil="true"/>
  <transporting-proteins nil="true"/>
  <moldb-smiles>CCC1=CC2=C(S1)N(C)C(=O)CN=C2C1=CC=CC=C1Cl</moldb-smiles>
  <moldb-formula>C16H15ClN2OS</moldb-formula>
  <moldb-inchi>InChI=1S/C16H15ClN2OS/c1-3-10-8-12-15(11-6-4-5-7-13(11)17)18-9-14(20)19(2)16(12)21-10/h4-8H,3,9H2,1-2H3</moldb-inchi>
  <moldb-inchikey>InChIKey=CHBRHODLKOZEPZ-UHFFFAOYSA-N</moldb-inchikey>
  <moldb-average-mass type="decimal">318.821</moldb-average-mass>
  <moldb-mono-mass type="decimal">318.059361509</moldb-mono-mass>
  <origin>Exogenous</origin>
  <state>Solid</state>
  <logp>3.18</logp>
  <hmdb-id>HMDB15512</hmdb-id>
  <chembl-id>CHEMBL1697737</chembl-id>
  <chemspider-id>2709</chemspider-id>
  <structure-image-file-name nil="true"/>
  <structure-image-content-type nil="true"/>
  <structure-image-file-size type="integer" nil="true"/>
  <structure-image-updated-at type="dateTime" nil="true"/>
  <biodb-id nil="true"/>
  <synthesis-reference>&lt;p&gt;Nakanishi, M., Araki, K.,Tahara, T. and Shiroki, M.; US. Patent 3,849,405; November 19, 1974; assigned to Yoshitomi Pharmaceutical Industries, Ltd.&lt;/p&gt;</synthesis-reference>
  <structure-image-caption nil="true"/>
</compound>
