TRICLOFOS

US Previously Marketed

Details

Stereochemistry	ACHIRAL
Molecular Formula	C2H4Cl3O4P
Molecular Weight	229.384
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OP(O)(=O)OCC(Cl)(Cl)Cl

InChI

InChIKey=YYQRGCZGSFRBAM-UHFFFAOYSA-N

InChI=1S/C2H4Cl3O4P/c3-2(4,5)1-9-10(6,7)8/h1H2,(H2,6,7,8)

HIDE SMILES / InChI

Description
Sources: http://www.druginfosys.com/drug.aspx?drugcode=1586&type=1 | http://www.sciencedirect.com/science/article/pii/B9780080552323627977 | https://www.ncbi.nlm.nih.gov/pubmed/15351088

Triclofos is primarily indicated in conditions like Insomnia, and can also be given in adjunctive therapy as an alternative drug of choice in Nausea, vertigo, labyrinthine disorders. It is also used sedate people suffering from anxiety or tension before medical investigations. Triclofos is converted to Trichloroethanol in the body .This act on brain and produces sleep. Trichloroethanol decreases time taken to fall asleep and lengthen the sleep. Triclofos is most commonly used agent for sedation in neonates as well as in older infants and children in Japan.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
GABA-A receptor; anion channel 202 Target ID: CHEMBL2093872 Sources: https://www.ncbi.nlm.nih.gov/pubmed/14302355 \| https://www.ncbi.nlm.nih.gov/pubmed/15351088 \| https://www.ncbi.nlm.nih.gov/pubmed/23370056	Agonist 2678

Conditions

Condition	Modality	Targets	Highest Phase	Product
Insomnia 108 Sources: https://www.ncbi.nlm.nih.gov/pubmed/5319225	Primary		Approved 8429	TRICLOS Approved Use Triclofos is used to treat sleeping problems (insomnia) in people. It is also used sedate people suffering from anxiety or tension before medical investigations.

T_1/2

Value	Dose	Co-administered	Analyte	Population
8 h REVIEW https://www.sciencedirect.com/science/article/pii/B9780080552323627977	1 g single, oral dose: 1 g route of administration: Oral experiment type: SINGLE co-administered:		TRICLOFOS plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
65% REVIEW https://www.sciencedirect.com/science/article/pii/B9780080552323627977	1 g single, oral dose: 1 g route of administration: Oral experiment type: SINGLE co-administered:		TRICLOFOS plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
100 mg/kg single, oral Highest studied dose Dose: 100 mg/kg Route: oral Route: single Dose: 100 mg/kg Sources: https://pubmed.ncbi.nlm.nih.gov/15238906	unhealthy, children Health Status: unhealthy Age Group: children Sources: https://pubmed.ncbi.nlm.nih.gov/15238906	Sources: https://pubmed.ncbi.nlm.nih.gov/15238906

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY447186	https://www.001chemical.com/chem/306-52-5
AHH Chemical co.,ltd	MR-1008646	http://www.ahhchemical.com/product/MR-1008646.html
Ambinter	Amb22733929	http://www.ambinter.com/reference/22733929
Boerchem	BC681093	http://www.boerchem.com/?product_39976.html
ChemMol	49416170	http://www.chemmol.com/chemmol/49416170.html
Molcore	MC447186	https://www.molcore.com/product/306-52-5
Smolecule	S576546	https://www.smolecule.com/products/s576546
THE BioTek	bt-308557	https://www.thebiotek.com/product/others/bt-308557
Yuhao Chemical	XJ0609	http://www.chemyuhao.com/306-52-5.html
iChemical	EBD49808	http://www.ichemical.com/chemicals/cas-306-52-5

PubMed

Title	Date	PubMed
Neonatal outcome following maternal opiate use in late pregnancy.	2001 Sep	11543747
A pediatric sedation/anesthesia program with dedicated care by anesthesiologists and nurses for procedures outside the operating room.	2004 Jul	15238906
[Severe airway obstruction relieved by sedation using sevoflurane in a pediatric patient with tracheobronchomalacia].	2005 Feb	15747514
Efficacy and adverse effects of rectal thiamylal with oral triclofos for children undergoing magnetic resonance imaging.	2006 Apr	16368209
Transient administration of triclofos sodium is helpful in minimizing anticonvulsants under polypharmacy.	2006 Dec	17109718
Modeling hydroxyl radical distribution and trialkyl phosphates oxidation in UV-H2O2 photoreactors using computational fluid dynamics.	2010 Aug 15	20704221
Procedural sedation analgesia.	2010 Jan	20668560

Patents

Sample Use Guides

In Vivo Use Guide

The usual adult dose as a hypnotic is 1 to 2 g orally at night. A suggested hypnotic dose for children 1 month to 1 year of age is 25 to 30 mg/kg; children aged 1 to 5 years may be given single doses of 250 to 500 mg, and children aged 6 to 12 years may be given single doses of 0.5 to 1 g.

Route of Administration: Oral

In Vitro Use Guide

Unknown

Name

Type

Language

TRICLOFOS

Official Name

English

Triclofos [WHO-DD]

Common Name

English

triclofos [INN]

Common Name

English

2,2,2-TRICHLOROETHANOL DIHYDROGEN PHOSPHATE

Systematic Name

English

NEGUVON

Brand Name

English

TRICLOFOS [HSDB]

Common Name

English

ETHANOL, 2,2,2-TRICHLORO-, DIHYDROGEN PHOSPHATE

Common Name

English

TRI-BETA-CHLOROETHYLPHOSPHATE

Common Name

English

TRICLOFOS [MI]

Common Name

English

TRICHLOROETHYL PHOSPHATE

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C29756