ETHYLMORPHINE HYDROCHLORIDE DIHYDRATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C19H23NO3.ClH.2H2O
Molecular Weight	385.882
Optical Activity	UNSPECIFIED
Defined Stereocenters	5 / 5
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure of ETHYLMORPHINE HYDROCHLORIDE DIHYDRATE

SMILES

O.O.Cl.CCOC1=C2O[C@H]3[C@@H](O)C=C[C@H]4[C@H]5CC(C=C1)=C2[C@@]34CCN5C

InChI

InChIKey=FKEDUFRSQFFLHR-VSYPDCRNSA-N

InChI=1S/C19H23NO3.ClH.2H2O/c1-3-22-15-7-4-11-10-13-12-5-6-14(21)18-19(12,8-9-20(13)2)16(11)17(15)23-18;;;/h4-7,12-14,18,21H,3,8-10H2,1-2H3;1H;2*1H2/t12-,13+,14-,18-,19-;;;/m0.../s1

HIDE SMILES / InChI

Description

Ethylmorphine is a derivative of morphine with analgesic and antitussive effect. It acts by activating the opioid receptors and thus has a direct influence on the CNS system. Ethylmorphine was approved in Europe for the treatment of dry cough (Codethyline, Dionine).

CNS Activity

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Opioid receptors; mu/kappa/delta 33	Agonist 2,752		345.0 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Cough 106	Primary		Approved 8,583	CODETHYLINE

C_max

Value	Dose	Co-administered	Analyte	Population
1.09 μM	1.5 mg/kg bw single, oral		ETHYLMORPHINE serum	Homo sapiens

AUC

Value	Dose	Co-administered	Analyte	Population
222 μM × min	1.5 mg/kg bw single, oral		ETHYLMORPHINE serum	Homo sapiens

T_1/2

Value	Dose	Co-administered	Analyte	Population
1.97 h	1.5 mg/kg bw single, oral		ETHYLMORPHINE serum	Homo sapiens

Doses

Show entries

Dose	Population	Adverse events
8.5 mg single, oral	healthy, 10 months	Other AEs: Sedation...
1.5 mg/kg single, oral	healthy, 24 years	Other AEs: Dizziness, Drowsiness...

Showing 1 to 2 of 2 entries

Previous1Next

AEs

Show entries

AE	Significance	Dose	Population
Sedation	grade 5	8.5 mg single, oral	healthy, 10 months
Loose stools	1 patient	1.5 mg/kg single, oral	healthy, 24 years
Dizziness	7 patients	1.5 mg/kg single, oral	healthy, 24 years
Drowsiness	slight, 2 patients	1.5 mg/kg single, oral	healthy, 24 years

Showing 1 to 4 of 4 entries

Previous1Next

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1,946		substrate 1,388

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer

Drug as victim

Show entries

Target	Modality	Activity	Metabolite	Clinical evidence
CYP2D6 1,388	substrate 4,014	yes
CYP3A4 1,946	substrate 4,014	yes

Showing 1 to 2 of 2 entries

Previous1Next

Sourcing

Sourcing

Show entries

Vendor/Aggregator	ID	URL
ABI Chem	AC1Q37UW
Ambinter	Amb22801513	http://www.ambinter.com/reference/22801513
Angene	AGN-PC-0OHUE6
Aurora Fine Chemicals LLC	A17.879.672	http://online.aurorafinechemicals.com/info?ID=A17.879.672
Chemieliva Pharmaceutical Co., Ltd	PBCM1411510

Showing 1 to 5 of 23 entries

Previous1 2 3 4 5Next

PubMed

Show entries

Title	Date	PubMed
Acute renal failure due to concomitant action of methotrexate and indomethacin.	1986 Jun 14	2872506
Biotransformation and pharmacokinetics of ethylmorphine after a single oral dose.	1995 Jun	7654478
Effects of ethanol on ethylmorphine metabolism in isolated rat hepatocytes: characterization by means of a multicompartmental model.	1997 Apr	9140136
Effects of fumonisin B1 present in Fusarium moniliforme culture material on drug metabolising enzyme activities in ducks.	2001 May 19	11369472
Genomic characterization and regulation of CYP3a13: role of xenobiotics and nuclear receptors.	2003 Sep	12958193

Showing 1 to 5 of 15 entries

Previous1 2 3Next

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dose in adults is 50 mg of codethyline per day, i.e. 10 tablets (1 tablet contains 5 mg of ethylmorphine hydrochloride) per day over several intakes, at a minimum of 4 hours apart. In children the normal dose is 1 tablet per intake, to be renewed after 6 hours if necessary, without exceeding 4 tablets per day.

Route of Administration: Oral

In Vitro Use Guide

Unknown

Show entries

Name

Type

Language

ETHYLMORPHINE HYDROCHLORIDE HYDRATE

Preferred Name

English

ETHYLMORPHINE HYDROCHLORIDE DIHYDRATE

Common Name

English

ETHYLMORPHINE HYDROCHLORIDE DIHYDRATE [MI]

Common Name

English

(5.ALPHA.,6.ALPHA.)-7,8-DIDEHYDRO-4,5-EPOXY-3-ETHOXY-17-METHYLMORPHINAN-6-OL HYDROCHLORIDE DIHYDRATE

Systematic Name

English

CODETHYLINE HYDROCHLORIDE DIHYDRATE

Common Name

English

Showing 1 to 5 of 7 entries

Previous1 2Next

Show entries

Classification Tree

Code System

Code

Agent Affecting Nervous System

NCI_THESAURUS

C67413

Showing 1 to 1 of 1 entries

Previous1Next

Show entries

Code System

Code

Type

Description

MERCK INDEX

m5154

PRIMARY

Merck Index

NCI_THESAURUS

C87358

PRIMARY

EPA CompTox

DTXSID90986728

PRIMARY

SMS_ID

300000037439

PRIMARY

FDA UNII

407X3NQV4N

PRIMARY

Showing 1 to 5 of 7 entries

Previous1 2Next

PARENT (SALT/SOLVATE)


					RWO67D87EU

ETHYLMORPHINE

SUBSTANCE RECORD


					407X3NQV4N

ETHYLMORPHINE HYDROCHLORIDE DIHYDRATE

SMILES

InChI

CNS Activity

Approval Year

Targets

Conditions

Cmax

AUC

T1/2

Doses

AEs

Overview

OverviewOther

Drug as victim

Sourcing

PubMed

Patents

Sample Use Guides

C_max

T_1/2