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Details

Stereochemistry RACEMIC
Molecular Formula C11H15NO5
Molecular Weight 241.2409
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of METHOCARBAMOL

SMILES

COc1ccccc1OCC(COC(=N)O)O

InChI

InChIKey=GNXFOGHNGIVQEH-UHFFFAOYSA-N
InChI=1S/C11H15NO5/c1-15-9-4-2-3-5-10(9)16-6-8(13)7-17-11(12)14/h2-5,8,13H,6-7H2,1H3,(H2,12,14)

HIDE SMILES / InChI

Description
Curator's Comment:: Description was created based on several sources, including https://www.drugs.com/methocarbamol.html

Methocarbamol is a central muscle relaxant for skeletal muscles, used to treat spasms. It is structurally related to guaifenesin. Methocarbamol's exact mechanism of causing skeletal muscle relaxation is unknown. It is thought to work centrally, perhaps by general depressant effects. It has no direct relaxant effects on striated muscle, nerve fibers, or the motor endplate. It will not directly relax contracted skeletal muscles. The drug has a secondary sedative effect. Methocarbamol is used for use as an adjunct to rest, physical therapy, and other measures for the relief of discomforts associated with acute, painful musculoskeletal conditions. Under the trade name Robaxin, Methocarbamol is marketed by Actient Pharmaceuticals in the United States and Pfizer in Canada.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
70.0 µM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Robaxin

Approved Use

Robaxin® and robaxin®-750 are indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute, painful musculoskeletal conditions.

Launch Date

-3.93379185E11
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
21.3 mg/L
1.5 g single, oral
dose: 1.5 g
route of administration: Oral
experiment type: SINGLE
co-administered:
METHOCARBAMOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
28.7 mg/L
1.5 g single, oral
dose: 1.5 g
route of administration: Oral
experiment type: SINGLE
co-administered:
METHOCARBAMOL plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
52.5 mg × h/L
1.5 g single, oral
dose: 1.5 g
route of administration: Oral
experiment type: SINGLE
co-administered:
METHOCARBAMOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
87.1 mg × h/L
1.5 g single, oral
dose: 1.5 g
route of administration: Oral
experiment type: SINGLE
co-administered:
METHOCARBAMOL plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
1.14 h
1.5 g single, oral
dose: 1.5 g
route of administration: Oral
experiment type: SINGLE
co-administered:
METHOCARBAMOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
1.24 h
1.5 g single, oral
dose: 1.5 g
route of administration: Oral
experiment type: SINGLE
co-administered:
METHOCARBAMOL plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
52%
1.5 g single, oral
dose: 1.5 g
route of administration: Oral
experiment type: SINGLE
co-administered:
METHOCARBAMOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
51.9%
1.5 g single, oral
dose: 1.5 g
route of administration: Oral
experiment type: SINGLE
co-administered:
METHOCARBAMOL plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Focal seizure following enflurane.
1992 Jan
Patents

Patents

Sample Use Guides

Usual Adult Dose for Muscle Spasm Oral: Initial dose: 1500 mg four times a day for the first 48 to 72 hours, up to a maximum dosage of 8 g/day for severe symptoms. Maintenance dose: 4000 to 4500 mg/day in divided doses. IV or IM: 1000 mg up to every 8 hours if necessary, not to exceed 3 g/day for more than 3 consecutive days except in the treatment of tetanus. A like course may be repeated after a lapse of 48 hours if the condition persists. Oral therapy should be instituted as soon as possible.
Route of Administration: Other
Unknown
Name Type Language
METHOCARBAMOL
GREEN BOOK   HSDB   INN   JAN   MART.   MI   ORANGE BOOK   USP   USP-RS   VANDF   WHO-DD  
INN  
Official Name English
METHOCARBAMOL [USP]
Common Name English
ROBAXISAL COMPONENT METHOCARBAMOL
Common Name English
1,2-PROPANEDIOL, 3-(2-METHOXYPHENOXY)-, 1-CARBAMATE, (+/-)-
Common Name English
NSC-170960
Code English
(+/-)-3-(O-METHOXYPHENOXY)-1,2-PROPANEDIOL 1-CARBAMATE
Common Name English
DELAXIN
Brand Name English
METHOCARBAMOL [MART.]
Common Name English
ROBAXIN
Brand Name English
FORBAXIN
Brand Name English
METHOCARBAMOL [MI]
Common Name English
METHOCARBAMOL [INN]
Common Name English
METHOCARBAMOL [VANDF]
Common Name English
METHOCARBAMOL [WHO-DD]
Common Name English
METHOCARBAMOL [ORANGE BOOK]
Common Name English
METHOCARBAMOL [JAN]
Common Name English
METHOCARBAMOL COMPONENT OF ROBAXISAL
Common Name English
METHOCARBAMOL [GREEN BOOK]
Common Name English
METHOCARBAMOL [USP-RS]
Common Name English
METHOCARBAMOL [HSDB]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C29696
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
CFR 21 CFR 522.1380
Created by admin on Sat Jun 26 12:36:41 UTC 2021 , Edited by admin on Sat Jun 26 12:36:41 UTC 2021
WHO-VATC QM03BA53
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
WHO-VATC QM03BA73
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
NDF-RT N0000175737
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
WHO-ATC M03BA03
Created by admin on Sat Jun 26 12:36:41 UTC 2021 , Edited by admin on Sat Jun 26 12:36:41 UTC 2021
WHO-VATC QM03BA03
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
LIVERTOX 618
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
WHO-ATC M03BA53
Created by admin on Sat Jun 26 12:36:41 UTC 2021 , Edited by admin on Sat Jun 26 12:36:41 UTC 2021
CFR 21 CFR 520.1380
Created by admin on Sat Jun 26 12:36:41 UTC 2021 , Edited by admin on Sat Jun 26 12:36:41 UTC 2021
WHO-ATC M03BA73
Created by admin on Sat Jun 26 12:36:41 UTC 2021 , Edited by admin on Sat Jun 26 12:36:41 UTC 2021
NDF-RT N0000175730
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
Code System Code Type Description
FDA UNII
125OD7737X
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
PRIMARY
MERCK INDEX
M7322
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
PRIMARY Merck Index
USP_CATALOG
1412008
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
PRIMARY USP-RS
IUPHAR
6829
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
PRIMARY
CAS
532-03-6
Created by admin on Sat Jun 26 12:36:41 UTC 2021 , Edited by admin on Sat Jun 26 12:36:41 UTC 2021
PRIMARY
EPA CompTox
532-03-6
Created by admin on Sat Jun 26 12:36:41 UTC 2021 , Edited by admin on Sat Jun 26 12:36:41 UTC 2021
PRIMARY
INN
776
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
PRIMARY
DRUG CENTRAL
1747
Created by admin on Sat Jun 26 12:36:41 UTC 2021 , Edited by admin on Sat Jun 26 12:36:41 UTC 2021
PRIMARY
PUBCHEM
4107
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
PRIMARY
EVMPD
SUB08852MIG
Created by admin on Sat Jun 26 12:36:41 UTC 2021 , Edited by admin on Sat Jun 26 12:36:41 UTC 2021
PRIMARY
WIKIPEDIA
METHOCARBAMOL
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
PRIMARY
ChEMBL
CHEMBL1201117
Created by admin on Sat Jun 26 12:36:41 UTC 2021 , Edited by admin on Sat Jun 26 12:36:41 UTC 2021
PRIMARY
ECHA (EC/EINECS)
208-524-3
Created by admin on Sat Jun 26 12:36:41 UTC 2021 , Edited by admin on Sat Jun 26 12:36:41 UTC 2021
PRIMARY
DRUG BANK
DB00423
Created by admin on Sat Jun 26 12:36:41 UTC 2021 , Edited by admin on Sat Jun 26 12:36:41 UTC 2021
PRIMARY
RXCUI
6845
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
PRIMARY RxNorm
MESH
D008721
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
PRIMARY
NCI_THESAURUS
C29252
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
PRIMARY
HSDB
3122
Created by admin on Sat Jun 26 12:36:42 UTC 2021 , Edited by admin on Sat Jun 26 12:36:42 UTC 2021
PRIMARY