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Details

Stereochemistry RACEMIC
Molecular Formula C11H15NO5
Molecular Weight 241.2405
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of METHOCARBAMOL

SMILES

COC1=C(OCC(O)COC(N)=O)C=CC=C1

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

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

Primary TargetPharmacologyConditionPotency
70.0 µM [Ki]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Robaxin

Cmax

ValueDoseCo-administeredAnalytePopulation
21.3 mg/L
1.5 g single, oral
METHOCARBAMOL plasma
Homo sapiens
28.7 mg/L
1.5 g single, oral
METHOCARBAMOL plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
52.5 mg × h/L
1.5 g single, oral
METHOCARBAMOL plasma
Homo sapiens
87.1 mg × h/L
1.5 g single, oral
METHOCARBAMOL plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
1.14 h
1.5 g single, oral
METHOCARBAMOL plasma
Homo sapiens
1.24 h
1.5 g single, oral
METHOCARBAMOL plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
52%
1.5 g single, oral
METHOCARBAMOL plasma
Homo sapiens
51.9%
1.5 g single, oral
METHOCARBAMOL plasma
Homo sapiens

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer

Drug as perpetrator​

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
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
In Vitro Use Guide
Unknown