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DB00423 - Methocarbamol


Identification
Name Methocarbamol
Accession Number DB00423 (APRD01102)
Type small molecule
Description A centrally acting muscle relaxant whose mode of action has not been established. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1206)
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 241.2405
Groups approved
Monoisotopic Weight 241.095022595
Pharmacology
Indication For use as an adjunct to rest, physical therapy, and other measures for the relief of discomforts associated with acute, painful musculoskeletal conditions.
Mechanism of action The mechanism of action of methocarbamol in humans has not been established, but may be due to central nervous system depression. It has no direct action on the contractile mechanism of striated muscle, the motor end plate or the nerve fiber.
Absorption Rapid. Onset of action is about 30 minutes after oral administration.
Protein binding Not Available
Biotransformation Hepatic.
Route of elimination Small amounts of unchanged methocarbamol also are excreted in the urine.
Toxicity Symptoms of overdose include blurred vision, coma, drowsiness, low blood pressure, nausea, and seizures.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Triprolidine The CNS depressants, Triprolidine and Methocarbamol, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Food Interactions
  • Take without regard to meals.
  • Avoid alcohol.

Targets


Carbonic anhydrase 1
Name Carbonic anhydrase 1
Gene Name CA1
Pharmacological action no
Actions inhibitor
References
  • Parr JS, Khalifah RG: Inhibition of carbonic anhydrases I and II by N-unsubstituted carbamate esters. J Biol Chem. 1992 Dec 15;267(35):25044-50. - Pubmed
DTHybrid score 0.3694

Predictions


Id Partner name Gene Name Score
357 Carbonic anhydrase 2 CA2 0.1919
592 Carbonic anhydrase 4 CA4 0.1343
466 Solute carrier family 12 member 3 SLC12A3 0.0643
6126 Carbonic anhydrase 7 CA7 0.045
558 Solute carrier family 12 member 1 SLC12A1 0.0417
3007 Carbonic anhydrase 12 CA12 0.0348
4205 Carbonic anhydrase 9 CA9 0.0347
1729 Solute carrier family 22 member 6 SLC22A6 0.0332
610 Calcium-activated potassium channel subunit alpha 1 KCNMA1 0.0326
806 Sodium/potassium-transporting ATPase alpha-1 chain ATP1A1 0.0225
1405 Thiopurine S-methyltransferase TPMT 0.0206
253 Sodium/potassium-transporting ATPase gamma chain FXYD2 0.0196
6123 Carbonic anhydrase 5A, mitochondrial CA5A 0.0196
4512 Cytochrome P450 3A4 CYP3A4 0.0172
4757 Cytochrome P450 2C9 CYP2C9 0.0157
6131 Carbonic anhydrase 14 CA14 0.0147
310 Solute carrier family 12 member 2 SLC12A2 0.0143
6122 Carbonic anhydrase 3 CA3 0.0141
1025 Aquaporin-1 AQP1 0.0098
781 ATP-sensitive inward rectifier potassium channel 11 KCNJ11 0.0084
3426 Glutamine synthetase glnA 0.0083
3987 Glutamine synthetase GLUL 0.0083
6124 Carbonic anhydrase 5B, mitochondrial CA5B 0.0064
6013 Cytochrome P450 2E1 CYP2E1 0.005
6046 Voltage-gated calcium channel beta 1 subunit splice variant CavB1d CACNB1 0.0044
4119 Cytochrome P450 2D6 CYP2D6 0.0042
6045 Voltage-dependent calcium channel subunit alpha-2/delta-3 CACNA2D3 0.004
6016 Cytochrome P450 2C19 CYP2C19 0.0039
997 Protein kinase C beta type PRKCB 0.0036
6024 Cytochrome P450 1A1 CYP1A1 0.0035
634 Squalene monooxygenase SQLE 0.0033
7196 Squalene monooxygenase ERG1 0.0033
1970 Protein kinase C alpha type PRKCA 0.0033
2408 Tyrosine-protein kinase SYK SYK 0.0032
3970 Voltage-dependent N-type calcium channel subunit alpha-1B CACNA1B 0.0031
6127 Carbonic anhydrase-related protein CA8 0.0027
6129 Carbonic anhydrase-related protein 11 CA11 0.0027
6133 Sodium channel subunit beta-2 SCN2B 0.0027
6128 Carbonic anhydrase-related protein 10 CA10 0.0027
6134 Sodium channel subunit beta-3 SCN3B 0.0027
6132 Sodium channel subunit beta-1 SCN1B 0.0027
6135 Sodium channel subunit beta-4 SCN4B 0.0027
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.0026
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0026
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0026
4111 Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S 0.0026
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0025
6130 Carbonic anhydrase 13 CA13 0.0025
2236 Casein kinase II subunit alpha CSNK2A1 0.0025
3803 Sodium channel protein type 3 subunit alpha SCN3A 0.0024
215 Sodium channel protein type 11 subunit alpha SCN11A 0.0023
6263 cAMP-dependent protein kinase catalytic subunit alpha PRKACA 0.0022
3802 Sodium channel protein type 2 subunit alpha SCN2A 0.0022
1024 Solute carrier family 22 member 11 SLC22A11 0.0021
3804 Sodium channel protein type 4 subunit alpha SCN4A 0.002
1995 Sodium channel protein type 9 subunit alpha SCN9A 0.002
5718 Cytochrome P450 2A6 CYP2A6 0.0018
15 Voltage-dependent T-type calcium channel subunit alpha-1I CACNA1I 0.0018
158 Sodium channel protein type 1 subunit alpha SCN1A 0.0018
535 Voltage-dependent T-type calcium channel subunit alpha-1G CACNA1G 0.0017
964 Voltage-dependent T-type calcium channel subunit alpha-1H CACNA1H 0.0017
6030 Cytochrome P450 2B6 CYP2B6 0.0017
6107 Cytochrome P450 3A7 CYP3A7 0.0016
4118 Cytochrome P450 3A5 CYP3A5 0.0016
4924 Cytochrome P450 2C8 CYP2C8 0.0015
6020 Aldehyde oxidase AOX1 0.0015
4200 Cytochrome P450 1A2 CYP1A2 0.0015
1588 Multidrug resistance protein 1 ABCB1 0.0014
220 Sodium channel protein type 5 subunit alpha SCN5A 0.0013
3939 Amine oxidase [flavin-containing] B MAOB 0.0013
3941 Amine oxidase [flavin-containing] A MAOA 0.0013
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