product name Methocarbamol
Description: Methocarbamol (also known as AHR 85) is a potent carbonic anhydrase inhibitor, and is used as a central muscle relaxant to treat skeletal muscle spasms. This compound is a carbamate of guaifenesin. Methocarbamol has been observed to bind to carbonic anhydrase I and II with 1000-fold more specificity for carbonic anhydrase I.
References: J Vet Pharmacol Ther. 2014 Feb;37(1):25-34; Equine Vet J Suppl. 1992 Feb;(11):41-4.
241.24
Formula
C11H15NO5
CAS No.
532-03-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 48 mg/mL (199.0 mM)
Water: < 1 mg/mL
Ethanol: 48 mg/mL (199.0 mM)
Solubility (In vivo)
Synonyms
AHR 85
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19404604
| In Vitro |
In vitro activity: Methocarbamol is metabolized via dealkylation and hydroxylation followed by conjugation to form both glucuronides and sulfates. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Methocarbamol results in a median terminal half-life, mean transit time, mean absorption time, and apparent oral clearance of 2.89 hours, 2.67 hours, 0.410 hours, and 16.5 mL/min/kg in the horse. Methocarbamol is rapidly absorbed and extensively metabolized after oral administration to horses as indicated by a short absorption time and modest systemic bioavailability of 54.4% in the horse. Methocarbamol is a centrally acting muscle relaxant available in both IV and oral forms in cats. Methocarbamol (100 mg/kg) does not change the heart rate, cardiac output, mean pulmonary arterial blood pressure, systolic, diastolic and mean aortic blood pressure, respiratory rate and arterial blood gases, but mild to moderate depression is observed in five of eight horses administered i.v. Methocarbamol, and in all horses administered oral Methocarbamol. Plasma Methocarbamol concentration declines very rapidly during the initial or rapid disposition phase after i.v. administration; the terminal elimination half-life ranged from 59 minutes to 90 minutes in horse. Peak plasma Methocarbamol concentrations following oral administration occur within 15 to 45 minutes in horse. |
| Animal model | |
| Formulation & Dosage | |
| References | J Vet Pharmacol Ther. 2014 Feb;37(1):25-34; Equine Vet J Suppl. 1992 Feb;(11):41-4. |
Related Posts
product name Methocarbamol
Description: Methocarbamol (also known as AHR 85) is a potent carbonic anhydrase inhibitor, and is used as a central muscle relaxant to treat skeletal muscle spasms. This compound is a carbamate of guaifenesin. Methocarbamol has been observed to bind to carbonic anhydrase I and II with 1000-fold more specificity for carbonic anhydrase I.
References: J Vet Pharmacol Ther. 2014 Feb;37(1):25-34; Equine Vet J Suppl. 1992 Feb;(11):41-4.
241.24
Formula
C11H15NO5
CAS No.
532-03-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 48 mg/mL (199.0 mM)
Water: < 1 mg/mL
Ethanol: 48 mg/mL (199.0 mM)
Solubility (In vivo)
Synonyms
AHR 85
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19404604
| In Vitro |
In vitro activity: Methocarbamol is metabolized via dealkylation and hydroxylation followed by conjugation to form both glucuronides and sulfates. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Methocarbamol results in a median terminal half-life, mean transit time, mean absorption time, and apparent oral clearance of 2.89 hours, 2.67 hours, 0.410 hours, and 16.5 mL/min/kg in the horse. Methocarbamol is rapidly absorbed and extensively metabolized after oral administration to horses as indicated by a short absorption time and modest systemic bioavailability of 54.4% in the horse. Methocarbamol is a centrally acting muscle relaxant available in both IV and oral forms in cats. Methocarbamol (100 mg/kg) does not change the heart rate, cardiac output, mean pulmonary arterial blood pressure, systolic, diastolic and mean aortic blood pressure, respiratory rate and arterial blood gases, but mild to moderate depression is observed in five of eight horses administered i.v. Methocarbamol, and in all horses administered oral Methocarbamol. Plasma Methocarbamol concentration declines very rapidly during the initial or rapid disposition phase after i.v. administration; the terminal elimination half-life ranged from 59 minutes to 90 minutes in horse. Peak plasma Methocarbamol concentrations following oral administration occur within 15 to 45 minutes in horse. |
| Animal model | |
| Formulation & Dosage | |
| References | J Vet Pharmacol Ther. 2014 Feb;37(1):25-34; Equine Vet J Suppl. 1992 Feb;(11):41-4. |