What Is Metaxalone?

Metaxone is a muscle relaxant used to relax muscles and relieve pain. It is a central muscle relaxant that can block multiple synaptic pathways in the spinal cord, has a sedative effect, and also has anticholinergic and antipyretic analgesic effects.

Metaxone is a muscle relaxant used to relax muscles and relieve pain. It is a central muscle relaxant that can block multiple synaptic pathways in the spinal cord, has a sedative effect, and also has anticholinergic and antipyretic analgesic effects.
Chinese name
Methadone
Foreign name
Metaxalone

Metaxone Basic Information

Chinese name: methadone [1]
Chinese alias: 5-[(3,5-xylyloxy) methyl] -2-oxazolidinone; oxazolyl ether; 5- (3,5-dimethylphenoxymethyl)- 2-oxazolidinone; 5-[(3,5-dimethylphenoxy) methyl] oxazolidin-2-one; 5-[(3,5-dimethylphenoxy) methyl] Oxazolidin-2-one.
English name: Metaxalone
English alias: 5- (3,5-Dimethylphenoxymethyl) -2-oxazolidinone;
5-[(3,5-dimethylphenoxy) methyl] -1,3-oxazolidin-2-one;
5-[(3,5-Xylyloxy) methyl] -2-oxazolidinone;
5-((3,5-Dimethylphenoxy) methyl) oxazolidin-2-one;
CAS number: 1665-48-1
Molecular formula: C 12 H 15 NO 3
Structural formula:
Molecular weight: 221.25200
Exact mass: 221.10500
PSA: 47.56000
LogP: 2.11940

Physicochemical properties of methadone

Appearance and properties: whitish solid powder
Density: 1.138 g / cm3
Melting point: 121-123ºC
Boiling point: 453.6ºC at 760 mmHg
Flash point: 228.2ºC
Refractive index: 1.524
Vapor pressure: 2.03E-08mmHg at 25 ° C

Methadone analysis

1 · NIST mass spectrometry analysis: [2]
Columnar
Active phase
Temperature (° C)
Retention Index (I)
references
Capillary column
VF-5MS
2221.8
Tretyakov, 2014
2.LC/MS/MS method
Zorbax SB-C18 was used as the chromatographic column. Water (containing 0.2% formic acid) -acetonitrile (50:50 by volume) was used as the mobile phase. The ESI ion source was used and multiple reaction monitoring was used for detection. Plasma samples were collected from dogs after oral methadone at 80 mg.kg. The established LC / MS / MS method was used to determine the plasma concentration of methadone and calculate the pharmacokinetic parameters. Results The methadone linearity was 0.05 10.00 mg.L (r = 0.997 2). The intra-day and inter-day precision are less than 12.2%, and the accuracy are within 8.19%. Conclusion This method is suitable for the pharmacokinetic study of methadone.

Pharmacological effects of methadone

This product is a central muscle relaxant that can block multiple synaptic pathways in the spinal cord.

Pharmacokinetics of methadone

The main pharmacokinetic parameters of methadone in Beagle dogs after oral administration are as follows: t 1/2 is (4.02 ± 3.04) h, and t max is (1.5 ± 0.35) h. p max is (1 402.31 ± 653.96) mg.L, AUC (0 24) is (2 735.72 ± 1 264.67) mg.L, and AUC (0 ) is (3 109.72 ± 1 283.57) mg.L. [3]

Methadone indications

Clinically, it is mainly used as auxiliary medicine for local muscle spasm pain caused by inflammation and trauma.

Methadone adverse reactions

1. Common adverse reactions include summer sleep, anorexia, nausea, vomiting, dizziness, dry mouth, urinary retention, anemia and jaundice, and severe cases may occur pyuria and kidney stones.
2. Avoid activities that require high concentration during the taking of this product, such as driving, climbing, and operating precision instruments.
3, pregnant, lactating women, children and those with liver dysfunction should be used with caution.
4. This product can interfere with the results of copper method urine glucose measurement.

Methadone dosage

Oral: Adult, 0.8g, 3-4 times / day. [4]

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