Metaxalone
Metaxalone Uses, Dosage, Side Effects, Food Interaction and all others data.
Metaxalone is a moderate to strong muscle relaxant used in the symptomatic treatment of musculoskeletal pain caused by strains, sprains, and other musculoskeletal conditions. It is marketed by King Pharmaceuticals under the brand name Skelaxin®. Its main mechanism of action is thought to involve general central nervous system depression. Metaxalone is associated with few side effects and is available as a 800 mg scored tablet.
Metaxalone is a skeletal muscle relaxant indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomforts associated with acute, painful musculoskeletal conditions. The mode of action of this drug has not been clearly identified, but may be related to its sedative properties. Metaxalone does not directly relax tense skeletal muscles in man.
Trade Name | Metaxalone |
Availability | Prescription only |
Generic | Metaxalone |
Metaxalone Other Names | Metassalone, Metaxalon, Metaxalona, Metaxalone, Metaxalonum |
Related Drugs | cyclobenzaprine, tizanidine, diazepam, methocarbamol, Flexeril, Soma |
Weight | 400mg, 800mg |
Type | Oral tablet |
Formula | C12H15NO3 |
Weight | Average: 221.2524 Monoisotopic: 221.105193351 |
Groups | Approved |
Therapeutic Class | |
Manufacturer | |
Available Country | United States |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Metaxalone is a muscle relaxant used to treat muscle pain or spasm.
For the treatment of painful peripheral musculoskeletal conditions and spasticity from upper motor neuron syndromes.
Metaxalone is also used to associated treatment for these conditions: Pain
How Metaxalone works
The mechanism of action of metaxalone in humans has not been established, but may be due to general central nervous system depression.
Toxicity
LD50=775mg/kg (Rat, oral); LD50=1690 mg/kg (Mouse, oral). When determining the LD50 in rats and mice, progressive sedation, hypnosis and finally respiratoryfailure were noted as the dosage increased. In dogs, no LD50 could be determined as the higher doses produced an emetic action in 15 to 30 minutes. Some adverse events associated with the drug include nausea, vomiting, drowsiness and CNS side effects such as dizziness, headache, and irritability.
Food Interaction
- Avoid excessive or chronic alcohol consumption. Alcohol may increase the CNS depressant effects of metaxalone.
- Take with or without food. The absorption of metaxalone is increased when taken with food, which may increase CNS depression, especially in the elderly.
[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.
Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.
Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.
Metaxalone Drug Interaction
Major: acetaminophen / hydrocodone, acetaminophen / hydrocodoneModerate: diphenhydramine, diphenhydramine, duloxetine, duloxetine, pregabalin, pregabalin, cetirizine, cetirizineUnknown: omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, montelukast, montelukast, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol
Metaxalone Disease Interaction
Volume of Distribution
- 800 L
Elimination Route
The absolute bioavailability of metaxalone from Skelaxin tablets is not known.
Half Life
9.2 (+/- 4.8) hours
Clearance
- 68 +/- 50 L/h [Subjects received 1×400mg tablet under fasted conditions]
- 66 +/- 51 L/h [Subjects received 2×400 mg tablets under fasted conditions]
Elimination Route
Metaxalone is metabolized by the liver and excreted in the urine as unidentified metabolites.
Innovators Monograph
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