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    Metaxalone molecular structure

    Metaxalone Stats & Data

    Skelaxin
    PubChem
    MW221.25
    FormulaC12H15NO3
    LogP2.2
    IUPAC5-[(3,5-dimethylphenoxy)methyl]-1,3-oxazolidin-2-one
    InChIKeyIMWZZHHPURKASS-UHFFFAOYSA-N
    Chemical Class Oxazolidinone
    Psychoactive Class Depressant

    Pharmacology

    DrugBank
    Half-life 9.2 (+/- 4.8) hours State Solid Vd * 800 L Metabolism Probably hepatic.

    Description

    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.

    Mechanism of Action

    The mechanism of action of metaxalone in humans has not been established, but may be due to general central nervous system depression.

    Pharmacodynamics

    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.

    Absorption

    The absolute bioavailability of metaxalone from Skelaxin tablets is not known.

    Indication

    For the treatment of painful peripheral musculoskeletal conditions and spasticity from upper motor neuron syndromes.

    Elimination

    Metaxalone is metabolized by the liver and excreted in the urine as unidentified metabolites.

    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

    Toxicity

    PubChem DrugBank

    Liver injury risk

    Low concern (rare serious cases reported)

    FDA LiverTox / DILIrank. Reflects published case reports of liver injury, not absolute risk.

    Toxicity (DrugBank)

    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.

    Tolerance & Pharmacokinetics

    drugs.wiki

    Tolerance Decay

    Full tolerance 3d Half tolerance 8d Baseline ~14d

    Experience Report Analysis

    Erowid
    21 Reports
    11 Single-substance
    2002–2020 Date Range
    9 With Age Data
    5 Effects Detected

    Demographics

    Gender Distribution

    Age Distribution

    Reports Over Time

    Effect Analysis

    Erowid

    Effects aggregated from 11 experience reports (11 single-substance Erowid)

    11 Reports
    5 Effects Detected
    2 Positive
    3 Adverse
    0 Neutral

    Effect Sentiment Distribution

    Confidence Distribution

    Each bar is the share of reports mentioning the effect; its whisker, and the band on the rows below, is the 95% interval: where the share could plausibly be with other reports of the same kind.

    Too few reports for bars: these effects come from 11 single-substance Erowid reports, and a bar is drawn only from 20 reports or more. With fewer, a percentage cannot tell a common effect from a rare one. Counts are shown instead. Why 20?

    Positive Effects 2

    Sedation 4 of 11 70%
    Euphoria 3 of 11 70%

    Adverse Effects 3

    Nausea 3 of 11 70%
    Sweating 3 of 11 70%
    Anxiety 3 of 11 70%

    Dosage Distribution

    Dose distribution from experience reports, one dose per report (the first listed). Doses above Q3 + 3×IQR, far above what people typically take, are left out of the median and range and listed under each route: most are real heavy doses or overdoses, not mistakes.

    Median: 800.0 mg IQR: 800.0–2275.0 mg n=10

    Real-World Dose Distribution

    Erowid

    From 31 of 37 recorded dose entries: those that state a weight (mg, g or µg), in routes with at least five of them. Values above Q3 + 3×IQR, far above what people typically take, are left out; they can include real heavy doses and overdoses, not only mistakes.

    Oral (n=31)

    Median: 800.0mg 25th: 800.0mg 75th: 1600.0mg 90th: 3200.0mg

    Common Combinations

    Most co-occurring substances, as a share of all 21 reports filed under Metaxalone; whiskers are 95% intervals

    Form / Preparation

    Most common forms and preparations, as a share of the 14 reports that give one

    Too few reports for bars: these forms come from 14 reports, and a bar is drawn only from 20 reports or more. With fewer, a percentage cannot tell a common effect from a rare one. Counts are shown instead. Why 20?

    • Pill / Tablet 13 of 14

    Body-Weight Dosing

    Dose per kg of body weight, one dose per report (the first listed), from reports giving a weight of 30–250 kg. Doses above Q3 + 3×IQR, far above what people typically take, are left out of the median and range and listed under each route.

    Median: 13.133 mg/kg IQR: 9.635–32.092 mg/kg n=10

    Redose Patterns

    Redosing behavior across 15 reports

    4 of 15 Redosed
    1.6 Avg Doses
    30m Median Interval

    Too few reports for a chart: redosing is known from 15 reports, and a split is drawn only from 20 reports or more. Counts are shown instead. Why 20?

    • Single dose 11 of 15
    • Redosed 4 of 15
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