Peringatan Keamanan

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.

Metaxalone

DB00660

small molecule approved

Deskripsi

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.

Struktur Molekul 2D

Berat 221.2524
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 9.2 (+/- 4.8) hours
Volume Distribusi * 800 L
Klirens (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]

Absorpsi

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

Metabolisme

Probably hepatic.

Rute Eliminasi

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

Interaksi Makanan

2 Data
  • 1. Avoid excessive or chronic alcohol consumption. Alcohol may increase the CNS depressant effects of metaxalone.
  • 2. Take with or without food. The absorption of metaxalone is increased when taken with food, which may increase CNS depression, especially in the elderly.

Interaksi Obat

1312 Data
Buprenorphine Metaxalone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Metaxalone.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Metaxalone.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Metaxalone.
Hydrocodone Metaxalone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Metaxalone.
Magnesium sulfate The therapeutic efficacy of Metaxalone can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Metaxalone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Metaxalone may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Metaxalone.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Metaxalone.
Orphenadrine Metaxalone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Metaxalone may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Metaxalone.
Pramipexole Metaxalone may increase the sedative activities of Pramipexole.
Ropinirole Metaxalone may increase the sedative activities of Ropinirole.
Rotigotine Metaxalone may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Metaxalone.
Sodium oxybate Metaxalone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Metaxalone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Metaxalone.
Thalidomide Metaxalone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Metaxalone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Metaxalone.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Metaxalone.
Mirtazapine Metaxalone may increase the serotonergic activities of Mirtazapine.
Ethanol Metaxalone may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Metaxalone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Metaxalone.
Fluvoxamine The risk or severity of adverse effects can be increased when Metaxalone is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Metaxalone is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Metaxalone is combined with Duloxetine.
Paroxetine The risk or severity of adverse effects can be increased when Metaxalone is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Metaxalone is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Metaxalone is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Metaxalone is combined with Nefazodone.
Zimelidine The risk or severity of adverse effects can be increased when Metaxalone is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Metaxalone is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Metaxalone is combined with Milnacipran.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Desvenlafaxine is combined with Metaxalone.
Seproxetine The risk or severity of adverse effects can be increased when Metaxalone is combined with Seproxetine.
Levomilnacipran The risk or severity of serotonin syndrome can be increased when Metaxalone is combined with Levomilnacipran.
Indalpine The risk or severity of adverse effects can be increased when Metaxalone is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Metaxalone is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Metaxalone is combined with Alaproclate.
Methylene blue Metaxalone may increase the serotonergic activities of Methylene blue.
Benzatropine Benzatropine may decrease the excretion rate of Metaxalone which could result in a higher serum level.
Disopyramide Disopyramide may decrease the excretion rate of Metaxalone which could result in a higher serum level.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Metaxalone.
Propiomazine The risk or severity of CNS depression can be increased when Metaxalone is combined with Propiomazine.
Propantheline Metaxalone may decrease the excretion rate of Propantheline which could result in a higher serum level.
Dicyclomine Metaxalone may decrease the excretion rate of Dicyclomine which could result in a higher serum level.
Tolterodine Metaxalone may decrease the excretion rate of Tolterodine which could result in a higher serum level.
Flavoxate Metaxalone may decrease the excretion rate of Flavoxate which could result in a higher serum level.
Tiotropium Metaxalone may decrease the excretion rate of Tiotropium which could result in a higher serum level.
Fesoterodine Metaxalone may decrease the excretion rate of Fesoterodine which could result in a higher serum level.
Aclidinium Metaxalone may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Trimebutine Metaxalone may decrease the excretion rate of Trimebutine which could result in a higher serum level.
Imidafenacin Metaxalone may decrease the excretion rate of Imidafenacin which could result in a higher serum level.
Propiverine Metaxalone may decrease the excretion rate of Propiverine which could result in a higher serum level.
Chlorpromazine The risk or severity of CNS depression can be increased when Chlorpromazine is combined with Metaxalone.
Maprotiline The risk or severity of CNS depression can be increased when Metaxalone is combined with Maprotiline.
Promethazine The risk or severity of CNS depression can be increased when Metaxalone is combined with Promethazine.
Quetiapine The risk or severity of CNS depression can be increased when Metaxalone is combined with Quetiapine.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Metaxalone.
Imipramine The risk or severity of CNS depression can be increased when Imipramine is combined with Metaxalone.
Doxepin The risk or severity of CNS depression can be increased when Metaxalone is combined with Doxepin.
Desipramine The risk or severity of CNS depression can be increased when Metaxalone is combined with Desipramine.
Zopiclone The risk or severity of adverse effects can be increased when Metaxalone is combined with Zopiclone.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Metaxalone.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Metaxalone.
Tryptophan The risk or severity of CNS depression can be increased when Tryptophan is combined with Metaxalone.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Metaxalone.
Lorazepam The risk or severity of CNS depression can be increased when Lorazepam is combined with Metaxalone.
Ethchlorvynol The risk or severity of CNS depression can be increased when Ethchlorvynol is combined with Metaxalone.
Succinylcholine The risk or severity of CNS depression can be increased when Succinylcholine is combined with Metaxalone.
Eletriptan The risk or severity of CNS depression can be increased when Eletriptan is combined with Metaxalone.
Enflurane The risk or severity of CNS depression can be increased when Enflurane is combined with Metaxalone.
Temazepam The risk or severity of CNS depression can be increased when Temazepam is combined with Metaxalone.
Reboxetine The risk or severity of CNS depression can be increased when Reboxetine is combined with Metaxalone.
Butabarbital The risk or severity of CNS depression can be increased when Butabarbital is combined with Metaxalone.
Butalbital The risk or severity of CNS depression can be increased when Butalbital is combined with Metaxalone.
Methysergide The risk or severity of CNS depression can be increased when Methysergide is combined with Metaxalone.
Cabergoline The risk or severity of CNS depression can be increased when Cabergoline is combined with Metaxalone.
Phenytoin The risk or severity of CNS depression can be increased when Phenytoin is combined with Metaxalone.
Topiramate The risk or severity of CNS depression can be increased when Topiramate is combined with Metaxalone.
Clemastine The risk or severity of CNS depression can be increased when Clemastine is combined with Metaxalone.
Venlafaxine The risk or severity of serotonin syndrome can be increased when Metaxalone is combined with Venlafaxine.
Etomidate The risk or severity of CNS depression can be increased when Etomidate is combined with Metaxalone.
Talbutal The risk or severity of CNS depression can be increased when Talbutal is combined with Metaxalone.
Pentobarbital The risk or severity of CNS depression can be increased when Pentobarbital is combined with Metaxalone.
Valproic acid The risk or severity of CNS depression can be increased when Valproic acid is combined with Metaxalone.
Zolmitriptan The risk or severity of CNS depression can be increased when Zolmitriptan is combined with Metaxalone.
Dihydroergotamine The risk or severity of CNS depression can be increased when Dihydroergotamine is combined with Metaxalone.
Tolcapone The risk or severity of CNS depression can be increased when Tolcapone is combined with Metaxalone.
Olanzapine The risk or severity of CNS depression can be increased when Olanzapine is combined with Metaxalone.
Cetirizine The risk or severity of CNS depression can be increased when Cetirizine is combined with Metaxalone.
Protriptyline The risk or severity of CNS depression can be increased when Protriptyline is combined with Metaxalone.
Trimethadione The risk or severity of CNS depression can be increased when Trimethadione is combined with Metaxalone.
Clobazam The risk or severity of sedation, somnolence, and CNS depression can be increased when Clobazam is combined with Metaxalone.

Referensi & Sumber

Synthesis reference: Spiridon Spireas, "Bioavailable compositions of metaxalone and processes for producing the same." U.S. Patent US20050276844, issued December 15, 2005.
Artikel (PubMed)
  • PMID: 18711953
    See S, Ginzburg R: Choosing a skeletal muscle relaxant. Am Fam Physician. 2008 Aug 1;78(3):365-70.
  • PMID: 6999895
    Elenbaas JK: Centrally acting oral skeletal muscle relaxants. Am J Hosp Pharm. 1980 Oct;37(10):1313-23.

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