Peringatan Keamanan

Overdose of methocarbamol may be associated with alcohol and other central nervous system depressants.Label Patients may experience nausea, drowsiness, blurred vision, hypotension, seizures, and coma.Label Treatment of overdose is generally through airway maintenance, monitoring urinary output, vital signs, and giving fluid intravenously if necessary.Label

The oral LD50 in rats is 3576.2mg/kg.L6295

The FDA has classified methocarbamol as pregnancy category C.Label Animal and human studies have not been performed to determine the risks to a fetus, however fetal and congenital abnormalities have been reported.Label Methocarbamol is excreted in the milk of dogs, however it is unknown if this is also the case for humans.Label Caution should be exercised when taking methocarbamol while breastfeeding.Label

Studies to assess the carcinogenicity, mutagenicity, or effects on fertility of methocarbamol have not been performed.Label

Methocarbamol

DB00423

small molecule approved vet_approved

Deskripsi

Methocarbamol was developed in the early 1950s as a treatment for muscle spasticity and the associated pain.A178441,A178450 It is a guaiacol glyceryl ether.A178450

Methocarbamol tablets and intramuscular injections are prescription medicines indicated in the United States as an adjunct to rest, physical therapy, and other measures for the relief of discomforts associated with acute, painful musculoskeletal conditions.Label,L6268 In Canada, methocarbamol can be sold as an over the counter oral medicine at a lower dose that may be combined with acetaminophen or ibuprofen.L6295 A combination product with acetylsalicylic acid and codeine is available in Canada by prescription.L6295

Methocarbamol was FDA approved on 16 July 1957.L6265

Struktur Molekul 2D

Berat 241.2405
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half life is 1.14 hours in healthy subjects and 1.24 hours in subjects with renal insufficiency.[A636] Older studies report half lives of 1.6-2.15 hours.[A178366]
Volume Distribusi Volume of distribution data in humans is scarce. In horses, the volume of distribution is 515-942mL/kg at steady state or 724-1130mL/kg.[A178426]
Klirens (Clearance) 0.2-0.8L/h/kg.[L6268]

Absorpsi

The time to maximum concentration is 1.1 hours for both healthy patients and those on hemodialysis.A636 The maximum plasma concentration is 21.3mg/L for healthy patients and 28.7mg/L in hemodialysis patients.A636 The area under the curve for healthy patients is 52.5mg/L\*hr and 87.1mg/L*hr in hemodialysis patients.A636 AUC% based on terminal elimination half life is 2% for healthy patients and 4% for hemodialysis patients.A636 Older studies report maximum plasma concentrations in 0.5 hours.A178366

Metabolisme

Methocarbamol is metabolized in the liver by demethylation to 3-(2-hydroxyphenoxy)-1,2-propanediol-1-carbamate or hydroxylation to 3-(4-hydroxy-2-methoxyphenoxy)-1,2-propanediol-1-carbamate.A178366 Methocarbamol and its metabolites are conjugated through glucuronidation or sulfation.A178366

Rute Eliminasi

In humans the majority of the dose is eliminated in the urine.A178366 In dogs, 88.85% of the dose is eliminated in urine and 2.14% in the feces.A178366 In rats, 84.5-92.5% of the dose is eliminated in the urine and 0-13.3% is eliminated in the feces.A178366

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

668 Data
Buprenorphine Methocarbamol 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 Methocarbamol.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Methocarbamol.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Methocarbamol.
Hydrocodone Methocarbamol 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 Methocarbamol.
Magnesium sulfate The therapeutic efficacy of Methocarbamol can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Methocarbamol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Methocarbamol may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Methocarbamol.
Mirtazapine Methocarbamol may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Methocarbamol.
Orphenadrine Methocarbamol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Methocarbamol 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 Methocarbamol.
Pramipexole Methocarbamol may increase the sedative activities of Pramipexole.
Ropinirole Methocarbamol may increase the sedative activities of Ropinirole.
Rotigotine Methocarbamol may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Methocarbamol.
Sodium oxybate Methocarbamol may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Methocarbamol 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 Methocarbamol.
Thalidomide Methocarbamol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Methocarbamol 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 Methocarbamol.
Eperisone The risk or severity of visual accommodation disturbances can be increased when Eperisone is combined with Methocarbamol.
Pyridostigmine The therapeutic efficacy of Pyridostigmine can be decreased when used in combination with Methocarbamol.
Ethanol Methocarbamol may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Methocarbamol 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 Methocarbamol.
Fluvoxamine The risk or severity of adverse effects can be increased when Methocarbamol is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Methocarbamol is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Methocarbamol is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Methocarbamol is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Methocarbamol is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Methocarbamol is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Methocarbamol is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Methocarbamol is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Methocarbamol is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Methocarbamol is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Methocarbamol is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Methocarbamol is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Methocarbamol is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Methocarbamol is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Methocarbamol is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Methocarbamol is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Methocarbamol is combined with Alaproclate.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Methocarbamol.
Cyproheptadine The risk or severity of CNS depression can be increased when Methocarbamol is combined with Cyproheptadine.
Imipramine The risk or severity of CNS depression can be increased when Methocarbamol is combined with Imipramine.
Nortriptyline The risk or severity of CNS depression can be increased when Methocarbamol is combined with Nortriptyline.
Amoxapine The risk or severity of CNS depression can be increased when Methocarbamol is combined with Amoxapine.
Propiomazine The risk or severity of CNS depression can be increased when Methocarbamol is combined with Propiomazine.
Maprotiline The risk or severity of CNS depression can be increased when Methocarbamol is combined with Maprotiline.
Doxepin The risk or severity of CNS depression can be increased when Methocarbamol is combined with Doxepin.
Desipramine The risk or severity of CNS depression can be increased when Methocarbamol is combined with Desipramine.
Pizotifen The risk or severity of CNS depression can be increased when Methocarbamol is combined with Pizotifen.
Dosulepin The risk or severity of CNS depression can be increased when Methocarbamol is combined with Dosulepin.
Zopiclone The risk or severity of adverse effects can be increased when Methocarbamol 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 Methocarbamol.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Methocarbamol.
Tryptophan The risk or severity of CNS depression can be increased when Tryptophan is combined with Methocarbamol.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Methocarbamol.
Lorazepam The risk or severity of CNS depression can be increased when Lorazepam is combined with Methocarbamol.
Ethchlorvynol The risk or severity of CNS depression can be increased when Ethchlorvynol is combined with Methocarbamol.
Succinylcholine The risk or severity of CNS depression can be increased when Succinylcholine is combined with Methocarbamol.
Reserpine The risk or severity of CNS depression can be increased when Reserpine is combined with Methocarbamol.
Eletriptan The risk or severity of CNS depression can be increased when Eletriptan is combined with Methocarbamol.
Enflurane The risk or severity of CNS depression can be increased when Enflurane is combined with Methocarbamol.
Temazepam The risk or severity of CNS depression can be increased when Temazepam is combined with Methocarbamol.
Reboxetine The risk or severity of CNS depression can be increased when Reboxetine is combined with Methocarbamol.
Butabarbital The risk or severity of CNS depression can be increased when Butabarbital is combined with Methocarbamol.
Butalbital The risk or severity of CNS depression can be increased when Butalbital is combined with Methocarbamol.
Methysergide The risk or severity of CNS depression can be increased when Methysergide is combined with Methocarbamol.
Cabergoline The risk or severity of CNS depression can be increased when Cabergoline is combined with Methocarbamol.
Phenytoin The risk or severity of CNS depression can be increased when Phenytoin is combined with Methocarbamol.
Topiramate The risk or severity of CNS depression can be increased when Topiramate is combined with Methocarbamol.
Clemastine The risk or severity of CNS depression can be increased when Clemastine is combined with Methocarbamol.
Venlafaxine The risk or severity of CNS depression can be increased when Venlafaxine is combined with Methocarbamol.
Etomidate The risk or severity of CNS depression can be increased when Etomidate is combined with Methocarbamol.
Morphine The risk or severity of CNS depression can be increased when Morphine is combined with Methocarbamol.
Talbutal The risk or severity of CNS depression can be increased when Talbutal is combined with Methocarbamol.
Pentobarbital The risk or severity of CNS depression can be increased when Pentobarbital is combined with Methocarbamol.
Valproic acid The risk or severity of CNS depression can be increased when Valproic acid is combined with Methocarbamol.
Zolmitriptan The risk or severity of CNS depression can be increased when Zolmitriptan is combined with Methocarbamol.
Dihydroergotamine The risk or severity of CNS depression can be increased when Dihydroergotamine is combined with Methocarbamol.
Tolcapone The risk or severity of CNS depression can be increased when Tolcapone is combined with Methocarbamol.
Hydromorphone The risk or severity of CNS depression can be increased when Hydromorphone is combined with Methocarbamol.
Olanzapine The risk or severity of CNS depression can be increased when Olanzapine is combined with Methocarbamol.
Cetirizine The risk or severity of CNS depression can be increased when Cetirizine is combined with Methocarbamol.
Protriptyline The risk or severity of CNS depression can be increased when Protriptyline is combined with Methocarbamol.
Trimethadione The risk or severity of CNS depression can be increased when Trimethadione is combined with Methocarbamol.
Clobazam The risk or severity of sedation, somnolence, and CNS depression can be increased when Clobazam is combined with Methocarbamol.
Chlorzoxazone The risk or severity of CNS depression can be increased when Chlorzoxazone is combined with Methocarbamol.
Clozapine The risk or severity of CNS depression can be increased when Clozapine is combined with Methocarbamol.
Meprobamate The risk or severity of CNS depression can be increased when Meprobamate is combined with Methocarbamol.
Thiethylperazine The risk or severity of CNS depression can be increased when Thiethylperazine is combined with Methocarbamol.
Palonosetron The risk or severity of CNS depression can be increased when Palonosetron is combined with Methocarbamol.
Sulpiride The risk or severity of CNS depression can be increased when Sulpiride is combined with Methocarbamol.
Alprazolam The risk or severity of CNS depression can be increased when Alprazolam is combined with Methocarbamol.

Target Protein

Carbonic anhydrase 1 CA1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 2253675
    Sica DA, Comstock TJ, Davis J, Manning L, Powell R, Melikian A, Wright G: Pharmacokinetics and protein binding of methocarbamol in renal insufficiency and normals. Eur J Clin Pharmacol. 1990;39(2):193-4.
  • PMID: 5548215
    Bruce RB, Turnbull LB, Newman JH: Metabolism of methocarbamol in the rat, dog, and human. J Pharm Sci. 1971 Jan;60(1):104-6.
  • PMID: 25050056
    Witenko C, Moorman-Li R, Motycka C, Duane K, Hincapie-Castillo J, Leonard P, Valaer C: Considerations for the appropriate use of skeletal muscle relaxants for the management of acute low back pain. P T. 2014 Jun;39(6):427-35.
  • PMID: 5413283
    Crankshaw DP, Raper C: Mephenesin, methocarbamol, chlordiazepoxide and diazepam: actions on spinal reflexes and ventral root potentials. Br J Pharmacol. 1970 Jan;38(1):148-56. doi: 10.1111/j.1476-5381.1970.tb10343.x.
  • PMID: 9109959
    Muir WW 3rd, Sams RA, Ashcraft S: The pharmacology and pharmacokinetics of high-dose methocarbamol in horses. Equine Vet J Suppl. 1992 Feb;(11):41-4.
  • PMID: 20325834
    Authors unspecified: Methocarbamol-A New Lissive Agent. Can Med Assoc J. 1958 Dec 15;79(12):1008-9.
  • PMID: 13538683
    O'DOHERTY DS, SHIELDS CD: Methocarbamol; new agent in treatment of neurological and neuromuscular diseases. J Am Med Assoc. 1958 May 10;167(2):160-3.

Contoh Produk & Brand

Produk: 525 • International brands: 16
Produk
  • A.S.A. With Methocarbamol Night-time Extra Strength
    Tablet • - • Oral • Canada • OTC • Approved
  • Acetaminophen 325mg + Methocarbamol 400mg Caplets
    Tablet • - • Oral • Canada • OTC • Approved
  • Acetaminophen 500mg + Methocarbamol 400mg Extra Strength Caplets
    Tablet • - • Oral • Canada • OTC • Approved
  • Advil Back Pain
    Tablet • - • Oral • Canada • OTC • Approved
  • Analgesic and Muscle Relaxant
    Tablet • - • Oral • Canada • OTC • Approved
  • Analgesic and Muscle Relaxant Caplets
    Tablet • - • Oral • Canada • OTC • Approved
  • Aspirin Backache
    Tablet • - • Oral • Canada • OTC • Approved
  • Aspirin Night-time
    Tablet • - • Oral • Canada • OTC • Approved
Menampilkan 8 dari 525 produk.
International Brands
  • Bolaxin — Ying Yuan
  • Carbaflex — Paill
  • Delaxin
  • DoloVisan — Dr.Kade Pharmaceutische Fabrik
  • Fubaxin — Grape King
  • Lumirelax — Juvise
  • Metocarbamol — AZ Pharma
  • Mioflex — Labinco
  • Miorel — Cheminter
  • Musxan — Pharmasant

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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