Methylphenobarbital

Methylphenobarbital (INN), also known as mephobarbital (USAN, JAN) and mephobarbitone (BAN), marketed under brand names such as Mebaral, Mephyltaletten, Phemiton, and Prominal, is a drug which is a barbiturate derivative and is used primarily as an anticonvulsant,[1] but also as a sedative and anxiolytic. It is the N-methylated analogue of phenobarbital and has similar indications, therapeutic value, and tolerability.

Methylphenobarbital
Clinical data
Trade namesMebaral, generics
AHFS/Drugs.comInternational Drug Names
MedlinePlusa605022
Pregnancy
category
  • US: D (Evidence of risk)
    Routes of
    administration    		By mouth (tablets)
    ATC code
    Legal status
    Legal status
    • CA: Schedule IV
    • DE: Prescription only (Anlage III for higher doses)
    • UK: Class B
    • US: Schedule IV
    Pharmacokinetic data
    Protein binding70–76%
    MetabolismLiver
    Elimination half-life34 hours
    Identifiers
    CAS Number
    PubChem CID
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard100.003.714
    Chemical and physical data
    FormulaC13H14N2O3
    Molar mass246.3 g/mol g·mol−1
    3D model (JSmol)
      (verify)

    Approval history
    • 1935 – Mebaral was introduced by Winthrop Pharmaceuticals.
    • 2001 – Methylphenobarbital discontinued in the UK.
    • 2003 – Mebaral was acquired by Ovation Pharmaceuticals (a specialty pharmaceutical company that acquired under-promoted branded pharmaceutical products).
    • 2009 – Ovation was acquired by Lundbeck, which now markets Mebaral.
    • 2012 – Lundbeck announced that they were abandoning the product in the US as of January 6, 2012. The stated reason was because "the company thoroughly evaluated all avenues for keeping Mebaral available to patients, but ultimately concluded that no matter what steps they [i.e. Lundbeck] took, patients would be forced to transition to a new therapy."

    The company further stated in a letter on its website [2] that under the FDA's Unapproved Drugs Initiative, FDA is no longer willing to allow the drug to be grandfathered. A new drug application would have needed to have been submitted to gain marketing approval, which would have taken an estimated five years, during which time patients would be required to change their therapies in any case. The last available tablets bore an expiration date of March 31, 2012, and the drug will no longer be available in the US when supplies are depleted.

    Overdose

    Symptoms of overdose of mephobarbital include confusion, decrease in or loss of reflexes, somnolence, fever, irritability, hypothermia, poor judgment, shortness of breath or slow/troubled breathing, slow heartbeat, slurred speech, staggering, trouble in sleeping, unusual movements of the eyes, weakness.

    See also

    References
    1. S. D. Shorvon; David R. Fish; Emilio Perucca; W. Edwin Dodson, eds. (2004). The Treatment of Epilepsy (2nd ed.). Blackwell. ISBN 0-632-06046-8.
    2. Letter from Lundbeck to prescribers
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