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Article
Title Pharmacology and neurochemistry of methadone 
Author Vendramin Andrea, Sciacchitano Annella M  
Article Information Abstract
Publication Heroin Addiction and Related Clinical Problems  Contrary to what might be thought initially, the pharmacology of
methadone is only partly known, and current research continues to
investigate into its distinctive aspects. Clinical evidence provides key
guidance to pharmacological research on the opiate system; on the other
hand, evolving expectations from therapeutic drugs or putative agents
for addiction treatment provide a key incentive to the broadening
of pharmacological knowledge. Apart from the classic description of
receptorial opioid agonism, narcotic blockade and
tolerance/withdrawal dynamics, some crucial issues need to be
clarified in a comprehensive way. For instance, studies have proved
the importance of metabolic polymorphism in treatment planning and
offered interpretations of apparent resistance to normal dosages, so
authorizing the employment of high dosages on a sound pharmacological
basis. Also, dosages should not be regarded as stable through time,
especially in the first few months, and clinicians may schedule dose
variations that take into account such expected variations while
pursuing stabilization. Methadone's action profile in the central
nervous system is not exclusively based on opioid receptors, and a
thorough knowledge of its 'collateral' effects may explain its
beneficial action against specific psychopathological abnormalities.
The role of the inactive enantiomer in the context of racemous
methadone's tolerability and action profile has also been outlined.
Lastly, some of the therapeutic effects of methadone endure without
being neutralized by the emergence of tolerance; one of these is its
crucial anticraving property. In order to clarify this issue, the
mechanisms of cell membrane endocytosis and signal transduction have been
illustrated and compared between different opiates.


Reference BUPP10092 
Year 2009 
Logged 17/02/2010 
Volume 11 
Part
Pages 11-28 
ISSN 1592-1638 
Keywords  
Comparison Drug  
Language English 

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