Amantadine: Difference between revisions

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<applet  load="" size="480" color="" frame="true"  spin="on" Scene ="Amantadine/Amantadine/1" align="right" caption="Amantadine, also known as Symmetrel ([[2kqt]])"/>
<StructureSection load='' size='340' side='right' caption='Amantadine, also known as Symmetrel ([[2kqt]])' scene=Amantadine/Amantadine/1'>
===Better Known as: Symmetrel===
===Better Known as: Symmetrel===
* Marketed By: Endo Pharmaceuticals
* Marketed By: Endo Pharmaceuticals
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* Importance: One of the the first treatments approved by the FDA and the first approved for treatment of [[Influenza]] Infections. Nearly 100% of influenza viruses had developed resistance to rimantadine, and it is no longer recommended as a treatment for the flu. Interestingly, in 1969 it was also discovered that Amantadine helped reduce the symptoms of Parkinson's Disease.  
* Importance: One of the the first treatments approved by the FDA and the first approved for treatment of [[Influenza]] Infections. Nearly 100% of influenza viruses had developed resistance to rimantadine, and it is no longer recommended as a treatment for the flu. Interestingly, in 1969 it was also discovered that Amantadine helped reduce the symptoms of Parkinson's Disease.  
* See [[Pharmaceutical Drugs]] for more information about other drugs and disorders.
* See [[Pharmaceutical Drugs]] for more information about other drugs and disorders.
* (<scene name="Amantadine/Amantadine/1">Restore initial scene</scene>).


===Mechanism of Action===
===Mechanism of Action===
The [[Influenza]] A Virus viral envelope is dotted with various [[ion channels]] including [[M2 Proton Channel|M2 Proton Channels]]. The <scene name='Amantadine/M2/1'>M2 protein</scene> plays a critical role in the life cycle of the Influenza virus. It enables hydrogen ions to enter the virion form the endosome. The result of this is a more acidic environment within the virus, causing dissociation of the viral matrix protein M1 from the ribonucleoprotein RNP. Dissociation of the viral matrix protein is a crucial step in uncoating of the virus and exposing its contents to the cytoplasm of the host cell, allowing the virus to hijack the cellular machinery to replicate. <scene name='Amantadine/Bound/1'>Amantadine binds to the pore</scene> formed by the M2 protein, utilizing Val 27, Ala 30 and Ser 31 in each M2 protein chain, effectively disabling the protein from transferring protons into the viral particle.<ref>PMID: 18235503</ref>
The [[Influenza]] A Virus viral envelope is dotted with various [[ion channels]] including [[M2 Proton Channel|M2 Proton Channels]]. The <scene name='Amantadine/M2/1'>M2 protein</scene> plays a critical role in the life cycle of the Influenza virus. It enables hydrogen ions to enter the virion form the endosome. The result of this is a more acidic environment within the virus, causing dissociation of the viral matrix protein M1 from the ribonucleoprotein RNP. Dissociation of the viral matrix protein is a crucial step in uncoating of the virus and exposing its contents to the cytoplasm of the host cell, allowing the virus to hijack the cellular machinery to replicate. <scene name='Amantadine/Bound/1'>Amantadine binds to the pore</scene> formed by the M2 protein, utilizing Val 27, Ala 30 and Ser 31 in each M2 protein chain, effectively disabling the protein from transferring protons into the viral particle.<ref>PMID: 18235503</ref>
 
</StructureSection>
===Pharmacokinetics===
===Pharmacokinetics===
{| class="wikitable" border="1" width="45%" style="text-align:center"
<table style="background: cellspacing="0px"  align="" cellpadding="0px" width="42%">
|-
<tr>
!  colspan="7" align="center"| M2 Proton Channel Inhibitor [[Pharmacokinetics]]<ref>PMID:3662473</ref><ref>PMID:17156962</ref>
<td style="width:100%; vertical-align:top;border-width:0px; border-style:inset">
|-
<div style="height:100%; width: 100%">
! Parameter
{{:M2 Proton Channel Inhibitor Pharmacokinetics}}
! [[Rimantadine]]
</div>
! [[Amantadine]]
</td>
|-
</tr>
! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)
</table>
! 4.3
! 2.5
|-
! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)
! 310
! 402
|-
! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%)
! >90
! >90
|-
! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%)
! 40
! 67
|-
! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
! 27.7
! ~15
|-
! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
! 11917
! 5420
|-
! Dosage (mg)
! 100
! 100
|-
! Metabolism
! Negligible
! Negligible
|}


===References===
===References===

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

David Canner, Eric Martz, Alexander Berchansky