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Rimantadine
From Proteopedia
(Difference between revisions)
(New page: <applet load="" size="480" color="" frame="true" spin="on" Scene ="Tacrine/Tacrine/3" align="right" caption="Tacrine, also known as Cognex"/> ===Better Known as: Cognex=== * Marketed By...) |
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| - | <applet load="" size="480" color="" frame="true" spin="on" Scene =" | + | <applet load="" size="480" color="" frame="true" spin="on" Scene ="" align="right" caption="Rimantadine, also known as Flumadine"/> |
| - | ===Better Known as: | + | ===Better Known as: Flumadine=== |
| - | * Marketed By: | + | * Marketed By: Forest Labs<br /> |
| - | * Major Indication: [[ | + | * Major Indication: [[Influenza]] Infection<br /> |
| - | * Drug Class: [[ | + | * Drug Class: [[M2 Proton Channel]] Inhibitor |
| - | * Date of FDA Approval (Patent Expiration): 1993 ( | + | * Date of FDA Approval (Patent Expiration): 1993 (2001)<br /> |
| - | * 1994 Sales: | + | * 1994 Sales: N/A |
| - | * Importance: One of the the first treatments for | + | * Importance: One of the the first treatments for [[Influenza]] Infections. Since 1994, nearly 100% of influenza viruses had developed resistance to rimantadine, and it is no longer recommended as a treatment for the flu. |
* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information | * The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information | ||
===Mechanism of Action=== | ===Mechanism of Action=== | ||
| - | Tacrine is an [[Acetylcholinesterase]] (AChE) inhibitor. It binds to the active site of <scene name='Tacrine/Ache/1'>AChE</scene>, utilizing many of the same residues which <scene name='Tacrine/Ac/1'>bind and break down acetylcholine</scene>. By inhibiting AChE, the important neurotransmitter, [[acetylcholine]], is degraded at a slower rate, helping reverse the marked decrease in neuronal function evident in [[Alzheimer's Disease]] patients. Tacrine <scene name='Tacrine/Bound/2'>primarily interacts with residues</scene> Phe 330, His 440, Trp 84, & Ser 200 in tightly binding to the AChE binding site via pi stacking interactions. It is clearly visible how <scene name='Tacrine/Inter/3'>Tacrine interferes</scene> with the binding of acetylcholine, outcompeting acetylcholine for nearly the same space in the active site. <ref>PMID:8415649</ref> | ||
===Pharmacokinetics=== | ===Pharmacokinetics=== | ||
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|- | |- | ||
! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%) | ! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%) | ||
| - | ! | + | ! >90 |
| - | ! | + | ! >90 |
|- | |- | ||
! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%) | ! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%) | ||
| - | ! | + | ! 40 |
| - | ! | + | ! 67 |
|- | |- | ||
! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr) | ! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr) | ||
! 27.7 | ! 27.7 | ||
| - | ! | + | ! ~15 |
|- | |- | ||
! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr) | ! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr) | ||
| Line 46: | Line 45: | ||
|- | |- | ||
! [[Pharmaceutical_Drugs#Clearance_.28Cl.29|Clearance]] (L/h) | ! [[Pharmaceutical_Drugs#Clearance_.28Cl.29|Clearance]] (L/h) | ||
| - | ! [[Rimantadine]] | ||
| - | ! [[Amantadine]] | ||
| - | |- | ||
| - | ! [[Pharmaceutical_Drugs#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM) | ||
! [[Rimantadine]] | ! [[Rimantadine]] | ||
! [[Amantadine]] | ! [[Amantadine]] | ||
Revision as of 12:30, 6 December 2010
|
Better Known as: Flumadine
- Marketed By: Forest Labs
- Major Indication: Influenza Infection
- Drug Class: M2 Proton Channel Inhibitor
- Date of FDA Approval (Patent Expiration): 1993 (2001)
- 1994 Sales: N/A
- Importance: One of the the first treatments for Influenza Infections. Since 1994, nearly 100% of influenza viruses had developed resistance to rimantadine, and it is no longer recommended as a treatment for the flu.
- The following is a list of Pharmacokinetic Parameters. See: Pharmaceutical Drugs for more information
Mechanism of Action
Pharmacokinetics
| M2 Proton Channel Inhibitor Pharmacokinetics[1] | ||||||
|---|---|---|---|---|---|---|
| Parameter | Rimantadine | Amantadine | ||||
| Tmax (hr) | 4.3 | Amantadine | ||||
| Cmax (ng/ml) | 310 | Amantadine | ||||
| Bioavailability (%) | >90 | >90 | ||||
| Protein Binding (%) | 40 | 67 | ||||
| T1/2 (hr) | 27.7 | ~15 | ||||
| AUC (ng/ml/hr) | 11917 | Amantadine | ||||
| Clearance (L/h) | Rimantadine | Amantadine | ||||
| Dosage (mg) | 100 | Amantadine | ||||
| Metabolism | Rimantadine | Amantadine | ||||
References
- ↑ Anderson EL, Van Voris LP, Bartram J, Hoffman HE, Belshe RB. Pharmacokinetics of a single dose of rimantadine in young adults and children. Antimicrob Agents Chemother. 1987 Jul;31(7):1140-2. PMID:3662473
