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23 Cards in this Set
- Front
- Back
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Amantadine, Rimantadine mechanism
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Blocking of M2 ion channel; membrane can't fuse with the phagolysosomal membrane
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Amantdine, Rimantadine are used for what virus?
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Influenza A
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Mechanism of resistanse to Amantadine, Rimantadine
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Point mutations in transmembrane region of M2 drug.
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Amantadine, Rimantadine absorption
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Well absorbed orally; 80% bioavalability
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Amantadine distribution
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Well distributed
Penetrates CSF better than rimantadine |
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Rimantadine distribution
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Well distributed
Penetrates CSF |
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Amantadine metbolism
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Little metabolism
T1/2 = 15 hr. |
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Rimantadine metabolism:
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Extensive metabolism
T1/2 = 30 hr. |
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Amantadine, Rimantadine excretion
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Renal
For both the parent compound (amantadine) and the metabolites (rimantadine) |
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Amantadine, Rimantadine adverse effects
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GI irritation
CNS effects: nervousness, lightheadedness, insomnia, difficulty concentration (worse iwth amantadine) |
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Amantadine clinical uses
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Influenza A only
Anti-parkinsonian effects: increased dopamine synthesis from the substantia nigra |
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Zanamavir, Oseltamavir mechanism
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Competitive Inhibition of viral neuramidase
Sialic acid is unable to bind; viruses can't get away from host cells Specific for viral neuramindases |
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Zanamavir, Oseltamavir clinical activity
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Prevention of influenza A, B
-Reduce infection -Reduces illness with fever Treatment of influenza A, B |
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Resistance to Zanamavir, Oseltamavir
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Point mutations in neuraminidase decrease affinity of enzyme for drugs
H274Y mutation in N1 produces resistance to oseltamivir, but not zanamivir |
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Zanamivir absorption
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Inhalation
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Oseltamivir absorption
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Oral
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Zanamivir distribution
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Oropharynx 78%
Lungs 13% |
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Oseltamivir distribution
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Systemic
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Zanamivir metabolism
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None
T1/2 = 2 - 5 hr. |
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Oseltamivir metabolism
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Converted to a carboxylate by serum esterases
T1/2 = 6-10 hr. |
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Zanamavir, Oseltamavir excretion
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Renally as unchanged, active drug
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Zanamivir adverse effects
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Lung problems in pts. with pre-existing lung disease
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Oseltamivir adverse effects
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GI upset.
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