viruses have 2 surface proteins. hemagglutinins are responsible for the binding and uptake of the virus, while neuraminidases are responsible for release of new virus (via sialic acid cleavage). NIs block this cleavage, preventing release of new virus.
Tamiflu oral, Relenza inhaled (so not for folks c respiratory disease)
GI. Tamiflu unusual dreams. Relenza possible bronchospasm
uncoating inhibitors drugs
amantadine (Symmetrel), rimantadine (Flumadine)
uncoating inhibitors MOA
flu A: thought to prevent influx of protons through viral M2 channels that causes the pH-dependent process of RNA-protein coat dissociation. parkinsons: amantadine may increase dopamine release and block ACh receptors, enhancing motor control.
uncoating inhibitors kinetics
amantadine more lipophilic, so more CNS SE than rimantadine (but better for Parkinsons)
nucleoside analogues MOA
viral enzymes convert nucleoside analogues to active nucleoside triphosphates, which are then incorporated and mess with viral DNA strands.
taken up by cytosine permease, an enzyme present only in fungi. it is then metabolized (> 5-FU > 5-FDUMP) and goes on to inhibit thymidine synthetase (needed for DNA replication)
severe fungal infections. use in combo with amphotericin B to prevent resistance.
N/V (give capsules a few at a time over a 15 min period). BBW renal impairment. lots of other kick ass SE including TEN.
ALL THE QUINES. chloroquine (Aralen), hydroxychloroquine (Plaquenil).
largely unknown. chloroquine possibly concentrates in parasitic food vacules, causing toxic heme buildup. primaquine is the only drug that works on both the exoerythrocytic and erythrocytic phases of malarial infection (P vivax, P ovale).
malaria (chloroquine first line). also RA, SLE, cutaneous skin disorders. quinine+clindamycin also for babesial infections.
mefloquine seizures, some psych issues.
quinine+mefloquinine (QT prolongation, seizures). quinine+Aluminum antacids (messes c absorption/excretion).
chloroquine visual disturbances (hydroxychloroquine is a less toxic alternative). quinine cinchonism (tinnitus, HA, nausea, dizziness, flushing, visual disturbances)
slow elimination of mefloquine (second line) allows for single dose treatment (f/u c primaquine for liver bugs)