Term
| MOA and clinical effects of rimantidine and amantidine |
|
Definition
both block the uncoating on the viral RNA inside the human cells by interfering with the function of the viral M2 protein which functions as an ion channel
redcue symptoms if tx begun within 48h of onsect, prophylaxis decreases risk of infection by 50-90%
Resistance has rendered these drugs in effective for most current flu viruses
Rimantadine has fewer CNS S/E so better for elderly and renal disease
decrease duration of symptoms for 1 day |
|
|
Term
| MOA and therapeutics of Zanamavir and Oseltamivir |
|
Definition
Zan nasal spray and oseltamivir oral, both expensive
both block the release of new viral particles from infected cells via the inhibition of viral neuraminidase |
|
|
Term
|
Definition
valacyclovir
F = 48%
valis the prodrug which is converted to acyclovir
oral tx with valacyclovir results in plasma acyclovir concentrations that are 3-5x greater than those achieved with oral acyclovir
decrease dose with renal failure |
|
|
Term
|
Definition
| poor, so use valacyclovir |
|
|
Term
| MOA of acyclovir, valacyclovir, penciclovir, ganciclovir, and valganciclovir |
|
Definition
inhibit viral DNA synthesis so they are not effective agaisnt non-replicating, latent viruses
the triphosphate forms of acyclovir and ganciclovir compete with dGTP at the viral DNA polymerase and also causes chain termination when incorporated into the viral DNA |
|
|
Term
| most common form of Res to acyclovir |
|
Definition
| mutation of the viral thymidine kinase which prevents the conversion of acyclovir to acyclovir monophosphate |
|
|
Term
| MOA and therapeutic use of cidofovir |
|
Definition
cidofovir is an analog of cytosine nucleotide which is converted to the active diphosphate by host-cell enzymes
the active diphosphate inhibits the viral DNA polymerase and is incorporated into the viral DNA
Used to treat CMV retinities |
|
|
Term
| Drugs used to treat CMV retinitis |
|
Definition
ganciclovir - DOC
valganciclovir
cidofovir
foscarnet
fomivirsen |
|
|
Term
|
Definition
given IV, it is an inorganic pyrophosphate which acts directly to inhibit viral DNA and RNA polymerases and HIV erverse trnscriptase
no activation via viral or host cell enzymes is required
used to treat HSV and VZV which are resistant to acyclovir
used to treat CMV which is resistant to ganciclovir and cidofovir |
|
|
Term
| MOA and therapeutic use of trifluridine, aka trifluorothymidine |
|
Definition
Trifluridine is converted to trifluridine triphosphate by host-cell enzymes: the active metabolite inhibitis viral DNA synthesis
Ocular drops are used to treat herpes keratitis, by HSV |
|
|
Term
| MOA and therapeutic use of vidarabine |
|
Definition
host cell enzymes produce the active metabolite vidarabine triphosphate which inhibits viral DNA polymerase
ocular drops are used to treat herpes keratitis |
|
|
Term
| MOA and therapeutic use of docosanol |
|
Definition
inhibits the fusion of the lipid enveloped herpes virus with the plasma membrane of the cell. Since the virus is not able to enter the cell viral replication is blocked
Used to treat oral -facial herpes keratitis |
|
|
Term
| Therapeutic uses of po acyclovir and valacyclovir |
|
Definition
DOC for HSV
fever blisters - begin therapy
primary or recurrent genital herpes
suppressive therapy for recurrent genital herpes
treatment of HSV proctitis
herpes zoster - dermatomes shingles
Resist is low
S/E of acyclovir and val = N/V, diarrhea and headache |
|
|
Term
|
Definition
converst active drug to monophosphate form which cannot be done by the host cell by itself
from there the host cell continues phosphorylation to create a nucleoside analog that interupts replication |
|
|
Term
|
Definition
enfuvirtide
a synthetic peptide which blocks fusion fo the viral and T-cell membrans so HIV cannot enver the CD4 T cell
Enfuvirtide shows no cross res with other classes of antiretroviral drugs
Used to treat patients who exhibit high viral loads despite continued therapy |
|
|
Term
|
Definition
nucleoside reversoe transcriptase inhibitors
these nucleosides are converted to "false" nucleotides (triphos) by intracellular kinases, they competitively inhibit HIV reverse transcriptase and cause chain termination of the viral DNA |
|
|
Term
|
Definition
zidovudine
lamivudine
stavudine
didanosine
zalcitabine
abacavir
emtricitabine
tenofovir
abacavir + lamivudine + zidovudine |
|
|
Term
| HIV post exposure prophylaxis |
|
Definition
|
|
Term
| Often effective when HIV has become Res to NRTIS' |
|
Definition
|
|
Term
|
Definition
non-nucleoside reverse transcritpate inhibitors
do not require phosphorylation to be active inhibitors
directly inhibit reverse transcriptase to stop HIV replication
bind to a site different than that of NRTI's and thus do not compete with nucleotides for binding to the reverse transcriptase
net effect is the blockade of both reverse transcriptase and DNA-dep DNA polymerase |
|
|
Term
|
Definition
neviraphine
delavirdine
efavirenz |
|
|
Term
|
Definition
Resistance develops quickly with monotherapy b/c all of these drugs have the same MOA
Resistance to one NNRTI means resistance to all NNRTI's
Used with NRTI's b/c they have a different MOA
Many Cyp450 reactions |
|
|
Term
|
Definition
| some cross resistance in this class b/c each of the drugs has a slightly different MOA |
|
|
Term
|
Definition
raltegravir given p.o.
MOA: blockade of viral integrase prevents the insertion of viral DNA into human DNA
used to treat MDR HIV infections |
|
|
Term
|
Definition
| Block viral protease to prevent the cleavage of viral polyproteins into the final stuctural proteins needed for the assembly of the mature virion core required for infectious particles |
|
|
Term
|
Definition
saquinavir
ritonavir
indinavir
nelfinavir
amprenavir
atazanavir
lopinavir+ritonavir |
|
|
Term
| Ritonavir drug interaction |
|
Definition
ritoavir is an inhibitor of CYP2A4 thus giving increased concentrations of lopinavir since this CYP metabolizes saquinavir
thus ritonavir is a pharmacokinetic enhancer |
|
|
Term
|
Definition
palivizumab is a monoclonal antibody directed against a surface proteins of RSV
used for prophylactic therapy in high-risk infants
i.m. once monthly |
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