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3.14 Antivirals II
By Dr. Hill
108
Pharmacology
Professional
03/15/2012

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Cards

Term
What is HAART?
Definition
highly active anti-retroviral therapy
Term
What is the initial treatment for HIV?
Definition
NRTI + NNRTI + protease inhibitor
Term
What are the reserve treatments given for HIV?
Definition
receptor blocker of HIV entry, fusion inhibitor, integrase inhibitor
Term
What is the structure of AZT?
Definition
pyrimidine nucleoside with abnormal sugar (sugar has three nitrogens)
Term
What does AZT stand for?
Definition
azidothymidine
Term
What is the MOA of azidothymidine?
Definition
chain terminator and inhibits reverse transcriptase
Term
What does ddC stand for?
Definition
dideoxycytidine
Term
What is the structure of dideoxycytidine?
Definition
pyrimidine nucleoside analog (looks like deoxycytidine)
Term
How is ddC administered?
Definition
orally
Term
What is the MOA of ddC?
Definition
inhibits reverse transcriptase and is a chain terminator
Term
T/F Neither AZT nor ddC or ddI have very toxic side effects.
Definition
false, they are all very toxic
Term
What does ddI stand for?
Definition
dideoxyionosine
Term
What is the structure of ddI?
Definition
PURINE nucleoside analog
Term
How is ddI administered?
Definition
orally
Term
What is the MOA of ddI?
Definition
inhibits reverse transcriptase and is a chain terminator
Term
What is the structure of 3TC?
Definition
pyrimidine analog with an abnormal sugar
Term
What is the full name of 3TC?
Definition
lamivudine
Term
Whatis the MOA of 3TC?
Definition
chain terminator
Term
How is 3TC administered?
Definition
orally
Term
What is the toxicity associated with lamivudine (3TC)?
Definition
pancreatitis
Term
What is 3TC used to treat?
Definition
antiretroviral adjuvant and hepatitis B adjuvant
Term
What is the full name for d4T?
Definition
stavudine
Term
What is the structure of d4T (stavudine)?
Definition
pyrimidine analog
Term
What is the MOA of stavudine?
Definition
chain terminator
Term
What is d4T (stavudine) used for?
Definition
antiretroviral adjuvant
Term
What is the administration of d4T?
Definition
oral administration
Term
What is the toxicity associated with d4T (stavudine)?
Definition
peripheral neuropathy
Term
What is the full name of ABV?
Definition
abacavir
Term
What is the use of ABV?
Definition
antiretroviral adjuvant
Term
What is the structure of ABV?
Definition
purine analog
Term
How is ABV administered?
Definition
orally
Term
What is the toxicity associated with ABV?
Definition
mild rash, diarrhea, asthenia
Term
What are the pyrimidine nucleoSIDE analogues?
Definition
IdU, TFT, AZT, ddC, 3TC, d4T
Term
What are the purine nucleoside analogues?
Definition
Ara-A, ACG, ganciclovir, famciclovir, valacyclovir, ribavirin, ddI, ABV
Term
What is the full name for NVP?
Definition
nevirapine
Term
What is the structure of nevirapine (NVP)?
Definition
non-nucleoside analog
Term
What is the use of NVP (nevirapine)?
Definition
anti-retroviral adjuvant
Term
What is the MOA of nevirapine?
Definition
inhibits HIV reverse transcriptase
Term
How is nevirapine administered?
Definition
oral administration
Term
What is the toxicity associated with nevirapine (NVP)?
Definition
severe skin rashes
Term
What is the full name for DMP?
Definition
efavirenz
Term
What is the structure of DMP?
Definition
non-nucleoside
Term
What is the use of efavirenz (DMP)?
Definition
antiretroviral adjuvant
Term
What is the MOA of efavirenz (DMP)?
Definition
inhibits HIV reverse transcriptase
Term
What is the route of administration for efavirenz (DMP)?
Definition
oral
Term
What is the toxicity of DMP (efavirenz)?
Definition
low, some rashes
Term
What is the full name for DLV?
Definition
delavirdine
Term
What is the use of delavirdine (DLV)?
Definition
nonnucleoside antiretroviral adjuvant
Term
What type of compound is delavirdine?
Definition
piperazine compound
Term
How is delavirdine administered?
Definition
orally
Term
What are the toxicities of delavirdine?
Definition
leukopenia, anemia, rash
Term
What is the MOA of protease inhibitors?
Definition
aspartic protease
Term
How effective are protease inhibitors?
Definition
they are poorly absorbed and have low potency and resistance can develop, but they significantly increase longevity
Term
What suffix is common to the protease inhibitors?
Definition
"-navir"
Term
What receptors does HIV use to enter cells?
Definition
CCR5, CXCR4, CCR5 + CXCR4, CD4-R
Term
What is the full name of MAR?
Definition
maraviroc
Term
What is the MOA of maraviroc?
Definition
CCR-5 co-receptor antagonist that inhibits attachment and entry
Term
Maraviroc does not work in which HIV viruses?
Definition
those that are CXCR4-ropic HIV-1 or a dual CXCR4 + CCR5
Term
What is the full name for RAL?
Definition
raltegravir
Term
What is the MOA of raltegravir?
Definition
blocks integration of HVI genome into host genome by inhibiting "integrase"
Term
What is the full name for T-20?
Definition
enfuvirtide
Term
What is the MOA of enfuvirtide (T-20)?
Definition
binds to HIV gp 41; inhibitor of attachment and entry
Term
What is the structure of T-20 (enfuvirtide)?
Definition
peptidomimetic
Term
What makes the combination drug Kaletra more efficient?
Definition
contains lopinavir and ritonavir; ritonavir inhibits teh CYP3A mediated metabolism of lopinavir resulting in increased plasma concentrations of lopinivar
Term
Name the three nucleoTIDE antivirals?
Definition
cidofovir, adefovir, tenofovir
Term
What was the first nucleotide analog?
Definition
cidofovir
Term
what is the use of cidofovir?
Definition
broad spectrum antiviral (antiherpetic, anti-adeno, anti-HPV) ESPECIALLY CMV retinitis
Term
Wat is the structure of cidofovir?
Definition
pyrimidine (cytidine) analog
Term
What is the mechanism of action of cidofovir?
Definition
chain terminator
Term
What is the full name of HPMPC?
Definition
cidofovir
Term
How is cidofovir administered?
Definition
topically and systemically
Term
Is cidofovir activated by a host or a viral enzyme?
Definition
host enzyme
Term
What are the toxicities associated with cidofovir?
Definition
nephrotoxic: must check kidney function bi-weekly
Term
What is the full name of ADV, PMEA?
Definition
adefovir dipivoxil
Term
What is the spectrum of adefovir dipivoxil?
Definition
very broad spectrum (CMV and HIV, and hep B adjuvant)
Term
Is adefovir dipivoxil activated by host or viral enzymes?
Definition
host
Term
What is given with adefovir dipivoxil to reduce toxicity?
Definition
L-carnitine
Term
What is the mechanism of adefovir dipovoxil?
Definition
reverse transcriptase inhibitor and chain terminator
Term
What is the structure of tenofovir?
Definition
nucleotide antiviral
Term
What is the MOA of tenofovir?
Definition
anti-retroviral, inhibitor of HIV reverse transcriptase
Term
What viruses are treated with tenofovir?
Definition
HIV and hepatitis B
Term
What is the major toxicity of tenofovir?
Definition
neutropenia and fatigue
Term
What is fomivirsen used for?
Definition
cytomegalovirus retinitis
Term
What is the structure and MOA of fomivirsen?
Definition
21-mer oligonucleotide sequence is complimentary to the mRNA for the immediate early gene product of huan cytomegalovirus (phosphorothioate backbone)
Term
What is the only antisense antiviral?
Definition
fomivirsen
Term
List the non-systemic antivirals (topical only).
Definition
IDU, TFT, PCV, IMIQ, DOL
Term
What is the mechanism of action of foscarnet?
Definition
inhibits DNA polymerase by acting as a noncompetitive inhibitor at the pyrophosphate binding site on the viral enzyme
Term
What drugs are used to treat CMV retinitis?
Definition
gancyclovir, valganciclovir, foscarnet, formivirsen, cidofovir
Term
What can be used to treat hepatitis B?
Definition
tenofovir, adefovir dipivoxil, lamivudine, entecavir, famciclovir, thymosine alpha 1, interferon alpha 1
Term
What is the structure of entecavir?
Definition
guanosine nucleoside analogue with abnormal sugars
Term
What is the mechanism of action of entecavir?
Definition
chain termination
Term
What does ENT stand for?
Definition
entecavir
Term
What virus is treated with entecavir?
Definition
hepatitis B virus
Term
What is TDF, PMPA stand for?
Definition
tenofovir
Term
What is the structure of tenofovir?
Definition
purine nucleotide analogue with an abnormal sugar
Term
What is the MOA of tenofovir?
Definition
chain terminator and reverse transcriptase inhibitor
Term
What is the full name of TA-1?
Definition
thymosin alpha 1
Term
What is the structure of TA-1 (thymosin alpha 1)?
Definition
28 amino acid polypeptide
Term
What is the MOA of TA-1?
Definition
immuno enhancer
Term
Thymosin alpha 1 is usually used in combination with _______ when treating hepatitis B.
Definition
famciclovir and lamivudine (3TC)
Term
What is the treatment for hepatitis C?
Definition
combinations (ribovirin, IFN-alpha)
Term
List the protein/peptide antivirals.
Definition
interferon alpha, TA-1 (thymosin alpha 1)
Term
Which pyrimidine nucleoside analogs are used to treat HIV?
Definition
azidothymidine, ddC, lamivudine, stavudine
Term
Which purine nucleoside analogs are used to treat HIV?
Definition
ddI
Term
How is ddI unique from the other purine nucleoside analogues?
Definition
used to treat HIV and is a RNA chain terminator
Term
Which non-nucleoside analogues are used to treat HIV?
Definition
nevirapine, efavirenz, delaviriden (hydroxyurea)
Term
Which non-nucleoside analogs inhibit neuraminidase?
Definition
zanamivir, oseltamir
Term
Name the antivirals that are immunomodulators/immunoenhances.
Definition
INF-alpha, TA-1, imiquimod
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