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3.15 Antivirals I
by Dr. Hill
97
Pharmacology
Professional
03/15/2012

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Term
Which antivirals act as ion channel blockers to prevent viral uncoating?
Definition
amantidadine and rimantadine
Term
What does IDU stand for?
Definition
5-iodo-2-deoxyuridine
Term
What reaction does thymidine kinase catalyze?
Definition
Tdr -> TMP (IdUrd -> IdUMP)
Term
What reaction does thymidylate kinase catalyze?
Definition
TMP-> TDP ->TTP
IdUMP-> IdUDP -> IdUTP
Term
What is the structure of IDU?
Definition
pyrimidine analog of thymidine where teh 5' base carbon is substituted with iodine
Term
What is the mechanism of IDU?
Definition
IDU triphosphate becomes incorporated into the viral genome inhibiting replication
Term
What was the first antiviral?
Definition
IDU
Term
What is IDU used for?
Definition
antiherpetic used for HSV keratitis
Term
How is IDU administered?
Definition
topical only
Term
What enzyme is required for use of IDU?
Definition
TdR kinase
Term
T/F Resistance develops against IDU.
Definition
true
Term
What does TFT stand for?
Definition
trifluidine, or 5-triflouro-methyl-2'-deoxyuridine
Term
What is the structure of trifluidine?
Definition
pyrimidine analog of thymidine with three flourides added to the 5' carbon
Term
What is the MOA of TFT?
Definition
incorporatesinto teh viral DNA causing faulty translation of viral DNA and faulty transcription of mRNA leading to biosynthesis of abnormal proteins
Term
Is TFT the drug of choice for epithelial HSV keratitis?
Definition
no, it used to be but is no longer the DOC
Term
What is TFT used for?
Definition
antiherpetic= HSV keratitis
Term
How is trifluidine administered?
Definition
topically
Term
T/F There is drug resistance against trifluidine (TFT).
Definition
false; almost NO drug resistance
Term
What enzyme is required for TFT to be effective?
Definition
TdR kinase
Term
What are the side effects of TFT?
Definition
some ocular toxicity
Term
What is the molecular structure of Ara-A?
Definition
deoxyadenosine analog; purine analogue with abnormal sugar
Term
What is the full name for Ara-A?
Definition
adenine arabinose
Term
What enzymes are necessary for Ara-A?
Definition
cellular enzymes to add a triphosphate; DOES NOT REQUIRE THYMIDINE KINASE
Term
What is Ara-A used for?
Definition
antiherpetic (encephalitis, systemic infection)
Term
What was the first IV antiviral?
Definition
Ara-A
Term
What is the mechanism of Ara-A?
Definition
DNA chain terminator
Term
T/F Ara-A has limited solubility.
Definition
true
Term
Which drug is the "penicillin of antivirals"?
Definition
acycloguanosine
Term
What does ACV stand for?
Definition
acycloguanosine
Term
What is the structure of ACV?
Definition
purine analog of deoxyguanosine with an incomplete sugar ring (acyclic carbohydrate moiety)
Term
What is the MOA of ACV?
Definition
viral TK phosphorylates ACV to acycloguanosine monophosphate. Cellular enzymes phosphorylate the monophosphate into acycloguanosine triphosphate. Acycloguanosine triphosphate incorporates into the viral DNA which terminates the chain and viral DNA polymerase is inactivated
Term
How does acycloguanosine specifically target cells with the virus?
Definition
it needs to be phosphorylated by viral thymidine kinase which is only present in infected cells
Term
T/F Most all human cells have a thymidine kinase.
Definition
true
Term
T/F Most viral infections result in teh production of a viral thymidine kinase?
Definition
true
Term
What is acycloguanosine used for?
Definition
antiherpetic
Term
What was the first oral antiviral?
Definition
acycloguanosine
Term
What enzyme is required for ACG?
Definition
TdR kinase
Term
T/F Resistance develops against ACG.
Definition
true
Term
What is the structure of ganciclovir?
Definition
purine analog of deoxyguanosine structurally similar to ACV; has an additional carbon and a hydroxyl group on the acyclic side chain
Term
What is the drug name for DHPG?
Definition
ganciclovir
Term
What is the MOA of DHPG?
Definition
phorylated to a monophosphate by a viral thymidine kinase, cellular enzymes phophorylate to the triphosphate form, inhibits binding of doxyguanosine triphosphate to the DNA polymerase terminating DNA elongation
Term
What is the use of DHPG therapy?
Definition
antiherpetic and CMV retinitis in immunocompromised patients
Term
What is zirgan?
Definition
.15% ganciclovir gel
Term
What is .15% ganciclovir gel used for? How is it administered?
Definition
antiherpetic= treatment of HSV keratitis. Topically oly
Term
What is the name for PVC?
Definition
penciclovir
Term
What is the use of penciclovir?
Definition
antiherpetic (fever blisters),
Term
How is penciclovir administered?
Definition
topically only
Term
How is PCV different from ACV?
Definition
greater stability (longer half life) and higher affinity for viral thymidine kinase
Term
What is famciclovir used for?
Definition
antiherpetic (genital herpes and VZV infections), hepatitis B adjuvent
Term
What is the name for FCV?
Definition
famciclovir
Term
How is famciclovir administered?
Definition
orally
Term
What is the structure of famciclovir?
Definition
pro-drug of penciclovir where sugar alcohols are acetylated
Term
What is the advantage to giving famciclovir over penciclovir?
Definition
famciclovir has increased bioavailability
Term
What is the oral prodrug of acycloguanosine?
Definition
valacyclovir
Term
How is valacyclovir administered?
Definition
orally
Term
What is the advantage to giving VACV over ACV?
Definition
increased bioavailability and reduced dosing
Term
What is the structure of valacyclovir?
Definition
L-valine added to acycloguanosine
Term
What is the MOA of valacyclovir?
Definition
chain terminator
Term
What is valacyclovir used to treat?
Definition
anti-herpetic (treats genital HSV and VZV)
Term
What is valganciclovir used for?
Definition
anti-herpetic (primarily CMV) can be used for CMV retinitis and prophylactically in transplant patients
Term
What is the structure of valganciclovir?
Definition
purine nucleoside with an abnormal sugar; L-valyl ester of DHPG
Term
What is the full name for VDHPG?
Definition
valgancyclovir
Term
What is the name for MIQ?
Definition
imiquimod
Term
What is the structure of imiquimod?
Definition
not a protein or nucleoside or nucleotide. It is an imidazoquinoline
Term
What is the MOA of imiquimod?
Definition
activates the immune system (immunoenhancer)
Term
How is imiquimod administered?
Definition
topically as a cream
Term
What is imiquimod used for?
Definition
adjuvant therapy for HSV-2 genital lesions; adjuvant therapy for HPV warts
Term
What is the name for DOL?
Definition
docosanol
Term
What is docosanol used for?
Definition
antiherpetic (liquid enveloped viruses) broad spectrum against HSV-1, -2, HHV-6, RSV, HIV, Influenza A
Term
How is docosanol administered?
Definition
topically only (1% cream)
Term
What is the structure of docosanol?
Definition
behenyl alcohol (22-carbon saturated fatty alcohol)
Term
What is the mechanism of action of docosanol?
Definition
highly lipophilic and inhibits viral entry of lipid-enveloped viruses
Term
What is ribavirin used for?
Definition
influenza, hepatitis C adjuvant (braod-spectrum antiviral)
Term
What is the structure of ribavirin?
Definition
guanosine (purine) analog
Term
How is ribavirin administered?
Definition
aerosol generator
Term
What is the MOA of ribavirin?
Definition
interferese with GMP formation; exact MOA not known
Term
List the nucleoside analogs that are pyrimidines?
Definition
IdU, TFT, AZT, ddC, 3TC, d4T
Term
List the nucleoside analogs that are purines?
Definition
Ara-A, ACG, DHPG, penciclovir, famciclovir, valacyclovir, ddI, ABV, ribavirin
Term
What is the structure of amantadine and rimantidine?
Definition
tricyclic amines
Term
How are amantadine and rimantadine administered?
Definition
orally
Term
What are rimantadine and amantadine used for?
Definition
prophylactically against influenza A
Term
What is the MOA of amantadine and rimantadine?
Definition
inhibits viral uncoating by blocking ion channels
Term
What type of molecule is interferon?
Definition
glycoprotein
Term
How is interferon produced?
Definition
recombinant DNA technology
Term
What viral diseases is interferon used to treat?
Definition
genital papillomas and hepatitis C in combination with other antivirals
Term
What is the structure of zanamivir?
Definition
non-nucleoside antiviral
Term
How is zanamivir administered?
Definition
inhalation
Term
What viruses is zanamivir used for?
Definition
influenza A and B
Term
What is the MOA of zanamivir?
Definition
viral neuraminidase
Term
What is the structure of oseltamivir?
Definition
non-nucleoside antiviral
Term
How is oseltamivir administered?
Definition
orally (tablet)
Term
What viruses is oseltamivir effective against?
Definition
influenza A and B
Term
What is the MOA of oseltamivir?
Definition
inhibits viral neuraminidase
Term
What is the structure of foscarnet?
Definition
non-nucleoside antiviral
Term
What is the MOA of foscarnet?
Definition
inhibits viral DNA polymerase
Term
How is foscarnet administered?
Definition
IV or directly to the retina
Term
What virus is foscarnet used to treat?
Definition
CMV retinitis
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