Anti Flashcards
Acyclovir
Mechanism:
Structural analog of deoxyguanosine
viral DNA polymerase adds and causes chain termination
resistance:
Mutations in TK or viral polymerase
Toxicity: Well tolerated
Use:
HCV
VZV
Oral bioav.
Valacyclovir has higher bioavailability
Foscarnet
Mechanism:
Binds to pyrophosphate site of viral polymerase
x100 viral > human
Resistance:
mutation in polymerase
Toxicity:
Hepatoxicity, but reversible
hypocalcemia/CNS toxic
Use:
HSV/CMV that is acyclovir resistant
Tenofovir
Mechanism:
nucleoside/nucleotide reverse transcriptase (RT) inhibitor (NRTI)
competes with dATP and causes chain termination
Resistance:
mutation in RT
Toxicity:
Hepatotoxicity
Use
1st line of defense for HIV
often used with efavirenz
HBV
orally active, penetrates CNS
Efavirenz
Mechanism:
Non-nucleoside reverse transcriptase inhibitor NNRTI
does not bind to active site like NRTI (non-competitive)
Resistance:
mutations to RTase
Toxicity:
CNS effects such as insomnia, confusion, and depression
Use
1st line of defense of HIV
used with tenofovir
orally active
Darunavir, Ritonavir
Mechanism:
HIV-1 protease inhibitor
prevent processing precursor polyproteins into final structure proteins into virions
Resistance:
pol gene mutations
pol gene encodes protease
Toxicity:
GI effects
long term use effects carb and lipid metabolism
Use
Combined with HIV RTase
orally active
*Ritonavir –> inhibits CyP3A4 which boosts HIV and HCV protease inhibitors
Raltegravir
Mechanism:
inhibits viral DNA from integrating into host DNA
Resistance:
mutations to integrase
Toxicity:
well tolerated
Use
in combination to other 1st line HIV drugs
orally active
Maraviroc
Mechanism:
CCR5 coreceptor on CD4/macrophage
prevents binding of gp120 to allow HIV viral entry
Resistance:
mutation of CCR5 receptor
Toxicity:
well tolerated, but can cause CNS effects
Use
after 1st line of HIV viral drugs fail,
*CXCRY coreceptor is not inhibited
orally active
Enfuvirtide
Mechanism:
binds to gp41 of viral envelope preventing fusion of viral and cellular envelope
Resistance:
mutation of gp41
Toxicity:
injection site symptoms
Use
alternative treatment multiviral resistance (HIV)
injection
interferon
Mechanism:
act through Jak/Stat pathway affecting gene transcription and cell signaling
Resistance:
Toxicity:
fever, fatigue, marrow suppression, depression, flu-like symptoms
Use
HPV, Hep B/C, HSV III, treatment for all alien viruses
Sofosbuvir
Mechanism:
HCV NS5B RNA-dependent polymerase inhibitor
Use
very expensive
used in combo with ledipasvir
HCV
Ledipasvir
Mechanism:
interferes with NS5A protein needed for viral replication in HCV
Use
very expensive
used in combination of sofosbuvir
HCV
Paritaprevir
Mechanism:
Hep C protease inhibitor
Use
ritonavir boosts this PI effectiveness
Oseltamivir
Mechanism:
inhibit viral neuraminidase to prevent release of infections particles
Resistance:
mutations to neuraminidase
Use
reduce duration of flu especially if used 24 hours of onset,
prophylactic treatment