Didanosine
Nucleoside Reverse Transcriptase Inhibitor (NRTI) - Adenosine
Tenofovir
Nucleotide Reverse Transcriptase Inhibitor (has a P step already completed) - Adenosine
Zidovudine
Nucleoside Reverse Transcriptase Inhibitor (NRTI) - Thymidine
Stavudine
Nucleoside Reverse Transcriptase Inhibitor (NRTI) - Thymidine
Zalcitabine
Nucleoside Reverse Transcriptase Inhibitor (NRTI) - Cytosine
Lamivudine
Nucleoside Reverse Transcriptase Inhibitor (NRTI) - Cytosine
Emtricitabine
Nucleoside Reverse Transcriptase Inhibitor (NRTI) - Cytosine
Nucleoside Reverse Transcriptase Inhibitor (NRTI) MOA
Viral DNA chain termination via inhibition of RT enzyme (DNA analogs)
Resistance to Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
Reverse transcriptase has a mutation so analog can’t bind
Nucleoside Reverse Transcriptase Inhibitor (NRTI) general side effects
Lactic acidosis, GI issues
Tenofovir (NRTI) side effect
Nephrotoxicity
Zidovudine (NRTI) side effect
Hematotoxicity - macrocytic anemia
Lamivudine/Emtricitabine (NRTIs) side effects
FEW!!!
Zalcitabine (NRTI) side effect
peripheral neuropathy
Abacavir
Nucleoside Reverse Transcriptase Inhibitor (NRTI) - Guanine
Abacavir (NRTI) side effect
HS rxn (HLA association)
Efavirenz
Non-Nucleoside RT Inhibitors (NNRTIs)
Nevirapine
Non-Nucleoside RT Inhibitors (NNRTIs)
Rilpivirine
Non-Nucleoside RT Inhibitors (NNRTIs)
Etravirine
Non-Nucleoside RT Inhibitors (NNRTIs)
Efavirenz (NNRTI) side effect
CNS symptoms (vivid dreams), teratogenic
Nevirapine (NNRTI) side effect
Rash, hepatitis, hepatic necrosis, induces p450
Rilpivirine (NNRTI) side effect
Rash, QT prolongation
Etravirine (NNRTI) side effect
Rash, increased LFTs
Ritonavir
Protease inhibitor
Fosamprenavir
Protease inhibitor
Lopinavir/Ritonavir
Ritonavir at low doses boosts levels of other PIs when given together (P4503A4 inhibition in liver/gut)
Atazanavir
Protease inhibitor
Darunavir
Protease inhibitor
Non-Nucleoside RT Inhibitors (NNRTIs) MOA
bind directly to RT adn inhibit its action
Protease Inhibitor MOA
PI binds to active pocket within viral protease, inhibits binding of virus –> no protease cleavage = virus cannot cause infection
Protease Inhibitor side effects
N/V/D
Metabolic syndrome: dyslipidemia, hyperglycemia, lipodystrophy
Maraviroc
CCR5 antagonist (entry inhibitor)
Enfuvirtide
Prevents fusion of gp41 to CD4+ (entry inhibitor)
Raltegravir
Integrase inhibitor
Elvitegravir
Integrase inhibitors
Dolutegravir
Integrase inhibitors
Interferon
Used for HCV - establishes antiviral state within cells
Ribavirin
Nucleoside analog (chain termination) for HCV - hematotoxic, teratogenic
Sofosbuvir
Competes with virus nucleotide (uridine), causes chain termination of HCV RNA - relatively safe!!
Ledipasvir
Inhibits HCV NS5A - viral phosphorotein needed for viral replication
Simeprevir, Telaprevir, Boceprevir
NS3/4A Protease inhibitors (anemia, rash, itchy, GI)
Acyclovir
Requires phosphorylation through viral TK - copetes iwth DNA analogues to cause viral chain termination
Acyclovir’s analogs
Valacyclovir, Peniciclovir, Famciclovir
Acyclovir+family side effects
CNS malaise/confusion, N/V/D, renal dysfunction at high doses due to crystallization (but no bone marrow suppression because the viral TK is what phosphorylates it!! only touches viral infected cells!!)
Ganciclovir
Requires phosphorylation through UL97 phosphotransferase, found in ANY cell, not just viral
Acyclovir uses
HSV1 and 2, VZV
Ganciclovir uses
HSV1, 2, VZV, but really for CMV!!!!!!!
Ganciclovir side effects
myelosuppression (neutropenia) - CNS toxicity, hepatotoxicity, GI intolerance (can get phosphorylated in any cell!)
Foscarnet
Directly inhibits herpers DNA polymerases or HIV RTs
Why is Foscarnet good for acyclovir resistant viruses?
Does not use TK
Foscarnet side effects
Nephrotoxicity (ATN), Electrolyte problems, CNS side effects, hypocalcemia, myelosuppresion
Oseltamivir (tamiflu), Zanamivir (Relenza)
Inhibit neuraminidase so virus can’t be released from infected cells