Anti-Virals Flashcards
Rimantadine
M-2 Inhibitor:
=> Prevents acidification around virion, preventing uncoating.
M-2 is a Viral ion channel.
Virus: Influenza A Only
-Prophylaxis, Treatment
Excretion: Renal
Effects: Nausea, Insomnia, Confusion
Oseltamivir
Neuraminidase Inhibitor:
=> Causes buildup of Viral particles within cell
Neuraminidase is responsible for release of newly formed particles from the host cell.
Virus: Influenza A and B
-Prophylaxis, Treatment
Excretion: Renal
Effects: Nausea
(Zanamavir: Bronchospasm)
Acyclovir
Nucleoside (Antimetabolite) DNA Polymerase Inhibitor
Virus: HSV, VZV
Resistance: Mutated Thymidine Kinase
=> Results in Lack of Phosphorylation
Excretion: Renal
Effects:
1) Oral: Nausea, Vomiting, Headaches
2) IV: Crystal Nephropathy, Renal Failure if Dehydrated
Valacyclovir
Nucleoside (Antimetabolite) DNA Polymerase Inhibitor
HSV, VZV
Prodrug of Acyclovir.
Better GI Absorption (Has an Ester on it)
Ganciclovir
Nucleoside (Antimetabolite) DNA Polymerase Inhibitor
More active vs. CMV
IV only
Effects: Severe Bone Marrow Suppression
Cidofovir
Nucleotide (Antimetabolite) DNA Polymerase Inhibitor
HSV, CMV, Pox viruses
Already Phosphorylated
-Doesn’t need Kinase for activation
Resistance: Mutated DNA Polymerase
Effects: Nausea, Vomiting, Headache, Renal Failure
Ribavirin
Inhibits Nucleic Acid Replication
Hepatitis C, RSV
Interferon Alpha
or Peginterferon Alpha
Immunostimulant. Endogenous protein
Hepatitis C
Better in combo w/ Ribavirin
Effects: -Flu-like illnes -Depression -Bone Marrow Suppression (Anemia, Neutropenia)
Simeprevir
Protease Inhibitor:
-Thus inhibits viral replication
Hepatitis C
Used in combo w/ Ribavirin and w/ Pegylated Interferon
Effects: Photosensitivity, Rash, Nausea
Sofosbuvir
RNA Polymerase NS5B Inhibitor:
=> Incorporates into growing viral RNA chain, terminating the chain.
Hepatitis C
Effects: Fatigue, Headache
Ledipasvir
NS5A Inhibitor:
-Protein involved in Replication, Assembly, and Release from cell
Hepatitis C
Can be combined w/ Sofosbuvir
Zidovudine
Nucleoside (“Nukes”)
Reverse Transcriptase Inhibitor
HIV
Nausea, Vomiting, Hepatotoxic,
Bone Marrow Suppression
Nukes:
-Steatohepatitis, Lactic Acidosis
Lamivudine
Nucleoside (“Nukes”)
Reverse Transcriptase Inhibitor
HIV, Hepatitis B
Minimal Side-Effects.
(If given alone, Resistance in 2 weeks)
Nukes:
-Steatohepatitis, Lactic Acidosis
Emtricitabine
Nucleoside (“Nukes”)
Reverse Transcriptase Inhibitor
HIV
Nukes:
-Steatohepatitis, Lactic Acidosis
Tenofovir
NucleoTide
Reverse Transcriptase Inhibitor
HIV, Hepatitis B
Excretion: Renal
Very well Tolerated.
Renal Toxicity
Efavirenz
Non-Nucleoside (Non-Nuke)
Reverse Transcriptase Inhibitor
HIV
Binds to different part of enzyme (are not antimetabolites)
Excretion: Liver
Effects: Skin Rash, Hepatitis
Darunavir
Protease Inhibitor
HIV
Few Side-Effects
Protease Inhibitors:
- Hyperglycemia, Dyslipidemia,
- Fat Redistribution,
- Drug Interactions
Excretion: Liver
Rinoavir
Protease Inhibitor
HIV
Added only to Boost others by P450 Inhibition
Protease Inhibitors:
- Hyperglycemia, Dyslipidemia,
- Fat Redistribution,
- Drug Interactions
Excretion: Liver
Raltegravir
Integrase Inhibitor
HIV
Very well tolerated
Usually, start w/ 2 Nukes and 1 Integrase Inhibitor.
Fusion Inhibitors
Fusion Inhibitors:
- Bind to Envelope Glycoprotein 41.
- Prevents Fusion of Virion to Host cell and subsequent entry.
HIV
CCR5 Antagonists
CCR5 Antagonists:
- Binds to CCR5 Receptor @ CD4 cells.
- Prevents Entry of virus into cell
