Anti-Virals

Question 1

Rimantadine

Answer 1

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

Question 2

Oseltamivir

Answer 2

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)

Question 3

Acyclovir

Answer 3

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

Question 4

Valacyclovir

Answer 4

Nucleoside (Antimetabolite) DNA Polymerase Inhibitor

HSV, VZV

Prodrug of Acyclovir.
Better GI Absorption (Has an Ester on it)

Question 5

Ganciclovir

Answer 5

Nucleoside (Antimetabolite) DNA Polymerase Inhibitor

More active vs. CMV

IV only

Effects: Severe Bone Marrow Suppression

Question 6

Cidofovir

Answer 6

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

Question 7

Ribavirin

Answer 7

Inhibits Nucleic Acid Replication

Hepatitis C, RSV

Question 8

Interferon Alpha

or Peginterferon Alpha

Answer 8

Immunostimulant. Endogenous protein

Hepatitis C

Better in combo w/ Ribavirin

Effects:
-Flu-like illnes
-Depression
-Bone Marrow Suppression 
(Anemia, Neutropenia)

Question 9

Simeprevir

Answer 9

Protease Inhibitor:
-Thus inhibits viral replication

Hepatitis C

Used in combo w/ Ribavirin and w/ Pegylated Interferon

Effects: Photosensitivity, Rash, Nausea

Question 10

Sofosbuvir

Answer 10

RNA Polymerase NS5B Inhibitor:
=> Incorporates into growing viral RNA chain, terminating the chain.

Hepatitis C

Effects: Fatigue, Headache

Question 11

Ledipasvir

Answer 11

NS5A Inhibitor:
-Protein involved in Replication, Assembly, and Release from cell

Hepatitis C

Can be combined w/ Sofosbuvir

Question 12

Zidovudine

Answer 12

Nucleoside (“Nukes”)
Reverse Transcriptase Inhibitor

HIV

Nausea, Vomiting, Hepatotoxic,
Bone Marrow Suppression

Nukes:
-Steatohepatitis, Lactic Acidosis

Question 13

Lamivudine

Answer 13

Nucleoside (“Nukes”)
Reverse Transcriptase Inhibitor

HIV, Hepatitis B

Minimal Side-Effects.
(If given alone, Resistance in 2 weeks)

Nukes:
-Steatohepatitis, Lactic Acidosis

Question 14

Emtricitabine

Answer 14

Nucleoside (“Nukes”)
Reverse Transcriptase Inhibitor

HIV

Nukes:
-Steatohepatitis, Lactic Acidosis

Question 15

Tenofovir

Answer 15

NucleoTide
Reverse Transcriptase Inhibitor

HIV, Hepatitis B

Excretion: Renal

Very well Tolerated.
Renal Toxicity

Question 16

Efavirenz

Answer 16

Non-Nucleoside (Non-Nuke)
Reverse Transcriptase Inhibitor

HIV

Binds to different part of enzyme (are not antimetabolites)

Excretion: Liver

Effects: Skin Rash, Hepatitis

Question 17

Darunavir

Answer 17

Protease Inhibitor

HIV

Few Side-Effects

Protease Inhibitors:

• Hyperglycemia, Dyslipidemia,
• Fat Redistribution,
• Drug Interactions

Excretion: Liver

Question 18

Rinoavir

Answer 18

Protease Inhibitor

HIV

Added only to Boost others by P450 Inhibition

Protease Inhibitors:

• Hyperglycemia, Dyslipidemia,
• Fat Redistribution,
• Drug Interactions

Excretion: Liver

Question 19

Raltegravir

Answer 19

Integrase Inhibitor

HIV

Very well tolerated

Usually, start w/ 2 Nukes and 1 Integrase Inhibitor.

Question 20

Fusion Inhibitors

Answer 20

Fusion Inhibitors:

• Bind to Envelope Glycoprotein 41.
• Prevents Fusion of Virion to Host cell and subsequent entry.

HIV

Question 21

CCR5 Antagonists

Answer 21

CCR5 Antagonists:

• Binds to CCR5 Receptor @ CD4 cells.
• Prevents Entry of virus into cell