Antivirals

Question 1

• Oseltamivir
• Zanamivir

Answer 1

Question 2

• Acyclovir
• Famciclovir
• Valacyclovir

Answer 2

Question 3

Ganciclovir

Answer 3

Question 4

Foscarnet

Answer 4

Question 5

Cidofovir

Answer 5

Question 6

NRTIs (mechanism)

Nucleoside Reverse Transcriptase Inhibitors.

Answer 6

Question 7

NRTIs (clinical)

Nucleoside Reverse Transcriptase Inhibitors.

Answer 7

Question 8

Integrase Inhibitors

The Tegravirs.

Answer 8

Question 9

Protease Inhibitors (mechanism)

Answer 9

Question 10

Protease Inhibitors (clinical use)

Answer 10

Question 11

NS5A Inhibitors

Answer 11

Question 12

NS5B Inhibitors

Answer 12

Question 13

NS3/4A Inhibitors

Answer 13

Question 14

Oseltamivir is structurally and analog of what?

Answer 14

Sialic acid analogs.

Question 15

Off-target adverse effect of Ganciclovir?

Answer 15

• Bone marrow supression
• Nephrotoxicity

Question 16

Most likely reason for resistance to Acyclovir (HSV/VZV) and Ganciclovir (CMV):

Answer 16

• Resistance to viral thymidine kinase (acyclovir)
• Resistance to CMV kinase (ganciclovir)

Question 17

Foscarnet’s 3 actions & structure:

Answer 17

Pyrophosphate analog

Inhibits:
1. viral DNA polymerase
2. viral RNA polymerase
3. HIV reverse transcriptase

Question 17

Acyclovir’s action & structure?

Answer 17

Guanosine analog.

Inhibits
* Viral DNA Polymerase

Question 18

Cidofovir’s action & structure:

Answer 18

Cytidine monophsophate analog.

Inhibits:
* Cellular kinases (NOT viral kinases)

Question 19

NRTI drug names

Answer 19

1. Abacavir
2. Zidovudine
3. Emtricitabine
4. Lamivudine
5. Dianosine
6. Stavudine
7. Tenofovir

Question 20

What’s special about the NRTI Tenofovir?

Answer 20

It doesn’t require phosphorylation because it already comes in a nucleotide form.

Question 21

Distinguishing Didanosine from the other 6 NRTIs?

Answer 21

Pancreatitis.

Question 22

Distinguishing Zidovudine from the other 6 NRTIs?

Answer 22

Bone marrow suppression & anemia.

• Can be reversed with G-CSF and EPO

Question 23

Distinguishing Abacavir from the other 6 NRTIs?

Answer 23

Hypersensitivity (Type 4) with HLA B57:01 allele

Question 24

**NNRTI**s (mechanism)

Answer 24

Question 25

**NNRTI**s (clinical)

Answer 25

Question 26

How do NRTIs work?

Answer 26

They are **competitive inhibitors** of **Reverse Transcriptase**. * Nuceloside analogs that pretend to be DNA building blocks * Fit into the enzyme's active site

Question 27

How do **NNRTIs** work?

Answer 27

They bind Reverse Transcriptase at a location different from the active site (where NRTIs bind).

Question 28

**NNRTI** drug names

Answer 28

1. **Efavirenz** 2. **Nevirapine** 3. Delavirdine

Question 29

**Efavirenz** (NNRTI) has what interesting side effect?

Answer 29

**Vivid dreams**.

Question 30

**HAART** regimen.

Answer 30

Usually **3 drugs** * 2 NRTIs * Integrase or Protein Inhibitor

Question 31

Distinguishing **Integrase Inhibitors** from the other antiviral therapies?

Answer 31

**Myositis** in patients * Increase in **creatine kinase** on bloodwork Also, it is actively against both HIV-1 & HIV-2.

Question 32

**Protease** Inhibitor drug names

Answer 32

1. Atazanavir 2. Darunavir 3. Indinavir 4. Lopinavir 5. Ritonavir 6. Saquinavir 7. Fosamprenavir

Question 33

**Entry Inhibitors** * Enfuvirtide ## Footnote **Antiviral peptide** that **targets viral fusion**.

Answer 33

Question 34

**Entry Inhibitors** * Maraviroc ## Footnote **Antiviral peptide** that **targets viral fusion**.

Answer 34

Question 35

**Indinavir** (protease inhibitor) is known to cause what **specific adverse** effects?

Answer 35

1. Renal Toxicity 2. Thrombocytopenia

Question 36

**Adverse** profile for the **Protease Inhibitor** class:

Answer 36

1. **Hyperglycemia** -- can cause **diabetes** 2. **GI Upset** 3. **Cushing-like syndrome** (CYP-450 enzymes) * **Avoid use of rifampin **(TB drug) due to CYP450 induction

Question 37

**Ritonavir** (protease inhibitor) is known to cause what **specific adverse** effect?

Answer 37

**Inhibits CYP-450** enzymes * May be used to **"boost"** the concentration of **other** drugs metabolized by the liver.

Question 38

**CCR-5** is present on which cells?

Answer 38

Monocytes and **macrophages**

Question 39

For which virus are **NS5A, NS5B, & NS3/4A Inhibitors** prescribed?

Answer 39

**Hepatitis C** virus. **NS5A Inhibitors** * Ledipasvir * Ombitasvir * Velpatasvir **NS5B Inhibitors** * Sofosbuvir * Dasabuvir **NS3/4A Inhibitors** * Grazoprevir * Simeprevir

Question 40

What exactly do **NS5B Inhibitors** target to inhibit viral replication?

Answer 40

Inhibition of viral **RNA-dependent RNA polymerase**.

Question 41

What exactly do **NS5A Inhibitors** target to inhibit viral replication?

Answer 41

Inhibition of **viral** **phosphoprotein (NS5A)**.

Question 42

What exactly do **NS3/4A Inhibitors** target to inhibit viral replication?

Answer 42

**NS3/4A**, a viral protease.