Antivirals

Question 1

Name some antisense (ssRNA) viruses.

Answer 1

Measles, mumps, rabies, influenza

Question 2

Name some sense (ssRNA) viruses.

Answer 2

polioviruses, rhinoviruses, coronaviruses, Hep A

Question 3

Name some dsRNA viruses

Answer 3

reoviruses, several plant viruses

Question 4

Name some retroviruses

Answer 4

HIV-1, HIV-2, HTLV-1, HTLV-2

Question 5

Name a ssDNA virus

Answer 5

parvovirus

Question 6

Name a dsDNA virus

Answer 6

smallpox, varicella-zoster, HSV-1 and HSV-2

Question 7

What time of virus is cytomegalovirus?

Answer 7

dsDNA virus

Question 8

Name some viral DNA polymerase inhibitors.

Answer 8

Nucleoside analogs - aciclovir, valaciclovir, ganciclovir - all of which are pro-drugs

Non-nucleoside analogs - foscarnet, cidofovir

Question 9

Name some viral RNA reverse transcriptase inhibitors.

Answer 9

Nucleoside RT inhibitors - zidovudine, didanosine, zalcitabine, lamivudine - all of which are pro-drugs

Non-nucleoside RT inhibitors - nevirapine, efavirenz

Question 10

Name some viral RNA protease inhibitors.

Answer 10

saquinavir, ritonavir, indinavir

Question 11

How many phosphates must be added to get to the viral DNA polymerase inhibitors to the active site.

Answer 11

3

Question 12

How are viral DNA polymerase inhibitors phosphorylated?

Answer 12

by thymidine kinases

Question 13

Name some side effects of ganciclovir.

Answer 13

Range of haematological adverse effects such as granulocytopenia, neutropenia, anaemia, thrombocytopenia.

Question 14

What is important when taking aciclovir by I.V.?

Answer 14

Large doses may result in crystallization of drug in renal tubules, so hydration is important with high doses

Question 15

What time of oral bioavailability does aciclovir have?

Answer 15

Poor oral bioavailability

Question 16

What type of oral bioavailability does penciclovir have?

Answer 16

poor

Question 17

What is the function of integrase?

Answer 17

Integrase (IN) is a retroviral enzyme that catalyzes the insertion of viral DNA (vDNA) into host chromosomal DNA

Question 18

What is HAART therapy?

Answer 18

Highly active anti-retroviral therapy.
2 nucleoside analogs + protease inhibitor
2 nucleoside analogs + non-nucleoside reverse transcriptase inhibitor

Question 19

Name some viral RNA reverse transcriptase inhibitors (treatment for HIV).

Answer 19

Nucleoside RT inhibitors - zidovudine (requires tri-phosphorylation), didanosine, zalcitabine, lamivudine (all prodrugs)
Nucleotide reverse transcriptase inhibitors - tenofovir (requires di-phosphorylation)
Non-nucleoside RT inhibitors - nevirapine, efavirens (does not require phosphorylation)

Question 20

Name some M2 inhibitors

Answer 20

amantadine, rimantadine

Question 21

Name some neuraminidase inhibitors.

Answer 21

oseltamivir, zanamivir

Question 22

Name a potent inhibitor of CYP3A4.

Answer 22

Ritonavir - used to boost other levels of PIs

Question 23

Name some side effects of ritonavir.

Answer 23

GI disturbances, blood disorders, CNS effects, risk of hyperglycaemia, dyslipidaemia, lipodystrophy, atherosclerosis

Question 24

Name some newer drugs to treat HIV.

Answer 24

Fusion inhibitors - enfuvirtide
Integrase inhibitors - raltegravir
Co-receptor inhibitors - maraviroc (black box warning for hepatotoxicity)

Question 25

Which type of influenza virus does the M2 inhibitors work in.

Answer 25

Influenza A

Question 26

What type of oral bioavailability do M2 inhibitors have?

Answer 26

Good - 90%

Question 27

What type of oral bioavailability do neuraminidase inhibitors have?

Answer 27

Oseltamivir - 80%