Antivirals

Question 1

4 targets for antivirals in HIV drugs

Answer 1

entry, reverse transcriptase, integrase, protease

Question 2

mechanism of action for NRTI’s

Answer 2

viral DNA chain termination via inhibition of reverse transcriptase enzyme. pose as pieces of DNA and get picked up and stop the enzyme!

Question 3

NRTI class side effects

Answer 3

lactic acidosis (much less common with newer agents). GI side effects.

Question 4

NRTI agents

Answer 4

zidovudine, stavudine, didanosine, tenofovir, abacavir, zalcitabine, lamivudine, emtricitabine

Question 5

NNRTI mechanism of action

Answer 5

bind directly to reverse transcriptase and inhibit its actions

Question 6

NNRTI agents

Answer 6

efavirenz, nevirapine, etravirine, rilpivirine

Question 7

NNRTI side effects

Answer 7

cause a rash. may cause CNS effects like vivid dreams, drowsiness.

Question 8

protease inhibitor agents

Answer 8

norvir, lexiva, kaletra, reyataz, prezista

Question 9

protease inhibitor mechanism of action

Answer 9

bind within active pocket of protease, inhibiting binding of the virus. without protease cleavage, virus cannot cause infection!

Question 10

what is curious about ritonavir?

Answer 10

ritonavir at low doses enhances blood levels of other protease inhibitors! give together to increase clinical effectiveness and require less doses of other drugs!

Question 11

protease inhibitor class toxicities

Answer 11

GI: N/V, diarrhea
Metabolic: dyslipidemia, hyperglycemia, lipodystrophy

Question 12

enfuvirtide mechanism of action

Answer 12

messes with GP41, which makes the connection for CD4 binding. messes with HIV attachment and fusing

Question 13

enfuvirtide adverse effects

Answer 13

local injection sight reaction. increased rate of bacterial pneumonia. hypersensitivity.

Question 14

CCR5 antagonists

Answer 14

HIV often uses CCR5 as a co-receptor necessary to enter T cells. Maraviroc is only agent. Only drug that acts on the host cell, all others act on HIV molecules.

Question 15

CCR5 adverse effects

Answer 15

hepatotoxicity. cough, fever, URI, rash, musculoskeletal, ab pain, dizziness

Question 16

integrase inhibitor agents

Answer 16

raltegravir, elvitegravir, dolutegravir.

Question 17

integrase inhibitor mechanism of action

Answer 17

inhibit viral enzyme integrase. necessary for insertion of viral DNA into human genomic DNA

Question 18

integrase inhibitor adverse effects

Answer 18

generally few adverse effects. commonly seen: Nausea, headache, diarrhea, pyrexia. myopathy seen sometimes

Question 19

basics of HAART

Answer 19

use at least 3 active agents representative of 2 classes of agents

Question 20

goals of HAART

Answer 20

suppress viral load, restore immune function, improve quality of life, reduce HIV related morbidity and mortality, minimize risk for antiretroviral resistance

Question 21

NS5B polymerase inhibitors agents

Answer 21

sofosbuvir, paritaprevir

Question 22

NS5B polymerase inhibitors mechanism of action

Answer 22

inhibitor of Hep C NS5B RNA dependent RNA polymerase. competes with natural viral nucleotides to cause chain termination

Question 23

NS5A inhibitor agents

Answer 23

ledipasvir, daclatasvir, ombitasvir

Question 24

NS5A inhibitor mechanism of action

Answer 24

inhibits hep C NS5A, a viral phosphoprotein required for viral replication.

Question 25

NS3/4A protease inhibitor agents

Answer 25

simeprevir, boceprevir, telaprevir

Question 26

NS3/4A protease inhibitor mechanism of action

Answer 26

prevent viral maturation through the inhibition of protein synthesis

Question 27

acyclovir mechanism of action

Answer 27

after phosphorylation by cellular enzymes, acyclovir triphosphate competes with DNA analogues to cause viral DNA chain termination. needs viral thymidine kinase to become active

Question 28

other drugs like acyclovir

Answer 28

valacyclovir, peniciclovir, famciclovir

Question 29

acyclovir toxicity concerns

Answer 29

CNS: malaise, headache, confusion. N/V, diarrhea. renal dysfunction seen in high doses of IV therapy due to drug crystallizing in kidneys

Question 30

ganciclovir

Answer 30

active mainly against Cytomegalovirus. (CMV). Use the prodrug when you need to give orally, as the actual drug has bad bioavailability. biggest side effect is myelosuppression

Question 31

foscarnet

Answer 31

inhibitory effect on herpesvirus and HIV. directly inhibits herpesvirus DNA polymerase or HIV reverse transcriptase.

Question 32

foscarnet tox issues

Answer 32

nephrotox, electrolyte/metabolic abnormalities, CNS side effects, myelosuppression. only used when people have resistance to other herpes drugs

Question 33

neuraminidase inhibitors

Answer 33

oseltamivir, zanamivir, peramivir. inhibit enzyme critical in penetration of respiratory tract mucus and in the release of virus from infected cells. active against flu A and B

Question 34

neuraminidase inhibitor adverse effects

Answer 34

N/V, diarrhea. neuropsychiatric events reported. zanamavir can cause bronchospasm. peramivir is used only in critically ill