Antivirals Flashcards Preview

MS2 Unit 6 Pharm > Antivirals > Flashcards

Flashcards in Antivirals Deck (34):
1

4 targets for antivirals in HIV drugs

entry, reverse transcriptase, integrase, protease

2

mechanism of action for NRTI's

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

3

NRTI class side effects

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

4

NRTI agents

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

5

NNRTI mechanism of action

bind directly to reverse transcriptase and inhibit its actions

6

NNRTI agents

efavirenz, nevirapine, etravirine, rilpivirine

7

NNRTI side effects

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

8

protease inhibitor agents

norvir, lexiva, kaletra, reyataz, prezista

9

protease inhibitor mechanism of action

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

10

what is curious about ritonavir?

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

11

protease inhibitor class toxicities

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

12

enfuvirtide mechanism of action

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

13

enfuvirtide adverse effects

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

14

CCR5 antagonists

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.

15

CCR5 adverse effects

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

16

integrase inhibitor agents

raltegravir, elvitegravir, dolutegravir.

17

integrase inhibitor mechanism of action

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

18

integrase inhibitor adverse effects

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

19

basics of HAART

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

20

goals of HAART

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

21

NS5B polymerase inhibitors agents

sofosbuvir, paritaprevir

22

NS5B polymerase inhibitors mechanism of action

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

23

NS5A inhibitor agents

ledipasvir, daclatasvir, ombitasvir

24

NS5A inhibitor mechanism of action

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

25

NS3/4A protease inhibitor agents

simeprevir, boceprevir, telaprevir

26

NS3/4A protease inhibitor mechanism of action

prevent viral maturation through the inhibition of protein synthesis

27

acyclovir mechanism of action

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

28

other drugs like acyclovir

valacyclovir, peniciclovir, famciclovir

29

acyclovir toxicity concerns

CNS: malaise, headache, confusion.

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

30

ganciclovir

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

31

foscarnet

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

32

foscarnet tox issues

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

33

neuraminidase inhibitors

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

34

neuraminidase inhibitor adverse effects

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