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Flashcards in Pharm antivirals Deck (59)
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1

are antiretrovirals virustatic or virucidal?

virustatic

2

what are the five major classes of antiretroviral medications?

1. nucleoside reverse transcriptase inhibitors (NRTI's) and nucleotide RTI's (tenofovir))
2. non-nucleoside reverse transcriptase inhibitors (NNRTI's)
3. protease inhibitors
4. entry inhibitors
5. integrase inhibitors

3

what are the NRTI's?

zidovudine, lemivudine, emtricitabine, abacavir, tenofovir

4

what is the mechanism of NRTI's?

viral DNA chain termination via inhibition of viral reverse transcriptase. Tenofovir is a nucleoTide, the others are nucleosides and need to be phosphorylated to be active

5

what does zidovudine mimic? lemivudine? emtricitabine? abacavir? tenofovir?

zidovudine = thymidine.
lemivudine = cytosine.
emtricitabine = cytosine.
abacavir = guanine.
tenofovir = adenosine.

6

which NRTIs can also be used for HBV?

lamivudine, emtricitabine, tenofovir

7

zidovudine side effects

granulocytopenia, anemia, nausea, vomiting

8

lamivudine and emtricitabine side effects

headache, nausea, vomiting, rash, neutropenia, pancreatitis (NOT SERIOUS)

9

abacavir side effects

hypersensitivity reaction - associated with HLA-B5701 mutation

10

tenofovir side effects

nephrotoxicity

11

what are the NNRTI's?

efavirenz, nevirapine, rilpivirine, etravirine

12

NNRTI's mechanism

inhibit reverse transcriptase through direct enzyme inhibition (do not require phosphorylation to be active) - NONCOMPETITIVE!

13

what are NNRTI's and NRTI's used to treat?

HIV

14

NNRTIs side effects

rash and hepatotoxicity - efavirenz also has vivid dreams and CNS symptoms (stop when ax wielding elves appear in dream!), teratogenic, P450 metabolism

15

what are the HIV protease inhibitors?

-navir (NA VIRUS! NO NEW VIRUS!)
ritonavir, fosamprenavir, atazanavir, darunavir, lopinavir

16

HIV protease inhibitors (-navir) mechanism

prevent cleavage of protein chain into functional subunits

17

which HIV protease inhibitor has "good" drug interactions? how?

ritonavir "boosts" other drug concentrations by inhibiting cytochrome P-450

18

HIV protease inhibitors (-navir) side effects

GI intolerance (n/v, diarrhea), metabolic toxicities!! (dyslipidemia, hyperglycemia, lipodystrophy)

19

what are the 3 steps of HIV attachment and fusion?

1. HIV gp120 binds CD4 molecule
2. conformational change occurs in gp120 and then binds the coreceptor CCR5 or CXCR4
3. further conformational changes in gp120 expose gp41 protein which mediates fusion of the viral and cell membranes

20

what are the HIV entry inhibitors?

enfuvitide and maraviroc

21

enfuvirtide mechanism

binds gp41, inhibiting viral entry

22

enfuvirtide side effects

skin reaction at injection sites

23

maraviroc mechanism

binds CCR-5 on surface of Tcells/monocytes, inhibiting interaction with gp120 - TARGET IS ON HOST CELL!

24

maraviroc side effects

hepatotoxicity (rare) - cough, fever, URI, rash, musculoskeletal symptoms, ab pain, dizziness

25

what are the integrase inhibitors?

-tegravir (GRAB the HIV before it integrates!)
raltegravir, elvitegravir, dolutegravir

26

integrase inhibitors mechanism

inhibits HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase

27

integrase inhibitors (-tegravir) side effects

myopathy and rhabdo - headache, neausea, diarrhea, pyrexia

28

what are the common HAART regimen combinations?

3 active agents together; typically 2 NRTIs + integrase inhibitor, PI, or NNRTI

29

what is commonly prescribed as initial therapy in HIV? disadvantage of this class?

NNRTI based regimen because of advantage of lower pill burden (preserve PI for later use). disadvantage is only one single mutation is needed to confer resistance and cross resistance develops for entire class

30

what is the preferred NNRTI? exception?

efavirenz - exception pregnancy