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Anti-Infectives Exam 3 > Lecture 4 - Antiviral Agent 3 > Flashcards

Lecture 4 - Antiviral Agent 3 Flashcards

1
Q

Nevirapine ADE

A

Rash = dose titration
Most severe form - Erythema Multiforme

Hepatitis = AVOID in women with higher CD4 counts

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2
Q

Efavirenz ADE

A

CV - Dyslipidemia
Rash
CNS

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3
Q

Etravirine ADE

A

Rash
CNS, less than efavirenz
CV - Dyslipidemia

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4
Q

Rilpivirine ADE

A

Rash
CNS
CV - Dyslipidemia

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5
Q

Doravirine ADE

A

Rash
CNS = much less than Efavirenz, 8.8% vs 37% dizziness, 12.1 vs 25.5% abnormal dreams
** Positive effects on lipids **

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6
Q

NNRTI drugs are strong inducers so they will….

A

reduce lvls of substrate drug

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7
Q

Antidepressants that are less effected by NNRTI

A

Fluoxetine
Fluvoxamine
Paroxetine

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8
Q

Enzyme inducers reduce lvls of NNRTIs are….

A 
Rifampin
Rifabutin
Phenytoin
Phenobarbital
Carbamazepine
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9
Q

Enzyme inhibitors that increase lvls of NNRTIs

A 
Itraconazole
Voriconazole
Fluconazole
Posaconazole
Isavuconazonium
Clarithromycin
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10
Q

Most common NNRTI Resistance Mutations

A

K103N = wipe out 1st gen NNRTI

Y181C

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11
Q

Importnat points about NNRTI resistance

A

Extensive cross-resistance between 1st gen, excludes….
Doravirine
Etravirine
Rilpivirine

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12
Q

Protease inhibitor MOA

A

interfere with viral replication by blocking the protease enzyme involved in the production of structural proteins-results in imperfect non-infectious virus

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13
Q

Protease inhibitors will do what to lvls of substrate drug?

A

increase

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14
Q

Ribavirin should be avoided with

A

didaosine
stavudine
zidovudine

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15
Q

Sofosbuvir should be avoided with

A

tipranavir

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16
Q

Ledipasvir/Sofosbuvir can be used with….

A

Most ARVs

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17
Q

Glecaprevir/Pibrentasvir should not be used with

A

atazanavir
ritonavir-containing regimens
efavirenz
etravirine

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18
Q

Elbasvir/Grazoprevir should not be used with…

A 
Cobicistat
efavirenz
etravirine
nevirapine
or HIV protease inhibitors
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19
Q

Giving Azole with Protease inhib?

A

increased QT prolongation

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20
Q

Giving Protease inhib with anti-psychotics

A

increase side effects

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21
Q

Giving protease inhib with PDE5?

A

decrease dose for ED, dont use in PAH

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22
Q

Protease inhib effect on methadone?

A

lvl decreased**

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23
Q

Protease inhib with OC?

A

decrease in Hormone lvls

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24
Q

Protease inhib with Warfarin?

A

play with doses

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25
Protease inhib with Steroids?
use beclomethasone as alternative inhalation steroid use less potent steroids
26
pH altering with Protease inhibitors
``` Atazanavir = greatst risk for dec solubility an absorption Ritonavir = next Lopinavir = less risk for solubility changes ```
27
Unique SE Atazanavir
Asymptomatic jaundice
28
Unique SE Indinavir
Kidney Stones
29
Unique SE Fosamprenavir
Severe skin rash
30
Unique SE Tipranavir
Intracranial hemorrhage
31
Unique SE Saquinavir
QT prolongation
32
Lipodystrophy with Protease Inhibitors
up to 50-80% of pts after 12-18 months Risk factors: > 65yrs old low BW before therapy using boosted PI combo Prolonged used
33
Impact of PIs to Diabetes
Longer PI use associated with increased onset of diabetes TGs also associated with diabetes
34
Special SE Indinavir
Lots of Kidney Stones, stay hydrated
35
SE Lopinavir/Ritonavir
Long PR interval
36
Atazanavir SE
Increased bilirubinemia = jaundice
37
Fosamprenavir SE
Hypersensitivity, sulfonamide allergy
38
Darunavir SE
Hepatitis | Caution w/ severe sulfa allergy
39
Tipranavir SE
Severe Hepatitis | Intracranial hemorrhage
40
Darunavir will...
maintain more activity through mutations compared to other drugs
41
Mariviroc (entry Inhibitor) MOA
CCR5 Antagonist Binds to CCR5 co-receptor site on the host cell and prevents penetration of HIV
42
Mariviroc can only be used for....
R5 not X4 Prior to initiation, requires tropism test to evaluate the predominant virus If virus is mixed x4/r5 or x4 virus, Mariviroc will fail
43
ADE Mariviroc
Hepatotoxicity
44
Mariviroc DI
Azole, PI strong inhibition = increase in Mariviroc Strong inducers = dec in Mariviroc so need to inc dose
45
How to avoid Mariviroc toxicity w/ enzyme inhibitor?
Decrease mariviroc dose to 150 BID
46
Enfuvirtide (T-20) MOA
Fusion inhibitor Binds to viral gp41 and prevents a conformational change required for fusion of the virus to the CD4 cell
47
Enfuvirtide ADE
Injection site reactions Hypersensitivity Elevated CK
48
Enfuviritide clearance?
no renal or hepatic, no dose adjustments
49
Gas powered injection system?
Helps to to disperse drug so it doesn't sit in one spot under the skin leads to less injection site reactions
50
Enfuvirtide Mutations & Resistance?
Gp41 (binding site) amino acid substitutions
51
INSTI MOA
Prevents HIV integrase enzyme from inserting HIV genetic material into cellular DNA
52
Which INSTI has lower bioavailability?
Elvitegravir
53
INSTI SE profile?
***Weight gain CNS Rash CK elevation
54
Highest CNS SE of INSTI?
Efavirenz | Raltegravir also has decent amount
55
ADE Elvitegravir
1. need to use with Cobicistat, acts as booster | 2. Cobicistat associated with more GI adverse effects
56
Dolutegravir ADE?
Marked by CNS side effects**weird dreams Hypersensitivity Increase in LFTs in pts co-infected with HBC or HCV
57
Which INSTIs avoided with Rifampin
EVG BTG CAB
58
DHHS guidelines for HIV?
DTG for persons of child bearing age
59
BIC only affected by.....
IRON
60
Dofetilide should be avoided with....
INSTI
61
When using Metformin with INSTI.....
dose has to be less than 1000mg daily less so problem with BIC and CAB
62
PPI not significant interaction wit INSTI when....
using a boosted combo
63
INSTI resistance number
148Q Mostly EV and RAL, less so BIC and DTG
64
How to get passed Q148 mutation?
using higher dose of DTG
65
BIC has most activity against....
wild type and G140S+Q140H mutation
66
Ibalizumab
Used for extremely drug resistant HIV Q2weeks ADE: infusion related DI: none Cl: no adjustments
67
Ibalizumab MOA
blocks postattachment HIV entry into CD4+ T-cells without altering normal cell function
68
Fostemsavir
Attachment inhibitor, prodrug used as a salvage. so add on with others no renal or hepatic dose adjustment
69
Fostemsavir ADE
QT prolonged | Hepatic dysfunction
70
Avoid Fostemsavir with....
Efavirenz Etravirine Rifampin Carbamazepine + Phenytoin will dc lvl
71
Fostemsavir effects on OATP1B1
inhibits it need to dose adjust Estrogen, Statins, Grazoprevir, Voxilaprevir will inc lvl od drug elim

Anti-Infectives Exam 3 (7 decks)

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