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Test 3 Pharm for ANP > antivirals > Flashcards

antivirals Flashcards

1
Q

major antiviral target

A

polymerases

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2
Q

key characteristics of antivirals targeting DNA/RNA polymerases

A

mimic natural nucleoside/tides and require conversion to a triphosphate derivative

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3
Q

Anti HSV/VZV drugs, MOA, AEs

A

Acyclovir and Valacyclovir
MOA: nucleoside analogs - inhibit viral DNA/RNA polymerase
AEs: nephrotoxic/seizure risk

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4
Q

Anti CMV drugs, MOA, AEs

A

Ganciclovir and Valganciclovir
MOA: nucleoside analogs, inhibit viral DNA/RNA polymerase
AEs: bone marrow suppression and bad sperm - use BC

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5
Q

mechanism of resistance to anti-HSV agents:

A

mutations in viral kinases and mutations to viral DNA polymerase

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6
Q

Drugs reserved for resistant CMV/HSV, MOA, AEs

A

Cidofovir - nucleoTIDE analog, inhibits viral DNA polymerase, patient must hydrate r/t renal AEs
Foscarnet - pyrophosphate analog, inhibits viral DNA polymerase, is a vesicant, seizure risk, and renal AEs

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7
Q

CMV prophylaxis for bone marrow transplant drug and MOA

A

Letermovir - inhibits viral DNA terminase

“I received a LETER in the mail saying I am PRE-APPROVED for a BONE MARROW TRANSPLANT so my DNA isn’t TERMINATED”

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8
Q

Characteristics of ALL anti-HBV drugs

A

ALL inhibit HBV polymerase
ALL are PO
ALL are renally excreted
ALL can cause lactic acidosis, HBV exacerbation after discontinuation, and can cause HIV resistance r/t underdosing HIV when taking for HBV - patient must be screened for both viruses

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9
Q

Ant-HBV drugs that are nucleoTIDE analogs and their AEs

A

TenoFOVIR disoproxil - nephrotoxic and decreased bone density
TenoFOVIR alafenamide - less renal/bone toxicity
Adefovir - dose dependent nephrotoxicity and NOT approved for HIV treatment

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10
Q

Anti-HBV nucleoSIDE drugs and AEs

A

Entacavir - food decreases its absorption

Lamivudine - pancreatitis

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11
Q

HBV - monotherapy or combo therapy?

A

Monotherapy. HBV can not be cured.

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12
Q

Does HBV have a vaccine

A

Yes

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13
Q

HCV - monotherapy or combo therapy?

A

combo therapy - attempt to hit 3 steps in virus life cycle

>90% of individuals treated with direct acting antiviral drugs have been cured

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14
Q

does HCV have a vaccine?

A

No

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15
Q

HCV direct acting antiviral targets:

A

NS5B - polymerase
NS5A - unknown but important
NS3/4A - protease

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16
Q

HCV direct acting antivirals: NS5B

A

NS5B DAA = polymerase inhibitors
“P” in Polymerase upside down is “B” for Buvir and for NS5B
Sofosbuvir - nucleotide polymerase inhibitor
Dasabuvir - non-nucleoside/tide polymerase inhibitor (doesn’t require phosphorylation)

17
Q

HCV direct acting antivirals: NS5A

A

“asvir” drug endings

Asvir is 5 letters and begins with an A = NS5A inhibitor

18
Q

HCV direct acting antivirals: NS3/4A

A

NS3/4A = protease inhibitors
“previr”
previr sounds like premiere - I am PRO going to the movie PREMIERE even at 3/4 am.

19
Q

Same Pro-Drug idea:

A

Sofosbuvir and Tenofovir Alafenamide

20
Q

Significant Key Features of HCV direct acting antivirals:

A

ALL have significant DDIs and are contraindicated with inducers of CYP3A4

21
Q

Combo of Sofosbuvir (NS5B polymerase inhibitor) and Amiodorone can cause:

A

Bradycardia

22
Q

Regimens with Ledipasvir (NS5A inhibitor) or Velpatasvir (NS5A inhibitor) - absorption is affected by:

A

decreased absorption when taken with antacids, H2R antagonists, and PPIs

23
Q

Technivie and VieKira are HCV DAA that contain:

A

Ritonavir (a strong CYP3A4 inhibitor)

Caution when using with meds dependent on CYP3A4 metabolism

24
Q

Human Immunodeficiency Virus 1 (HIV-1)

A 
no vaccine
infected for life
combo therapy - sustained viral suppression is critical
infects immune cells and destroys CD-4
single strand - think mRNA
25
Q

Anti-HIV drug CLASSES

A

ENNIP

entry inhibitors
nucleoside/tide RT inhibitors
non-nucleoside/tide RT inhibitors
integrase inhibitors (tegravir)
protease inhibitors (navir)
26
Q

Anti-HIV drugs (ENNIP): Entry inhibitors

MOA: Designed to

A

Designed to block HIV-1 entry

Fostemsavir: (PO) binds to gp120 and prevents binding to CD4
Maravoric: (PO) CCR5 antagonist that prevents gp120 CD4 complex from binding to CCR5
Ibalizumab: (IV) prevents gp120 CD4 complex binding to CCR5 or CXCR4 - used for heavily treatment experienced patients only
Enfuviritide: (SC) prevents HIV fusion with Tcell membrane - used for heavily treatment experienced patients only

27
Q

Anti-HIV drugs (ENNIP): nucleoside/tide RTIs
MOA:
Key features:

A

MOA: COMPETITIVELY inhibits HIV RT and requires phosphorylation
Drugs:
Abacovir (side) - may cause hypersensitivity
Emtricitabine (side) - may cause hyperpigmentation
Lamivudine (side)
Zidovudine (side) - may cause bone marrow suppression and is used IV for laboring moms to prevent transfer
Tenofovir disoproxil (tide)
Tenofovir alafenamide (tide)
Key features:
NO CYP DDIs
REQUIRE renal dose adjustment
Boxed warning: lactic acidosis and hepatomegaly

28
Q

Anti-HIV drugs (ENNIP): Non-nucleoside/tide RTIs
MOA:
Drugs:
Key features:

A

MOA: NON-competitive bind to RT causing conformational change, do NOT require phosphorylation
Drugs:
Doravirine
Efavirenz - hallucinations/insomnia/confusion
Etravirine
Nevirapine
Rilpivirine - QT prolonger
Key features:
DO have CYP DDIs
NO renal dose needed
Fast development of resistance and always used in combo

29
Q

Anti-HIV drugs (ENNIP): integrase inhibitors
MOA:
Features:

A 
HIV Integrase Inhibitors = "TEGRAVIR"
MOA: prevent covalent insertion of HIV DNA into host cell genome. *KEY bc once this happens HIV is permanent*
Features:
NO CYP3A4 DDIs
Chelation with polyvalent cations
HAs/insomnia
30
Q

Anti-HIV drugs (ENNIP): Protease Inhibitors
MOA:
Key features:

A

HIV Protease Inhibitors = “NAVIR”
MOA: competitively inhibit cleavage of non-functional viral precursor proteins into functional proteins
Key features:
*due to extensive first pass metabolism they are given with PK boosters (Ritonavir and cobicistat = CYP3A4 Pgp inhibitors)
NO renal adjustment
CYP450 DDIs
Serious AEs: GI, insulin resistance, fat accumulation, CVD risk, ECG changes, rash, bleeding, hepatotoxicity

31
Q

Influenza virus surface proteins

A

Hemagglutinin (HA)
Neuraminidase (NA)

these surface proteins mutate seasonally and there is a vaccine for the flu developed based off mutation

32
Q

Neuraminidase inhibitors

A

Tamiflu (PO)
Relenza (inhaled - not for COPD patients)
Rapivab (IV for ER patients)

neuropsychiatric effects

must receive within 48 hours on symptom onset

33
Q

New Flu drug - Cap-dependent Endonuclease

A

Viral RNA polymerase binds to cap of host pre-mRNA, cuts it off, and uses it to initiate viral synthesis.

Baloxavir marboxil - inhibits endonuclease activity of RNA polymerase and prevents cap-snatching

Test 3 Pharm for ANP (1 decks)

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