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antivirals Flashcards

1
Q

HIV fusion inhibition

A

attachment: maravirocpenetration: enfuvirtide

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2
Q

HIV inTEGRAse inhibition

A

doluTEGRAvir, elviTEGRAvir, ralTEGRAvir

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3
Q

HIV protease inhibition

A

atazanavir, darunavir, fosamprenavir, indinavir, lopinavir, ritonavir, saquinavir

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4
Q

HIV reverse transcriptase inhibition

A

NRTIS, NNRTI

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5
Q

NRTIs

A

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

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6
Q

NNRTIs

A

delaviridine, efavirenz, nevirapine

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7
Q

HBV, HCV protein synthesis inhibition

A

INF-a (binds via PKR)

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8
Q

uncoating (influenza)

A

amantadine, rimantadine(no longer used, high resistance)

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9
Q

Guanosine analogs

A

acyclovir (HSV, VZV)Ganciclovir (CMV)

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10
Q

viral DNA polymerase inhibitors

A

cidofovir (HSV)foscarnet (CMV)

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11
Q

guanine nucleoside synthesis inhibitor

A

ribavirin (RSV, HCV)

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12
Q

release of progeny inhibitors

A

neuraminidase inhibitors (Oseltamivir, Zanamivir) in flu A,B

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13
Q

Ganciclovir MOA

A

5’-monophosphate formed by CMV viral kinase. Guanosine analog. Triphosphate formed by cellular kinases. preferentially inhibits viral DNA polymerase

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14
Q

Ganciclovir use

A

CMV, esp. in IC pts.

Valganciclovir, prodrug of ganciclovir, has better oral bioavailability

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15
Q

Ganciclovir ADR

A

bone marrow suppression (leukopenia, neutropenia, thrombocytopenia); renal toxicity

more toxic to host than acyclovir

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16
Q

Ganciclovir resistance

A

mutated viral kinase

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17
Q

Foscarnet MOA

A

Viral DNA/RNA polymerase inhibitor and HIV reverse transcriptase inhibitor.

Binds to pyrophosphate-binding site of enzyme.

*Does not require any kinase activation

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18
Q

Foscarnet use

A

CMV retinitis in IC patients when ganciclovir fails; acyclovir-resistant HSV

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19
Q

Foscarnet ADR

A

nephrotoxicity, electrolyte abnormalities lead to seizures

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20
Q

Foscarnet Mech of resistance

A

mutated DNA polymerase

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21
Q

Cidofovir MOA

A

preferentially inhibits viral DNA polymerase. Does not require phosphorylation by viral kinase

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22
Q

Cidofovir use

A

CMV retinitis in IC patients;

acyclovir-resistant HSV.

Long-half life

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23
Q

Cidofovir ADR

A

nephrotoxicity (coadmin w/ probenecid and IV saline to dec)

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24
Q

HIV triple therapy

A

2 NRTIs and preferably an integrase inhibitor

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25
NRTIs MOA (HIV)
competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain (lack 3' OH group)
26
NRTI make-up
``` nucleoSides that need to be phosphorylated to be active except Tenofovir (nucleoTide) ```
27
Zidovudine (ZDV) use
general prophylaxis and during pregnancy to dec risk of fetal transmission
28
NRTI toxicity
bone marrow suppression, peripheral neuropathy
29
NRTI bone marrow suppression TX
granulocyte colony-stimulating factor and EPO
30
NRTI nucleoside ADR
lactic acidosis
31
ZDV ADR
anemia
32
didanosine ADR
pancreatitis
33
Abacavir contraindication
pt has HLA-B*5701 mutation
34
NNRTIs MOA (HIV)
bind to reverse transcriptase at site different from NRTIs. Do not require phosphorylation to be active or compete with nucleotides
35
NNRTI ADR
rash and hepatotoxicity
36
NNRTIs contraindicated in pregnancy
delavirdine and efavirenz
37
Efavirenz ADR
vivid dreams and CNS sx
38
Protease Inhibitors (-navir) MOA (HIV)
assembly of virions depends on HIV-1 protease (pol gene), which cleaves polypeptide products of HIV mRNA into their functional parts. ***thus protease inhibitors prevent maturation of new viruses**
39
Ritonavir use
"boosts" other drug concentrations by inhibiting p450
40
Protease inhibitor ADR
hyperglycemia, GI intolerance, lipodystrophy (Cushing-like syndrome)
41
Indinavir ADR
nephropathy, hematuria
42
what drug should never be used with protease inhibitors?
Rifampin (potent CYP/UGT inducer) bc it decreases protease inhibitor concentration
43
integrase inhibitors MOA
inhibits HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase
44
integrase inhibitors ADR
inc. creatine kinase
45
Enfuvirtide MOA
fusion inhibitor binds gp41, inhibiting viral entry
46
Enfuvirtide ADR
skin rxn at injection site
47
Maraviroc MOA
binds CCR-5 on surface of T cells/monocytes, inhibiting interaction with gp120
48
Interferons MOA
glycoproteins norm synthesized by virus-infected cells, exhibiting wide range of antiviral and antitumoral properties
49
INF-a use
chronic HBV and HCV; Kaposi sarcoma; hairy cell leukemia; condyloma acuminatum; renal cell carcinoma; malignant melanoma
50
INF-b use
multiple sclerosis
51
INF-y use
chronic granulomatous disease
52
interferons ADR
flu-like symptoms, depression, neutropenia, myopathy
53
Ribavirin (HCV) MOA
inhibits synthesis of guanine nucleotides by competitively inhibiting inosine monophosphate dehydrogenase
54
Ribavirin use
chronic HCV, RSV
55
Ribavirin ADR
hemolytic anemia, severe teratogen
56
RSV tx in kids
palivizumab
57
Sofosbuvir MOA
inhibits HCV RNA-dependent RNA polymerase acting asa chain terminator
58
Sofosbuvir use
chronic HCV in combo w/ ribavirin **don't use as monotherapy**
59
Sofosbuvir ADR
fatigue, HA, nausea
60
Simeprevir MOA
HCV protease inhibitor; prevents viral replication
61
Simeprevir use
chronic HCV in combo w/ ledipasvir (NS5A inhibitor) **don't use as monotherapy**
62
Simeprevir ADR
photosensitivity rxns, rash

step 1 microbiology (7 decks)

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