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Antivirals Flashcards

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1
Q

6 classes of antiretrovirals

A

NRTI
NNRTI
Protease inhibitors
Entry inhibitors
Fusion inhibitors
Integrase inhibitors

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2
Q

Common ending to NRTIs

A

-dine (not all)

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3
Q

Common ending to protease inhibitors

A

-navir

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4
Q

ONLY NRTI that doesn’t have to be phosphorylated and why

A

Tenofovir

It is a nucleoTide

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5
Q

NRTI mechanism of action

A

Inhibit diester bond formation
—> viral DNA premature termination

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6
Q

Main side effect of all NRTIs

A

Mitochondrial toxicity
Lactic acidosis

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7
Q

Lamivudine

A

NRTI
Also used for hepatitis B
Peripheral neuropathy
One of the less toxic

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8
Q

Tenofovir uses

A

HIV
Hepatitis B

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9
Q

Zidovudine

A

NRTI
Pregnancy and breastfeeding
Infant prophylaxis

Myelosuppression
Lipodystrophy

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10
Q

Stavudine

A

NRTI
Children and adults
Peripheral neuropathy
Lipodystrophy

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11
Q

Didanosine

A

NRTI
Pancreatitis dose-dependent
Peripheral neuropathy

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12
Q

Abacavir

A

NRTI
Hypersensitivity: HLA-B57:01
—> type IV, delayed rash

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13
Q

NNRTI MOA

A

Binds allosterically —> inhibits reverse transcriptase
—> halt DNA polymerase

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14
Q

NNRTI 3 main side effects

A

Hepatic failure - life-threatening within 6 weeks

CNS: hallucinations, dizzy, ache, insomnia

Teratogenic

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15
Q

NNRTIs (inhibit/induce) P450.

A

Induce ++++

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16
Q

Nevirapine

A

NNRTI
Infants and children
Rash

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17
Q

Efavirenz

A

NNRTI
Only in combination!
Very effective and tolerable except psychiatric effects

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18
Q

NNRTIs are more effective versus HIV 1 or 2?

A

HIV 1

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19
Q

NRTIs are more effective versus HIV 1 or 2?

A

Both <3

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20
Q

Protease inhibitors are more effective versus HIV 1 or 2?

A

Both <3

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21
Q

What gene are proteases encoded by? Why are they needed?

A

POL

To create virions into mature versions

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22
Q

How do strains of HIV obtain resistance?

A

POL mutations

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23
Q

Protease inhibitors main side effects

A

METABOLIC
- Insulin resistance —>hyperglu —> diabetes
- Dyslipidemia
- Lipodystrophy

Inhibit P450

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24
Q

Indinavir

A

Protease inhibitor

Nephrolithiasis within days - give H2O
Least protein-bound

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25
Ritonavir
Protease inhibitor BOOSTS other drug duration by inhibiting P450 GI effects
26
Atazanavir
Protease inhibitor
27
Darunavir
Protease inhibitor FAST
28
Fosamprenavir
Protease inhibitor Long half-life
29
Tipranavir
Protease inhibitor ONLY if resistant to other meds, can cause hepatotoxicity or intracranial bleeding Given with ritonavir
30
Lopinavir
Protease inhibitor Pediatric with ritonavir
31
Saquinavir
Protease inhibitor Rarely used
32
Which medication is used to boost effect duration of protease inhibitors?
Colbistat Also ritonavir
33
Which drug is contraindicated with protease inhibitors?
Rifampin!!! (Induces P450)
34
Maraviroc
Entry inhibitor Binds to CCR5, can’t bind to gp120
35
Gene in charge of structure proteins in HIV
Env gene —> gp41, gp120
36
Enfuvirtide
Fusion inhibitor in HIV Inhibits gp41 ONLY HIV 1 Subcutaneous
37
Raltegravir
Integrase inhibitor in HIV Prevents mRNA formation after DNA Well tolerated, rare rhabdomyolysis Both HIV 1 and 2
38
Threshold for HBV treatment
>= 10,000 copies/mL AND high ALT
39
3 possible drugs for HBV
Entecavir Tenofovir TDF IFN
40
IFN can only be given if cirrhosis is (compensated/decompensated)
Compensated
41
What is important about pegylated interferons?
Longer half-life Steady concentrations 1 weekly dose
42
IFN why are they not recomended?
Flu-like symptoms Neurotoxicity Myelosuppression Lupus Tinnitus Retinopathy Etc. AND EXPENSIVE
43
IFN uses
Hepatitis B and C Cancers Multiple sclerosis (beta) Chronic granulomatous disease (gamma)
44
Treatment of choice for decompensated cirrhosis by hepatitis virus
Nucleoside analogues
45
Which is the cheapest anti-hepatitis? Why isn’t it given as monotherapy?
Lamivudine High resistance, 71% mutation
46
First line treatment for HBV
ENTECAVIR
47
TDF —> tenofovir
TDF is prodrug, cleaved by esterases
48
Entecavir side effects
Nausea, fatigue, headache Lactic acidosis Hepatomegaly
49
Entecavir
Guanosine analogue FIRST line for HBV
50
Adefovir
Adenosine monophosphate analogue for HBV Inhibits viral DNA polymerase
51
Why is entecavir preferred over adefovir?
Adefovir —> resistance and NEPHROTOXICITY
52
Lamivudine
Nucleoside analogue for HBV High resistance, add tenofovir or adefovir
53
HCV genotypes and most common one
6 total 1 is the most common, followed by 3
54
NS5B enzyme
RNA-polymerase inhibitors for HCV In ALL GENOTYPES Ex. Sobosfuvir
55
NS3/4A
Protease inhibitors for HCV Inhibit P450 Ex. Simeprevir for genotype 1 or 4
56
Ribavirin
Nucleoside analogue Inhibits RNA polymerase of HCV Given with PEG-IFN
57
Ribavirin main side effects (2)
Hemolytic anemia dose-dependent 20% Teratogenic category X
58
First-line treatment for HCV
Ribavirin + PEG-IFN
59
HSV first line treatment
Acyclovir
60
Acyclovir
Guanosine nucleoside for HSV 1. +P by VIRAL thymidine-kinase 2. +2p by cellular enzymes Triphosphate —| DNA synthesis
61
Acyclovir indications
HSV encephalitis Neonatal
62
Acyclovir side effects
Interstitial nephritis Crystalline nephropathy Can be avoided by drinking H2O
63
Ganciclovir
Guanosine nucleoside for HSV 1. +P by VIRAL thymidine-kinase 2. +2p by cellular enzymes Triphosphate —| DNA polymerase
64
Valganciclovir
Ganciclovir prodrug More bioavailability
65
(Val)ganciclovir side effect
Myelosuppression —> possible leukemia
66
Oseltamivir
Sialic acid analogue Inhibits neuraminidases in influenza —> no virion release GI effects
67
First line of treatment for influenza
Oseltamivir
68
Zanamivir
Neuraminidase inhibitor
69
Why is oseltamivir preferred over zanamivir? What other difference is there between both?
Zanamivir can cause severe side effects if there is a pre-existent airway disease. Oseltamivir: oral Zanamivir: inhaled
70
First line treatment for CMV
(Val)ganciclovir
71
Safest antiretroviral
Lamivudine
72
NRTIs = La Zebra Anda TENsa, Es Season De VIH
Lamivudine Zidovudine Abacavir Tenofovir Emcitrabine Stavudine Didanosine

Pharmacology (13 decks)

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