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Foundations 7 > Antiviral Agents > Flashcards

Antiviral Agents Flashcards

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1
Q

Antiviral therapy for HIV patients

A

Recommended for ALL patients ragrdless of CD4 counts

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2
Q

General HIV therapy for tx naive patient

A

2 RT inhibitors with either ingrase inhibitor, non-nucleside RT inhibitor or protease inhibitor

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3
Q

Abacavir mechanism of action

A

Nucleoside RT inhibitor…specific to retroviruses because of RT

Incorporated into the viral DNA and terminate growing polypeptide

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4
Q

Human enzyme similar to RT

A

Telomerase

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5
Q

RTI selectivity

A

Higher affinity for RT than normal nucleotides and prefernetiall bind RT compared ot host DNA polymerases

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6
Q

Limitation of RTIs

A

Do not inhibit the virus from binding, only the replication inside of the cell

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7
Q

Kinetics/dynamis of abacavir

A

Phosphorylated by host adenosine kinase, then guanylate kinase, then multiple kinases…products can feedback and inhibit original host enzyme

Can be taken orally

Prodrug

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8
Q

Side effects of abacavir

A

Hypersensitivity (increased with HLA-B5701), nausea, headache, fatigue

HLA marker will bind to abacavir and present as foreign antigen

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9
Q

Other important nucleoside transcriptase inhibitor

A

lamivudine

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10
Q

Tenofovir mechanism

A

Nucleotide RTI inhibitor
Monophosphate that requires phosphorylation to work

Inhibit RT directly and incorporate into DNA

Phosphorylated by cellular kinases

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11
Q

Typical combination of nucleoside/nucleotide inhibitors

A

Abacavir/lamivudine

or tenofovir/emtrcitabine

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12
Q

NNRTIs

A

Bind to different site of RT than the nucleoside RTIs…lots of resistance

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13
Q

PI mechanism of action

A

Target protease that cleaves pol and gag proteins
Virions still produced but inactive
Typically used with RTIs

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14
Q

PI side effects

A

Hyperglycemia and abnormal fat distribtuion

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15
Q

Darunavir metabolism

A

CYP3A4 metabolilzed
Potent CYP450 inhibitor
Given with another CYP450 inhibitor in order (ritnoavir) in order to keep it around longer

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16
Q

Darunavir drug interactions

A

Statins, pain meds, antifungals , reflux meds, antibiotics

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17
Q

Statins in HIV patients

A

Probably a bad idea

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18
Q

Integrase inhibitor mech

A

Prevent integration of viral DNA

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19
Q

Elvitegravir mech and how used

A

Integrase inhibitor - binds metal ions essential for integrase…not only targeting infected cells
Used in genvoya with tenofovir and cobicistat (used as P450 inhibitor)

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20
Q

Elvitegravir side effects

A

Modest, but increase with combination

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21
Q

Combination regimen side effects

A

Abnormal fat, high LDL/low HDL and coronary artery dz

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22
Q

Patients with diabetes should avoid

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A

Regimen with PIs

23
Q

For patients at high risk of resistane

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A

Can use genetic profiling to determine best drug

24
Q

Enfuvirtide

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A

Fusion inhibitor that interacts with Gp41 and blocks entry

25
Enfuvritide side effects and issues
Pain and hardening at injecton site...GI upset and weight loss Expensive
26
____ elevated in patients who have long been on retroviral therapy
CXCR-4
27
Maraviroc use and mech
Inhibitor of CCR5...only used in R5-trophic patients
28
Maraviroc side effects
Liver, skin, and allergic...more than others because targeting host cell protein
29
Maravoric metab and kinetics
Taken as a pill with other HIV drugs | It is a P450 and P glycoprotein substrate and some other HIV drugs are P450 inhibitors
30
ganciclovir use
Preferred tx. for CMV in immunocompromised patients
31
Other drugs like ganciclovir
Acyclovir and valacyclovir
32
Acyclovir vs ganciclovir
Acyclovir HSV1/2>VSV>EBV, CMV | Ganciclovir is more active against CMV
33
Mech of acyclovir family
Inhibt viral DNA polymerase preferentially compared to host DNA polymerase...makes inactive enzyme complex Also incorporated into viral DNA to cause chain termination
34
Resistance rates of herpesvirsues
Lower than HIV because the viral DNA polymerase has a exonuclease function so fewer mutations
35
Acyclovir kinetics
Phosphorylated first by viral, then by cellular...product feeds back onto itself Means this is more specific because targeting infected cells more than healthy cells Distributes throughout body except for CSF
36
Administration of acyclovir fam
Acy - IV and poor oral Ganc - Poor oral Val - better oral because of valine side group
37
Side effects of ganciclovir
Neutropenia (also caused by CMV), local irritation, CNS effects, and fever
38
HSV treatment
Acyclovir...no effect on latency Must be taken systemically If frequent recurrence, then take daily
39
Pregnancy and acyclovir family
Acy - safe after 36 weeks but little is known | Can give acyclovir to the child once born
40
How to tx cancer patient positive for HSvV
Prophylactically with acyclovir
41
What is used in cases of acyclovir infection
Foscarnet
42
Hep B first tx
Lamivudine...tenofovir is alternative
43
Hep B weird sturctutre
Hep B produces RNA which is RT'd into single stranded DNA and then partially dsDNA by HBV polymerase DNA virus that uses RNA intermediate and RT
44
Resistant hep B
Mutations in HBV polymerase use tenofovir Measure efficacy with ALT
45
EBV tx
Normally none
46
VZV tx
Can be treated with acyclovir
47
RNA virus challenge
Use RNA replicase that is very mutagenic
48
Influenza tx that is not recommended
Amantidine inhibits viral ion channel M2 Better prophylactically Causes neuro side effects
49
Better influenza txs and side effects
Oseltamavir and zanamivir Neuraminidase inhibitors that prevent detachment Should be used within 2 days of symptoms...used more for prophylaxis Nausea, vomiting, mood changes
50
Hep C tx 1
Ribavirin
51
Tx 2 for Hep C
Pegylated IFN
52
Tx 3 for Hep C and mechs
Sofosbuvir and ledipasvir Sofosbuvir is inhibitor of the RNA dependent RNA polymerase of the virus...does NOT inhibit host DNA or RNA polymerases Ledipasvir - inhibits a large phosphoprotein required for replication...may genotype to use this
53
Side effects of sofosbuvir
Fatigue and headaches
54
Hep C tx 4 and mech and side effects
Paritaprevir inhibits viral protease and arrests course of infection Does NOT cure Side effects include sleep loss, rash, and itching Part of Viekra pak

Foundations 7 (19 decks)

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