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Foundations 7 > Antiviral Agents > Flashcards

Antiviral Agents Flashcards

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

A

Regimen with PIs

23
Q

For patients at high risk of resistane

A

Can use genetic profiling to determine best drug

24
Q

Enfuvirtide

A

Fusion inhibitor that interacts with Gp41 and blocks entry

25
Q

Enfuvritide side effects and issues

A

Pain and hardening at injecton site…GI upset and weight loss
Expensive

26
Q

____ elevated in patients who have long been on retroviral therapy

A

CXCR-4

27
Q

Maraviroc use and mech

A

Inhibitor of CCR5…only used in R5-trophic patients

28
Q

Maraviroc side effects

A

Liver, skin, and allergic…more than others because targeting host cell protein

29
Q

Maravoric metab and kinetics

A

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
Q

ganciclovir use

A

Preferred tx. for CMV in immunocompromised patients

31
Q

Other drugs like ganciclovir

A

Acyclovir and valacyclovir

32
Q

Acyclovir vs ganciclovir

A

Acyclovir HSV1/2>VSV>EBV, CMV

Ganciclovir is more active against CMV

33
Q

Mech of acyclovir family

A

Inhibt viral DNA polymerase preferentially compared to host DNA polymerase…makes inactive enzyme complex

Also incorporated into viral DNA to cause chain termination

34
Q

Resistance rates of herpesvirsues

A

Lower than HIV because the viral DNA polymerase has a exonuclease function so fewer mutations

35
Q

Acyclovir kinetics

A

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
Q

Administration of acyclovir fam

A

Acy - IV and poor oral
Ganc - Poor oral
Val - better oral because of valine side group

37
Q

Side effects of ganciclovir

A

Neutropenia (also caused by CMV), local irritation, CNS effects, and fever

38
Q

HSV treatment

A

Acyclovir…no effect on latency
Must be taken systemically
If frequent recurrence, then take daily

39
Q

Pregnancy and acyclovir family

A

Acy - safe after 36 weeks but little is known

Can give acyclovir to the child once born

40
Q

How to tx cancer patient positive for HSvV

A

Prophylactically with acyclovir

41
Q

What is used in cases of acyclovir infection

A

Foscarnet

42
Q

Hep B first tx

A

Lamivudine…tenofovir is alternative

43
Q

Hep B weird sturctutre

A

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
Q

Resistant hep B

A

Mutations in HBV polymerase
use tenofovir
Measure efficacy with ALT

45
Q

EBV tx

A

Normally none

46
Q

VZV tx

A

Can be treated with acyclovir

47
Q

RNA virus challenge

A

Use RNA replicase that is very mutagenic

48
Q

Influenza tx that is not recommended

A

Amantidine inhibits viral ion channel M2
Better prophylactically

Causes neuro side effects

49
Q

Better influenza txs and side effects

A

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
Q

Hep C tx 1

A

Ribavirin

51
Q

Tx 2 for Hep C

A

Pegylated IFN

52
Q

Tx 3 for Hep C and mechs

A

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
Q

Side effects of sofosbuvir

A

Fatigue and headaches

54
Q

Hep C tx 4 and mech and side effects

A

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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