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Pharmacology > Antivirals for HIV > Flashcards

Antivirals for HIV Flashcards

1
Q

2 main goals of Highly active anti-retroviral therapy (HAART)

A

Reduce viral load
Maintain immune function

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2
Q

Common adverse effect in the first year of ART where the patient’s recovering immune system responds to a previously acquired opportunistic infection with inflammatory response

A

Immune reconstitution inflammatory syndrome (IRIS)

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3
Q

Describes a sustained reduction in HIV RNA level below the limit of detection

A

Virologic suppression

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4
Q

Testing in which the virus are sequenced to identify the resistance mechanism
Should be performed prior to initiating ART and after ART fails

A

Resistance testing

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5
Q

7 classes of anti-HIV drugs

A

NRTIs
NNRTIs
Protease inhibitors
Fusion inhibitors
Integrase inhibitors
CCR5 antagonists
CD4 post-attachment inhibitor

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6
Q

Zidovudine, Emtricitabine, Lamivudine, Abacavir, and Tenofovir are examples of this class of anti-HIV drug

A

NRTIs (nucleoside reverse transcriptase inhibitors)

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7
Q

MOA of NRTIs

A

Inhibit HIV reverse transcriptase
Inhibitor of viral life cycle following lethal synthesis

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8
Q

Creating a toxin from a non-toxic precursor

A

Lethal synthesis

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9
Q

Class of anti-HIV drugs:
Converted to active triphosphate form that competes for nucleoside triphosphates for access to reverse transcriptase
Missing essential 3’-hydroxyl group prevents additional nucleoside addition to DNA chain
Blocks viral replication and infection of new cells

A

NRTIs (Nucleoside reverse transcriptase inhibitors)

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10
Q

These general adverse reactions are of which class of anti-HIV drug?
Fat deposit accumulation
Myopathy
Peripheral neuropathy
Anemia
Pancreatitis
Hep B flare upon discontinuation

A

NRTIs (Nucleoside reverse transcriptase inhibitors)

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11
Q

hepatitis B flare upon discontinuation is characteristic of this anti-HIV drug

A

NRTIs (Nucleoside reverse transcriptase inhibitors)
These reverse transcriptase inhibitors also suppress hep B virus but at doses well below the doses used to suppress HIV (Emtricitabine, Lamivudine, and Tenofovir)

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12
Q

NRTIs also suppress this other virus, but at doses well below the doses used to suppress HIV

A

Hep B

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13
Q

NRTI inhibition of these account for potentially lethal toxicity

A

Cellular and mitochondrial DNA polymerases and kinases

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14
Q

Primary toxicities of NRTIs are associated with the action of this

A

Mitochondrial action

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15
Q

NRTI that is the worst primary toxicity associated with mitochondrial action

A

Zidovudine

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16
Q

2 primary toxicities of NRTIs associated with mitochondrial action

A

Lactic acidosis
Severe hepatomegaly with hepatic steatosis

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17
Q

Anti-viral HIV drug whose risk of resistance may increase with interrupted therapy
There should be NO drug holidays (not currently recommended for any HIV therapy)

A

NRTIs

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18
Q

NRTI that inhibits stavudine’s action

A

Zidovudine

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19
Q

Zidovudine inhibits the action of this drug

A

Stavudine

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20
Q

4 black box warnings of Zidovudine

A

Myopathy with long-term use
Lactic acidosis
Hepatomegaly with hepatic steatosis
Fat redistribution and accumulation

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21
Q

Stavudine black box (2)

A

Lactic acidosis and severe hepatomegaly
Pancreatitis

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22
Q

NRTI that most prominently causes pancreatitis

A

Didanosine

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23
Q

NRTI that contains phenylalanine, so use should be avoided in phenylketonurics

A

Didanosine

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24
Q

2 black box warnings of Lamivudine

A

Lactic acidosis with severe hepatomegaly
Non-interchangeable forms (form used for Hep B is not appropriate for HIV)

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25
Q

NRTI with higher incidence of hypersensitivity (risk highest in patients with HLA-B*5701)

A

Abacavir

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26
Q

Abacavir is contraindicated in patients with this

A

HLA-B*5701 genotype
Highest risk of hypersensitivity

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27
Q

Major black box warning of Abacavir

A

Hypersensitivity
(more than 2 of the following: fever, rash, nausea, vomiting, diarrhea, malaise, fatigue or achiness, dyspnea, cough)

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28
Q

NRTI that:
Long duration of action allows for once daily dosing
No interactions with biotransformation pathways
Causes hyperpigmentation of soles and palms

A

Emtricitabine

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29
Q

2 black box warnings of Emtricitabine

A

Lactic acidosis and severe hepatomegaly
Hep B exacerbation upon discontinuation of therapy

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30
Q

2 NRTIs with Hep B exacerbation upon discontinuation of therapy

A

Emtricitabine and Tenofovir

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31
Q

Emtricitabine has exacerbation of this upon discontinuation of therapy

A

Hep B

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32
Q

Prodrug converted to diphosphate form that competes with deoxyadenosine triphosphate (dATP) for access to reverse transcriptase
Results in chain termination

A

Tenofovir disoproxil fumarate

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33
Q

NRTI with lower incidence of mitochondrial toxicity

A

Tenofovir

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34
Q

Tenofovir has lower incidence of this than other NRTIs

A

Mitochondrial toxicity

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35
Q

Class of anti-HIV drugs that Inhibit reverse transcriptase by binding near the active site and inducing a conformational change that blocks enzyme activation (also known as: allosteric antagonists)
No activation required
All cause rash, sometimes severe
All biotransformed by cytochrome P450

A

Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

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36
Q

Rashes ranging from mild to severe (even life-threatening) are characteristic of this class of anti-HIV drugs

A

Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

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37
Q

Class of anti-HIV drugs that are all biotransformed by cytochrome P450

A

Non-nucleoside reverse transcriptase inhibitors (NNRTIs)
Need to check for interactions before using with any other drug

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38
Q

Doravirine, Efavirenz, Etravirine, Nevirapine, and Rilpivirine are examples of this class of anti-HIV drug

A

Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

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39
Q

Class of anti-HIV drug where central toxicity occurs in about half of all patients
Dizziness, headache, insomnia, euphoria, impaired cognition, nightmares, hallucinations
Most common in first weeks or months of therapy and fade with continued use
Old FDA pregnancy category D

A

Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

40
Q

NNRTI central toxicity occurs this frequently

A

In about half of all patients

41
Q

Class of anti-HIV drugs that is an inducer of CYP3A4

A

Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

42
Q

Class of anti-HIV drugs that is an inhibitor of CYP2C9 and CYP2C19

A

Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

43
Q

NNRTIs are inducers of this

A

CYP3A4

44
Q

NNRTIs are inhibitors of these

A

CYP2C9 and CYP2C19

45
Q

NNRTI that is contraindicated during 1st trimester pregnancy or in women planning to conceive

A

Efavirenz

46
Q

This NNRTI is contraindicated in women with pretreatment CD4>250 cells/mm and men with CD4>400 cells/mm taking NNRTIs

A

Nevirapine

47
Q

2 contraindications of NNRTIs

A

Efavirenz
Nevirapine

48
Q

Saquinavir, Ritonavir, Atazanavir, Tipranavir, Darunavir, and Fosamprenavir are examples of this class of anti-HIV drugs

A

Protease inhibitors

49
Q

Class of anti-HIV drugs that inhibits the immunodeficiency virus aspartic protease enzyme
Blocks posttranslational processing of the essential viral protein products

A

Protease inhibitors

50
Q

Protease inhibitors inhibits this

A

The immunodeficiency virus aspartic protease enzyme
Blocks posttranslational processing of the essential viral protein products

51
Q

Protease inhibitors have this action on CYP3A4

A

Are both CYP3A4 substrates and inhibitors
Many drug interactions at the biotransformation level

52
Q

Protease inhibitors are both substrate and inhibitors of this

A

CYP3A4

53
Q

Class of anti-HIV drugs that are both CYP3A4 substrates and inhibitors

A

Protease inhibitors

54
Q

2 common adverse effects of protease inhibitors

A

GI upset
Lipid disorders (fat redistribution and accumulation, PI-induced metabolic syndrome)

55
Q

Lipid disorders; fat redistribution and accumulation, PI-induced metabolic syndrome (hyperglycemia, elevated cholesterol, LDL and triglycerides, reduced HDL)
These are common adverse effects of this class of anti-HIV drug

A

Protease inhibitors

56
Q

Common adverse effect of protease inhibitors that involves hyperglycemia, elevated cholesterol, LDL and triglycerides, and reduced HDL

A

PI-induced metabolism syndrome

57
Q

3 severe adverse effects of protease inhibitors

A

Hyperglycemia/diabetes/pancreatitis
Kidney stones
Stevens-Johnson syndrome (immune disorder)

58
Q

Hyperglycemia/diabetes/pancreatitis, Kidney stones and Stevens-Johnson syndrome (immune disorder) are severe adverse effects of this class of anti-HIV drug

A

Protease inhibitors

59
Q

Protease inhibitor not well-tolerated at high doses; low doses used to “boost” other PIs

A

Ritonavir

60
Q

Most potent CYP3A4 inhibitor of protease inhibitors

A

Ritonavir

61
Q

Ritonavir inhibits these

A

Most potent CYP3A4 inhibitor of protease inhibitors
Also inhibits CYP2D6 and other CYP isoforms

62
Q

Ritonavir is this class of anti-HIV drug

A

Protease inhibitor

63
Q

Intracranial hemorrhage is most common with this anti-HIV drug combination

A

Ritonavir - tipranavir combination

64
Q

2 black box warnings of Tipranavir

A

Hepatotoxicity
Intracranial hemorrhage (most common with ritonavir-tipranavir combination)

65
Q

This adverse effect is most common with ritonavir - tipranavir combination

A

Intracranial hemorrhage

66
Q

Hepatotoxicity and intracranial hemorrhage are black box warnings of this

A

Tipranavir (PI)

67
Q

Enfuvirtide is in this class of anti-HIV drugs

A

Fusion inhibitor

68
Q

MOA of Enfuvirtide (fusion inhibitor)

A

Prevents the virally induced conformational change in transmembrane glycoprotein subunit (GP41) permitting viral-host cell membrane fusion
Unique mechanism may add effectiveness to existing HIV therapies

69
Q

Enfuvirtide (a fusion inhibitor) prevents the virally induced conformational change in this which permits viral-host cell membrane fusion

A

Transmembrane glycoprotein subunit (GP41)

70
Q

Hypersensitivity (eosinophils) in up to 10% of patients occurs in this fusion inhibitor

A

Enfuvirtide (Fuseon)

71
Q

2 adverse effects of Enfuvirtide (fusion inhibitor)

A

Injection site reactions
Hypersensitivity (eosinophils) in up to 10% of patients

72
Q

Anti-HIV drug that interferes with entry of HIV into host cells by inhibiting fusion with outer membrane
Only effective with HIV strains that are CCR5-tropic (some virus strains utilize CXCR4)

A

Maraviroc (CCR5 antagonist)

73
Q

Maraviroc MOA

A

Interferes with entry of HIV into host cells by inhibiting fusion with outer membrane
Only effective with HIV strains that are CCR5-tropic (some virus strains utilize CXCR4)

74
Q

Maraviroc is only effective with HIV strains that are CCR5-tropic, but some strains utilize this instead

A

CXCR4

75
Q

Black box warning of Maraviroc (CCR5 antagonist)

A

Hepatotoxicity

76
Q

3 adverse effects of Maraviroc (CCR5 antagonist)

A

Hypersensitivity
Cardiovascular events (MIs, hypotension)
Hepatotoxicity

77
Q

Drug interaction that increases risk of serious cardiovascular events in Maraviroc (CCR5 antagonist)

A

Thioridazine (antipsychotic)

78
Q

Dolutegravir, Elvitegravir, Cabotegravir, Raltegravir and Bictegravir are examples of this class of anti-HIV drug

A

Integrase inhibitors

79
Q

3 adverse effects of integrase inhibitors

A

Rhabdomyolysis
Depression with suicidal ideation
Neural tube defects when used prior to conception (RAL)

80
Q

Rhabdomyolysis, Depression with suicidal ideation, and Neural tube defects when used prior to conception (RAL) are adverse effects of this class of anti-HIV drug

A

Integrase inhibitors

81
Q

Humanized monoclonal antibody indicated for treatment-resistant HIV1 in experienced patients
binds to the CD4 receptors on T cells to prevent attached HIV-1 particles from entering the cell

A

Ibalizumab

82
Q

MOA of ibalizumab

A

Binds to the CD4 receptors on T cells to prevent attached HIV-1 particles from entering the cell

83
Q

Adverse effect of ibalizumab (CD4 post-attachment inhibitor)

A

Opportunistic infection susceptibility

84
Q

What is the recommended HIV treatment for naive adults (who have not tried any therapy yet)?

A

Two nucleoside/nucleotide reverse transcriptase inhibits AND:
Protease inhibitor (boosted), or
Non Nucleoside reverse transcriptase inhibitor, or
Integrase inhibitor

85
Q

2 reasons why monotherapy with NRTI and dual NRTI regimens should be avoided

A

Rapid resistance development
Inferior antiretroviral activity

86
Q

This treatment regimen has a high rate of nonresponse in treatment of naive patients

A

Triple NRTI regimens

87
Q

Only exception when triple NRTI regimens can be used

A

Patients for whom other options are worse

88
Q

Integrase inhibitor that is approved as PrEP

A

Cabotegravir (Apretude)

89
Q

Cabotegravir (Apretude) is this class of anti-HIV drug

A

Integrase inhibitor

90
Q

2 drugs that are combinations of Emtricitabine and Tenofovir

A

Truvada and Descovy

91
Q

Truvada and Descovy are combinations of these 2 drugs

A

Emtricitabine and Tenofovir

92
Q

Truvada and Descovy are used as this

A

Pre-exposure prophylaxis (PrEP)

93
Q

Truvada and Descovy are used in combination with an integrase inhibitor for this

A

Post-exposure prophylaxis (PEP)

94
Q

Truvada and Descovy are used in combination with this as post-exposure prophylaxis (PEP)

A

Integrase inhibitor

95
Q

Pharmacological enhancer of HIV drugs
No action alone, but enhances HIV suppression used with protease inhibitors

A

Cobicistat (Tybost)

Pharmacology (14 decks)

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