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Antiretrovirals Flashcards

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1
Q

What allows HIV to mutate so rapidly?

A

Really error prone reverse transcriptase

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2
Q

What is the enzyme that integrates HIV genetic material into host DNA?

A

integrase

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3
Q

What is the enzyme that is packaged with the HIV virus, and cleaves viral proteins to mature proteins?

A

Protease

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4
Q

What is the viral antigen of HIV that is measured in the serum to follow the early course of the disease?

A

p24

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5
Q

What is the antibody that is followed with HIV infections?

A

Anti-HIV ab (gp120)

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6
Q

What is the MOA of Nucleotide reverse transcriptase inhibitors?

A

Mimic nucleotides to inhibit nucleotide binding to the catalytic site, and cause chain termination

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7
Q

What are the adverse effects of Nucleoside reverse transcriptase inhibitors?

A

Lactic acidosis
Fatty liver disease
Lipodystrophy

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8
Q

Why can NRTIs be used in Hep B infections?

A

Has reverse transciptase

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9
Q

What type of drug is Abacavir? Route of administration? Adverse effects?

A

NRTI
PO
Increase chances of MI

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10
Q

What drug does Abacavir interfere with?

A

Methadone

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11
Q

How is resistance to abacavir brought about?

A

Multiple mutations in HIV reverse transcriptase

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12
Q

What type of drug is Lamivudine? Route of administration? Adverse effects?

A

NRTI
PO
CNS effects, but safer than most

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13
Q

How is resistance to Lamivudine brought about?

A

Single base change

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14
Q

Which HIV drugs are safe for use in pregnancy?

A

Lamivudine
Nevirapine
***

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15
Q

What type of drug is Emtricitabine? Route of administration? Adverse effects?

A

Fluorinated analog of lamivudine (NRTI)
PO
HA, n/v/d

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16
Q

How is resistance to Emtricitabine brought about?

A

single mutation in reverse transcriptase

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17
Q

What type of drug is Tenofovir? Route of administration? Adverse effects?

A

NRTI
PO
Renal and bone toxicity

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18
Q

How is resistance to Tenofovir brought about?

A

single mutation in reverse transcriptase

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19
Q

What type of drug is Zidovudine (AZT)? Route of administration? Adverse effects?

A

NRTI
PO
Myelosuppression

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20
Q

How is resistance to Zidovudine brought about?

A

Multiple mutations in HIV needed

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21
Q

What is the MOA of Non-nucleoside reverse transcriptase inhibitors? What is the major difference between these and NRTIs?

A

bind to a site on the enzyme distinct from the active site

Do NOT need to be phosphorylated to become activated

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22
Q

How is resistance to NNRTIs brought about?

A

Single amino acid change

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23
Q

What is the major adverse reaction that is common to the class of NNRTIs?

A

Drug-Drug interactions d/t p450 effects

Stven-Johnson syndrome

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24
Q

What type of drug is Efavirenz? Route of administration? Adverse effects?

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A

NNRTI
PO
CNS effects

25
Resistance to Efavirenz will often mean resistance to what other NNRTI?
Nevirapine
26
What type of drug is Nevirapine? Route of administration? Adverse effects?
NNRTI PO Hepatitis
27
What is the MOA of the proteases used for treating HIV?
mimic peptides for the protease
28
Generally, how is resistance to protease inhibitors brought about?
Multiple mutations
29
What are the common adverse effects of protease inhibitors?
Drug-drug interactions high d/t p450
30
What is the major difference between mature and immature HIV viruses?
Well formed blob on EM with mature, whilst immature have poorly defined blob
31
What type of drug is Atazanavir? Route of administration? Adverse effects?
Protease inhibitor PO Peripheral neuropathy, cardiac effects
32
What class of drugs cannot be administered concurrently with Atazanavir? Why?
PPIs, since acid required for absorption
33
What type of drug is Ritonavir? Route of administration? Adverse effects?
Peptidomimetic protease inhibitor PO POTENT inhibitor of p450
34
What is the therapeutic indication for Ritonavir?
Booster to increase the half-life of coadministered ARV drugs d/t inhibiting p450 effects
35
What type of drug is Darunavir? Adverse effects?
Protease inhibitor | Increased serum amylase
36
What is different about the resistance with Darunavir?
90% of HIV-1 isolates that are resistant to multiple protease inhibitors are still susceptible to this
37
What is the MOA of CCR5 receptor antagonists?
Inhibits the coreceptor CCR5
38
What are the two coreceptors for HIV? Which causes a lower susceptibility to HIV infection?
CCR5 | CXCR4--cause lower susceptibility***
39
What is the role of gp120 on HIV?
Envelope protein/anchor on cells
40
What is the role of gp41 protein on HIV?
Fusion protein
41
What type of drug is Maraviroc? Adverse effects?
Co-receptor antagonist | URT infections/increased cardiac events
42
What is the therapeutic indications for Maraviroc?
For HIV experience pts, who have a *predominantly CCR% tropic virus*
43
How is resistance brought about with Maraviroc?
Change in tropism or mutations in gp120
44
What is the MOA of fusion inhibitors?
Inhibits gp41 from fusing cell membranes of HIV
45
What is the only type of antiretroviral that is administered IV?
Fusion inhibitors
46
What type of drug is Enfuvirtide? Adverse effects?
Peptide fusion inhibitor | Injection pain, bacterial pneumonia
47
How is resistance to Enfuvirtide brought about?
Multiple mutations in gp41
48
What is the therapeutic index of enfuvirtide?
Treatment experienced patients with evidence of ARV resistance
49
What is the MOA of integrase inhibitors?
Inhibit HIV integrase, and prevents DNA strand transfer
50
What type of drug is Raltegravir? Adverse effects?
Integrase inhibitor | Myopathy/rhabdo
51
How is resistance to Raltegravir ad Elvitegravir brought about?
Single mutation in integrase gene
52
What type of drug is Elvitegravir? Adverse effects?
Integrase inhibitor | Usual side efects
53
What type of drug is Dolutegravir? Adverse effects?
Integrase inhibitor | Elevation of serum aminotransferases, fat redistribution syndrome
54
What is the therapeutic indications for Dolutegravir?
Need to weigh 40 kg and be over 12 yo
55
What is significant about the resistance profile of Dolutegravir?
Retains activity against some viruses resistant to both raltegravir and elvitegravir
56
What is the clinical definition of AIDS?
Less than 250 cells/mm3 of CD4 cells
57
True or false: all pts who have HIV are recommended to take antiretroviral agents
True
58
What is the standard of care for HIV?
Use at least 3 antiretroviral drugs, usually form at least two different classes. 1 PI + 2 NRTIs 1 II + 2 NRTIs

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