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IHO Week 6 > HIV Drugs > Flashcards

HIV Drugs Flashcards

1
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

A

Zidovudine (Azidothymidine or AZT)
Lamivudine
Abacavir
Emtricitabine

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2
Q

Nucleotide Reverse Transcriptase Inhibitors (NRTI)

A

Tenofovir

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3
Q

Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

A

Etravirine
Efavirenz
Rilpivirine

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4
Q

Protease Inhibitors

A

Atazanavir +/- ritonavir (ritonavir boosting)

Darunavir + rionavir (ritonavir boosting)

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5
Q

Integrase Inhibitors

A

Raltegravir

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6
Q

Fusion Inhibitors

A

Enfuvirtide (T-20)

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7
Q

CCR5 agonist

A

Maraviroc

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8
Q

Goal of HIV treatment

A

Fully undetectable levels of virus

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9
Q

The lower the viral RNA is driven.. the lower the rate of ___

A

drug resistance

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10
Q

Less resistance =

A

longer therapeutic effect

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11
Q

To achieve maximal and durable suppression of viral RNA, _____ and ____ are required

A

Drug combinations

Compliance

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12
Q

What two things should you monitor in HIV treatment

A

CD4+ counts

HIV RNA levels (viral load)

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13
Q

Typical treatment regime

A

(NNRTI, Protease Inhibitor, integrase inhibitor) + Dual NRTI

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14
Q

Nucleoside RTI mechanism

A
  • Competitively inhibits reverse transcriptase and can be incorporated into the viral DNA chain - cause termination
  • Requires phosphorylation by cellular enzymes to triphosphate form to be activated
  • Resistance to one may result in resistance to another in the class
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15
Q

AE of Nucleoside RTI

A
  • Lactic acidosis with hepatic steatosis probably due to mt toxicity (No ETC on mt means pyruvate to lactic acid)
  • fat redistribution and hyperlipidemia
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16
Q

Zidovudine (Azidothymidine or AZT) AE

A

NRTI
granulocytopenia and anemia
CNS disturbances - severe headache, nausea, insomnia, malaise

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17
Q

Didanosine

A

NRTI

more toxic than AZT

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18
Q

Lamivudine and Emtricitabine

A

NRTI
Best tolerated NRTIs (nucleoside)
Active against Hepatitis B

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19
Q

Abacavir

A

NRTI
Hypersensitivity
MUST test for HLA-B*5701

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20
Q

HLA-B*5701

A

Hypersensitivity to to Abacavir

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21
Q

Tenofovir class

A

Nucleotide Reverse Transcriptase Inhibitor

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22
Q

Tenofovir mechanism

A

competitive inhibition of reverse transcriptase.

Encorporated into viral DNA chain and causes termination

23
Q

AE of Tenofovir

A

nausea, vomiting, diarrhea, RENAL FAILURE

Lactic acidosis with hepatic steatosis (mt toxicity)

24
Q

Do not give Tenofovir to patients with low _____

A

baseline GFR (indicating reduced kidney function)

25
What should you think of when thinking of NNRTIs?
Drug interactions
26
NNRTI mechanism
- bind directly to the reverse transcriptase at a site distinct from that of the NRTI. The site cannot then produce viral DNA - Does not require phosphorylation for activity and are primarily effective against HIV1
27
No cross resistance with NNRTIs and NRTIs and ___
protease inhibitors
28
Do NNRTIs require phosphorylation?
No - acts at a distinct site from NRTIs
29
General AE of NNRTIs
Varying levels of GI intolerance and skin rash | Metabolized by and can affect hepatic CYP450 drug interactions (induce, inhibit or mixed)
30
Efavirenz
NNRTI Once a day CNS effects (vivid dreams, nightmares, hallucinations)
31
Etravirine
NNRTI | Rash, Nausea, Peripheral neuropathy
32
Rilpivirine
NNRTI | Do not use in a patient with pretreatment viral loads >100,000 copies/ml
33
MOA of protease inhibitors?
- Prevent protease action. As virus buds, proteolytic cleavage occurs. Without, virus in not infectious. - Protease is required for cleavage of polypeptide precursors for structural proteins
34
Protease inhibitors prevent the post translational cleavage of the ____ polyprotein
gag-pol | prevent the processing of viral proteins into functional conformations
35
With protease inhibitors, new viral particles cannot
mature (therefore, cannot become infectious)
36
Inhibiting HIV protease activity presents HIV replication
in vitro
37
Protease inhibitors are active against HIV strains that are resistant to
reverse transcriptase inhibitors (NRTIs/ NNRTIs)
38
General AE of protease inhibitors
GI disturbances, hepatotoxicity, hyperglycemia/insulin resistance, dyslipidemia, cardiac conduction abnormalities, Peripheral lipoatrophy and central fat accumulation
39
Protease inhibitors are metabolized by
CYP3A4, therefore can inhibit as well
40
Ritonavir boosting
- High doses of protease inhibitor ritonavir is poorly tolerated. - Used at lower doses to increase serum concentration of other protease inhibitors and decrease frequency of other PI
41
Why does Ritonavir boosting work?
Potent inhibitor of CYP3A4 (which metabolizes several PIs)
42
Cobicistat
Inhibits CYP3A4 and intestinal proteins - booster for PIs. | By itself is not a protease inhibitor
43
Enfuvirtide (T-20)
Fusion inhibitor After HIV binds to host, conformation change occurs in gp41 and virus enters. Enfuviritide is a 36 aa synthetic peptide that binds to gp41 and prevents conformational change
44
Enfuvirtide administration
Subcutaneous 2x daily high incidence of local reactions with pain, erythema, induration, nodules and cysts rare systemic hypersensitivity Higher incidence of bacterial pneumonia?
45
Enfuviritide is active against HIV classes that are...
resistant to other drug classes
46
Raltegravir
Integrase Inhibitor Integrase is a viral enzyme essential to the rep of HIV1 and HIV2. Binding integrase inhibits strand transfer - the final step of provirus integration
47
CCR5 Antagonist MOA
CCR5 and CXCR4 are two major co recpetors used by HIV1 to gain entry into the host cell with the R5 strains predominating during early stages of infection and 50-60% of the late stage disease. BINDS TO host CCR5 SELECTIVELY
48
CCR5 Antagonist Name
Maravironic
49
Integrase inhibitor name
Raltegravir
50
Why is Raltegravir beneficial?
Fewer drug interactions than NRTIs or PIs
51
Maraviroc AE
Pyrexia, rash, postural dizziness
52
HAART
- Highly active antiretroviral therapy | - Therapy with RTI and PI
53
HHART AE
lipodystrophy | other secondary effects
54
Lipodystrophy and HHART
25-50% of patients Wasting of subcutaneous fat Central adiposity Hyperlipidemia, insulin resistance and diabetes m. Usually NRTI and PI together, sometimes just NRTI

IHO Week 6 (7 decks)

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