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A13AMC @ UoN > L11 - Treatment of HIV Infection > Flashcards

L11 - Treatment of HIV Infection Flashcards

1
Q

What sort of genetic material does the HIV virion have?

A

ssRNA (+)

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2
Q

Describe the two types of glycoprotein expressed by the HIV virion

A

gp41 (transmembrane glycoprotein)

gp120 (surface glycoprotein)

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3
Q

Describe the two antigens expressed by the HIV virion

A

p17 (matrix antigen)

p24 (capsid antigen)

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4
Q

What sort of membrane does the HIV virion have?

A

Lipid bilayer envelope

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5
Q

What three enzymes are responsible for inserting the HIV ssRNA (+) into the human genome?

A

Reverse Transcriptase
Integrase
Protease

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6
Q

What is the function of reverse transcriptase?

A

To convert the ssRNA viral genome into cDNA

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7
Q

What is the function of integrase?

A

To integrate the dsDNA produced by RT into the human genome

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8
Q

What is the function of protease?

A

To cleave larger combination proteins into their functional forms

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9
Q

What is Azidothymidine?

A

A nucleoside analogue reverse transcriptase inhibitor (NRTI) - 2’3’ dideoxy nucleoside analogue that is phosphorylated by host cells

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10
Q

What is the MoA of Azidothymidine?

A

It acts as a DNA chain terminator and RT inhibitor

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11
Q

What is the therapeutic life of Azidothymidine?

A

6 months

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12
Q

What are ddC and ddI?

A

Both NRTIs (2’3’ dideoxy NAs) with the same MoA as Azidothymidine

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13
Q

Define NRTIs

A

Nucleoside/Nucleotide Reverse Transcriptase Inhibitors

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14
Q

Describe the general structure of NRTIs

A

All analogues of nucleotides, lack a 3’OH group on the ribose ring
Require phosphorylation by cellular kinases

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15
Q

Give four examples of NRTIs and their corresponding nucleosides

A

Zidovudine/AZT (Thymidine)
Lamivudine (Cytosine)
Abacavir (Guanosine)
Didanosine (Adenosine)

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16
Q

What is Tenofovir DF?

A

A nucleotide analogue RT inhibitor

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17
Q

What is the MoA of Tenofovir DF?

A

Tenofovir DF is converted to Tenofovir (serum esterases)

Tenofovir is a nucleotide analogue of adenosine monophosphate

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18
Q

What are the currently used NRTIs?

A 
Zidovudine (AZT)
Stavudine (D4T)
Lamivudine (3TC)
Emtricitabine (FTC)
Abacavir (ABC)
Didanosine (DDI)
Tenofovir DF (TDF)
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19
Q

What are the adverse effects of NRTIs?

A 
Lactic acidosis
Hepatic steatosis
Peripheral neuropathy
Myopathy
Lipoatrophy
20
Q

What causes the adverse effects of NRTIs?

A

They may inhibit the activity of normal cellular DNA polymerases (mitochondrial DNA pol-Y)
May also interfere with CYP450 enzymes (D/D interactions)

21
Q

What are the first choice NRTIs?

A 
Abacavir (ABC)
Tenofovir DF (TDF)
22
Q

Why are ABC & TDF the first choice NRTIs?

A

Minimal DNA pol-Y inhibitory effects

No interaction with CYP450 enzymes

23
Q

What is the main side effect of ABC?

A

Associated with a potentially fatal hypersensitivity syndrome

24
Q

What is the main side effect of TDF?

A

Nephrotoxicity

25
Q

Define NNRTIs

A

Non-Nucleoside Analogue Reverse Transcriptase Inhibitors

26
Q

What is the MoA of NNRTIs?

A

They are non-competitive RT inhibitors that induce conformational changes within RT

27
Q

Give three examples of NNRTIs

A

Nevirapine
Efavirenz
Etavirine

28
Q

Describe combination therapy

A

Giving NRTIs AND NNRTIs together to increase and sustain the decrease in viral load

29
Q

What are the side effects of NNRTIs?

A

CNS s/e (vivid dreams, insomnia, hallucinations, depression)
Teratogenicity
Substrates of CYP enzymes (D/D interactions)

30
Q

What are Protease Inhibitors?

A

A class of antiretroviral HIV drugs

31
Q

What is the MoA of PIs?

A

PIs inhibit HIV protease-mediateed cleavage of HIV polyprotein precursors
Renders virus particles non-infectious

32
Q

What are the problems associated with PIs?

A

They are heavily metabolised by CYP enzymes (+Ritonavir)

Resistance can develop

33
Q

What is the mechanism by which resistance to PIs arises?

A

Mutations modify the number/nature of points of contact between PI and protease

34
Q

What are the side effects of PIs?

A

Dyslipidaemia (leading to atherosclerosis)
Insulin resistance
Lower GI symptoms

35
Q

Give four examples of commonly used PIs

A

Lopinavir + Ritonavir (Kaletra)
Atazanavir
Darunavir

36
Q

What is the MoA of Entry Inhibitors

A

They block co-receptor binding/fusion to prevent the HIV virion binding to and entering human cells

37
Q

Give two examples of EIs

A

Maraviroc (block binding)

Enfurvitide (block fusion)

38
Q

Define INSTIs

A

Integrase Strand Transfer Inhibitors

39
Q

What is the MoA of INSTIs?

A

They block the strand transfer effect of HIV integrase

Inhibit both HIV-1 AND HIV-2

40
Q

What is the 1st approved INSTI?

A

Raltegravir

41
Q

Define HAART

A

Highly Active Antiretroviral Therapy

42
Q

Define cART

A

combination Antiretroviral Therapy

blocks selection of mutants

43
Q

How does cART block the selection of mutants?

A

Due to combination therapy multiple mutations are required simultaneously for resistance to occur to all drugs in the regimen

44
Q

When should ART begin?

A 
History of AIDS-defining illness
Symptomatic HIV disease
CD4 count <350/ul
HIV-infected pregnant women
HIV-associated nephropathy
When treating HBV infection
Upon first diagnosis
45
Q

What is the ideal HAART regimen?

A

Two NRTIs + NNRTI/PI/INSTI

Tenofovir + Abacavir + Rilpiravirine/Darunavir/Raltegravir

A13AMC @ UoN (20 decks)

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