HIV Therapy

Question 1

What is the makeup of HAART therapy?

Answer 1

2 Nucleoside reverse transcriptase inhibitors and
1 Non nucleotide reverse transcriptase inhibitor or
1 Protease Inhibitor or
1 Integrase Inhibitor

Question 2

What are the protease inhibitors?
MOA
Use
SE

Answer 2

They all end in NAVIR (never tease a protease)

Prevent pol gene from making proteases that cut the long polyprotein mRNA into functional parts

Ritonavir is P450 inhibitor (can’t get RIT O’ drugs with RITOnavir)

SE: Hyperglycemia, GI Intolerance (n/v diarrhea), Lipodystrophy,

Indinavir - Nephropathy, Hematuria,

Question 3

What are the NRTIs?
MOA
Use
SE

Answer 3

Inhibit reverse transcriptase then terminate DNA chain. Have to be PO4’d first bc they are NUCLEOSIDES

Competitively inhibit nucleotide binding to RTase and terminate the DNA chain bc they don’t have a functional 3’OH group.

Tenofovir is only NucleoTide so doesn’t need to be PO4’d

Zidovudine: Preggo prophylaxis and general prophylaxis, causes anemia tho

SEs: Bone marrow suppression (reverse with GM-CSF) and EPO

Peripheral Neuropathy, lactic acidosis

Pancreatitis from Didanosine

Question 4

What are the NNRTIs?
MOA
Use
SE

Answer 4

Neva Efa Deliva this disease
Nevirapine
Efavirenz
Delavirdine

Work like NRTIs but have a different structure so bind in a different spot. NO PO4’N required

SE:
Rash and Hepatotox
Vivid dreams and CNS SYMPTOMS with Efa

Deliva and Neva are not for preggos

Question 5

What is the Integrase Inhibitor?
MOA
Use
SE

Answer 5

Raltegravir (InteGRAVe Inhibitor)

Blocks HIV from integrating into host DNA by reversibly inhibiting viral integrate

SE: Hypercholesterolemia
(High cholesterol sends you to the GRAVE)

Question 6

What are the fusion inhibitors?
MOA
Use?

Answer 6

Enfurvitide (no fun invite)
Blocks gp41 so no VIRAL ENTRY
Skin Rxn at entry site

Maraviroc
Mavericks bind at 120%
Binds CCR5 on T cells / monocytes, so p120 can’t bind there. PREVENTS ATTACHMENT