HIV antivirals mod 2

Question 1

Antiretrovirals

Answer 1

HAART or (ART): Highly Active (Antiretroviral Therapy)
Reason we use HAART instead of monotherapy?
Treatment goals:
Delay or reverse loss of immune function
Decrease AIDS-related complications
Prolong life
Benefits vs. drawbacks of HAART
Pricy, long-term side effects, serious drug interactions, take for life

Question 2

classes

most PO

Answer 2

Reverse Transcriptase Inhibitors
- Nucleoside Reverse Transcriptase Inhibitors
 --------Zidovudine (Retrovir)
- Non-nucleoside Reverse Transcriptase Inhibitors
 ------ Efavirenz (Sustiva)
Protease Inhibitors
- Raltegravir (Isentress)*
Integrase Inhibitors
- Lopinavir/Ritonavir (Kaletra)
HIV entry Inhibitors
- Fusion Inhibitors
 ------ Enfuvirtide (Fuzeon)*
- CCR5 Antagonists
------ Maraviroc (selzentry)*

Question 3

Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

Zidovudine (Retrovir)(AZT)

must be in combo

Answer 3

MOA: Inhibit reverse transcriptase
used with other drugs: Decreases viral load
Delays onset of AIDS
Reduces symptom severity

SE: Severe anemia and neutropenia
Lactic acidosis in female or obese persons

Question 4

Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs)

Efavirenz (Sustiva)

Answer 4

MOA: Inhibit reverse transcriptase
AE: Rash
CNS symptoms

drug interactions: Inhibits and induces Cytochrome P450 system

very long half life

Question 5

Integrase Inhibitor

Raltegravir (Isentress)

Answer 5

MOA: Inhibits integrase
well tolerated
drug interactions - Metabolized by an enzyme known as UGT
Caution with UGT inhibitors or inducers

Question 6

Protease Inhibitors
Lopinavir/Ritonavir (Kaletra)

most effective, looks like cushing’s disease

Answer 6

MOA: Inhibits protease
Adverse effects:
-Hyperglycemia
-Lipodystrophy
-Hyperlipidemia
Bone loss
-Drug interactions?yes, cyp 450

Question 7

Fusion Inhibitor

Enfuvirtide (Fuzeon)

no significant drug interactions

Answer 7

MOA: Blocks entry of HIV into CD4 T cells
SE: Injection site reactions
Pneumonia
Hypersensitivity

Question 8

CCR5 Antagonist

Maraviroc (Selzentry)

black box: liver!

Answer 8

Maraviroc (Selzentry)
MOA: Blocks entry into CD4 cells
Only works with certain strains of HIV
Problems with resistance?
Adverse effects: Black Box Warning
Liver injury
Drug interactions
A substrate of CYP 3A4