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Flashcards in HIV Drugs Deck (10):
1

Enfuvirtide/Fuzeon

Fusion inhibitor; Binds gp41

SubQ injection

AE: Injection site reaction, increased rate of bacterial pneumonia, hypersensitivity

2

Maraviroc

CCR5 antagonist (only works against CCR5-tropic virus)

Consider use if failed 2 regimens or other ART

Blocks co-receptor to viral entry

Metabolized by p450

AE: cough, fever, rash, URT infection, abdominal pain, postural dizziness

3

Raltegravir

Intregrase inhibitor

approved for patients that have failed other treatments

Rifampin can enhance elimination, Divalent cations may inhibit actions

4

Zidovudine (AZT), lamivudine (3TC), emtricitabine, abacavir (ABC)

Nucleoside analogues

Inhibit revers transcriptase

AE: Pancreatitis, peripheral neuropathy, myopathy, cardiomyopathy, heaptic steatosis, lipid dystrophy

Zidovudine- induced anemia and neutropenia
Abacavir- hypersensitivity (HLA dependent)

All are renal eliminated (dose adjusted w/ renal insufficiency)
p450 metabolism

5

Tenofovir

Nucleotide analogue

Does not require phosphorylation

6

Efavirenz, delavirdine, nevirapine

Non-Nucleoside reverse transcriptase inhibitors

inhibit reverse transcriptase but do not act at the active site

Nevirapine- Rash (steven-johnson syndrome reported), hepatitis (substrate for CYP450 and inducer of 3A)
Efavirenz- teratogenic in animals

7

Ritonavir, lopinavir, amprenavir

Protease inhibitor

AE: N/V/D, hyperglycemia, lipodystrophy, hyperlipidemia, hepatotoxicity, osteonecruses/osteopenia/osteoporosis

Inhibitor of p450 (ritonavir used to prolong action of other drugs)

8

NNRTI based regiments

Efavirenz + tenofovir/emtricitabine or zidovudine/lamivudine
except for pregnant women or women with pregnancy potential

9

PI based regiments

Lopinavir/Ritonavir+ (tenofovir/emtricitabine or zidovudine/lamivudine)

10

Integrase based regiments

Raltegravir + (tenofovir/emtricitabine or zidovudine/lamivudine)