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Naplex
HIV
35
Pharmacology
Not Applicable
06/26/2011

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Term
NRTI MOA
Definition
Binds to catalytic site of reverse transcriptase and interferes with HIV viral RNA-dependent DNA polymerase, resulting in inhibition of viral replication.
Term
NRTI Black Box
Definition
Lactic acidosis and severe heapatomegaly with steatosis. Toxicities include peripheral neuropathy, pancreatitis, lipoatrophy, myopathy, anemia.
Mainly eliminated by the kidney.
Term
Abacavir + lamivudine
(Ziagen) + (Epzicom)
Definition
Must screen for HLA-B*5701 allele (increased hypersen rxn)
BB: hypersen rxn: fever , rash, CI upset
Term
NRTIs
Definition
Abacavir + lumivudine
Didanosine
Emtricitabine
Lamivudine
Tenofovir + emtricitabine
Term
Didanosine BB
Definition
pancreatitis
avoid combo with stavudine
Peripheral neuropathy
Term
Emtricitabine BB
Definition
May exacerbate HepB once drug is d/c
Term
Lamivudine BB
Definition
Do not use Epivir-HBV for tx of HIV
Term
Stavudine BB
Definition
Pancreatitis
Term
Tenofovir + emtricitabine BB
Definition
May exacerbate Hep B once d/c
Term
NNRTI MOA
Definition
Binds to reverse transcriptase and blocks the RNA-dependent and DNA-dependent DNA polymerase activities including HIV-1 replication
Term
NNRTI Class Effects
Definition
rash, most common with nevirapine, increased LFT's
Mainly cleared by liver
Term
NNRTIs
Definition
Delavirdine
Efavirenz
Etravirine
Nevirapine
Term
PI MOA
Definition
inhibits HIV-1 protease and renders the enzyme incapable of cleaving the gag-pol plyprotens, resulting in the production of immature, noninfectious virions.
Term
PI Class Effects
Definition
hyperglycemia, insulin insensitivity, fat redistribution and lipodystrophy, increased bleeding with heophilia, hyperlipidemia, rare hypersensitivity rxs. Strong inhibitors of 3A4
Term
PIs
Definition
Ataznavir
Darunavir
Ritonavir
Lopinavir + Ritonavir= Kaletra
Term
Entry Inhibitors MOA
Definition
Inhibit the fusion of the HIV-1 virus with the CD4 cells by blocking the conformational change in gp41
Enfurviritide
Term
CCR5 Antagonist MOA
Definition
Binds to the CCR5 receptor on the CD4 cells nad prevents the conformational change required for cell entry
Maraviroc
Term
Intigrase Inhibitors MOA
Definition
Inhibits the catalytic activity of HIV-1 integrase, thus preventing the insertion of HIV DNA into the host genome and virus cannot replicate
Raltegravir
Term
Indications to initiate ART
Definition
History of AIDs-defining illness
CD4 count <350
pregnant
HIV-associated nephropathy
Coninfected with HBV when HBV treatment indicated
Term
ART recgimens for treatment-naive HIV patients
Definition
NNRTI + 2NRTIs or
PI (prefer ritonavir) + 2NRTIs or
INSTI + 2NRTIs
Term
Preferred Regimens
Definition
Efavirenz+Tenofovir+Emtricitabine
Atazanavir+Ritonavir+Tenofovir+Emtricitabine
Darunavir+Ritonavir+Tenofovir+Emtricitabine
Raltegravir+Tenofovir+Emitricitabine
Term
Preferred Pregnancy Regimen
Definition
Lopinavir+Ritonavir+Zidovudine+Lamivudine
Term
When to initiate ART?
Definition
history of AIDS-defining illness
or
CD4 <500
or
pregnant, HIV-nephropathy, HEP B
Term
Emtricitabine (Emtriva)
+efavirenz and tenofovir (Atripla)
Definition
Atripla: tk on empty stomach hs
BB: exacerbates Hep B when dc
Hyperpigmentation of palms
Term
Tenofovir (Viread)
Definition
BB: may exacerbate Hep B once dc
Term
NNRTIs Class Effects
Definition
All can cause a rash
Increase LFT's
Mainly cleared by the liver
Term
Efavirenz (sustiva)
Definition
Tk on empty stomach hs
Preg D
strong inducer of 3A4
Term
Atazanavir (Reyataz) SE
Definition
May prolong the PR interval, nephrolithiasis, hyperbilirubinemia
Term
Darunavir (Prezista)
Definition
Tk with food
Must be given with ritonavir
Caution with sulfa allergy
Term
Ritonavir (Norvir)
Definition
Tk with food
Store capsules in fridge
BB:interacts dangerously with other meds
Term
Ritonavir (Norvir)
Definition
Tk with food
Store capsules in fridge
BB:interacts dangerously with other meds
Term
Lopinavir + Ritonavir (Kaletra)
Definition
solution tk with food
Fatal pancreatitis
Strong 3A4 inducer
Term
Enfuvirtide (Fuzeon)
Definition
injection site rxns, pneumonia, hypersensitivity rxns
Term
Maraviroc(Selzentry)
Definition
Med will not work with CXCR4-tropic disease
BB: hepatotoxicity
CI: 3A4 inhibitors or CrCl<30
Term
Raltegravir(Isentress)
Definition
Immune reconstitution syndrome, myopathy, increased CPK, rhabdo
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