Pharm/Antiretrovirals Flashcards
Enfuvirtide
fusion inhibitor
Fusion inhibitors adverse effects
Injection site reactions
Risk of bacterial pneumonia
Maraviroc class
fusion inhibitor
Maraviroc MoA
Chemokine receptor 5 antagonist prevents virus from entering host cell
Enfuvirtide MoA
synthetic peptide that binds gp41 of viral envelope and prevents conformational change needed for viral fusion
Maraviroc adverse effects
Cough, pyrexia, rash, M/S, CYP3A interactions
What do the pyrimidine nucleoside analogs end in?
-udine or -abine
MOA for NRTIs?
two-fold
Competitive inhibitor of v-RT
DNA chain termination
NRTIs indication
Prevent acute infection of susceptible cells
Little effect on those already infected
What drug is used when an HIV+ mother gives birth
Zidovudine
Which 2 drugs are primarily metabolized by glucuronidation?
Zidovudine and raltegravir
What 2 NRTI drugs should be taken without food?
Zidovudine and didanosine
NRTI metabolism
does not use P450 system, excreted unchanged in urine with some exceptions
How is abacavir metabolized?
By alcohol dehydrogenase
Common toxicities of NRTIs
GI distress
Lactic acidosis due to mito DNA damage
Which drug has the worst incidence of lactic acidosis?
Stavudine
Zidovudine important toxicities
myelosuppression
Didanosine important toxicities
pancreatitis; peripheral neuropathy
Stavudine side effects
pancreatitis; peripheral neuropathy
Don’t drink and ____
take abacavir
WHy is tenofovir special?
NucleoTide RT inhibitor
Only needs 2 P events for activation
Why are nucleotide RT inhibitors more rapid than nucleoside RT inhibitors?
2 P vs 3 P events
Tenofovir MOA
inhibit v-RT
What is truvada and what is it used for?
Tenofovir + emtricitabine
useful for chemoprophylaxis
What are the NNRTIs?
Delavirdine
Nevirapine
Efavirenz
NED never nods
NNRTIs MOA
Binds RT causing conform change to block activity; doesn’t need +P
What is the best NNRTI?
Efavirenz…it’s “favirable”
Which NNRTI is a CYP3A inhibitor?
Delavirdine; the other two are inducers
How are NNRTIs metabolized?
P450
What are the common adverse effects of NNRTIs?
Maculopapular rashes on trunk and extremities
What is the one integrase inhibitor?
Raltegravir
Raltegravir MOA
Inhibits integrase
Raltegravir metabolism?
glucuronidation in liver; no P450 stuff
How are the protease inhibitors named?
end in -avir (except Abacavir)
What is the indication for protease inhibitors?
Most effective ART
Effective for both acute and chronic infections
Effective for both monocytes and macrophages
How are PIs metabolized?
P450
PIs and drug interactions?
Potent inhibitor of P3A4
Which PI is the strongest P3A4 inhibitor?
Ritonavir
What are some cons about ritonavir?
P3A4 inhibition
Autoinduction of metabolism
hepatotoxic at high doses
Common adverse effects of PIs?
Lipodystrophy - buffalo hump neck
Unique side effect of indinavir
Kidney stones
Unique side effect of atazanavir
hyperbilirubinemia
