Pharm - HIV Flashcards
HAART
Highly Active Antiretroviral Therapy
Strongest indication for use of HAART
low CD4+ count
high viral load
3 drug regimen (goal of combos)
prevent resistance
3-drug regimen (actual drugs)
2 NRTIs and 1 of the following
NNRTI or protease inhibitor or integrase inhibitor
NRTIs and ADME - what is their involvement with cytochrome P450?
virtually none
CYP3A4 neutral
NRTIs
route of admin for NRTIs
oral
route of metabolism for Abacavir
metabolized by alcohol dehydrogenase
Abacavir - potential interactants
wild turkey 101, jack daniels, dickel, four roses, woodford, jim beam, early times, johnny walker, patron, RBVs, pipe bombs, gin + juice, jager bombs …
you have counseled your patient not to drink alcohol while one this drug. What drug did ou prescribe?
Abacavir
route of admin for NNRTIs
oral
NNRTIs involvement with CYP metabolism
substrate, inhibitor,or inducer
Woman of childbearing age just got prego while taking an oral contraceptive. What drugs could have potentially allowed this?
Efavirenz and Nevirapine
Efavirenz and Nevirapine involvement with CYP
induce 3A4
How are oral contraceptives metabolized
3A4
oral contraceptives are effective unless…
they are effective as long as they are not metabolized too quickly
what does any drug that is inducer of 3A4 put the pt at risk for
failure of oral contraceptives
what else is a potential interactant with Abacavir?
bud diesel, nasty light, silver bullets, busch, steel reserve, cobra 40, high life, keystone
If you are giving pt Efavrienz, what two drugs would you need to increase their dose if giving concurrently
rifampin and rifabutin
why do you need to increase the dose of some drugs given concurrently with Efavirenz
rifampin and rifabutin –> metabolized by 3A4, so need to generate clinically relevant levels
Protease inhibitors and ADME
all involved with CYP somehow
what 2 drugs would be contraindicated with Protease inhibitors
rifampin and rifabutin -
Protease inhibitors and 3A4
they all inhibit
drug to give to “boost” other drugs (buzz word)
Ritonavir
reason for giving ritonavir with other drugs to “boost”
Ritonavir inhibits 3A4, 2D6, pgp, UGT –> help to keep levels of other drugs high, drugs that are metabolized by 3A4
what drugs did Sweatman mention specifically for giving with Ritonavir to “boost”
Arunavir, Lopinavir
What is the only drug (HIV)that is not given orally
Enfuviritide
route of admin for Enfuviritide
subQ
Drug that is not an antiviral that is given to “boost” (buzz word pt 2)
Cobicistat
Cobicistat MOA
Cyp3A4 inhibitor
methodology of Cobicistat
same idea as Ritonavir boosting -
advantage of Cobicistat
may avoid some of the toxicitiy you could see with Ritonavir boosting
What 2 drugs specifically are mentioned to use with Cobicistat
Darunavir and Atazanavir
Why do you worry about you pt stopping or starting the use of another drug?
that is when the serum drug levels of your drug can change
pts w/ HIV are susceptible to what (generalities here)
opportunistic infections
drugs used to treat fungal opportunistic infections
Azoles
Azoles and ADME
Cyp3A4 - potential for interaction
Voriconzaole does what (ADME wise)
inhibits 2C9 and 3A4
pt has TB, that comes up after imuunosuppression - you got to your script pad - what do you write them?
Rifampin
what should you have chekced for before writing that script?
potential drug interactions - Rifampin is a 3A4 inducer
Atripla
tenofovir, emtricitabine, efavirenz
There are only 2 combos we talked about in class that are once daily pills that constitute a complete regimen
Atripla, Stribild
there is another HIV combo drug in the notes that is listed as once daily that constitutes a complete regimen
Complera
class wide side effect of NRTIs
hepatic disease, lactic acidosis
class wide effect of NRTIs - might manifest how
pancreatitis (“elevation of enzyme levels, pain radiating to back”)
neutropenia (NRTI)
Zidovudine
neuropathy (NRTI)
Stavudine»_space; didanosine
something that can occur (more likely in women, especially fat ones) due to chronic prolonged exposure to these HIV regimens
obesity and prolonged exposure –> hepatic problems and lactic acidosis - more frequent in this population
Didanosine - counsel your patients to not do what
coldbeers
why cannot pts taking Didanosine not drink coldbeer?
b/c it has potential for hepatic toxicity
what other NRTIs can the pt not drink while on?
mentions stavudine, probably all of them - they all have some risk for hepatic disease
NNRTIs
Nevirapine has all the BBWs - Rash and hepatotoxicity, and hepatitis
who is more prone to hepatic problems with nevirapine?
hello ladies
Nevirapine should not be used if you have a CD4 count of what or higher?
250
vivid dreams and CNS symptoms
efavirenz
contraindicated during pregnancy
Delaviridine and efavirenz
Protease inhibitors
GI intolerance - pts don’t like them
Protease inhibitors - fat
lipodystrophy - bufallo hump
protease inhibitors inhibit what else (not a CYP thing)
Glut4 - lead to hyperglycemia
Protease inhibitors also dyslipidemia - what is this bad for
predispose pt to CV issues
peripheral neuropathy
NRTIs Stavudine»didanosine
what else causes neuropathy
HIV itself - can confound in a pt being tx with NRTI
lipodystrophy
protease inhibitors
lipodystropy most common
Atazanivir (PI)
HAART in pregnancy
drugs can produce some mitochondrial dysfunction - can do so in developing neonate
But, advantage of HARRT in pregnancy
can prevent the transmission of infection maternal-fetal in pregnancy
NRTI recommended agents for HAART in pregnancy
lamivudine, zidovudine
NNRTIs and pregnancy
nevirapine
PIs and pregnancy
lopinavir, ritonavir
tx for CMV
valganciclovir - b/c has ganciclovir has shitty bioavailability - so give it as oral pro drug instead
M of resistance for valganciclovir
mutation in viral kinase (1st step of activation)
if mutation forms in viral kinase, what can you use as back up
foscarnet
elimination of valganciclovir
renal - glomerular filtration and active RTS
potential problems with valganciclovir and the fact that it goes through the kidney RTS (2)
1) competitive inhibition of RTS with another drug specific for same mech
2) renal failure
side effects of valganciclovir
renal toxicity, leukopenia, thrombocytopenia, neutropenia
Foscarnet - soluble or nah?
nahhhh
Foscarnet - what do you need pt to be
hydrated - can give saline
route of admin for Foscarnet
infusion pump - if you slam the IV, it will precipitate out in the blood
toxicity of Foscarnet
nephrotoxic
EBV
Vidarabine
route of admin for Vidarabine
to treat EBV of eye - topically
bioavailability of Vidarabine
poor - it is topical
risk of systemic effects w/ Vidarabine
low
Kaposi Sarcoma
Cidofovir
route of admin of Cidofovir
IV
clearance of Cidofovir
renal
toxicity of Cidofovir
nephrotoxicity
What can’t patient drink while on Abacavir
ALCOHOL