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HIV/ARV Agents- SIDE EFFECTS EDITION!
common side effects/ characteristics of ARV agents
26
Pharmacology
Graduate
10/27/2011

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Cards

Term
Maraviroc
Definition
hepatotoxicity
dizziness/OSH
increased CV events- MI (caution)
CYP3A4 Substrate
not 1st line
Tropism assay prior to tx!!!
Term
Enfuvirtide
Definition
bind to gp41
injection site reactions
inc. risk pneumonia
counseling points...
e$$pensive
not 1st line
Term
NRTIs
Definition
lactic acidosis with hepatic steatosis
(non specific s/sx)
NOT inhibitors OR inducers of CYP 450
RENAL DOSE (except for one..)
Term
Zidovudine
Definition
BONE MARROW SUPPRESSION
myopathy
nail pigmentation
NAUSEA, headache
antag. with d4T
can be used intrapartum
Term
Didanosine
Definition
pancreatitis
peripheral neuropathy
non-cirrhotic portal hypertension (?)
TDF incr. Cmax and AUC
WEIGHT based
usually ES. but if TDF usually with food
Term
Stavudine
Definition
lipoatrophy
hyperlipidemia
DI with AZT
WEIGHT BASED
not really used. womp womp.
Term
Lamivudine
Definition
well tolerated
hbv activity
flare if abrupt d/c
Term
Emtricitabine
Definition
well tolerated
hyperpigmentation of palms and soles
hpv activity
flare if abrupt d/c
Term
Abacavir
Definition
possible inc. risk of MI
hypersensitivity rxn- HLA-B*5701
no renal adj.! yayyy
Term
Tenofovir
Definition
nucleoTIDE- phosphorylated 2x
pretty well tolerated (mostly GI)
nephrotoxicity- monitor sCr
DI with ddI, ATV
activity against HBV
Term
NNRTIs
Definition
Rash
Hepatotoxicity
impact CYP system!
lower genetic barrier to resistance- NEED REAL GOOD ADHERENCE
Term
Nevirapine
Definition
heptotox. and rash more problematic
not recommended for women
HPV and HCV co-infection
CYP inducer
dose titration at start
Term
Efavirenz
Definition
CNS effects
mixed cyp inhibitor/inducer
food inc. concentrations (mickey's D)- Take on ES
Teratogenicity
+ cannabinoid test
Term
Delavirdine
Definition
less potent
TID
not used
Term
Etravirine
Definition
may be effective a/g NVP or EFV resistant strains
GI (if any)
NEED FOOD.. (food inc. absorption)
CYP3A4-inducer
not 1st line
BID (WITH FOOD)
tablets dispersable in water
Term
Rilpivirine
Definition
2nd. Gen.
avoid with high viral loads (>100,000)
taken with food, (high fat)
DI with acid reducing, dexamethasone
Term
Raltegravir
Definition
GI upset, HA, elevation in CPK (generally well-tolerated)
DI by UGT 131
BID
hepatic metabolism
Term
PI
Definition
resistance (BE MORE ADHERENT)
hepatic metabolism- no renal adjustment
lipodystrophy
changes in lipids
insulin resistance
elevated transaminases
GI upset
inc. bleeding in hemophiliacs
DRUG INTERACTIONS!!- all CYP3A4 Inhibitors
most must be taken with food
Term
Atazanavir
Definition
hyperbilirubinemia (cosmetic)
nephrolithiasis
OTc prolongation
skin rash
DI (see class ones)
acid reducing agents
tenofovir
standard doing- interaction based
Term
Darunavir
Definition
skin rash (sulfa moiety)
boosting needed
dosing based on experience
Term
Ritonavir
Definition
perioral paresthesias, taste disturbances, more GI intolerability, lipid abnl
boooooostaaah
dosing different in for use alone and for us in combo
refig capsules
Term
Lopinavir/ritonavir
Definition
gi and lipid abnml (TG)
pancreatitis
booster included
soln with food and refig.
dosing based on experience
Term
Fosamprenavir
Definition
sulfa moiety (caution)
unboosted- no req.
boosted- with food
susp- with food
prodrug of amprenavir
dosing based on experience
Term
Indinavir
Definition
nephrolithiasis, hyperbilirubinemia, ES if unboosted
Term
Nelfinavir
Definition
DIARRHEA
no boosting
Term
Tipranavir
Definition
Hepatitis, rash, ICH, sulfa moiety, ref. capsules, soln RT
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