ART ADE Flashcards
Enfurvitide
BID SQ injections, local reaction, sclerotic lesion
Fostemsavir
Nausea, diarrhea
Ibalizumab
IV only
Dizziness, diarrhea, nausea, rash
Maraviroc
Rash
Hepatotoxicity
INSTIs
Weight gain
esp Dolutegravir + TAF, Biktarvy
DTG
BIC
Increase in CrCl by inhibition of OCT2 transporter
EVG
Combined with cobi so GI sx, DDI, increase Cr
RAL
Fewest drug interactions among INSTI
Elevated CK
Proximal myopathy (with normal CK)
SJS/TEN
ddI
D4T
Mitachondrial and metabolic effects: Lactic acidosis Hepatic steatosis Myopathy Cardiomyopathy Peripheral Neuropathy Pancreatitis Lipodystrophy
Neuropathy and lipodystrophy irreversible (or partially)
ddI
D4T
ZDV
Hyperlipidemia
ABC
Hypersensitivity Reaction (+HLAB*5701)
Cardiovascular risk?
FTC
Discoloratoin of skin, nails, tongue
TAF
Weight gain
Renal (CI if CrCl <30)
BMD
(less than TDF)
Monitoring same as TDF:
- Cr - baseline, 2-8 weeks, Q3-6mo
- UA - baseline, Q6mo
- Serum phos if CKD
TDF
Bone demineralization
Screening:
-DXA postmenopausal women and men >50
Nephrotoxicity:
-Decreased GFR, Phosphate wasting, Fanconi Syndrome
ZDV
Bone marrow suppression
Myopathy (up to 17%)
Fatigue
Lipoatrophy
EFV
QTc prolongation Dyslipidemia Hepatotoxicity Neuropsychiatric Rash
ETR
Rash (mild-moderate)
NVP
Hypersensitivity reaction with life-threatening rash and/or hepatotoxicity
-Can be accompanied by fever, fatigue, myalgias/arthralgias, blisters, oral lesions, conjunctivitis, facial edema, eosinophila,
RPV
QTc prolongation (avoid if other QTc prolonging med) Elevated Cr (inhibition of tubular secretion) Neuropsychiatric (but <<< than efavirenz)
Ritonavir
Inhibits CYP450 3A enzyme
GI side effects
Cobicistat
Inhibits CYP3A enzyme
Reduces tubular secretion of creatinine via competitive inhibition of MATE1 secretion - Benign increase in Cr and (not true) decrease in GFR
-Typically Cr rises 0.1-0.15 in first 8 weeks then stabilizes
—-> Change in Cr >0.4 suggests other cause
GI symptoms
PIs
More GI side effects than other classes
—Older PIs worse than newer PIs
Cardiovascular risk
- –HLD, insulin resistance, premature atherosclerosis, MI
- —–Only indinavir and lopinavir-ritonavir w clear MI association
Prolonged PR, AV block (avoid r-boosted PIs if conduction defects or other PR prolonging meds)
Bleeding risk in hemophilia
Indinavir
Lopinavir-ritonavir
MI risk association
Atazanavir-ritonavir
Lopinavir-ritonavir
Saquinavir-ritonavir
Prolonged PR and AV block
Saquinavir-ritonavir
Prolonged QTc
Indinavir
Saquinavir
Lipaccumulation, especially with thymadine-analog NRTIs (d4T and ZDV)
Atazanavir
Lower potency
Hyperbilirubinemia (indirect from inhibition of conjucation)
Nephrolithiasis (occurs average 2 years after starting) with rod-shape crystals, stones Ca phosphate or atazanavir - often radiolucent)
–Can have crystal nephropathy without stones (rising Cr or sterile pyuria)
Cholelithiasis (rare)
Darunavir
Abdominal pain/diarrhea - up to 14%
Rash 10%, usually mild within first mo then resolves
- –Severe rash with fever +/- tranaminitis 1%
- —–Increased risk with sulfa allergy (not contraindication)
Indinavir
Nephrotoxicity
Twice daily
Urologic and renal abnormalities: Dysuria, flank pain, renal colic, hematuria, crystalluria, nephrolithiasis, AKI, CKD, papillary necrosis)
—Nephrolithiasis in 1/5
Lopinavir-ritonavir
Hyperlipidemia (esp total cholesterol and TG)
Diarrhea
Alcohol in liquid formulation (do not give to pregnant women or with disulfiram or metronidazole)
High pill burden
Ritonavir liquid formulation
Alcohol in liquid formulation (do not give to pregnant women or with disulfiram or metronidazole)
Saquinavir
High pill burden
Prolongd QTc and PR, increases risk of AVB and TdP
—Should not be taken with other QT prolonging meds or if hx prolonged QT
Tipranavir
High pill burden
Intracranial hemorrhage
Hepatotoxicity
—Contraindicated w class B or C hepatic insufficiency
Bictegravir
Dolutegravir
Rilpivirine
Cobicistat
Increase Cr by inhibition of tubular Cr secretion but don’t impact true GFR
DTG
Headache
Insomnia
Greater weight gain than other ART
