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25 Cards in this Set
- Front
- Back
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resistance patterns ___>___>___? ADR ___<___<___? |
resistance: PI > NNRTI > INSTI - PI: higher barrier of resistance = need more mutations to stop drug from working (better) - INSTI: Low barrier of resistance= need low amt of mutations to stop drug from working (worse) ADR: PI < NNRTI < INSTI |
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NRTI (Nucleoside Reverse Transcriptase Inhibitors) CLASS BBW? other ADEs? which drugs at ↑ or ↓ risk of ADEs? which drugs have BBW hep B flare? which drugs have renal adjustment req'd? which drug require HLA-B*5701 testing? |
BBW: lactic acidosis, & severe hepatomegaly w/ steatosis (fatty Δ) - mitochondrial tox (periphaeral neuropathy, pancreatitis, muscle atrophy) - (↑ risk) ddI>D4T>ZDV>>>TDF/3TC/FTC/ABC (↓ risk) Hepatitis B flare (BBW): TDF, emtricitabine (FTC), lamivudine (3TC) renal adj req'd: TDF, TAF (not enough data), emtricitabine (FTC), lamivudine (3TC) testing--abacavir |
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NRTI-Tenofovir DF (TDF) BBW? other ADEs? (7) ___ adjustment req'd? |
BBW: hepatitis B flare - HA, N/V/D - osteopenia (study stat sig ↓ hip & spine bone mineral density in TDF, than TAF) - renal insufficiency - fanconi syndrome (glucose & AAs lost through urine, causes bone & kidney damage) renal adjustment req'd |
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NRTI-Tenofovir AF (TAF) BBW? other ADEs? (7) ___ adjustment req'd? |
BBW: hepatitis B flare - HA, N/V/D - ↑ TC, LDL, HDL, TG - ↓ risk bone mineral density & renal tox (than TDF) -generally well tolerated :) renal adjustment req'd |
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NRTI-emtricitabine (FTC) BBW? other ADEs? (1) ___ adjustment req'd? |
BBW: hepatitis B flare - HYPERpigmentation of palms & soles (esp those w/ darker pigmentation already) - generally well tolerated :) renal adjustment req'd |
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NRTI-abacavir (ABC) BBW? testing? what's it called? ___ adjustment req'd? |
BBW: hypersensitivity rxn, if have ≥2 Sx groups d/c drug: 1. F 2. rash 3. N/V/D 4. fatigue 5. dyspnea/SOB, cough, pharyngitis testing: CI--HLA-B*5701 pos hepatic adjustment req'd |
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INSTI (Integrase Strand Transfer Inhibitor) CLASS - does this class have higher or lower barrier of resistance? - rash & ↑CPK (raltegravir > or < dolutegravir) - what INSTI combo brands have CrCL contraindications & what are the contraindications? |
no class ADRs documented generally well tolerated :) lower barrier to resistance (need low amt of mutations to stop drug from working (bad)) *R*ash (*R*altegravir > dolutegravir) ↑CPK (dolutegravir > raltegravir) CI: CrCl < 70 mL/min (start), CrCl <50 mL/min (during) - {Genvoya} (Elvitegravir, Cobicistat, Emtricitabine & Tenofovir AF) - {Stribild} (Elvitegravir, Cobicistat, Emtricitabine & Tenofovir DF) |
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INSTI-dolutegravir (DTG) ADEs DDI ___ adj? |
- HA,Insomnia - Rash (raltegravir > dolutegravir) - ↑CPK (dolutegravir > raltegravir)→ marker for Myopathy, Rhabomylsis - ↑LFT (Esp in HCV or HBV infection) - ↑SCr 0.1-0.2 (benign, inhib SCr excretion, not kidney issue, plateau in 2-3 weeks) DDI: tk DTG 2hrs before or 6hrs after cations (Al, Ca, Fe, Mg) renal adj note: effective in some INSTI resistance |
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INSTI-elvitegravir (EVG) ADEs DDI boosting req'd? tk w/ or w/out food? |
- HA,Fatigue, Depression, Rash, N/V/D DDI: separate antacids by 2 hrs boosting req'd (w/ ritonavir or cobicistat) EVG must be given w/ PI & ritonavir; {Stribild} or {Genovya} canbe given alone tk w/ food note: cross resistance w/ raltegravir |
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INSTI-raltegravir (RAL) ADEs DDI/CI what about its dosing makes it different from other INSTIs? |
- HA,N/D - Rash (raltegravir > dolutegravir) - ↑CPK (dolutegravir > raltegravir)→ marker for Myopathy, Rhabomylsis CI/DDI: Al, Mg antacids - Ca antacids safe Note: BID dosing; effective in experienced Pts |
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PI (Protease Inhibitors) CLASS (card 1/2) - ADEs (~5) - DDIs (3) - tk w/ or w/out food? - which recommended for preg? |
- Metabolicdisturbances (HYPERglycemia, HYPERlipidemia, etc) - InsulinResistance - Lipodystrophy--fat in diff locations - GI (N/V/D) - EKG Δs DDIs: opioids, statins, anything w/ narrow therapeutic index - all PIs tk w/ food! - preferred agent in preg: atazanavir (ATV) & lopinavir(LPV/r, KAL)/ritonavir(RTV) {Kaletra} |
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PI (Protease Inhibitors) CLASS (card 2/2) - which have hepatic adj? - which renal & hepatic adj? - which boost? - which UNboost or boost? |
- hepatic adj: darunavir (DRV), fosamprenavir (FOS-APV or FPV), lopinavir(LPV/r, KAL)/ritonavir(RTV) {Kaletra} - renal & hepatic adj: atazanavir (ATV) - BOOST: darunavir (DRV), lopinavir(LPV/r, KAL)/*ritonavir*(RTV) (already boosted) - UNboost OR boost: ~ atazanavir (ATV), boost when give w/ TDF/TAF ~ fosamprenavir (FOS-APV or FPV), unboosted have DDI antacids & H2RAs |
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PI-atazanavir (ATV) ADEs (4) DDI (req what type of environment for abs?) ___ adj req'd? is food or no food req'd? is boosting req'd? if so w/ what drug? CI or indicated for preg? |
- Indirecthyperbilirubinemia - Nephrolithiasis,Cholelithiasis - Potential PR prolong - note: Less metabolic issues vs other PIs DDI: Requires acidic environment for abs (PPI, H2RA & Antacids ↓drug levels) - renal & liver adj req'd - food req'd - can be UNboosted - boosting req'd when ATV given w/ tenofovir (TDF, TAF) ~ note: alt PI Tx for naive Tx: atazanavir(PI,ATV) + (ritonavir or cobicistat or none) + {Truvada} OR {Descovy} - Preferred agent in Pregnancy |
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PI-darunavir (DRV) ADEs DDI what if Pt has sulfa allergy? ___ adj req'd? tk w/ or w/out food? is boosting req'd? |
- Rash (SJS & TEN) - HA - abd discomfort (N/V/D) - HYPERlipidemia, HYPERglycemia DDI: methadone (monitor for w/drawl Sx) - caution (not CI) sulfa allergy - hepatic adj req'd - tk w/ food - boosting req'd ~ note: alt PI Tx for naive Tx: darunavir(PI,DRV) + cobicistat + {Truvada} OR {Descovy} note: useful for experienced Pts or resistant virus |
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PI-fosamprenavir (FOS-APV or FPV)--note not really available anymore ADEs DDI - what if Pt has sulfa allergy? - is boosting req'd? ___ adj req'd? tk w/ or w/out food? |
- Rash, HA,N/V/D - Nephrolithiasis DDI: - boosted: don't worry about antacids or H2RAs - UNboosted: antacids (2hr before, 1hr after); H2RA (≥2hrsbefore) - Contains sulfa moiety (Use caution but not CI) - hepatic adj req'd - tk w/ food - tk boosted or UNboosted (refer to DDI part) |
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PI-lopinavir(LPV/r, KAL)/ritonavir(RTV) {Kaletra} (only avail as combo) ADEs DDI ___ adj req'd? tk w/ or w/out food? is boosting req'd CI or indicated for preg? |
- DIARRHEA!! - asthenia (abnormal physical weakness/↓energy) - dyslipidemia (esp TG) DDI - disulfram rxn (metronidazole & alcohol solution)--no OH! - oxycodone (↓dose) - hepatic adj - tk w/ food - boosting req'd (hence the "ritonavir" combo...duh) - recommended w/ preg |
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PI/PK enhancer-ritonavir (RTV) ADEs indication CI w/ what drug? |
- N/V/D - Taste Δ - Hepatotoxicity - Rash - Dyslipidemia - ↑ CV events (MI, Ischemia) indication: PI that's ONLY used for boosting - not w/ nelfinavir (NFV) (will cause toxic levels) in alcohol soln (worry about disulfram rxn) |
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NNRTI (Non-Nucleoside Reverse Transcriptase Inhibitors) CLASS ADEs? (4) which have liver adjustments req'd? which tk w/ food? which tk w/ NO food? note: PO only |
- rash (including Steven Johnson's Syndrome) - ↑ LFTs - long t1/2 (except delavirdine(DLV)) - sig cross resistance - sig DDIs liver adj req'd: efavirenz (EFV), nevirapine (NVP) tk w/ food: rilpivirine (RPV), etravirine (ETR) tk w/ NO food: efavirenz (EFV) |
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NNRTI-Efavirenz (EFV) ADEs DDIs? __ adj req'd? tk w/ or w/out food? |
- vivid/abnormal dreams - insomnia, drowsiness, dizziness, hallucinations - false pos cannabinoid & BZD screens DDI: CYP 3A4 inhibitor & inducer, tacrolimus, sirolimus, cyclosporine, simvastatin, atorvastatin, oral contraceptives - hepatic adj req'd (?evidence?) -tk on EMPTY stomach, avoid high fat snacks |
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NNRTI-rilpivirine (RPV) ADEs DDIs? (what drugs CI?) tk w/ or w/out food? requires what for abs? |
- rash, HA, depression, insomnia -↑ risk failure in CD4<200, or VL>100,000 DDIs - CYP3a inhibitor & substrate - CI dexamethasone >1dose - CI PPI - H2RA (H2RA≥12 hrsbefore or ≥ 4 hrsafter) - Antacids (antacids 2 hrsbefore or 4 hrsafter) requires FOOD (390-540 kcal) & acidic environment for abs |
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NNRTI-etravirine (ETR) ADEs DDIs? tk w/ or w/out food? |
- rash (including SJS) - N/D, dyslipidemia, ↑LFTs, peripheral neuropathy -DDI: PDE5 req ↑dose -tk w/ food! info, not ADEs: -active against several NRTI mutations, high barrier to resistance, experienced Pts only - tabs can be dissolved in H20 (tk immediately after dissolve) |
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NNRTI-nevirapine (NVP) ADEs ___ adjustment req'd? CI CD4 levels in males & females (@ initial phase)? lead pd req'd, for how long? |
- rash - severe acute hepatitis (CD4 count related, occurs in 1st 6-8wks of Tx) & asymptomatic hepatitis (treat through, has ↑LFTs) - hypersensitivity rxn (rash, F, hepatitis, arthralgias) - hepatic adj req'd CI (@ initial phase): - males: CD4>400 - females: CD4>250 req lead in pd: 200mg x2wk, then ↑ to 400mg) |
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CCR5 Antagonist-maraviroc (MVC) ADEs DDI |
- N/V/D,HA, Fatigue - URI,Cough - OrthostaticHypotension (Dose dependent, Adjust dose in ↓ CrCl) DDI: 3A4 inhibitors/inducers (dose adjust), pgp pump (dose adjust) note: req CCR5 tropism; experienced Pts only! |
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Fusion inhibitor-enfuviritide (T20/ENF) ADEs |
- inj site rxn - bacterial pneumonia no DDIs note: experienced Pts, SC only |
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PK Enhancer-Cobicistat (COBI) ADEs DDI tk w/ or w/out food? what drugs studied/indicated w/? |
- N/V/D,Rash - Dyslipidemia - ↑LFT - Jaundice,Ocular Icterus - ↑SCr 0.1-0.2 (benign, inhib SCr excretion) DDI: CYP 3A4 inhibitor tk w/ food note: Only studied/indicated with Atazanavir, Darunavir, Elvitegravir |
