Term
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Definition
| convert viral RNA to DNA; nucleoside analogs work as chain terminators; generally pick 2 from this class |
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Term
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Definition
| GI (nausea, vomiting, flatulence), lactic acidosis, liver steatosis; overall minimum drug interaction potential |
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Term
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Definition
| first HIV antiretroviral approved; active metabolite - myelosuppressive; comes in IV formulation for pregnant women |
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Term
| abacavir hypersensitivity |
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Definition
| class I allele (HLA-B*5701 high association with reaction; if positive test record as severe allergy and pt should NOT receive this drug |
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Term
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Definition
| metabolized by alcohol dehydrogenase and GT: EtOH may lead to increased drug which may worsen EtOH-related SEs and decreased alcohol tolerance |
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Term
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Definition
| fluorinated 3TC; very similar to 3TC: in resistance pattern, active against HBV (similar hep B warning) |
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Term
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Definition
| active against both HIV and HBV: similar warning with 3TC and FTC; with or without food (like most nukes) |
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Term
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Definition
| TFV 300 mg + FTC 200 mg daily |
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Term
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Definition
| 3TC 300 mg + ABC 600 mg daily |
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Term
| Nukes w/ the exception of ABC: |
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Definition
| dosing adjustment needed with CrCl < 50 mL/min; Atripla, Combivir, Trizivir, Epzicom: not recommended w/ CrCl < 50 mL/min; Truvada not recommended with CrCl < 30 mL/min |
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Term
| Hepatic impairment in Nukes |
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Definition
| ABC dose adjustment needed according to the Child-Pugh score |
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Term
| Lactic acidosis and severe hepatomegaly w/ steatosis |
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Definition
| stop ART especially nukes, re-evaluate therapy |
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Term
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Definition
| Drug interactions- extensively hepatic: CYP3A4, 2D6, 2C8.. (huge list of interactions) |
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Term
|
Definition
| Naïve or tx-experienced w/ no DVR mutations: 800 mg (with 100 mg RTV) daily; experienced w/ at least 1 DVR mutation: 600 mg (w/ 100 mg RTV) BID; take with food |
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Term
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Definition
| remains the preferred and most commonly prescribed NNRTI; metabolized by 3A4 (also induces), others |
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Term
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Definition
| newest NNRTI; approved June 2011; watch patients with viral load > 100,000, cross-class resistance (with efavirenz) |
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Term
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Definition
| Atripla, Complera: not recommended if CrCl <50mL/min |
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Term
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Definition
efavirenz: no recommendation: "use with caution"
nevirapine: use in pts w/ Child-Pugh Class B or C is contraindicated
etravirine, rilprivirine: no dose adjustment in pts w/ Child Pugh class A or B; not evaluated in Child-Pugh Class C |
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Term
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Definition
| potently and selectively binds to RTI enzyme; bioavailability is very good; well tolerated; resistance can develop quickly |
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Term
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Definition
| Ritonavir at 100-200 mg doses daily-BID; Advantages: increases AUC and Cmin, helps overcome inducing drug interactions, BID drugs to daily, decrease first PI pill burden; Cons: RTV drug interactions, $$ |
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Term
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Definition
mainly metabolized by CYP450 3A4 (substrates); also inhibitor of 3A4; Contraindication w/ statins (simvastatin, lovastatin)
drugs ot watch: amiodarone, astemazole, cisapride, ergots, statins, triazolam, rifampin |
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Term
| Atripla (efavirenz + emtricitabine + tenofovir) |
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Definition
| first triple combo to be taken once daily; should be taken on empty stomach and at bedtime due to CNS side effects |
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Term
| Complera (emtricitabine + rilpivirine + tenofovir) |
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Definition
| approved in Aug 2011- complete regimen indicated for tx-naive adults only |
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Term
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Definition
| prevents viral entry into cells- inhibits fusion; very large, complex manufactured protein |
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Term
|
Definition
| CCR5 inhibitor; testing required prior to start : Tropism- $1,960 |
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Term
|
Definition
| inhibits enzyme that integrates or splices the HIV DNA with host DNA |
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Term
|
Definition
| first integrase inhibitor; potent and well tolerated; also UGT1A1 metabolism |
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Term
|
Definition
| second integrase inhibitor- only available in combo; potent (most data in drug-resistant virus); 1 tab daily w/ food; only use pts with CrCl > 70 mL/min |
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Term
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Definition
| third integrase inhibitor; potent: well tolerated; UGT1A1 metabolized, some CYP3A4-- not recommended in Child-Pugh score C |
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Term
| How many antiretroviral meds make up a "typical" HIV regimen? |
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Definition
| 3 or 4 (e.g. 2 "nukes" + non-nuke or boosted PI) |
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