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HIVManagement.org |
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etravirine |
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Detailed Prescribing Information |
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May 2011 |
| etravirine = Intelence | |
| Forms Available | 100 mg, 200 mg dispersible tablets |
| Dosing |
Take 2 x 100 mg tablets twice a day or 1 x 200
mg tablets twice a day, both with food Although not approved for once daily dosing, the pharmacokinetics of etravirine would support it. |
| Meal dependence | Food increases absorption of etravirine |
| Contraindication | None |
| Adverse Effects |
10% incidence of rash Elevated ALT, AST approximately 7% which is more common in the setting of hepatitis B or C coinfection (26%) |
| Interactions |
etravirine
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Tipranavir/ritonavir may produce a significant decrease in etravirine levels - tipranavir/ritonavir should not be co-administered Maraviroc:
Increases digoxin levels - initiate therapy at lowest dose and monitor digoxin levels Decreases levels of amiodarone, bepridil, disopyramide, flecainide, lidocaine - antiarrhythmics should be administered with caution and levels should be monitored if possible Warfarin levels are increased - monitor INR carefully Anticonvulsants carbamazepine, phenobarbital, phenytoin decrease etravirine levels and produce possible loss of therapeutic effect - etravirine should not be co-administered Antifungals fluconazole, voriconazole: fluconazole and voriconazole significantly increases etravirine exposure - both agents should be used with caution Antifungals itraconazole, ketoconazole, posaconazole: concentrations of etravirine may be increased while concentrations of itraconazole and ketoconazole may be decreased - dose adjustments for these antifungal agents may be necessary Clarithromycin exposure was decreased while 14-hydroxy-clarithromycin concentrations were increased. Alternatives to clarithromycin should be considered when treating Mycobacterium avium complex. Rifampin, rifapentine are potent inducers of CYP450 enzymes and decrease etravirine concentrations and produce loss of therapeutic effect - neither agent should be co-administered with etravirine Rifabutin should be adminstered at 300 mg daily if not co-adminstered with a ritonavir-boosted protease inhibitor --> if etravirine is co-administered with darunavir/ritonavir, lopinavir/ritonavir, or saquinavir/ritonavir, rifabutin should not be co-administered due to possible loss of therapeutic effect of etravirine |
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| Resistance Profile | Etravirine is a second-generation NNRTI that was approved in late 2007. It's resistance profile is distinct from that of the the first-generation NNRTIs. In particular it maintains full susceptibility to the K103N mutation, and unlike the first generation NNRTIs it loses its activity only after 3 or more mutations that include the following: V90I, A98G, L100I, K101E, K101P, V106I, V179D, V179F, Y181C, Y181I, Y181V, G190A, and G190S. |
| Suggested lab follow-up | Liver profile at 30 days and every 2-3 months and as indicated |
| Warning | Severe, potentially life-threatening and fatal skin reactions have been reported, including Stevens-Johnson syndrome, hypersensitivity reaction, toxic epidermal necrolysis and erythema multiforme. Etravirine should be immediately discontinued for severe hypersensitivity, severe rash, or rash with systemic symptoms or liver transaminase elevations develops. |
| Complete prescribing information | http://www.intelence-info.com |
| Links to Antiretroviral Sections (click on anything) |
| Nucleoside & Nucleotide Reverse Transcriptase Inhibitors (NRTI) |
| AZT | ddI | d4T | 3TC | ABC | FTC | TDF | Combivir | Trizivir | Epzicom | Truvada |
| Nonnucleoside Reverse Transcriptase Inhibitors (NNRTI) |
| etravirine | nevirapine | delavirdine | etravirine | rilpivirine |
| Protease Inhibitors (PI) | Boosted Protease Inhibitors |
| saquinavir | indinavir | ritonavir | nelfinavir | lopinavir + ritonavir | atazanavir | fosamprenavir | tipranavir |
| Fusion Inhibitors |
| enfuvirtide |
Updated 5.23.2011