For treatment-experienced patients with viral strains resistant to an NNRTI and other antiretroviral drugs only
One 200 mg tablet, twice daily with food. Approved for adults and children 2 years and older weighing at least 22 pounds (10 kg). See the package insert for specific weight-based dosing in children. Also available in 25 mg and 100 mg tablets. Must be taken in combination with another antiretroviral(s) which does not contain medication from the same drug class.
Take missed dose as soon as possible, unless it is closer to the time of your next dose. Do not double up on your next dose. People unable to swallow pills (Intelence tablets are “chalky”) can dissolve tablets in 1 teaspoon (5 mL) of water or at least enough liquid to cover the medication, stir well until the water turns milky, add more water if desired—use orange juice or milk as an alternative, always placing tablets in water first. Avoid warm (over 104° F) or carbonated beverages. Drink immediately, rinse the glass several times with water, orange juice, or milk and completely swallow the rinse each time to make sure the entire dose is taken. Taking Intelence without food could result in a 50% decrease in the drug absorption and may lead to HIV drug resistance.
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- See package insert for more complete information on potential side effects and interactions.
- Tell your provider or pharmacist about all medications, herbals, and supplements you are taking or thinking of taking, prescribed or not, as there are other drug interactions which are not listed here.
Generally well tolerated, but most common side effects include rash as well as numbness, tingling, or pain in the hands or feet. Rare side effects include severe rash and peripheral neuropathy. Discontinue Intelence immediately if signs or symptoms of severe skin reactions or hypersensitivity reactions develop (including, but not limited to, severe rash or rash accompanied by fever, general malaise [general ill feeling], fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, facial edema, hepatitis, eosinophilia, or angioedema). Levels of liver enzymes called transaminases should be monitored. Rash is associated with all of the current NNRTIs, but if you develop a rash from Intelence, you may still be able to take one of the other NNRTIs.
If Intelence is taken in combination with a protease inhibitor, the PI must be boosted with low-dose Norvir. Avoid Intelence with boosted Aptivus or Lexiva. It should be avoided with Tivicay unless administered with one of the following combinations: Reyataz/Norvir, Prezista/Norvir, or Kaletra. Taking it in combination with Selzentry requires a Selzentry dose adjustment to 600 mg twice daily when used without a boosted PI and 150 mg twice daily when used with a boosted PI. Do not take Intelence with Tegretol, Luminal, Dilantin, Priftin, Rifadin, or the herb St. John’s wort. Use with caution when combined with the antifungals Diflucan and Vfend. Dose adjustments of the antifungals ketoconazole, itraconazole, and posaconazole may be needed. Dosage adjustments of certain cholesterol medications may be needed based on clinical response, including Lipitor, Lescol, Mevacor, Livalo, and Zocor. Monitor the effectiveness of Coumadin (warfarin) and adjust dose as needed based on clinical response. Alternatives to Plavix should be considered when used with Intelence. Alternatives to clarithromycin, such as azithromycin, should be considered for treatment of MAC. Lower Valium dose may be needed. Use caution with systemic dexamethasone or consider alternatives. Intelence can be taken with Mycobutin 300 mg daily; however, it should be avoided by those who are also taking a boosted PI. Intelence can be safely combined with methadone or buprenorphine with additional monitoring for potential signs of withdrawal. Intelence can also be safely combined with Viagra, Cialis, and Levitra, though a dosage adjustment of Viagra may be necessary. Can be taken with Daklinza (increase Daklinza dose to 90 mg). Interactions with Sovaldi and Harvoni have not been studied; but based on the metabolism, a clinically significant interaction is not expected. Taking with Olysio, Viekira Pak, or Zepatier is not recommended.
For patients who have had virologic failure on an NNRTI-containing regimen, do not use Intelence in combination with a nucleoside backbone alone. Although taking once daily is not FDA approved, some providers are prescribing Intelence once daily (2 of the 200 mg tablets) based on clinical trials that showed that once-daily Intelence was not inferior to Sustiva-based regimens. In Europe, it is approved as a once-daily medication. The once-daily dosing may improve patient adherence. The TRIO study reported the combination of Intelence with Prezista/Norvir and Isentress in highly treatment-experienced patients was successful in getting many patients to undetectable. Some patients complain of hard-to-swallow, large chalky pills; see dissolving instructions in dose section or package insert. For individuals with HIV-2, commonly found in some other countries, an NNRTI would not be recommended as HIV-2 is inherently resistant to NNRTIs.
Etravirine is a second-generation NNRTI that has shown significant viral load reduction in individuals who developed resistance to the first generation of NNRTIs (efavirenz and nevirapine). Like other NNRTIs, etravirine’s drug-drug interactions are many and complicated. It is important to understand the interactions and inform the doctor of all over-the-counter medications, supplements, and herbals. They might affect the absorption of etravirine. It is well tolerated but may cause some rare side effects like rash or increased cholesterol. It is a good second-line alternative for treatment-experienced people. The size of the pill makes it hard to swallow and it leaves a chalky taste in the mouth. There is the option of dissolving it in water.