Isentress and Isentress HD

In general, raltegravir is very well tolerated with infrequent side effects. Those reported in up to 3–4% of study subjects include insomnia, nausea, and headache. The side effect profile in children is comparable to adults. New data associate INSTIs and TAF with weight gain; see “Weighty Concerns,” beginning on page 8, and go to aidsinfo.nih.gov. Isentress may cause elevated levels of creatine kinase (a muscle enzyme). Inform your provider or pharmacist if you have a history of rhabdomyolysis, myopathy, or increased creatine kinase, or if you also take medications that may contribute to these conditions such as statins, fenofibrate, or gemfibrozil. INSTIs have been associated with adverse neuropsychiatric effects in some retrospective cohort studies and case series. The DHHS guidelines recommend closely monitoring people with pre-existing psychiatric conditions on an INSTI. Chewable tablets contain phenylalanine, which can be harmful to patients with phenylketonuria.

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 not listed here. It is important to take Isentress HD and Isentress only with other HIV drugs recommended by your provider because they and similar drugs are contained in other HIV medications: Biktarvy, Genvoya, Stribild, Tivicay, Triumeq, Dovato, and Juluca. Isentress HD cannot be used with rifampin, but Isentress can; increase Isentress to 800 mg twice daily when using rifampin. Remember to decrease the raltegravir back to its original dose when you finish taking rifampin. There are no data on dosing of the chewable tablets with rifampin. There is no need to increase the raltegravir dose with rifabutin. With both Isentress HD and Isentress, avoid Gaviscon and other antacids containing aluminum or magnesium. Calcium-containing antacids like Tums (calcium carbonate) can be used with Isentress, but not Isentress HD. Other acid reducers (such as Pepcid, Zantac, Prilosec, and Prevacid) are okay to use. Raltegravir is not recommended with carbamazepine or phenobarbital. Raltegravir can be used with Harvoni, Zepatier, or Epclusa. Unlike Isentress, Isentress HD cannot be used with Intelence or boosted Aptivus.

Isentress HD was approved in 2017. While the original formulation, Isentress, was well tolerated and highly effective, its twice-daily dose was seen by some as a small inconvenience. According to DHHS HIV treatment guidelines, most INSTIs on the market are recommended as components of initial ART regimens for most people; Isentress HD has been added to this list. Raltegravir-based regimens may be preferred for patients with high cardiovascular risk. Isentress is the preferred INSTI medication in HIV treatment guidelines for pregnancy, 400 mg twice a day in combination with 2 NRTIs. In pediatric HIV guidelines, Isentress was downgraded in 2017 from “preferred” to an “alternative” part of an initial regimen for children ages 6–12.

Dr. Ross Slotten says:

Isentress was the first INSTI approved in 2007. At the time of approval, it offered another potent option for patients who were resistant to other medications, like efavirenz. Initially, it was approved for twice-daily dosing. A bit too late, its manufacturer, Merck, developed a once-daily formulation, but by that time Tivicay had become available. And now there are STRs containing another INSTI, rendering Isentress a less ideal option. Nevertheless, Isentress HD has few interactions with other medications. In combination with TDF/FTC, it retains a B1 status with DHHS experts.

Activist Bridgette Picou says: Isentress HD and Isentress can be used for both treatment-naïve and treatment-experienced patients, in particular those who have not taken integrase inhibitors before with multi-drug resistance. The 600 mg Isentress HD tablet is two pills taken once daily, and the 400 mg tablet is one pill twice a day. This medication is also part of the current guidelines for use in PEP (post-exposure prophylaxis) prevention regimens