Isentress HD (and Isentress)
Isentress: One 400 mg film-coated tablet twice daily, with or without food, for people with HIV treatment experience or individuals who are new to HIV therapy.
Must be taken in combination with another antiretroviral(s) from a different drug class.
Isentress HD is for adults and children weighing at least 88 pounds (40 kg). Isentress is for adults and children weighing at least 4.4 pounds (2 kg). Both Isentress HD and Isentress can be taken with or without food.
Isentress (but not Isentress HD) pediatric formulations are available as an oral suspension. Isentress dosing is based on weight for children less than 55 pounds; see package insert for dosing and mixing instructions. Dosing of the granules for oral suspension is not equivalent to tablets. Do not substitute oral suspension for film-coated tablets.
Take missed dose as soon as possible, unless it’s closer to the time of your next dose. Do not double up on your next dose.
- See package insert for more complete information on potential side effects and interactions.
isentresshd.com
isentress.com
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JO-ANN JOSE, MD, MPH:
The raltegravir once-daily in the high-dose formulation is a pretty large pill, whereas the newer integrase inhibitors are smaller pills and once-daily dosing is standard. So I think for those reasons, raltegravir has less and less of a role in regimens now. There are people on raltegravir because they were on it historically and it works well for them. They are highly adherent to it and they don't want to switch for whatever reason. That's a legitimate reason to be on it. There are also people who are on raltegravir because they have drug interactions or other situations in which this might be the best drug for them, even though a better drug on paper may exist somewhere. So I think there's still room for these drugs in people's regimens, but not as much room as there was previously, and there may be good reasons to switch off it and consider something else. In pregnancy, raltegravir has to be given twice daily, which might present a challenge for adherence.
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, Cabenuva 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 such as 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. In pregnancy, raltegravir must be given at 400 mg twice daily. 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.
In general, raltegravir is very well tolerated with infrequent side effects. Those reported in up to 3–4% of study participants include insomnia, nausea, headache and fatigue. The side effect profile in children is comparable to adults. INSTIs have been associated with weight gain.
Isentress may cause elevated levels of creatine phosphokinase (CPK, a muscle enzyme). Inform your provider or pharmacist if you have a history of rhabdomyolysis, myopathy or increased creatine phosphokinase, 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 (such as depression, sleep disturbances and dizziness) in some retrospective cohort studies and case series. The HHS guidelines recommend closely monitoring people with pre-existing psychiatric conditions on an INSTI. Chewable tablets contain phenylalanine, which can be harmful to people with phenylketonuria.
Isentress HD was approved in 2017. While the original formulation, Isentress, was well tolerated and highly effective, its twice-daily dose was considered by some as a relative inconvenience. According to HHS HIV treatment guidelines, raltegravir was downgraded from a preferred component of an initial regimen in most individuals to a component of a regimen in only certain clinical situations due to the higher pill burden as well as the relatively lower genetic barrier against the development of resistance compared to second generation INSTIs. Raltegravir-based regimens may be preferred for people with high cardiovascular risk. Raltegravir along with Truvada or Descovy is a preferred drug regimen for PEP (post-exposure prophylaxis—preventing HIV acquisition after a potential exposure), as well as two other regimens: Biktarvy or Tivicay plus Truvada or Descovy. Isentress, but not Isentress HD, is one of the preferred INSTI medications 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, but the powder formulation remains a preferred initial regimen for newborn and infant treatment and PEP following birth.
Pregnant individuals can voluntarily enroll in the Antiretroviral Pregnancy Registry through their provider; GO TO apregistry.com.
JUAN MICHAEL PORTER II:
Isentress (raltegravir) was the first ever integrase inhibitor. One of my colleagues calls it the most well tolerated drug of its class. Few people complain of side effects, but it does have a couple of drawbacks: It has to be taken with a regimen containing two other drugs—meaning you could be taking up to three individual tablets a day—and it has a lower barrier to drug resistance than other options. That said, it is safe and easy to use for pregnant people and among people who experience side effects from dolutegravir.