Isentress HD (and Isentress)
Standard DoseIsentress HD: Two 600 mg film-coated tablets once daily for individuals new to HIV therapy (treatment-naïve) or who are virologically suppressed (have undetectable viral load) on an initial regimen of Isentress.
Isentress: One 400 mg film-coated tablet twice daily for people with HIV treatment experience; this Isentress dose may also be taken by those new to HIV therapy.
Isentress HD is for adults and children weighing at least 88 pounds (40 kg). Isentress is for adults and children weighing at least 4 pounds (2 kg). Both Isentress HD and Isentress can be taken without regard to food.
Isentress (but not Isentress HD) pediatric formulations are available as an oral suspension and flavored chewable tablets. Isentress dosing is based on weight for children less than 55 pounds; see package insert for dosing. The chewable tablets may be chewed or swallowed whole. Do not substitute chewable tablets or 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.
ManufacturerMerck and Co.
AWPIsentress HD: $1,800/month
Isentress 400 mg: $1,800/month
Potential Side Effects and Toxicity
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. 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.
Potential Drug 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 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, and Triumeq. 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 Daklinza, Harvoni, Olysio, Sovaldi, Viekira Pak, Zepatier, or Epclusa. Unlike Isentress, Isentress HD cannot be used with Intelence or boosted Aptivus.
Isentress HD was approved in 2017. While the previous version, Isentress, was well tolerated and highly effective, its twice-daily dose was seen by some as a small hindrance. According to DHHS HIV treatment guidelines, all 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 last year for children ages 6–12.
See package insert for more complete information on potential side effects and interactions.
Dr. David Hardy says:
Isentess HD was approved by the FDA in May 2017. It was developed to offer the option for a once-daily Isentress regimen. It’s hard to imagine what the advantage of taking two Isentress HD plus another pill, all once daily, would be over taking one of the single-tablet regimens. Isentress was the first integrase approved, in 2007. It is the only INSTI which must be taken twice daily. Early clinical trials demonstrated very rapid (and still the most rapid) drops in viral loads (compared to protease inhibitor and NNRTI regimens), suggesting that it was more potent than older classes of antiretrovirals. However, we soon learned that this rapid drop in viral load did not correlate with resistance to HIV resistance, as this occurs at a rate similar to that for Atripla. At the time when Isentress was approved, it provided a critical new medication for many individuals who had run out of treatment options and kept them alive. With the development of newer once-daily INSTIs (Tivicay) and STRs (Stribild, Genvoya), the usefulness of Isentress has waned in favor of simpler ART regimens.
Activist Moisés Agosto-Rosario says:
Raltegravir is an INSTI used in combination with other HIV antivirals. It is for use in adults and children. For children, it is formulated as an oral suspension or as chewable tablets. The addition of raltegravir to the menu of HIV treatment options is welcome by those with drug resistance and not able to build a new regimen. There is a 600 mg film-coated tablet once a day and a 400 mg film-coated tablet twice a day. Raltegravir has demonstrated to be effective and well tolerated. Concerns about drug resistance exist, but its quick effect in suppressing HIV has made it a choice not only for those with multidrug resistance but for those starting treatment for the first time.