From the Guidelines
Rilpivirine is the NNRTI least associated with nausea. When considering NNRTIs for HIV treatment, rilpivirine typically causes fewer gastrointestinal side effects compared to other drugs in this class, as noted in the 2018 recommendations of the international antiviral society-USA panel 1. The standard dose is 25mg once daily, taken with a meal to optimize absorption. Other NNRTIs such as efavirenz have higher rates of adverse effects, including neuropsychiatric effects and rash 1. Rilpivirine's improved tolerability profile makes it a preferable option for patients who are at risk of nausea or other gastrointestinal disturbances. However, rilpivirine does have important limitations - it requires food for proper absorption, should not be used in patients with high viral loads (>100,000 copies/mL) or low CD4 counts (<200 cells/μL) at initiation, and is susceptible to resistance if adherence is poor, as outlined in the study 1.
Some key points to consider when prescribing rilpivirine include:
- It must be taken with a meal (at least 390 calories) to optimize absorption 1
- It should not be administered with proton-pump inhibitors; stagger dosing if given with an H blocker 1
- It is not recommended for patients with HIV RNA levels >100,000 copies/mL or CD4 cell count <200/μL because of increased risk of virologic failure 1
- It has a lower risk of metabolic adverse effects compared to other NNRTIs 1
- It has the lowest risk of rash among NNRTI-based therapies 1
From the Research
NNRTI Options
- Rilpivirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) that has been shown to have a better tolerability profile compared to other NNRTIs, such as efavirenz 2, 3, 4, 5, 6.
Comparison to Efavirenz
- Rilpivirine has been compared to efavirenz in several clinical trials, and has been found to have a lower rate of discontinuation due to adverse events, as well as lower rates of central nervous system effects, rash, and lipid abnormalities 2, 3, 4, 5, 6.
Nausea Association
- While the studies do not specifically mention nausea as a side effect, they do suggest that rilpivirine has a more favorable toxicity profile compared to efavirenz, which may imply that it is less associated with nausea 2, 3, 4, 5, 6.
Key Findings
- Rilpivirine has been found to be non-inferior to efavirenz in terms of efficacy, but has a lower rate of virologic failure in patients with baseline viral loads less than 100,000 copies/ml 3, 5, 6.
- Rilpivirine has also been found to have a higher rate of new resistance-associated mutations emerging at virologic failure, mainly in patients with baseline viral load greater than 100,000 copies/ml 6.