From the Guidelines
UPTRAVI (selexipag) must be titrated slowly to minimize side effects while achieving an effective therapeutic dose, with a recommended starting dose of 200 mcg twice daily and weekly increases of 200 mcg twice daily until reaching the highest tolerated dose, not exceeding 1600 mcg twice daily, as supported by the dosing guidelines outlined in the 2023 study published in Nature Reviews Rheumatology 1. The importance of slow titration lies in the management of dose-dependent side effects such as headache, diarrhea, jaw pain, nausea, and flushing, which are commonly associated with prostacyclin analogues like selexipag.
- These side effects are typically most pronounced during the initial titration phase and often decrease in intensity over time as the body develops tolerance.
- The slow titration approach allows for the adjustment of the dose based on the patient's tolerance, ensuring that the therapeutic benefits of selexipag in treating pulmonary arterial hypertension are maximized while minimizing adverse effects.
- The mechanism of action of selexipag, which involves the selective activation of the prostacyclin (IP) receptor to cause vasodilation and inhibit platelet aggregation, underscores the need for careful dose adjustment to achieve optimal clinical benefit without compromising patient safety and quality of life.
- As noted in the study, the dosing of selexipag, like other pulmonary hypertension-specific therapies, requires careful consideration of the potential risks and benefits, including the monitoring of liver enzymes and hemoglobin levels due to the risk of hepatotoxicity and anemia associated with certain therapies 1.
From the FDA Drug Label
Your healthcare provider will slowly increase your dose to find the dose of selexipag tablets that is right for you. If you have side effects, your healthcare provider may tell you to change your dose of selexipag tablets.
Selexipag (Uptravi) must be titrated slowly to find the right dose for the patient and to manage potential side effects. This approach allows the healthcare provider to monitor the patient's response to the medication and adjust the dose as needed to minimize adverse reactions.
From the Research
Dose Titration of Uptravi (Selexipag)
- Uptravi (selexipag) must be titrated slowly due to its dose-dependent adverse-effect profile, which includes nausea, vomiting, diarrhea, headache, and musculoskeletal pain 2.
- The recommended initial selexipag dosage is 200 μg twice daily, and it can be increased as tolerated up to a maximum dose of 1600 μg twice daily 3, 4.
- Slow dose titration is a common strategy used to reduce the risk of adverse events and improve tolerability, as seen in other medications such as topiramate 5.
- Although there is no direct evidence on the titration of selexipag in the provided studies, the general principle of slow dose titration to minimize adverse effects can be applied 6.
- The studies on selexipag focus on its efficacy and safety in the treatment of pulmonary arterial hypertension, rather than the specific titration schedule 2, 3, 4.