Selexipag
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Drug Status
Government Approvals
US(FDA), UK(BNF)
WHO Essential Medicine
NO
Known Teratogen
NO
Pharmaceutical Class
Prostacyclin Receptor Agonist
Controlled Drug Substance
NO
Selexipag
Summary
Selexipag is used to treat pulmonary arterial hypertension (PAH), a condition characterized by high blood pressure in the arteries of the lungs. It helps to slow the worsening of symptoms and reduce the risk of hospitalization.
Selexipag works by activating a receptor called the IP prostacyclin receptor. This leads to the relaxation of blood vessels in the lungs, which helps to reduce pulmonary arterial pressure and improve blood flow. This action alleviates symptoms of PAH.
The usual starting dose of Selexipag for adults is 200 micrograms taken by mouth twice daily. The dose may be increased at weekly intervals to the highest individually tolerated dose, which can range from 200 micrograms to 1600 micrograms twice daily.
The most commonly reported side effects of Selexipag include headache, diarrhea, nausea, and jaw pain. Serious adverse effects can include shortness of breath, rapid breathing, dizziness, and weakness.
Selexipag should not be used with certain medications like gemfibrozil. It is not recommended for use during pregnancy or breastfeeding. It is also contraindicated in patients with severe coronary heart disease, unstable angina, recent myocardial infarction, severe arrhythmias, and severe liver impairment.
Indications and Purpose
How does Selexipag work?
Selexipag works by activating the IP prostacyclin receptor, which leads to the relaxation of blood vessels in the lungs. This action helps reduce pulmonary arterial pressure and improves blood flow, alleviating symptoms of pulmonary arterial hypertension. It also has anti-proliferative and anti-fibrotic effects, contributing to its therapeutic benefits.
Is Selexipag effective?
Selexipag's effectiveness was demonstrated in a long-term, double-blind, placebo-controlled study involving 1,156 patients with pulmonary arterial hypertension (PAH). The study showed a 40% reduction in the occurrence of morbidity or mortality events compared to placebo. The beneficial effect was primarily due to a reduction in hospitalizations for PAH and other disease-progression events. The study also showed improvements in exercise capacity and a reduction in the risk of PAH-related death or hospitalization.
What is Selexipag?
Selexipag is used to treat pulmonary arterial hypertension (PAH) in adults, helping to slow the worsening of symptoms and reduce hospitalization risk. It works by relaxing blood vessels in the lungs, allowing blood to flow more easily. Selexipag is a selective nonprostanoid IP prostacyclin receptor agonist, which helps improve exercise capacity and manage PAH symptoms.
Directions for Use
For how long do I take Selexipag?
Selexipag is used for the long-term treatment of pulmonary arterial hypertension (PAH). It is important to continue taking it as prescribed by your doctor, even if you feel well, as it helps manage symptoms and reduce the risk of hospitalization. The duration of use is determined by your healthcare provider based on your condition and response to treatment.
How do I take Selexipag?
Selexipag should be taken by mouth, usually with food, twice a day at the same times each day. Swallow the tablets whole without splitting, chewing, or crushing them. There are no specific food restrictions, but it is important to follow your doctor's instructions and maintain a normal diet unless advised otherwise.
How should I store Selexipag?
Selexipag should be stored in its original container, tightly closed, and kept out of reach of children. It should be stored at room temperature, away from excess heat and moisture, and not in the bathroom. Unneeded medication should be disposed of through a medicine take-back program, not by flushing down the toilet.
What is the usual dose of Selexipag?
For adults, the usual starting dose of Selexipag is 200 micrograms taken twice daily, approximately 12 hours apart. The dose is increased in increments of 200 micrograms, usually at weekly intervals, to the highest individually tolerated dose, which can range from 200 micrograms to 1,600 micrograms twice daily. Selexipag is not recommended for use in children as its safety and efficacy have not been established in this population.
Warnings and Precautions
Can I take Selexipag with other prescription drugs?
Selexipag interacts with several medications. It should not be used with strong CYP2C8 inhibitors like gemfibrozil, as this increases exposure to the active metabolite. Moderate CYP2C8 inhibitors like clopidogrel may require dose adjustments. Inducers of CYP2C8, such as rifampicin, may reduce the effectiveness of Selexipag. Patients should inform their doctor of all medications they are taking to avoid potential interactions.
Can Selexipag be taken safely while breastfeeding?
It is unknown whether Selexipag or its metabolites are excreted in human milk. In animal studies, Selexipag or its metabolites were excreted in milk, and a risk to the suckling child cannot be excluded. Therefore, Selexipag should not be used during breastfeeding. Consult a doctor for advice on alternative treatments if necessary.
Can Selexipag be taken safely while pregnant?
Selexipag is not recommended during pregnancy due to a lack of data on its effects in pregnant women. Animal studies have not shown direct harmful effects on reproduction, but safety margins for potential effects are lower than for non-IP-related effects. Women of childbearing potential should use effective contraception while taking Selexipag. If pregnancy occurs, consult a doctor immediately.
Is it safe to exercise while taking Selexipag?
Selexipag is used to treat pulmonary arterial hypertension, which can improve exercise capacity by reducing symptoms like shortness of breath. However, if you experience any side effects that affect your ability to exercise, such as dizziness or weakness, consult your doctor. They can provide guidance on managing these symptoms and advise on safe exercise practices.
Is Selexipag safe for the elderly?
For elderly patients (65 years and older), no adjustment to the dose regimen is needed. However, there is limited clinical experience with Selexipag in patients over the age of 75 years, so it should be used with caution in this population. Elderly patients should be monitored closely for any adverse effects, and dose adjustments may be necessary based on their tolerance and response to the medication.
Who should avoid taking Selexipag?
Selexipag is contraindicated in patients with severe coronary heart disease, unstable angina, recent myocardial infarction, severe arrhythmias, and severe liver impairment. It should not be used with strong CYP2C8 inhibitors like gemfibrozil. Caution is advised for patients with hypotension, hyperthyroidism, or pulmonary veno-occlusive disease. Women of childbearing potential should use effective contraception, and Selexipag should not be used during pregnancy or breastfeeding.
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