Selexipag

What is selexipag?

• selexipag (UPTRAVI) is a prostacyclin receptor agonist used to treat pulmonary arterial hypertension.

What are the uses of this medicine?

• This medicine is used to treat pulmonary arterial hypertension (PAH) which is high blood pressure in the arteries of your lungs.
• UPTRAVI can help slow down the progression of your disease and lower your risk of being hospitalized for PAH.

How does this medicine work?

• Selexipag (se lex' i pag) is a selective prostacyclin receptor agonist that is used to treat pulmonary arterial hypertension (PAH).
• Inhibition of the prostaglandin receptors disrupts the intracellular pathways that lead to vasoconstriction, thus causing vasodilation.
• Because these receptors are found in highest concentration in the lungs, selexipag primarily causes vasodilation in the pulmonary vasculature and decreases pulmonary vascular pressure.
• In prospective, randomized controlled trials, selexipag was effective in alleviating symptoms, improving exercise capacity and prolonging the time to clinical worsening in patients with idiopathic PAH.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• take gemfibrozil because this medicine may affect how UPTRAVI works and cause side effects.

What drug interactions can this medicine cause?

• Concomitant administration of UPTRAVI with strong inhibitors of CYP2C8 (e.g., gemfibrozil) is contraindicated.
• Increase dose up to twice of UPTRAVI when co-administered with rifampin. Reduce UPTRAVI when rifampin is stopped.

Is this medicine FDA approved?

• It was approved for use in the United States in 2015.

How should this medicine be used?

Recommended Dosage: UPTRAVI tablets starting dose:

• 200 mcg twice daily.
• Increase the dose by 200 mcg twice daily at weekly intervals to the highest tolerated dose up to 1600 mcg twice daily.
• Maintenance dose is determined by tolerability.

Moderate hepatic impairment:

• Starting dose 200 mcg once daily, increase the dose by 200 mcg once daily at weekly intervals to the highest tolerated dose up to 1600 mcg.

• Use UPTRAVI for injection in patients who are temporarily unable to take oral therapy.
• Administer UPTRAVI for injection twice daily by intravenous infusion at a dose that corresponds to the patient's current dose of UPTRAVI tablets.
• Administer UPTRAVI for injection as an 80-minute intravenous infusion.

Administration UPTRAVI tablets

• Take UPTRAVI exactly as your healthcare provider tells you to take it. Do not stop taking UPTRAVI unless your healthcare provider tells you to stop.
• Your healthcare provider will slowly increase your dose to find the dose of UPTRAVI that is right for you.
• If you have side effects, your healthcare provider may tell you to change your dose of UPTRAVI.
• UPTRAVI can be taken with or without food. Taking UPTRAVI with food may help you tolerate UPTRAVI better.
• UPTRAVI is usually taken 2 times each day.
• Swallow UPTRAVI tablets whole. Do not split, crush or chew UPTRAVI tablets.
• If you miss a dose of UPTRAVI, take it as soon as you remember. If your next scheduled dose is due within 6 hours, skip the missed dose. Take the next dose at your regular time.
• If you miss 3 or more days of UPTRAVI, call your healthcare provider to see if your dose needs to be changed.
• If you take too much UPTRAVI, call your healthcare provider or go to the nearest hospital emergency room right away.

UPTRAVI given by intravenous (IV) injection

• Your healthcare provider will give you UPTRAVI into your vein through an intravenous (IV) line.
• Your healthcare provider will decide how much UPTRAVI for injection you will receive each day, based on your current dose of UPTRAVI tablets.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 200 mcg, 400 mcg, 600 mcg, 800 mcg, 1000 mcg, 1200 mcg, 1400 mcg, 1600 mcg.
• For Injection: 1800 mcg of selexipag as a lyophilized powder in a single-dose vial for reconstitution and dilution.

This medicine is available in fallowing brand namesː

• UPTRAVI

What side effects can this medication cause?

The most common side effects of this medicine include:

• headache
• jaw pain
• muscle pain
• pain in arms or legs
• pain in joints
• decreased appetite
• diarrhea
• nausea
• vomiting
• flushing
• low red blood cell count
• rash

What special precautions should I follow?

• Pulmonary edema in patients with pulmonary veno-occlusive disease. If confirmed, discontinue treatment.

What to do in case of emergency/overdose?

• Mild, transient nausea was the only reported consequence.

Management of overdosage:

• In the event of overdose, supportive measures must be taken as required.
• Dialysis is unlikely to be effective because selexipag and its active metabolite are highly protein-bound.

Can this medicine be used in pregnancy?

• There are no adequate and well-controlled studies with UPTRAVI in pregnant women.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

• Active ingredient: selexipag
• Inactive ingredients: glycine, phosphoric acid, polysorbate 20, and sodium hydroxide.

Who manufactures and distributes this medicine?

Manufactured for: Actelion Pharmaceuticals US, Inc. a Janssen Pharmaceutical Company South San Francisco

What should I know about storage and disposal of this medication?

UPTRAVI tablets

• Store at 20°C to 25°C (68°F to 77°F).
• Excursions are permitted between 15°C and 30°C (59°F and 86°F) .
• Keep out of reach of children.

Storage conditions for UPTRAVI for injection:

• Store the original carton containing glass vial in a refrigerator at 2°C to 8°C (36ºF to 46ºF) until use in order to protect from light.

• Dailymed label info on Selexipag
• FDA Selexipag

Selexipag Resources
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