Palopag

Indications

Selexipag is used for the long-term treatment of pulmonary arterial hypertension (PAH), a condition in which the blood vessels in the lungs become narrow and the pressure in them rises, putting strain on the right side of the heart. It helps delay the worsening of the disease and is used alone or together with other PAH medicines.

How It Works

Selexipag and its active breakdown product attach to the prostacyclin (IP) receptor on blood vessel walls. This relaxes and widens the lung blood vessels, lowers the pressure in them and reduces the workload on the heart. It also helps slow the thickening of the vessel walls.

Dosage and Administration

Use as prescribed by a specialist. Treatment starts at a low dose taken twice a day, and the dose is increased step by step, usually once a week, until the highest dose you can tolerate is reached. Your doctor will tell you your exact dose. Swallow the tablets whole with water, preferably with food, which helps reduce side effects. Do not stop suddenly; if you miss several days, ask your doctor before restarting because a lower dose may be needed.

Interactions

Strong CYP2C8 inhibitors such as Gemfibrozil must not be used with Selexipag because they greatly raise its level. Clopidogrel and other moderate CYP2C8 inhibitors also raise its level and the dose may need to be reduced. Rifampicin and similar enzyme inducers can lower its effect. Other medicines that lower blood pressure may add to its effect. Tell your doctor about all medicines you take.

Contraindications

• Allergy to Selexipag or any ingredient
• Severe coronary heart disease or unstable angina
• Heart attack in the last 6 months
• Uncontrolled heart failure not under close medical care
• Severe irregular heartbeat
• Stroke or mini stroke in the last 3 months
• Heart valve defects that affect heart function, not related to pulmonary hypertension
• Use with strong CYP2C8 inhibitors such as Gemfibrozil

Side Effects

Common side effects are headache, diarrhoea, nausea, vomiting, jaw pain, muscle and joint pain, pain in the arms or legs and flushing. These are often worse while the dose is being increased. Low blood pressure, dizziness, anaemia (low red blood cells), reduced appetite, rash and changes in thyroid tests can also occur.

Get urgent medical help if you faint, have severe breathlessness, chest pain, swelling of the face, lips or throat, or if breathing suddenly gets worse, which may be a sign of fluid in the lungs.

Pregnancy and Lactation

There is little information on use in pregnancy and it is generally not recommended. Women who could become pregnant should use reliable contraception during treatment. It is not known if it passes into breast milk; breastfeeding is not recommended during treatment.

Precautions and Warnings

Your blood pressure, blood count and liver and thyroid function may be checked. Take care with moderate liver problems or severe kidney problems. If you develop signs of fluid in the lungs, the doctor will check for a related condition called pulmonary veno-occlusive disease. Dizziness may affect driving.

Overdose

Too much may cause headache, flushing, nausea, vomiting, diarrhoea and low blood pressure. Seek medical help; treatment is supportive.

Therapeutic Class

Prostacyclin (IP) receptor agonist, medicine for pulmonary arterial hypertension

Storage

Store below 30°C in a dry place, away from light and out of the reach of children.