200, 400, 600, 800, 1000, 1200, 1400 and 1600 micrograms film-coated tablets
selexipag
What Uptravi is and what it is used for
Uptravi is a medicine that contains the active substance selexipag. It acts on blood vessels in a similar way to the natural substance prostacyclin, which causes vessels to relax and dilate.
Uptravi is used for the long-term treatment of pulmonary arterial hypertension (PAH) in adult patients whose disease cannot be controlled by treatment with other types of anti-PAH drugs, so-called endothelin receptor antagonists, and phosphodiesterase 5 inhibitors. Uptravi can be used alone if these medicines are not suitable for the patient.
In PAH, the pressure is too high in the blood vessels that carry blood from the heart to the lungs (pulmonary arteries). In people with PAH, these arteries become narrower and the heart, therefore, has to work harder to pump blood through them. It can make you feel tired, dizzy, short of breath, or get other symptoms.
By mimicking the action of the natural substance prostacyclin, this medicine widens the pulmonary arteries and makes them less stiff. It then becomes easier for the heart to pump blood through the pulmonary arteries. Uptravi reduces the pressure in the pulmonary arteries, relieves the symptoms of PAH, and slows the progression of the disease.
What you need to know before you take Uptravi
Do not take Uptravi
- if you are allergic to selexipag or any of the other ingredients of this medicine (listed in section 6).
- if you have heart problems, for example:
- poor blood flow to the heart muscle (severe heart disease or unstable angina), with symptoms such as chest pain
- had a heart attack in the last 6 months
- weak heart (decompensated heart failure ) that is not under close medical control
- very irregular heartbeat
- heart valve defects (congenital or acquired) that cause the heart to function poorly (unrelated to pulmonary hypertension )
- if you have had a stroke in the last 3 months or any other event that reduced the blood supply to the brain (e.g. transient ischemic attack, so-called TIA ).
- if you are taking gemfibrozil (a medicine to reduce the number of fatty substances ( lipids ) in the blood).
Warnings and precautions
Talk to your PAH doctor or nurse before taking Uptravi if you
- taking medication for high blood pressure
- have low blood pressure with symptoms such as dizziness
- have recently had a major blood loss or fluid loss, e.g. severe diarrhea or vomiting
- have problems with the thyroid gland
- have severe kidney problems or are undergoing dialysis
- have or have had severe problems with the liver not working properly
If you notice any of the above signs or if your condition changes, tell your doctor immediately.
Children and young people
Do not give this medicine to children under 18 years of age. Uptravi has not been tested in children.
Elderly patients
Experience using Uptravi in patients older than 75 years is limited. Uptravi should be used with caution in this age group.
Other medicines and Uptravi
Tell your doctor if you are taking, have recently taken, or might take any other medicines.
Other medicines can affect the effect of Uptravi.
Talk to your PAH doctor or nurse if you are taking any of the following medicines:
- Gemfibrozil (used to reduce the number of fatty substances ( lipids ) in the blood)
- Clopidogrel (used to prevent blood clots from forming in coronary artery disease)
- Deferasirox (used to reduce the amount of iron in the blood)
- Teriflunomide (for the treatment of relapsing-remitting multiple sclerosis )
- Carbamazepine (to treat certain forms of epilepsy, nerve pain, or to manage severe mood swings when certain other medicines have not worked)
- Phenytoin (a drug for epilepsy )
- Valproic acid (medicine against epilepsy )
- Probenecid (a drug for gout )
- Fluconazole , rifampicin or rifapentine ( antibiotics against infection )
Pregnancy and breastfeeding
Uptravi is not recommended during pregnancy and breastfeeding. If you are a woman and could become pregnant, you must use effective contraception while taking Uptravi. If you are pregnant or breastfeeding, think you may be pregnant, or are planning to have a baby, consult your doctor before using this medicine.
Driving ability and use of machinery
Uptravi can cause side effects such as headaches and low blood pressure (see section 4), which may affect your ability to drive. The symptoms of your illness can also make you unfit to drive.
How to take Uptravi
Uptravi should only be prescribed by a doctor experienced in treating PAH. Always take this medicine as directed by your doctor. Consult a doctor if you are unsure or have any questions.
If you experience side effects, talk to your doctor, as he/she may recommend that you change your Uptravidose.
If you are taking other medicines, tell your doctor, as he/she may recommend that you take Uptravi only once a day.
If you have reduced vision or loss of vision, be sure to have someone help you when you take Uptravi during your dose titration period (the process of gradually increasing your dose ).
Find the right dose for you
When treatment begins, you start with the lowest dose one. The lowest dose is one 200-microgram tablet in the morning and one 200-microgram tablet in the evening, approximately 12 hours apart. It is recommended that the treatment be started in the evening. The doctor will give you instructions to increase the dose step by step. This is called “titration”. The titration allows the body to get used to the new drug. The goal is to find the most appropriate dose. The most appropriate dose is the highest maintenance dose that you can tolerate, but no more than 1600 micrograms in the morning and the evening.
The first pack of tablets you receive contains light yellow 200-microgram tablets.
The doctor gives you instructions to increase the dose step by step, usually once a week, but it can also be longer between increases.
At each step, add one 200-microgram tablet in the morning and one 200-microgram tablet in the evening. The first time you take the higher dose, it is recommended that it takes place in the evening. The chart below shows the number of tablets you should take each morning and each evening during the first four steps.
If your doctor tells you to increase the dose by one more, add one 200-microgram tablet in the morning and one 200-microgram tablet in the evening for each new step. The first time you take the higher dose, it is recommended that it takes place in the evening.
If your doctor tells you to increase the dose by one more and go to step 5, you can do this by taking one green 800 microgram tablet and one light yellow 200 microgram tablet in the morning and one 800 microgram tablet, and one 200 microgram tablet in the evening.
The highest single dose of Uptravi is 1600 micrograms in the morning and 1600 micrograms in the evening. However, not all patients reach this dose because different patients need different doses.
The diagram below shows how many tablets to take each morning and each evening in each step, starting at step 5.
You will receive the titration pack containing a titration guide and package insert. The titration guide contains information about titration. There you can write down the number of tablets you take each day.
Remember to write down the number of tablets you take each day in the titration diary. Each stage lasts about a week. If your doctor tells you to continue with a step for longer than a week, there are extra pages in the diary where you can continue to write. Remember to talk to your PAH doctor or nurse periodically during titration.
Step down to a lower dose due to side effects
During titration, you may experience side effects such as headache, diarrhea, nausea, vomiting, jaw pain, muscle pain, leg pain, joint pain, or facial flushing (see section 4). If you have difficulty coping with the side effects, talk to your doctor about how they can be managed or treated. Some treatments can alleviate the side effects. Pain and headaches can, for example, be treated with painkillers such as paracetamol.
If the side effects cannot be treated or do not gradually improve on the dose you are taking, your doctor may change the dose by reducing the number of light yellow 200 microgram tablets that you take, one in the morning and one in the evening. The diagram below shows how to taper down to a lower dose. Do this only if your doctor has told you to.
If the side effects can be managed after you have reduced the dose, the doctor may decide that you should stay on that dose. See the maintenance dose section below for more information.
Maintenance dose
The highest dose you can tolerate during the titration phase will be your maintenance dose. The maintenance dose is the dose that you should continue to take regularly.
Your doctor will prescribe an appropriate tablet strength for the maintenance dose. Then you only need to take one tablet in the morning and one in the evening in the future, instead of several.
A full description of the Uptravi tablets, with color and marking, can be found in section 6 of this leaflet.
Your doctor may adjust your maintenance dose later if necessary.
If you get side effects that you cannot tolerate or side effects that affect your daily life, after taking the same dose for a long time, you should contact your doctor because the dose may need to be lowered. The doctor can then prescribe a tablet with lower strength. Remember to handle unused tablets correctly (see section 5).
Take Uptravi once in the morning and once in the evening about 12 hours apart.
Take the tablets with a meal because you can tolerate the medicine better then. The tablet coating provides protection. Swallow them whole with a glass of water. The tablets must not be split, crushed, or chewed.
If you have taken too much Uptravi
If you have taken more tablets than you should, you must consult your doctor.
If you forget to take Uptravi
If you forget to take Uptravi, take a dose as soon as you remember. Then continue taking the tablets at the usual time. If it is almost time for the next dose (less than 6 hours until you are due to take it), skip the missed dose and then continue taking the tablets at the usual time. Do not take a double dose to make up for a forgotten tablet.
If you stop taking Uptravi
If you suddenly stop taking Uptravi, it may cause your symptoms to get worse. Do not stop taking Uptravi unless your doctor tells you to. You may need to lower the dose gradually before stopping completely.
If for any reason you miss taking Uptravi for more than three days in a row (if you miss three mornings and three evening doses, or six doses in a row or more), contact your doctor immediately as the dose may need to be changed for you to avoid side effects. Your doctor may decide that you should restart treatment with a lower dose and gradually increase it until you have reached the previous maintenance dose.
If you have any further questions about this medicine, ask your doctor or nurse.
Possible side effects
Like all medicines, this medicine can cause side effects, although not everybody gets them. Side effects can occur not only during the titration period when the dose is increased, but also later when you have taken the same dose for a long time.
If you get any of the following side effects and cannot tolerate them or cannot be treated, contact your doctor as the dose may be too high for you and need to be reduced: headache, diarrhea, nausea, vomiting, jaw pain, muscle pain, leg pain, joint pain or facial flushing.
Very common side effects ( may affect more than 1 in 10 people)
- Headache
- Facial flushing
- Nausea and vomiting
- Diarrhea
- Jaw pain, muscle pain, joint pain, leg pain
- Nasopharyngitis (nasal congestion)
Common side effects ( may affect up to 1 in 10 people)
- Anemia (low red blood cell count )
- Hyperthyroidism (overactive thyroid gland )
- Decreased appetite
- Weight loss
- Hypotension (low blood pressure )
- Stomach pain, including indigestion
- Pain
- Change in certain blood tests that, for example, show the number of blood cells or thyroid function
- Skin rash, including hives that can cause a burning or stinging sensation and redness
Uncommon side effects ( may affect up to 1 in 100 people)
- Faster heartbeat
How to store Uptravi
Keep this medicine out of the sight and reach of children.
Use before the expiry date stated on the carton and blister pack after “EXP”. The expiration date is the last day of the specified month.
No special storage instructions.
No special instructions for destruction.
Contents of the packaging and other information
Contents declaration
The active substance is selexipag.
Uptravi 200 micrograms film-coated tablets contain 200 micrograms of selexipag
Uptravi 400 micrograms film-coated tablets contain 400 micrograms of selexipag
Uptravi 600 micrograms film-coated tablets contain 600 micrograms of selexipag
Uptravi 800 micrograms film-coated tablets contain 800 micrograms of selexipag
Uptravi 1000 micrograms film-coated tablets contain 1000 micrograms of selexipag
Uptravi 1200 micrograms film-coated tablets contain 1200 micrograms of selexipag
Uptravi 1400 micrograms film-coated tablets contain 1400 micrograms of selexipag
Uptravi 1600 micrograms film-coated tablets contain 1600 micrograms of selexipag
Other ingredients are:
Tablet core
Mannitol (E421)
Cornstarch
Low-substituted hydroxypropyl cellulose
Hydroxypropyl cellulose
Magnesium stearate
Film coating
Hypromellose
Propylene glycol
Titanium dioxide (E171)
Iron oxides (E172)
Carnauba wax
Uptravi 200 micrograms film-coated tablets contain yellow iron oxide (E172).
Uptravi 400 micrograms film-coated tablets contain red iron oxide (E172).
Uptravi 600 micrograms film-coated tablets contain red and black iron oxide (E172).
Uptravi 800 micrograms film-coated tablets contain yellow and black iron oxide (E172).
Uptravi 1000 micrograms film-coated tablets contain red and yellow iron oxide (E172).
Uptravi 1200 micrograms film-coated tablets contain black and red iron oxide (E172).
Uptravi 1400 micrograms film-coated tablets contain yellow iron oxide (E172).
Uptravi 1600 micrograms film-coated tablets contain black, red, and yellow iron oxide (E172).
Appearance and package sizes of the medicine
Uptravi 200 microgram film-coated tablets: Round, pale yellow film-coated tablets, debossed with “2” on one side.
Uptravi 400 micrograms film-coated tablets: Round, red film-coated tablets debossed with “4” on one side.
Uptravi 600 micrograms film-coated tablets: Round, light purple film-coated tablets debossed with “6” on one side.
Uptravi 800 micrograms film-coated tablets: Round, green film-coated tablets debossed with “8” on one side.
Uptravi 1000 micrograms film-coated tablets: Round, orange film-coated tablets debossed with “10” on one side.
Uptravi 1200 micrograms film-coated tablets: Round, dark purple film-coated tablets debossed with “12” on one side.
Uptravi 1400 micrograms film-coated tablets: Round, dark yellow film-coated tablets debossed with “14” on one side.
Uptravi 1600 micrograms film-coated tablets: Round, brown film-coated tablets debossed with “16” on one side.
Uptravi 200 micrograms film-coated tablets are packed in blister cards of 10 or 60 tablets and 60 or 140 tablets (titration packs).
Uptravi 400 micrograms, 600 micrograms, 800 micrograms, 1000 micrograms, 1200 micrograms, 1400 micrograms, and 1600 micrograms film-coated tablets are packed in blister cards of 60 tablets.
Not all pack sizes may be marketed.
Marketing Authorisation Holder
Janssen‑Cilag International NV
Turnhoutseweg 30
B‑2340 Beerse
Belgium
Manufacturer
Janssen Pharmaceutica NV
Turnhoutseweg 30
B-2340 Beerse
Belgium