Clinical Hub,Patient Education,Health and Nutrition Facts For You,Medication Instructions

Pulmonary Arterial Hypertension Medications – Endotherlin Receptor Antagonists (6718)

Pulmonary Arterial Hypertension Medications – Endotherlin Receptor Antagonists (6718) - Clinical Hub, Patient Education, Health and Nutrition Facts For You, Medication Instructions


Pulmonary Arterial Hypertension Medications
Endothelin Receptor Antagonists- Bosentan (Tracleer®) and Ambrisentan (Letairis®)
Macitentan (Opsumit®)

The Name of your medicine is: ____________________________

Bosentan (Tracleer®), Ambrisentan
(Letairis®), and Macitentan (Opsumit®) are
medicines used to manage an illness called
Pulmonary Arterial Hypertension (PAH).
These medicines are in pill form and can be
swallowed. They work by blocking the bad
effects of a substance in the body called
endothelin. They help to open up or dilate
blood vessels. This lowers the pressure
inside the blood vessels. Lower blood
pressure allows blood to flow more easily
through blood vessels. Pulmonary arteries
are found in the lungs. The right side of the
heart pushes blood through these arteries to
pick up oxygen. By lowering the pressure,
the heart doesn’t have to work so hard to do
this job. This may help delay or prevent
right sided heart failure. Most men and
women with PAH can use this type of
medicine. They should not be used during

Please ask your health care team if you have
any questions about this medicine.
Remember to keep this and all other
medicines out of the reach of children.
Never share your medicines with other

Before using this medicine:

Tell your health care team if you:
▪ Have liver disease.
▪ Are or plan to become pregnant.
▪ Have congestive heart failure.
▪ What other medicines you take.
▪ Have lower leg or ankle swelling.
▪ Have any blood illness like anemia.
▪ Are allergic to either Bosentan,
Ambrisentan or Macitentan, or any of
its parts.

Proper use of these medicines

Take the medicine exactly as ordered by
your doctor. Do not skip doses of the
medicine. Do not stop using the medicine
without your doctor’s direction.

The medicine can be taken with or without
food. The pills should not be crushed,
broken, or chewed.

Talk to your health care team before starting
any new medicines.

Precautions while using this medicine

Blood tests will need to be done before
starting this medicine. They also need to be
done at regular intervals while taking this
medicine. Your health care team will help
you set up these blood tests. If you are a
female of childbearing age, you will need to
have a monthly pregnancy test. We will
need to make sure you are using two
different forms of birth control while taking
this medicine. This will ensure that you can
safely use this medicine. This medicine can
cause birth defects to a baby if you get
pregnant while taking it. Birth control pills
alone are not enough to prevent pregnancy.
This medicine can lower the effectiveness of
birth control pills.

Usual dose of each medicine for PAH

Bosentan (Tracleer®)
62.5mg by mouth twice daily for 4 weeks,
then 125mg by mouth twice daily after that.

Ambrisentan (Letairis®)
5mg by mouth once daily; may increase to
10mg once daily if 5mg dose is tolerated
well. Dose adjustment may be made based
on your lab test results.

Macitentan (Opsumit®)
10mg by mouth once daily

Possible Side Effects of the medicine:

Call your doctor right away if you notice
any of these side effects:
▪ Allergic reaction(s) such as rash, hives,
itchiness, swelling
▪ Fainting or lightheadedness
▪ Signs of liver damage such as
yellowing of skin or whites of eyes
▪ Swelling (retention of fluid), in ankles
and legs
▪ Feeling of heart racing (palpitations) or
chest pain
▪ Bruising or bleeding easy
▪ Nausea or vomiting
▪ Pregnancy or suspected pregnancy
(even if taking birth control pills)
▪ Urinary tract infection

Side effects that most often do not require
medical attention:

These side effects may go away during
treatment. If they persist or bother you,
check with your health care team before
lowering the dose. Do not stop the
medicine suddenly.
▪ Headache
▪ Flushing
▪ Mild lightheadedness
▪ Mild stomach upset or nausea

Other side effects not listed above may also
occur in some patients. If you notice any
other effects, tell your health care team.

Inform your doctor immediately if you:
 Suspect or learn that you are pregnant
(even if you are taking birth control
pills, wear a birth control patch, or
have an IUD placed)

Your health care team may have given you this information as part of your care. If so, please use it and call if you
have any questions. If this information was not given to you as part of your care, please check with your doctor. This
is not medical advice. This is not to be used for diagnosis or treatment of any medical condition. Because each
person’s health needs are different, you should talk with your doctor or others on your health care team when using
this information. If you have an emergency, please call 911. Copyright © 12/2016 University of Wisconsin Hospitals
and Clinics Authority. All rights reserved. Produced by the Department of Nursing HF#6718