Opsumit
Opsumit (macitentan) is a medication for treating people with pulmonary arterial hypertension (PAH), or high blood pressure in the blood vessels in the lungs. It can be used alone or together with other PAH medications. Opsumit (macitentan) has several benefits, including lowering the risk of worsening of PAH and hospitalization due to PAH. But, it also has some side effects, such as headache, sore throat, and anemia.
What is Opsumit (macitentan)?
What is Opsumit (macitentan) used for?
- Pulmonary arterial hypertension (PAH)
How Opsumit (macitentan) works
Opsumit (macitentan) is an endothelin receptor antagonist. It works by blocking the effects of a protein in your body called endothelin. Doing so relaxes the blood vessels that go from your heart to your lungs and allows more blood to flow through. This lowers the amount of work your heart needs to pump blood to your lungs to get oxygen for your body. As a result, it's easier for you to exercise and breathe.
Drug facts
Side effects of Opsumit (macitentan)
The following side effects may get better over time as your body gets used to the medication. Let your healthcare provider know immediately if you continue to experience these symptoms or if they worsen over time.
Common Side Effects
- Cold-like symptoms or a sore throat (20%)
- Headache (14%)
- Anemia (13%)
- Bronchitis (12%)
- Urinary tract infection (9%)
- Flu (6%)
Less Common Side Effects
- Stuffy nose
- Swelling of the body (e.g., arms, feet, ankles)
- Low blood pressure
Opsumit (macitentan) serious side effects
Contact your healthcare provider immediately if you experience any of the following.
- Liver problems: swelling of your stomach, yellowing of your skin or the whites of your eyes, confusion, dark or brown urine
- Fluid buildup in the body: shortness of breath; swelling in the legs, ankles, or feet; irregular heartbeat; chest pain; unable to exercise; tiredness; unusual weight gain
The following Opsumit (macitentan) side effects have also been reported
Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor immediately if any of the following side effects occur:
More common
Decrease in the amount of urine
noisy, rattling breathing
pale skin
swelling of the fingers, hands, feet, or lower legs
troubled breathing with exertion
unusual bleeding or bruising
unusual tiredness or weakness
Less common
Abdominal or stomach pain or tenderness
clay colored stools
dark urine
difficult, burning, or painful urination
frequent urge to urinate
lower back or side pain
muscle aches and pains
difficulty with breathing
tightness in the chest
yellow eyes or skin
Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.
Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.
Pros and cons of Opsumit (macitentan)
Pros
- Works well to slow down the worsening of PAH and make it easier to breathe, exercise, and walk longer distances
- Taken by mouth once per day with or without food
- Might work better than ambrisentan (Letairis) or bosentan (Tracleer)
Cons
- Not a cure for PAH
- Can cause side effects like headache, fluid buildup in the body, and anemia
- Not safe to use during pregnancy
- Not recommended for breastfeeding mothers because we don't know if it's safe
Pharmacist tips for Opsumit (macitentan)
- Make sure to mark your appointments on your calendar for when you need to see your provider. These appointments are important to discuss how treatment is going for you and make sure Opsumit (macitentan) is safe for you to take. For example, your provider will need to check your liver health regularly and your blood cell counts periodically.
- Take Opsumit (macitentan) with or without food at the same time day every day.
- Swallow Opsumit (macitentan) tablets whole. Don't split, crush, or chew the tablets. If you're having trouble swallowing the tablets, contact your provider.
- Opsumit (macitentan) can cause your body to hold onto too much fluid and swell up. Contact your provider if you notice shortness of breath, unexpected weight gain, or swelling in the ankles or feet.
- Opsumit (macitentan) interacts with a lot of medications (prescription and over-the-counter), including amiodarone (Pacerone), diltiazem (Cardizem), and fluconazole (Diflucan), among many others. Make sure to let your provider know about all the medications you're taking (including vitamins and supplements) before starting Opsumit (macitentan) so that they can check for interactions. If there are interactions, your provider might switch you to a different medication to prevent harmful effects.
- If you're a woman who's able to have children, it's recommended that you use birth control during treatment with Opsumit (macitentan) and for at least 1 month after your last dose. In addition, you'll need to do a pregnancy test every month while you take Opsumit (macitentan). Let your provider know right away if you get pregnant while taking this medication. Opsumit (macitentan) can potentially harm an unborn baby.
- If you're a man and are prescribed Opsumit (macitentan), let your provider know if there's a possibility you might want to have children in the future. This medication might not be the best option for you because Opsumit (macitentan) can lower your sperm count. It's not known if this effect is reversible after you stop the medication.
Common questions about Opsumit (macitentan)
Pulmonary arterial hypertension (PAH) is when the pressure in the arteries (blood vessels) that go from your heart to your lungs gets too high. This high blood pressure causes the arteries to become narrower, which makes it harder for blood to get to the lungs for oxygen. As a result, your heart has to work harder to pump blood to the lungs, which can lead to heart muscle damage and heart failure in the long run. Symptoms of PAH include shortness of breath, tiredness, dizziness, irregular heartbeat, chest pain, and swelling in the ankles and feet. Opsumit (macitentan) can help relax these blood vessels, allow more blood to flow through, lessen the work your heart needs to do, and get oxygen to the rest of your body.
In clinical studies, people taking Opsumit (macitentan) had better improvements in walking distance at month 6 of treatment than people who took placebo. Six months into the study, people taking Opsumit (macitentan) also had less chest pain, fatigue, and shortness of breath with physical activity than those who took placebo. In addition, Opsumit (macitentan) lowered the chance of worsening of PAH and hospitalization for PAH each by almost half. Keep in mind that some people included in this study were also taking other PAH medications at the same time. Everyone responds differently to Opsumit (macitentan). For this reason, your provider will regularly follow up with you to make sure Opsumit (macitentan) is helping your PAH.
Opsumit (macitentan), ambrisentan (Letairis), and bosentan (Tracleer) are from the same family of medications called endothelin receptor antagonists and are all used for PAH. One recent study showed that people who switched from ambrisentan (Letairis) or bosentan (Tracleer) to Opsumit (macitentan) had better improvements in walking speed, walking distance, and their overall PAH condition. All three medications generally have similar side effects. But, Opsumit (macitentan) is more likely to cause anemia, ambrisentan (Letairis) is more likely to cause swelling in the legs and feet, and bosentan (Tracleer) is more likely to cause liver problems. Finally, Opsumit (macitentan) and ambrisentan (Letairis) are taken once per day, whereas bosentan (Tracleer) is taken twice per day.
Opsumit (macitentan) is only available through a Risk Evaluation and Mitigation Strategy (REMS) program called the Opsumit REMS program. Because of the medication's risk of causing severe and life-threatening harm to unborn babies if taken during pregnancy, the REMS program makes sure Opsumit (macitentan) is distributed and taken under the safest conditions possible. All providers who prescribe Opsumit (macitentan), pharmacies that dispense the medication, and women who are able to get pregnant and are prescribed Opsumit (macitentan) must register with the REMS program. Under the Opsumit REMS program, you're required to get monthly pregnancy tests and use birth control during treatment if you're a woman who can have children and are taking the medication. These requirements don't apply for men who are prescribed Opsumit (macitentan).
If you're thinking about having a baby, there are a few things you should consider before starting Opsumit (macitentan). If you get pregnant during treatment, you'll need to stop the medication because there's a risk for severe and life-threatening harm to unborn babies. For this reason, women who are able to get pregnant must enroll in the Opsumit REMS program, use birth control while taking Opsumit (macitentan) and for at least 1 month after the last dose, and get monthly pregnancy tests during treatment. Additionally, it's possible that Opsumit (macitentan) might lower sperm counts in men, which might affect their ability to have children. It's not completely clear if this effect is reversible after stopping the medication. Make sure to discuss with your provider about family planning before starting Opsumit (macitentan).
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Risks and warnings for Opsumit (macitentan)
Opsumit (macitentan) can cause some serious health issues. This risk may be even higher for certain groups. If this worries you, talk to your doctor or pharmacist about other options.
Not safe to use during pregnancy
Opsumit (macitentan) shouldn't be taken during pregnancy. While it hasn't been studied in human pregnancy, animal studies show that it can cause severe and life-threatening harm to unborn babies. Because of this risk, Opsumit (macitentan) is available only through the Opsumit REMS program. If you're a woman who's able to have children, your provider will ask you take a pregnancy test before you start Opsumit (macitentan), monthly during treatment, and once more a month after you stop the medication. Women who are able to get pregnant should use birth control during treatment with Opsumit (macitentan) and for at least 1 month after completing treatment. If you're pregnant or thinking of becoming pregnant, talk to your provider about the risks and benefits of using Opsumit (macitentan) during pregnancy.
Liver damage
Opsumit (macitentan) can cause liver problems that can sometimes lead to liver failure. You'll need to get blood tests to check your liver health before and during treatment. These blood tests make sure your liver is working properly. Get medical attention right away if you notice symptoms of liver problems, such as swelling of your stomach, stomach pain, yellowing of your skin or the whites of your eyes, stool changes (black, tarry, or bloody stools), nausea, vomiting, or dark or brown urine. You might need to stop taking Opsumit (macitentan) to prevent further liver damage.
Fluid buildup in the body
- Risk factors: Heart failure
Opsumit (macitentan) can cause fluid buildup in the body, leading to swelling or shortness of breath. If you have a history of heart failure, this fluid buildup can be severe and worsen your heart condition. Fluid buildup can start to happen within weeks of starting Opsumit (macitentan). If you have any heart problems or heart failure, let your provider know before starting Opsumit (macitentan). Contact your provider if you have any signs of heart failure, like shortness of breath; swelling in the legs, ankles, or feet; irregular heartbeat; not able to exercise; or tiredness while taking Opsumit (macitentan).
Anemia (low red blood cell count)
- Risk factors: Severe anemia
Opsumit (macitentan) might cause your hemoglobin levels to go down. Hemoglobin is the protein on your red blood cells that carries oxygen to the rest of your body. Low hemoglobin levels can lead to anemia. You will need regular blood tests while taking Opsumit (macitentan) to make sure your hemoglobin stays at a healthy level. If you have a history of anemia, speak with your provider before taking Opsumit (macitentan) so they can make sure it's safe for you to take. If you experience weakness, shortness of breath, dizziness, fast or irregular heartbeat, or pale skin while taking Opsumit (macitentan), let your provider know.
Opsumit (macitentan) dosage
Typical dosage for Opsumit (macitentan)
The typical dose is 10 mg by mouth once per day.
Interactions between Opsumit (macitentan) and other drugs
Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
- Apalutamide
- Boceprevir
- Carbamazepine
- Clarithromycin
- Cobicistat
- Conivaptan
- Enzalutamide
- Fluconazole
- Fosphenytoin
- Idelalisib
- Indinavir
- Itraconazole
- Ketoconazole
- Lopinavir
- Lumacaftor
- Mitotane
- Nefazodone
- Nelfinavir
- Phenytoin
- Posaconazole
- Rifampin
- Ritonavir
- Saquinavir
- St John's Wort
- Telaprevir
- Telithromycin
- Voriconazole
Opsumit (macitentan) contraindications
Contraindications are specific health conditions or situations in which a person should not take a medication due to safety concerns. If you have any of the following conditions or if any of the following apply to you, let your healthcare provider know because Opsumit (macitentan) will not be safe for you to take.
- Pregnancy
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