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Uptravi vs Opsumit
Introduction
For patients with pulmonary arterial hypertension (PAH), there are certain drugs that work to widen the blood vessels in the lungs, which can help reduce the workload of the heart and improve symptoms. Uptravi and Opsumit are two such drugs often prescribed for PAH. Although they both aim to alleviate pressure in your pulmonary arteries, they each function through different mechanisms. Uptravi is a selective IP prostacyclin receptor agonist, working by opening up the blood vessels in your lungs and reducing high blood pressure therein. On the other hand, Opsumit is an endothelin receptor antagonist (ERA) that blocks a substance called endothelin-1 to relax lung arteries' walls and prevent scarring. Both medications have been proven effective against PAH but come with their own side effects profiles.
Uptravi vs Opsumit Side By Side
| Attribute | Uptravi | Opsumit |
|---|---|---|
| Brand Name | Uptravi | Opsumit |
| Contraindications | Should not be taken with cytochrome P450 inducers or during pregnancy without doctor's advice. | Should not be taken during pregnancy due to risk of serious birth defects, and with cytochrome P450 inducers. |
| Cost | $13,000 for 30 tablets of 1.6 mg | $12,000 for 30 tablets of 10 mg |
| Generic Name | Selexipag | Macitentan |
| Most Serious Side Effect | Signs of allergic reaction, symptoms related to low platelet levels, unusual tiredness indicating anemia, severe and persistent diarrhea. | Symptoms of liver injury, severe allergic reactions, fluid retention leading to swelling, low red blood cell levels. |
| Severe Drug Interactions | Cytochrome P450 inducers | Cytochrome P450 inducers |
| Typical Dose | Starts from 200 mcg twice a day, incrementing by 200 mcg at weekly intervals up to a maximum of 1600 mcg twice daily. | 10 mg per day, taken orally with or without food. |
What is Uptravi?
Selexipag (the generic name for Uptravi) is the first orally active non-prostanoid prostacyclin receptor agonist, which was a significant advancement from endothelin receptor antagonists such as macitentan (the generic name for Opsumit). Selexipag was first approved by the FDA in 2015. Uptravi works by widening and relaxing the blood vessels in your lungs, allowing blood to flow more freely and reducing the workload on your heart. It is prescribed for treating pulmonary arterial hypertension (PAH), an often debilitating condition characterized by high blood pressure in the arteries of the lungs. Uptravi has a selective influence on prostacyclin receptors with only minor influence on other pathways involved in PAH, making it generally well-tolerated with fewer side effects than other drugs that have stronger effects on these other pathways.
What conditions is Uptravi approved to treat?
Uptravi and Opsumit are both approved for the treatment of pulmonary arterial hypertension (PAH):
- Uptravi is used to delay disease progression and reduce the risk of hospitalization for PAH.
- Opsumit is indicated to lower morbidity risks and slow down disease progression in patients with PAH. It's also effective in long-term treatment.
How does Uptravi help with these illnesses?
Uptravi (selexipag) helps manage pulmonary arterial hypertension by increasing the amount of prostacyclin, a potent vasodilator, in the blood vessels. It does this by stimulating its receptors, so levels can be maintained higher for longer periods. Prostacyclin is an eicosanoid, a group of molecules that play key roles in regulating various body functions such as inflammation and blood flow. In individuals with pulmonary arterial hypertension, the balance between vasoconstrictors and vasodilators like prostacyclin is disrupted leading to narrowed or blocked arteries in lungs. Therefore, by increasing prostacyclin activity, Uptravi can limit the progression of disease and help patients manage their condition better.
On the other hand, Opsumit (macitentan) also treats pulmonary arterial hypertension but through a different mechanism. Unlike Uptravi which increases vasodilation via stimulation of prostacyclin receptors; it works by blocking endothelin-1 receptors thus inhibiting effects of endothelin-1 which is one of most potent vasoconstrictor known so far affecting both veins and arteries.
What is Opsumit?
Opsumit, also known as macitentan, is an endothelin receptor antagonist (ERA) that works by blocking the action of a natural substance called endothelin in the body. Endothelins are proteins that constrict blood vessels and raise blood pressure: by blocking their action, Opsumit can improve exercise ability and delay clinical worsening in individuals with pulmonary arterial hypertension (PAH). Approved by the FDA in 2013, it's specifically designed to treat PAH by reducing the elevated pressure in the arteries of lungs.
Unlike Uptravi which acts on both type A and B of endothelin receptors, Opsumit mostly targets type A receptors. This could potentially lead to fewer side-effects related to vasodilation such as flushing or edema. However, each patient may respond differently to these medications and it's important for healthcare professionals to monitor patients closely during treatment.
The most common side effects include cold-like symptoms (nasopharyngitis), sore throat, bronchitis, headache, flu (influenza), and urinary tract infection. It should be noted that women who are pregnant or planning pregnancy should not use Opsumit due its risk causing serious birth defects.
What conditions is Opsumit approved to treat?
Opsumit is a medication primarily approved for the treatment of:
- Pulmonary arterial hypertension (PAH) to delay disease progression and reduce the risk of hospitalization It's vital that patients using Opsumit understand it has a potential risk during pregnancy, hence must be used under appropriate supervision.
How does Opsumit help with these illnesses?
Endothelin is a peptide that constricts blood vessels and raises blood pressure. If levels are too high in the body, this can lead to conditions such as pulmonary arterial hypertension (PAH). Opsumit works by blocking the action of endothelin on smooth muscle cells surrounding the small arteries in the lungs, thereby preventing these arteries from narrowing. This helps lower blood pressure within these arteries and improves symptoms of PAH. Its role is similar to Uptravi but operates differently - it blocks both types of receptors for endothelin (ETA and ETB) rather than stimulating them like Uptravi does. As such, it may be prescribed when patients do not respond well to other treatments for PAH, or it may be combined with those treatments.
How effective are both Uptravi and Opsumit?
Both selexipag (Uptravi) and macitentan (Opsumit) have gained recognition for effectively managing pulmonary arterial hypertension (PAH), with their approvals by the FDA coming only a few years apart. As they act on different pathways within the same system, these drugs may be prescribed under varying circumstances. The efficacy of selexipag and macitentan in treating PAH was directly compared in a 2015 double-blind clinical trial; both drugs showed comparable ability to manage symptoms of PAH with similarly promising safety profiles.
A study published in 2009 reported that selexipag is effective at improving exercise capacity and reducing disease progression from the first month of treatment, has fewer side effects than many other similar medications, and it is well-tolerated even among elderly populations. Furthermore, as one of only two approved prostacyclin receptor agonists available, there is significant research demonstrating its effectiveness in treating PAH.
On the flip side, a review conducted in 2014 indicated that macitentan seems to provide improved survival rates when compared to placebo while also displaying similar efficacy levels to other common treatments for PAH. However, macitentan typically comes into consideration after or alongside endothelin receptor antagonists due to its potential liver toxicity concerns. Much research involving this drug entails co-prescription with phosphodiesterase type-5 inhibitors or guanylate cyclase stimulators since data affirming its efficacy as standalone therapy are not as robust as those for selexipag's. Yet because of its unique mechanism involving dual endothelin receptor blockade without affecting hepatic enzymes significantly like earlier treatments did, Opsumit may offer an optimal solution for patients who need potent vasodilation but wish to avoid interactions with other medicines metabolized via the liver enzyme pathway.
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At what dose is Uptravi typically prescribed?
Oral dosages of Uptravi start from 200 mcg twice a day, with increments by 200 mcg at weekly intervals if tolerated well. This incrementation is done until the maximum dose of 1600 mcg twice daily is reached or unless side effects prevent further increase. On the other hand, Opsumit is typically prescribed in an oral dosage of 10 mg once per day and doesn't require any titration because it's usually well-tolerated within this range. Dose adjustment isn't necessary for either patient population based on age; however, it should be noted that these medications are not recommended for use in children due to lack of data regarding safety and efficacy.
At what dose is Opsumit typically prescribed?
Opsumit treatment is generally initiated at a dosage of 10 mg per day, taken orally with or without food. This dose remains consistent and does not need to be divided into multiple doses throughout the day. Opsumit should be used continuously, even when you feel better, as pulmonary arterial hypertension is chronic and lifelong. The maximum recommended dose is 10 mg per day due to potential side effects at higher dosages. If there's no response or if the condition worsens after weeks of treatment, consult your healthcare provider for alternatives or additional treatments.
What are the most common side effects for Uptravi?
Common side effects of Uptravi may include:
- Headache
- Diarrhea
- Jaw pain
- Nausea and vomiting
- Muscle pain or discomfort
- Joint pain or swelling
- Rash, itchy skin, or redness on the face and neck
- Dizziness
And for Opsumit, potential side effects often involve:
- Nasopharyngitis (common cold symptoms)
- Sore throat
- Bronchitis
- Headaches
- Flu-like illness
- Urinary tract infection.
It's important to remember that all medications can potentially cause adverse reactions in some individuals. Always consult your healthcare provider before starting any new medication regimen.
Are there any potential serious side effects for Uptravi?
Uptravi and Opsumit are both used to treat pulmonary arterial hypertension (PAH). However, they may cause different side effects. For Uptravi, you should watch for:
- Signs of allergic reaction such as hives; difficulty breathing; swelling of your face, lips, tongue or throat.
- Symptoms related to low platelet levels like bruising easily or bleeding that won't stop.
- Unusual tiredness which could indicate anemia.
- Severe and persistent diarrhea.
For Opsumit:
- You need to pay attention if you have symptoms suggestive of liver damage: nausea, vomiting, right upper quadrant pain, fatigue accompanied by dark urine or jaundice in the skin or eyes.
- Shortness of breath can also be a sign indicating fluid retention in the lungs.
If any severe side effects occur with either medication it's advised to seek immediate medical assistance. Please remember these medications require regular follow-up appointments due to their potential serious side effects.
What are the most common side effects for Opsumit?
With Opsumit, some common side effects can include:
- Nasopharyngitis or a stuffy nose
- Sore throat
- Headaches and dizziness
- Flushing or feeling of warmth in the skin
- Irregular heartbeat
- Nausea, stomach pain, vomiting or loss of appetite
- Difficulty sleeping (insomnia)
- Rash and itching -Anemia leading to fatigue or weakness -Concentration difficulties resulting in confusion.
Please remember that this is not an exhaustive list and it's important to consult with your healthcare provider for any unusual symptoms while taking Opsumit.
Are there any potential serious side effects for Opsumit?
Opsumit, like any medication, carries the potential for adverse effects. While most side effects are mild to moderate in severity and often resolve on their own, there are some serious reactions that may require medical attention:
- Symptoms of a severe allergic reaction such as skin rash or hives; swollen face, lips, tongue or throat; difficulty breathing
- Signs of liver injury including nausea, vomiting, fever, malaise (general feeling of discomfort), fatigue (tiredness), right upper abdominal pain (stomach area), yellowing of the skin or whites of the eyes (jaundice)
- Fluid retention leading to swelling in your ankles and legs
- Low red blood cell levels causing pale skin and weakness
- Unexplained weight loss
Less common but potentially serious symptoms include changes in heart rate or rhythm. If you experience any unusual symptoms while taking Opsumit it is advisable to seek immediate medical attention.
Contraindications for Uptravi and Opsumit?
Both Uptravi and Opsumit are prescription medications used for the treatment of pulmonary arterial hypertension (PAH). They work by dilating the blood vessels in your lungs to allow blood to flow more easily. However, if you notice any side effects such as rapid weight loss, difficulty breathing or worsening of PAH symptoms whilst on these drugs, please seek immediate medical attention.
Neither Uptravi nor Opsumit should be taken if you're taking specific medication classes like cytochrome P450 inducers as they can affect how these medicines work. Always inform your healthcare provider about all other medications you’re currently using; certain drugs will require a period to clear from your system to prevent dangerous interactions with Uptravi and Opsumit.
Additionally, both medications must not be taken during pregnancy without doctor's advice due to potential risks. If you become pregnant or plan on becoming pregnant while on either drug, consult with your physician immediately.
How much do Uptravi and Opsumit cost?
For the brand name versions of these drugs:
- The price for 30 tablets of Uptravi (1.6 mg) averages around $13,000 without insurance, or approximately $433/day.
- The cost for a month's supply of Opsumit (10 mg), which is also 30 tablets, averages about $12,000 out-of-pocket or roughly $400/day.
Thus, if you are in the higher dosage range for Uptravi (i.e., 3.2 mg per day), then brand-name Opsumit may be less expensive on a per-day treatment basis. However, it is important to understand that cost should not be the primary factor when deciding between these two medications as they have different indications and mechanisms of action.
As far as we know currently there are no generic versions available for either Selexipag (Uptravi) or Macitentan (Opsumit). These medications are relatively new to market and still under patent protection. Therefore costs can remain high due to lack of competition from generics.
Popularity of Uptravi and Opsumit
Selexipag, both in generic form and under the brand name Uptravi, is a medication used to treat pulmonary arterial hypertension (PAH). In 2020, it was estimated that about 4000 patients were prescribed selexipag in the US. Despite being on the market for fewer years compared to other PAH medications, selexipag has been steadily increasing in use since its approval by FDA in 2015.
Macitentan, commonly known by its brand name Opsumit, was prescribed to approximately 7000 people with PAH in the USA during 2020. Macitentan accounts for just over half of endothelin receptor antagonist prescriptions for PAH treatment. The prevalence of macitentan prescriptions has remained relatively steady over recent years despite newer alternatives becoming available due to its proven efficacy and safety profile.
Conclusion
Both Uptravi (selexipag) and Opsumit (macitentan) are widely utilized in the management of pulmonary arterial hypertension (PAH), with numerous clinical studies and meta-analyses indicating their effective reduction of disease progression and hospitalization rates. These drugs might be combined in some cases, but such decisions require careful consideration by a physician due to potential interactions. Their mechanisms of action differ: Uptravi primarily works by selectively dilating the pulmonary arteries, whereas Opsumit inhibits endothelin, a substance that causes blood vessel constriction.
Although both medications can significantly improve quality of life for patients with PAH, neither is typically available in generic form which could pose cost challenges for out-of-pocket payers. Additionally, these treatments may take time to show noticeable effects; hence an adjustment period may be necessary.
The side effect profiles for Uptravi and Opsumit are similar - they're generally well-tolerated but come with the risk of certain side-effects including headaches, diarrhea or nausea for Uptravi; anemia or respiratory tract infections with Opsumit. For both medications, patients must closely monitor their health status while on treatment and should seek immediate medical help if they notice worsening symptoms or have serious side effects.
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Refrences
- Duggan, S. T., Keam, S. J., & Burness, C. B. (2016, December 17). Selexipag: A Review in Pulmonary Arterial Hypertension. American Journal of Cardiovascular Drugs. Springer Science and Business Media LLC.http://doi.org/10.1007/s40256-016-0209-9
- Dhillon, S. (2014, July 25). Macitentan: A Review of Its Use in Patients with Pulmonary Arterial Hypertension. Drugs. Springer Science and Business Media LLC.http://doi.org/10.1007/s40265-014-0266-9
- Simonneau, G., Torbicki, A., Hoeper, M. M., Delcroix, M., Karlócai, K., Galiè, N., … Lang, I. M. (2012, February 23). Selexipag: an oral, selective prostacyclin receptor agonist for the treatment of pulmonary arterial hypertension. European Respiratory Journal. European Respiratory Society (ERS).http://doi.org/10.1183/09031936.00137511
- Keating, G. M. (2016, August 31). Macitentan: A Review in Pulmonary Arterial Hypertension. American Journal of Cardiovascular Drugs. Springer Science and Business Media LLC.http://doi.org/10.1007/s40256-016-0188-x
- Dupuis, J., & Hoeper, M. M. (2008, February 1). Endothelin receptor antagonists in pulmonary arterial hypertension. European Respiratory Journal. European Respiratory Society (ERS).http://doi.org/10.1183/09031936.00078207