Uptravi 1800mcg Inj, 1ml

Selexipag is an orally available, selective prostacyclin IP receptor agonist. It is metabolized to an active metabolite (ACT-333679), which is approximately 37 times more potent than selexipag at the human IP receptor. Activation of the IP receptor leads to vasodilation, inhibition of platelet aggregation, and antiproliferative effects. In PAH, these actions help to reduce pulmonary vascular resistance and improve hemodynamics.

Serious Side Effects: Seek Medical Attention Immediately

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical help right away:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
New or worsening trouble breathing
Wheezing or coughing
Feeling extremely tired or weak

Other Possible Side Effects

Like all medications, this drug can cause side effects. However, many people do not experience any side effects or only have mild ones. If you are bothered by any of the following side effects or if they do not go away, contact your doctor or seek medical help:

Headache
Diarrhea
Upset stomach or vomiting
Jaw pain
Muscle or joint pain
Pain in arms or legs
Flushing
Decreased appetite
* Pain, redness, or swelling at the injection site

Reporting Side Effects

This list does not include all possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you have liver disease, as this may affect the safety and efficacy of the medication.
* If you are currently taking gemfibrozil, as this can interact with the medication.

This list is not exhaustive, and it is crucial to disclose all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you have. Your doctor and pharmacist need this information to ensure safe treatment.

Remember, before starting, stopping, or changing the dose of any medication, you must consult with your doctor to confirm it is safe to do so in conjunction with this medication and your individual health profile.

It is essential to inform all of your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. If you are pregnant, planning to become pregnant, or are breast-feeding, you must discuss this with your doctor. This conversation will help you understand the potential benefits and risks of this medication to both you and your baby, allowing you to make an informed decision.

• Strong CYP2C8 inhibitors (e.g., Gemfibrozil): Concomitant use with strong CYP2C8 inhibitors significantly increases exposure to the active metabolite (ACT-333679), potentially leading to increased adverse effects. Avoid concomitant use. If unavoidable, consider reducing selexipag dose.

• Moderate CYP2C8 inhibitors (e.g., Clopidogrel, Deferasirox): May increase exposure to the active metabolite. Monitor for adverse effects and consider dose reduction if necessary.
• Strong CYP2C8 inducers (e.g., Rifampin): May decrease exposure to the active metabolite, potentially reducing efficacy. Avoid concomitant use. If unavoidable, monitor for reduced efficacy and consider dose increase.

• Other UGT1A3 inhibitors/inducers: Potential for minor pharmacokinetic interactions, but generally not clinically significant.

• Headache (common, often dose-limiting)
• Jaw pain
• Nausea
• Diarrhea
• Flushing
• Myalgia (muscle pain)
• Arthralgia (joint pain)
• Hypotension (dizziness, lightheadedness, syncope)
• Bleeding (unusual bruising, petechiae, epistaxis, GI bleeding)

Limited human data on selexipag use in pregnant women are insufficient to inform a drug-associated risk for major birth defects or miscarriage. Animal studies have shown adverse developmental effects (e.g., reduced fetal weight, skeletal variations) at exposures higher than clinical. Use only if the potential benefit justifies the potential risk to the fetus.

It is not known whether selexipag or its active metabolite are excreted in human milk. Selexipag and its active metabolite were excreted in the milk of lactating rats. Due to the potential for serious adverse reactions in breastfed infants, advise women not to breastfeed during treatment with selexipag.

Safety and effectiveness in pediatric patients have not been established. Use is not recommended.

No specific dose adjustment is required based on age. However, elderly patients may be more sensitive to the effects of selexipag, and dose titration should be done cautiously, monitoring for adverse effects.

• Uptravi IV is typically used for patients who are temporarily unable to take oral selexipag, or for initiation in patients who cannot tolerate oral titration.
• The IV dose is generally half of the last tolerated oral dose when transitioning from oral to IV.
• For new initiations with IV, careful titration is still required, starting at 200 mcg twice daily.
• Common side effects are dose-dependent and related to prostacyclin agonism (headache, jaw pain, nausea, diarrhea, flushing). These often improve with continued therapy or dose reduction.
• Patients should be educated on the importance of adherence and reporting side effects, especially during dose titration.
• Avoid concomitant use with strong CYP2C8 inhibitors (e.g., gemfibrozil) due to significantly increased exposure to the active metabolite and potential for severe adverse effects.

• Other prostacyclin pathway agents (e.g., epoprostenol, treprostinil, iloprost)
• Endothelin receptor antagonists (ERAs) (e.g., ambrisentan, bosentan, macitentan)
• Phosphodiesterase-5 (PDE5) inhibitors (e.g., sildenafil, tadalafil)
• Soluble guanylate cyclase (sGC) stimulators (e.g., riociguat)

If your symptoms or health problems do not improve or worsen over time, it is essential to contact your doctor for further evaluation and guidance. To ensure safe and effective treatment, never share your medication with others or take someone else's medication.

Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion or exposure. Properly dispose of unused or expired medications by checking with your pharmacist for guidance on the best disposal method. Unless instructed to do so, avoid flushing medications down the toilet or pouring them down the drain, as this can harm the environment. Many communities have drug take-back programs that provide a safe and responsible way to dispose of unwanted medications.

Some medications may come with an additional patient information leaflet, which can be obtained by consulting with your pharmacist. If you have any questions or concerns about your medication, it is crucial to discuss them with your doctor, nurse, pharmacist, or other healthcare provider.

In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide information about the medication taken, the amount, and the time it was taken, as this will help healthcare professionals provide appropriate treatment and care.