Opsumit (Macitentan)
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Prescription Required
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Product Details
Description
Opsumit, also known as Macitentan, serves as an endothelin receptor antagonist. This medication plays a key role in managing pulmonary arterial hypertension (PAH) by hindering endothelin's effects, a substance that narrows blood vessels and increases blood pressure. By blocking these receptors, Opsumit helps to dilate the arteries in the lungs, easing blood flow and reducing blood pressure. It is indicated to delay disease progression and may improve the ability to exercise, managing the underlying issues in the blood vessels of the lungs.
Fact Table
Formula
C19H20Br2N6O4S
License
US FDA (2013)
Bioavailability
~74% (oral)
Legal status
Prescription only (?)
Chemical Name
N-[5-(4-Bromophenyl)-6-[2-[(5-bromopyrimidin-2-yl)oxy]ethoxy]-2,3-dihydro-1,4-benzothiazin-7-yl]-methanesulfonamide
Elimination half-life
16 hours
Dosage (Strength)
10 mg tablets
Pregnancy
Contraindicated (Category X)
Brands
Opsumit
Protein binding
>99%
PubChem CID
16004610
MedlinePlus
a614029
ChEBI
CHEBI:72329
ATC code
C02KX04
DrugBank
DB08931
KEGG
D09713
Routes of administration
Oral
Directions
Opsumit is administered orally. The standard dosage is 10 mg once daily for adults. Patients may take the medication with or without food, according to their personal comfort or preference. It's important for patients to stick to the prescribed dosage, as higher doses than 10 mg daily have not been studied in PAH and are not recommended. In addition, patients should be aware that taking Opsumit may require regular monitoring due to potential side effects affecting the liver and white blood cell counts. If a dose is missed, patients should take it as soon as they remember, unless it is close to the time of the next scheduled dose, in which case they should simply continue with their regular dosing schedule.
Ingredients
Macitentan is the active ingredient in Opsumit. The inert ingredients may include lactose monohydrate, microcrystalline cellulose, pregelatinized starch, colloidal silicon dioxide, and magnesium stearate.
Contraindications
Patients and healthcare providers should be aware of these contraindications to avoid complications:
- Pregnancy: The drug can harm an unborn baby and is therefore not recommended during pregnancy
- Hypersensitivity reactions: Individuals who have had allergic reactions to Macitentan or any components of Opsumit should avoid this medication
Cautions
- Before taking Opsumit, tell your healthcare provider about:
- All medications you are taking, including over-the-counter drugs and supplements, to avoid harmful interactions
- Any existing medical conditions
- If you are or plan to become pregnant, due to the risk of harm to the unborn child associated with Opsumit
- If you are breastfeeding, as the drug can pass into breast milk
- Opsumit can cause liver damage, even leading to liver failure in severe cases. It's important to have liver enzymes checked before starting treatment and then monitor them as needed. Any signs of liver problems should be reported to a healthcare provider immediately.
- Patients taking Opsumit may experience fluid retention, which could require medical intervention. Monitoring for signs of fluid buildup, such as swelling in the legs or sudden weight gain, is important.
- Decreases in hemoglobin levels have been noted in patients using Opsumit. Regular blood tests to monitor hemoglobin levels may be necessary during treatment.
- For patients with pulmonary veno-occlusive disease, there's a risk of developing pulmonary edema (fluid in the lungs) when using Opsumit. If pulmonary edema is confirmed, discontinuing the medication is crucial.
- There have been observations of decreased sperm count in patients taking endothelin receptor antagonists, including Opsumit. Men planning to father children may want to discuss this potential effect with their healthcare provider.
Side Effects
Opsumit may cause several side effects. The most common Opsumit side effects experienced by patients include stuffy nose or sore throat, lower lung infections, headaches, flu symptoms, and urinary tract infections. These are generally mild and are reported by a significant number of patients.
The more severe side effects of Opsumit include serious birth defects, potential liver problems (indicated by symptoms like nausea, yellowing of the skin or eyes, and dark urine), fluid retention (marked by unusual weight gain or ankle/leg swelling), anemia (low red blood cell levels), and decreased sperm counts in men. Patients should consult their healthcare provider for any concerns about side effects that develop, persist, or worsen.
References:
- Opsumit (Macitentan) Product Monograph. Titusville, NJ: Actelion Pharmaceuticals; 2023.
- Opsumit (Macitentan) Drug Label Information. Titusville, NJ: Actelion Pharmaceuticals; 2023.
IMPORTANT NOTE: The above information is intended to increase awareness of health information and does not suggest treatment or diagnosis. This information is not a substitute for individual medical attention and should not be construed to indicate that use of the drug is safe, appropriate, or effective for you. See your health care professional for medical advice and treatment.Product Code : 14543
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