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  • opsumit 10 mg (Macitentan) 30 tablets

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    Description

    Opsumit (Macitentan) is a medication used in the treatment of Pulmonary Arterial Hypertension (PAH). It belongs to a class of drugs called endothelin receptor antagonists (ERAs). The active ingredient, macitentan, helps to relax blood vessels in the lungs, reducing pulmonary arterial pressure and improving exercise capacity in patients with PAH. It also helps to slow the progression of the disease.

    How It Works

    Opsumit works by targeting the endothelin receptors in the blood vessels of the lungs. Here’s how it functions:
    • Endothelin Blockade: Endothelin-1 is a substance that contributes to the narrowing of blood vessels (vasoconstriction), which increases blood pressure in the lungs. It also promotes the proliferation of smooth muscle cells in the blood vessel walls, contributing to vessel thickening.
    • Dual Receptor Antagonist: Macitentan blocks both ETA and ETB receptors. ETA receptors are mainly responsible for vasoconstriction and smooth muscle proliferation, while ETB receptors also play a role in vasoconstriction and clearance of endothelin-1. By blocking these receptors, Opsumit prevents the harmful effects of endothelin-1.
    • Vasodilation and Reduced Pulmonary Pressure: By blocking endothelin’s actions, Opsumit causes vasodilation (widening of the blood vessels), lowering the pressure in the pulmonary arteries. This leads to improved oxygen delivery, less strain on the heart, and increased ability to perform physical activities.
    • Slows Disease Progression: Opsumit is designed to not only relieve symptoms but also slow the progression of PAH, reducing the risk of hospitalization or worsening of the disease over time.

    Indications

    Opsumit is indicated for the treatment of:
    • Pulmonary Arterial Hypertension (PAH): To delay disease progression and improve exercise ability in patients with WHO Functional Class II or III PAH.
    • Systemic Sclerosis-Related PAH: Used in patients with PAH related to connective tissue diseases such as systemic sclerosis.

    Side Effects

    While Opsumit is effective in treating PAH, it can cause a range of side effects. Some side effects are common, while others are more serious and require careful monitoring. Common Side Effects:
    • Headache: A frequent complaint among patients taking Opsumit.
    • Nasal Congestion: Stuffy or runny nose may occur.
    • Flushing: Warmth or redness in the face, neck, or chest.
    • Fatigue: Feeling of tiredness or low energy.
    • Gastrointestinal Symptoms: Including nausea or abdominal pain.
    Serious Side Effects:
    • Liver Function Abnormalities: Elevation in liver enzymes is a serious side effect, requiring regular liver function tests.
    • Anemia: A decrease in red blood cells can occur, which may lead to fatigue or weakness.
    • Pulmonary Edema: In patients with pulmonary veno-occlusive disease, the use of Opsumit can worsen their condition and lead to fluid buildup in the lungs.
    • Teratogenicity: Opsumit can cause birth defects, and it is contraindicated in pregnancy. Female patients must use effective contraception during treatment.

    Contraindications

    Opsumit is contraindicated in:
    • Pregnancy: Due to the risk of serious birth defects, Opsumit must not be used by women who are pregnant or planning to become pregnant. A Risk Evaluation and Mitigation Strategy (REMS) is in place for female patients.
    • Severe Liver Impairment: Patients with significant liver dysfunction should avoid taking Opsumit, as the medication can further affect liver function.
    • Pulmonary Veno-Occlusive Disease (PVOD): Opsumit is contraindicated in patients with PVOD due to the risk of worsening pulmonary edema.
    • Hypersensitivity: Patients who are allergic to macitentan or any other ingredients in Opsumit should avoid its use.

    Pricing Table (in Different Countries)

    The cost of Opsumit (Macitentan) 10 mg varies by country and healthcare system. Below is a pricing comparison for 30 tablets of Opsumit in different regions.

    Opsumit (Macitentan) 10 mg Price Comparison

    Country Price (USD) Reference
    United States $9,000 for 30 tablets GoodRx
    United Kingdom £7,200 for 30 tablets NICE BNF
    Canada CAD $11,000 for 30 tablets DrugBank
    Australia AUD $13,000 for 30 tablets PBS Australia
    Germany €8,000 for 30 tablets G-BA Germany

    Top 5 Global Brands

    1. Actelion Pharmaceuticals (Johnson & Johnson): The original developer of Opsumit, Actelion (now part of Johnson & Johnson), is a leader in the development of therapies for PAH and rare diseases.
    2. United Therapeutics: A major player in the PAH space, United Therapeutics markets several treatments for PAH, including Remodulin and Tyvaso, alongside Opsumit.
    3. Bayer: A key competitor in the PAH market, Bayer offers Adempas (riociguat) for PAH and CTEPH (Chronic Thromboembolic Pulmonary Hypertension).
    4. Gilead Sciences: Another major pharmaceutical company in the PAH field, Gilead markets Letairis (ambrisentan), a competitor to Opsumit.
    5. Pfizer: With a broad portfolio, Pfizer has significant contributions to rare disease treatment and continues to research innovative PAH therapies.
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