ADEMPAS 1.5mg Tablets/Film-coated

What is ADEMPAS 1.5mg

ADEMPAS 1.5mg is a prescription medication primarily used to treat certain types of pulmonary hypertension, including chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH). Its active ingredient is Riociguat (micronized), which helps to relax blood vessels in the lungs, improving blood flow and reducing the heart’s workload.

• Therapeutic use: ADEMPAS is indicated for adults to improve exercise capacity and delay clinical worsening in patients diagnosed with PAH or inoperable or persistent/recurrent CTEPH after surgical treatment.
• Form and packaging: This medication is available as film-coated tablets, each containing 1.5 mg of micronized riociguat, packaged in blister packs of 42 tablets (3 strips of 14 tablets each).
• Mechanism target: It specifically targets the pulmonary vascular system to reduce pulmonary arterial pressure, which helps alleviate symptoms like shortness of breath, fatigue, and chest pain related to pulmonary hypertension.
• Prescription status: ADEMPAS should only be used under medical supervision because it requires dose titration and monitoring for efficacy and safety.
• Patient population: It is generally prescribed for adult patients with confirmed diagnosis, and its use in children or pregnant women is usually avoided or carefully controlled.

How to use ADEMPAS 1.5mg

Proper administration of ADEMPAS is essential to maximize its benefits and minimize potential risks. Below are detailed guidelines on how to use ADEMPAS safely and effectively:

• Dosage titration: Treatment with ADEMPAS typically starts at a low dose, which is gradually increased based on patient tolerance and therapeutic response. The usual starting dose is 1 mg three times daily, and adjustments are made in 0.5 mg increments.
• Frequency: The medication is taken orally three times daily (every 6-8 hours), consistently spaced to maintain steady blood levels.
• With or without food: ADEMPAS tablets can be taken with or without food. However, maintaining consistency in relation to meals is advisable to avoid fluctuations in absorption.
• Swallowing tablets: Take the film-coated tablets whole with water. Do not crush, break, or chew the tablets as it may affect drug release and absorption.
• Missed dose: If a dose is missed, take it as soon as possible unless it is near the time for the next dose. Do not double the dose to make up for a missed one.
• Regular monitoring: Patients should undergo regular clinical evaluations, including blood pressure and heart function monitoring, as ADEMPAS can cause systemic hypotension.
• Precautions: Inform your healthcare provider of all other medications, supplements, or health conditions before starting ADEMPAS, as it has several important drug and disease interactions.

Mode of Action ADEMPAS 1.5mg

ADEMPAS contains riociguat, a soluble guanylate cyclase (sGC) stimulator, which exerts its effects through a unique mechanism targeting the nitric oxide (NO) signaling pathway.

• Stimulates sGC enzyme: Riociguat directly stimulates soluble guanylate cyclase independent of nitric oxide, and also sensitizes sGC to endogenous NO, amplifying its effects.
• Increases cyclic GMP: Activation of sGC enhances the conversion of guanosine triphosphate (GTP) into cyclic guanosine monophosphate (cGMP), a key signaling molecule.
• Vasodilation: Elevated cGMP levels cause relaxation of the smooth muscle cells in the pulmonary arteries, leading to vasodilation and a reduction in pulmonary vascular resistance.
• Improves heart function: By lowering pulmonary arterial pressure, ADEMPAS reduces the strain on the right side of the heart, improving cardiac output and overall cardiovascular function.
• Anti-remodeling effects: Beyond vasodilation, riociguat may also inhibit vascular remodeling and proliferation, helping to stabilize or slow disease progression in pulmonary hypertension.
• Selective action: ADEMPAS acts primarily on the pulmonary circulation with limited systemic vascular effects, which helps minimize systemic hypotension risks when dosed correctly.

ADEMPAS 1.5mg Interactions ADEMPAS 1.5mg

ADEMPAS can interact with several medications, potentially altering its efficacy or increasing the risk of adverse effects. Understanding these interactions is vital for safe use.

• Contraindicated with nitrates: Combining ADEMPAS with nitrates or nitric oxide donors (e.g., nitroglycerin) can cause severe hypotension and is strictly contraindicated.
• Phosphodiesterase type 5 (PDE5) inhibitors: Co-administration with PDE5 inhibitors such as sildenafil or tadalafil is not recommended due to additive hypotensive effects and risk of severe low blood pressure.
• Strong CYP450 inhibitors: Drugs like ketoconazole, ritonavir, or clarithromycin may increase riociguat levels, requiring close monitoring or dose adjustments.
• Strong CYP450 inducers: Rifampicin or carbamazepine can reduce ADEMPAS plasma levels, potentially decreasing its effectiveness.
• Antacids and proton pump inhibitors: May alter absorption; take ADEMPAS at least 1 hour before or 1 hour after antacids.
• Anticoagulants: Caution advised when used with warfarin or other blood thinners; ADEMPAS may increase bleeding risk, so regular INR monitoring is important.
• Other blood pressure-lowering agents: Combining with antihypertensives requires monitoring for hypotension and dose adjustments.

Dosage of ADEMPAS 1.5mg

Dosage of ADEMPAS is individualized and carefully titrated to achieve optimal therapeutic effect while minimizing side effects. The following outlines typical dosing strategies:

• Starting dose: Usually, treatment begins at 1 mg three times daily (TID).
• Titration: Dose is adjusted in increments of 0.5 mg TID at intervals of 2 weeks or more, depending on blood pressure and tolerability.
• Maintenance dose: The effective dose typically ranges between 1.5 mg and 2.5 mg three times daily. Some patients may tolerate up to 2.5 mg TID.
• Maximum dose: 2.5 mg TID is considered the maximum recommended dose.
• Special populations: Patients with renal or hepatic impairment may require dose adjustments and more frequent monitoring.
• Missed dose: If a dose is missed, take it as soon as possible unless it is close to the next scheduled dose; do not double doses.
• Monitoring: Blood pressure, signs of hypotension, and clinical symptoms should guide dosing adjustments throughout therapy.

Possible side effects of ADEMPAS 1.5mg

Like all medications, ADEMPAS can cause side effects. Awareness of potential adverse reactions helps ensure early recognition and appropriate management.

• Common side effects: Headache, dizziness, dyspepsia (indigestion), nausea, diarrhea, and hypotension are frequently reported.
• Cardiovascular: Hypotension, syncope (fainting), palpitations, and tachycardia may occur, particularly during dose titration.
• Respiratory: Cough and upper respiratory tract infections have been reported in some patients.
• Gastrointestinal: Abdominal pain, vomiting, and constipation may occur but are generally mild.
• Serious adverse effects: Bleeding events (e.g., hemoptysis), severe hypotension, and anemia are less common but require immediate medical attention.
• Allergic reactions: Rash, itching, or swelling can occur rarely, necessitating discontinuation of the drug.
• Monitoring: Regular follow-ups and blood tests are important to identify and manage side effects early.

ADEMPAS 1.5mg Contraindications ADEMPAS 1.5mg

Certain conditions and concurrent medications make ADEMPAS unsafe or inappropriate. Patients should not use ADEMPAS under the following circumstances:

• Pregnancy and breastfeeding: ADEMPAS is contraindicated in pregnancy due to potential fetal harm. Effective contraception is essential during treatment and for one month after stopping.
• Concurrent use of nitrates or nitric oxide donors: This combination can cause severe hypotension and is strictly contraindicated.
• Use with PDE5 inhibitors: Concurrent use increases the risk of hypotension and is not recommended.
• Severe hepatic impairment: ADEMPAS should be avoided in patients with severe liver dysfunction due to altered metabolism and increased side effect risk.
• Hypotension: Patients with baseline low blood pressure (< 95 mmHg systolic) should not use ADEMPAS.
• Known hypersensitivity: Allergy to riociguat or any tablet excipients precludes use.

Storage of ADEMPAS 1.5mg

Proper storage of ADEMPAS ensures its stability and effectiveness throughout the shelf life.

• Temperature: Store tablets at controlled room temperature, between 20°C to 25°C (68°F to 77°F). Short excursions between 15°C and 30°C are allowed.
• Humidity: Keep the medication in its original blister pack to protect from moisture.
• Light protection: Store away from direct light and sunlight to avoid degradation.
• Keep out of reach of children: Store ADEMPAS in a secure place inaccessible to children and pets.
• Do not use after expiry date: Discard any tablets past the expiration date printed on the packaging.
• Disposal: Follow local regulations for safe disposal of unused or expired medication; do not flush tablets down the toilet or throw them in household trash.