ADEMPAS 2mg Tablets/Film-coated

What is ADEMPAS 2mg

ADEMPAS (active ingredient: Riociguat micronized) is a prescription medication primarily used to treat certain types of pulmonary hypertension, including chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH). It belongs to a class of drugs known as soluble guanylate cyclase (sGC) stimulators. These conditions involve high blood pressure in the arteries of the lungs, which can lead to symptoms such as shortness of breath, fatigue, and reduced exercise capacity.

Key points about ADEMPAS:

• Indications: Approved for treating adults with PAH and inoperable or persistent/recurrent CTEPH to improve exercise capacity and delay clinical worsening.
• Formulation: Available as film-coated tablets for oral administration, facilitating ease of use.
• Active Ingredient: Riociguat micronized enhances nitric oxide signaling in the pulmonary vasculature, leading to vasodilation.
• Impact: By reducing pulmonary arterial pressure, it improves symptoms, quality of life, and potentially long-term outcomes.
• Prescription-only: Must be used under close medical supervision with monitoring for effectiveness and adverse effects.

Overall, ADEMPAS is a targeted therapy for serious pulmonary vascular diseases, aiming to alleviate symptoms and improve patients’ functional status.

How to use ADEMPAS 2mg

Using ADEMPAS correctly is crucial for maximizing its therapeutic benefits and minimizing risks. Patients should strictly follow their healthcare provider’s instructions and the accompanying patient information leaflet.

• Dosage initiation: Treatment usually starts at a lower dose (e.g., 1 mg three times daily), then gradually increased based on individual tolerance and response to reach the maintenance dose, typically up to 2.5 mg three times daily.
• Administration: Tablets should be swallowed whole with water and can be taken with or without food.
• Timing: Maintain consistent timing by spacing doses approximately 6-8 hours apart throughout the day to ensure steady blood levels.
• Monitoring: Regular blood pressure monitoring is essential due to risk of hypotension; dose adjustments may be necessary.
• Avoid abrupt changes: Do not suddenly stop taking ADEMPAS without consulting your doctor as it may worsen symptoms.
• Missed dose: If a dose is missed, take it as soon as possible unless it is almost time for the next dose; do not double up doses.
• Medical follow-up: Regular follow-ups with pulmonary specialists and routine lab tests to assess liver function and efficacy are advised.

Mode of Action ADEMPAS 2mg

ADEMPAS works by stimulating soluble guanylate cyclase (sGC), an enzyme involved in the nitric oxide (NO) signaling pathway critical for vascular relaxation. Pulmonary hypertension involves constricted blood vessels in the lungs, increasing pressure and strain on the heart.

• NO-sGC-cGMP pathway: Normally, NO binds to sGC, activating it to convert GTP to cyclic GMP (cGMP), which causes smooth muscle relaxation and vasodilation.
• Riociguat’s action: ADEMPAS directly stimulates sGC independently of NO and also sensitizes sGC to available NO, enhancing cGMP production.
• Result: Elevated cGMP leads to relaxation of pulmonary artery smooth muscle cells, reducing pulmonary vascular resistance and lowering pulmonary arterial pressure.
• Dual action: The combination of NO sensitization and direct stimulation differentiates ADEMPAS from other vasodilators.
• Clinical effect: This vasodilation reduces right ventricular workload, improving cardiac output and exercise tolerance in pulmonary hypertension patients.

ADEMPAS 2mg Interactions ADEMPAS 2mg

ADEMPAS can interact with several drugs, potentially affecting its efficacy or increasing the risk of adverse effects. It is vital to inform healthcare providers about all medications and supplements currently used.

• Nitrates and NO donors: Co-administration can cause severe hypotension due to additive vasodilatory effects and should be strictly avoided.
• Phosphodiesterase type 5 (PDE5) inhibitors: Drugs like sildenafil or tadalafil increase cGMP by inhibiting its breakdown. Combined use with ADEMPAS is contraindicated because of risk of profound hypotension.
• Antacids: May reduce ADEMPAS absorption; separate administration times by at least 1 hour.
• Strong CYP3A4 inducers/inhibitors: Drugs such as rifampin (inducer) can lower ADEMPAS levels, reducing effectiveness; inhibitors like ketoconazole may increase ADEMPAS concentration, enhancing side effects.
• Anticoagulants: Riociguat may increase bleeding risk when used with warfarin or other anticoagulants; careful monitoring is recommended.
• Smoking: Induces CYP enzymes, potentially reducing ADEMPAS plasma concentration and efficacy; patients are advised to avoid smoking.

Dosage of ADEMPAS 2mg

The dosage of ADEMPAS is individualized and titrated carefully to balance effectiveness with safety, especially to avoid excessive hypotension.

• Starting dose: Typically 1 mg three times daily (TID).
• Titration: Dose may be increased every 2 weeks by 0.5 mg increments based on patient tolerance and blood pressure readings.
• Maximum dose: Generally, 2.5 mg TID is the maximum recommended maintenance dose.
• Renal or hepatic impairment: Dosage adjustments may be required; patients with moderate hepatic impairment should be monitored closely.
• Missed doses: Resume normal dosing schedule; do not double doses.
• Special populations: Not typically recommended for children or pregnant women without specialist guidance.
• Monitoring: Blood pressure, symptoms, and side effects should guide dosage adjustments throughout treatment.

Possible side effects of ADEMPAS 2mg

Like all medications, ADEMPAS can cause side effects, though not everyone experiences them. Awareness and early reporting of side effects help optimize treatment.

• Common side effects: Headache, dizziness, nausea, dyspepsia (indigestion), diarrhea, hypotension (low blood pressure), and flushing.
• Serious side effects: Syncope (fainting), bleeding complications, severe hypotension, and worsening pulmonary symptoms require immediate medical attention.
• Respiratory symptoms: Cough or worsening breathlessness should be monitored closely.
• Other possible effects: Anemia, peripheral edema (swelling), and arrhythmias.
• Allergic reactions: Rare but possible; signs include rash, itching, swelling, or difficulty breathing.
• Management: Side effects can often be managed by dose adjustments or symptomatic treatment; always report new or worsening symptoms to a healthcare provider.

ADEMPAS 2mg Contraindications ADEMPAS 2mg

Certain conditions and concurrent therapies contraindicate the use of ADEMPAS due to risks of serious adverse effects.

• Pregnancy and breastfeeding: ADEMPAS is contraindicated as it may harm the fetus and is not recommended during breastfeeding.
• Use with nitrates or NO donors: Co-administration is contraindicated due to risk of severe hypotension.
• Use with PDE5 inhibitors: Combination with sildenafil, tadalafil, or similar drugs is contraindicated.
• Severe hepatic impairment: ADEMPAS should not be used in patients with severe liver dysfunction (Child-Pugh C).
• Hypotension or uncontrolled hypertension: Caution is necessary; ADEMPAS should not be used if baseline blood pressure is low or unstable.
• Known hypersensitivity: Allergy to Riociguat or any tablet excipients.
• Recent use of PDE5 inhibitors or nitrates: Adequate washout periods must be observed before initiating ADEMPAS.

Storage of ADEMPAS 2mg

Proper storage of ADEMPAS helps maintain its effectiveness and safety.

• Temperature: Store tablets at room temperature, ideally between 20°C to 25°C (68°F to 77°F).
• Light protection: Keep tablets in their original blister packaging to protect from moisture and light.
• Moisture: Store in a dry place; avoid humid environments such as bathrooms.
• Keep out of reach of children: Store securely to prevent accidental ingestion.
• Do not use after expiration date: Discard any unused medication past its expiry.
• Disposal: Follow local guidelines for disposal of unused or expired medicines; do not flush or throw in household waste.
• Transport: When traveling, keep medication in original packaging and avoid extreme temperatures.