ADEMPAS 2.5mg Tablets/Film-coated

What is ADEMPAS 2.5mg

ADEMPAS 2.5mg is a prescription medication containing the active ingredient Riociguat (micronized). It is formulated as film-coated tablets designed for oral administration. ADEMPAS is primarily indicated for the treatment of certain types of pulmonary hypertension, including:

• Pulmonary arterial hypertension (PAH): A condition characterized by high blood pressure in the arteries of the lungs, leading to symptoms such as shortness of breath, fatigue, and reduced exercise capacity.
• Chronic thromboembolic pulmonary hypertension (CTEPH): A form of pulmonary hypertension caused by old blood clots obstructing the pulmonary arteries, which can lead to right heart failure if untreated.

The medication works by helping to relax and widen the blood vessels in the lungs, thereby reducing the blood pressure within them and improving the heart's ability to pump blood effectively. ADEMPAS is often prescribed when surgical treatment for CTEPH is not an option or if symptoms persist after surgery.

Key characteristics of ADEMPAS include its micronized formulation, which enhances absorption and bioavailability, ensuring consistent therapeutic effects. ADEMPAS tablets come in a pack size of 42 tablets, arranged as three blister packs of 14 tablets each, facilitating patient adherence to prescribed dosing regimens.

How to use ADEMPAS 2.5mg

Using ADEMPAS correctly is essential for its effectiveness and to minimize the risk of side effects. Here are detailed instructions and recommendations for administration:

• Dosage and Titration: ADEMPAS therapy usually begins with a low dose (often 1 mg three times daily) to assess tolerance. The dose is gradually increased at intervals of approximately two weeks, based on patient response and blood pressure monitoring, up to a maximum dose of 2.5 mg three times daily.
• Administration: Take the tablet whole with water. It can be taken with or without food; however, consistency in how you take it relative to meals is recommended to avoid variability in absorption.
• Timing: ADEMPAS should be taken approximately every 8 hours (three times daily), aiming for evenly spaced doses to maintain stable drug levels in the bloodstream.
• 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 to compensate for missed ones.
• Monitoring: Regular follow-up with your healthcare provider is necessary to monitor blood pressure, symptoms, and possible side effects. Dose adjustments may be required based on clinical response and side effects.
• Precautions: Avoid sudden discontinuation of ADEMPAS without medical advice, as this may worsen symptoms.

Mode of Action ADEMPAS 2.5mg

ADEMPAS (Riociguat) works through a unique mechanism targeting the nitric oxide (NO)-soluble guanylate cyclase (sGC) pathway in vascular smooth muscle cells. The detailed mode of action includes:

• Stimulation of sGC enzyme: Riociguat directly stimulates soluble guanylate cyclase (sGC), an enzyme in the cells lining blood vessels, independently of nitric oxide availability.
• Increased cyclic GMP production: Activation of sGC enhances the conversion of GTP to cyclic guanosine monophosphate (cGMP), a signaling molecule responsible for vascular relaxation.
• Vasodilation: Elevated cGMP levels cause relaxation of smooth muscle cells in pulmonary arteries, leading to vasodilation—widening of blood vessels.
• Reduced pulmonary vascular resistance: By relaxing and dilating the blood vessels in the lungs, ADEMPAS reduces resistance against which the right side of the heart must pump.
• Improved heart function: The reduced vascular resistance lowers pulmonary artery pressure and improves cardiac output, helping alleviate symptoms of pulmonary hypertension.
• Additional effects: Riociguat may also inhibit vascular remodeling and proliferation, addressing underlying disease mechanisms beyond simple vasodilation.

This dual action—stimulating sGC and enhancing the NO pathway—makes ADEMPAS distinct from other pulmonary hypertension treatments and effective even when NO production is impaired.

ADEMPAS 2.5mg Interactions ADEMPAS 2.5mg

ADEMPAS (Riociguat) has several clinically significant drug interactions that can affect its safety and efficacy. Important interactions include:

• Nitrates and nitric oxide donors: Co-administration with nitrates (e.g., nitroglycerin) or NO donors can cause severe hypotension (dangerous blood pressure drops) and is contraindicated.
• Phosphodiesterase type 5 (PDE5) inhibitors: Concurrent use with PDE5 inhibitors like sildenafil or tadalafil is contraindicated due to additive vasodilatory effects increasing the risk of hypotension.
• Antihypertensive drugs: ADEMPAS may potentiate the blood pressure-lowering effects of other antihypertensives, requiring close monitoring and possible dose adjustments.
• CYP enzyme modulators: Strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) can increase riociguat plasma levels, raising side effect risk; dose adjustments or avoidance may be necessary.
• Smoking: Smoking induces CYP1A1, which can reduce ADEMPAS effectiveness by increasing drug metabolism. Patients should be advised about this interaction.
• Antacids and proton pump inhibitors: These may reduce riociguat absorption; spacing administration times is advisable.

Always inform your healthcare provider about all medications and supplements you are taking to avoid harmful interactions.

Dosage of ADEMPAS 2.5mg

The dosing of ADEMPAS must be individualized based on tolerability, therapeutic response, and blood pressure monitoring. Key dosage guidelines are:

• Starting dose: Typically, 1 mg taken orally three times daily (every 8 hours).
• Titration: Dose may be increased by 0.5 mg increments every two weeks based on tolerance and systolic blood pressure, aiming for the maximum recommended dose.
• Maximum dose: 2.5 mg three times daily is the highest dose recommended to minimize risks such as hypotension.
• Renal and hepatic impairment: Dose adjustments may be required in patients with moderate to severe kidney or liver dysfunction; careful monitoring is essential.
• Special populations: Elderly patients should be carefully monitored during dose escalation due to increased risk of hypotension.
• 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 doses.

Strict adherence to dosing instructions and follow-up visits for blood pressure monitoring and dose adjustments are critical for safe and effective treatment.

Possible side effects of ADEMPAS 2.5mg

Like all medications, ADEMPAS can cause side effects. Most are manageable but some require medical attention. Common and notable side effects include:

• Common side effects:
  • Headache
  • Dizziness or lightheadedness, especially when standing up (due to low blood pressure)
  • Indigestion (dyspepsia)
  • Nausea
  • Fatigue or weakness
  • Low blood pressure (hypotension), which may cause fainting
• Serious side effects:
  • Severe hypotension requiring immediate medical attention
  • Bleeding complications (rare but possible)
  • Pulmonary edema (fluid in the lungs) presenting with worsening shortness of breath
  • Allergic reactions including rash, itching, or swelling
  • Severe headaches or vision changes
• Monitoring: Patients should report persistent or severe symptoms to their healthcare provider promptly. Regular blood pressure checks are essential to detect hypotension early.

Managing side effects may require dose adjustments or additional supportive treatments, always under medical supervision.

ADEMPAS 2.5mg Contraindications ADEMPAS 2.5mg

There are several important contraindications where ADEMPAS must not be used due to risks outweighing benefits:

• Concurrent use with nitrates or nitric oxide donors: The combination can cause severe hypotension and is strictly contraindicated.
• Use with PDE5 inhibitors (e.g., sildenafil, tadalafil): This can lead to dangerous blood pressure drops and is contraindicated.
• Pregnancy and breastfeeding: Safety has not been established; ADEMPAS should be avoided during pregnancy and lactation.
• Severe hepatic impairment: ADEMPAS is contraindicated in patients with severe liver dysfunction due to altered metabolism and increased toxicity risk.
• Hypersensitivity: Known allergy to riociguat or any tablet components contraindicates use.
• Pregnancy risk: ADEMPAS is teratogenic in animal studies; women of childbearing potential must use effective contraception.

Storage of ADEMPAS 2.5mg

Proper storage of ADEMPAS tablets helps maintain their stability and effectiveness. Recommendations include:

• Store at room temperature, ideally between 20°C to 25°C (68°F to 77°F).
• Keep tablets in their original blister packaging until use to protect from moisture and light.
• Avoid exposure to excessive heat, humidity, or direct sunlight.
• Keep out of reach and sight of children and pets.
• Do not use the medication past its expiration date printed on the packaging.
• If tablets become discolored, damaged, or show any unusual characteristics, do not use them and consult a pharmacist.

Proper disposal of unused or expired medication should follow local regulations or pharmacy guidance to avoid environmental contamination or accidental ingestion.