ADEMPAS 1mg Tablets/Film-coated

What is ADEMPAS 1mg

ADEMPAS 1mg is a prescription medication containing the active ingredient Riociguat (micronized), formulated as film-coated tablets. It is primarily used to treat specific types of pulmonary hypertension, including pulmonary arterial hypertension (PAH) and chronic thromboembolic pulmonary hypertension (CTEPH). These are serious conditions characterized by 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: ADEMPAS is approved for improving exercise ability and delaying clinical worsening in patients diagnosed with PAH and for patients with CTEPH who are not candidates for surgery or have persistent/recurrent pulmonary hypertension after surgical intervention.
• Active Ingredient: Riociguat acts by stimulating soluble guanylate cyclase, a key enzyme in the nitric oxide signaling pathway.
• Formulation: The tablets are micronized for better absorption and are film-coated to facilitate swallowing and improve stability.
• Packaging: Available in blister packs of 42 tablets (14 tablets per blister, 3 blisters total), ensuring a convenient supply for multiple weeks.
• Therapeutic Goal: By reducing pulmonary artery pressure, ADEMPAS helps to alleviate symptoms and improve patients’ quality of life and functional capacity.

It is important to use ADEMPAS strictly under medical supervision because pulmonary hypertension requires precise diagnosis and careful monitoring due to the complexity and severity of the disease.

How to use ADEMPAS 1mg

Using ADEMPAS correctly is critical for achieving its therapeutic benefits and minimizing risks. Follow these guidelines closely:

• Dosage Schedule: ADEMPAS is usually taken three times a day (every 6 to 8 hours), preferably at the same times each day to maintain consistent blood levels.
• Administration: Take the film-coated tablets orally with or without food. Swallow tablets whole with water; do not crush, chew, or split them.
• Starting Dose: The initial dose is typically low (e.g., 1 mg three times daily), then gradually titrated based on blood pressure response and tolerability to reach the optimal maintenance dose, which may vary per patient.
• Titration and Monitoring: Frequent clinical monitoring, including blood pressure measurements, is necessary during dose adjustment to avoid hypotension or other adverse effects.
• Missed Dose: If you miss a dose, take it as soon as you remember unless it is almost time for your next dose. Do not double the dose to catch up.
• Medical Supervision: Regular follow-ups with your healthcare provider are essential to monitor the treatment’s effectiveness and adjust doses safely.
• Special Considerations: Inform your doctor if you experience side effects or new symptoms, as dose modifications might be required.

Never stop taking ADEMPAS abruptly without consulting your healthcare provider, as this can worsen your condition.

Mode of Action ADEMPAS 1mg

ADEMPAS contains Riociguat, which is a novel soluble guanylate cyclase (sGC) stimulator. Understanding its mode of action is essential to appreciate its clinical benefits in pulmonary hypertension:

• Target Enzyme: Riociguat directly stimulates soluble guanylate cyclase, an enzyme in the smooth muscle cells of the blood vessels that plays a critical role in the nitric oxide (NO) signaling pathway.
• Nitric Oxide Pathway: Under normal conditions, NO binds to sGC, activating it to convert GTP into cyclic GMP (cGMP). cGMP causes relaxation of vascular smooth muscle, leading to vasodilation and decreased vascular resistance.
• Dual Action: Riociguat works by two complementary mechanisms:
  • It sensitizes sGC to endogenous NO, enhancing the enzyme's response.
  • It directly stimulates sGC independently of NO availability, which is particularly important in disease states where NO levels are reduced.
• Effect on Pulmonary Arteries: By increasing cGMP levels, Riociguat induces relaxation and dilation of the pulmonary arteries, reducing pulmonary arterial pressure and improving blood flow.
• Additional Benefits: The improved blood flow lowers the workload on the right side of the heart, which often suffers from increased strain in pulmonary hypertension.
• Overall Outcome: Enhanced exercise capacity, reduced symptoms, and potential delay in disease progression.

This mechanism distinguishes ADEMPAS from other vasodilators and provides a targeted approach to treating pulmonary hypertension at the molecular level.

ADEMPAS 1mg Interactions ADEMPAS 1mg

ADEMPAS (Riociguat) can interact with various medications and substances, potentially altering its effects or increasing the risk of adverse reactions. Understanding these interactions is important for safe use:

• Nitrates and Nitric Oxide Donors: Concurrent use with nitrates (e.g., nitroglycerin) or nitric oxide donors is contraindicated due to the risk of severe hypotension caused by additive vasodilatory effects.
• Phosphodiesterase Type 5 Inhibitors (PDE5i): Combining ADEMPAS with PDE5 inhibitors (e.g., sildenafil, tadalafil) is contraindicated because of an increased risk of dangerously low blood pressure.
• CYP Enzyme Modulators: Drugs that induce or inhibit CYP1A1, CYP3A4, and CYP2J2 enzymes may affect Riociguat metabolism:
  • Strong CYP inhibitors (e.g., ketoconazole) may increase ADEMPAS plasma levels, raising side effect risks.
  • CYP inducers (e.g., rifampicin, St. John’s Wort) may decrease ADEMPAS levels, reducing efficacy.
• Antacids: Antacids containing magnesium or aluminum can reduce ADEMPAS absorption if taken simultaneously; separate administration by at least 1 hour.
• Other Antihypertensive Agents: Combining ADEMPAS with other blood pressure-lowering drugs requires careful monitoring due to additive hypotensive effects.
• Smoking: Smoking induces CYP1A1 and may reduce ADEMPAS plasma concentrations, potentially requiring dose adjustments.

Always inform your healthcare provider about all medications, supplements, and lifestyle habits to prevent harmful interactions with ADEMPAS.

Dosage of ADEMPAS 1mg

Dosage of ADEMPAS must be individualized according to patient response, tolerability, and clinical condition. The following provides an overview of typical dosing recommendations:

• Initial Dose: Generally, therapy starts at 1 mg three times daily, taken approximately every 6 to 8 hours.
• Titration: Dose is gradually increased every 2 weeks by 0.5 mg increments based on blood pressure and clinical response.
• Maintenance Dose: The usual maintenance dose ranges from 1.5 mg to 2.5 mg three times daily. The maximum recommended dose is 2.5 mg three times daily.
• Adjustments for Renal or Hepatic Impairment: Caution is required, and dose titration should be slower, especially in patients with moderate to severe renal or hepatic dysfunction.
• Contraindications for Dose Increase: Avoid dose escalation if hypotension or other adverse effects occur.
• 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: Regular blood pressure checks and clinical assessments are necessary during dose titration and maintenance to optimize therapy.

Strict adherence to the prescribed dosing schedule and regular follow-up appointments enhance both safety and effectiveness of ADEMPAS treatment.

Possible side effects of ADEMPAS 1mg

ADEMPAS (Riociguat) may cause side effects, ranging from mild to serious. Awareness of potential adverse effects is important for timely recognition and management:

• Common Side Effects:
  • Headache
  • Dizziness or lightheadedness, especially when standing up (due to lowered blood pressure)
  • Gastrointestinal symptoms such as nausea, indigestion, diarrhea, or abdominal pain
  • Low blood pressure (hypotension), which may cause fatigue or fainting
• Less Common but Serious Side Effects:
  • Bleeding complications (e.g., nosebleeds, hemoptysis) due to vasodilation and effects on blood vessels
  • Severe hypotension leading to syncope or cardiovascular instability
  • Respiratory infections or worsening of pulmonary symptoms
  • Allergic reactions including rash, itching, or swelling
• When to Seek Medical Attention: Immediate care is warranted if symptoms of severe hypotension, chest pain, severe headache, or allergic reactions occur.
• Risk Mitigation: Regular monitoring and dose adjustments can help minimize side effects, especially hypotension.

Communicate any new or worsening symptoms to your healthcare provider promptly to ensure safe and effective treatment.

ADEMPAS 1mg Contraindications ADEMPAS 1mg

ADEMPAS should not be used in certain patients or situations due to potential risks. Contraindications include:

• Concurrent Use with Nitrates or Nitric Oxide Donors: Risk of severe hypotension is increased with these drugs.
• Combination with PDE5 Inhibitors: Sildenafil, tadalafil, and similar medications are contraindicated due to additive blood pressure-lowering effects.
• Pregnancy: ADEMPAS is contraindicated during pregnancy because of potential harm to the fetus (Pregnancy Category X). Effective contraception is necessary for women of childbearing potential.
• Severe Hepatic Impairment: Not recommended due to altered metabolism and increased risk of adverse effects.
• Hypersensitivity: Patients with known hypersensitivity to Riociguat or any excipients should not use this medication.
• Severe Hypotension: Patients with baseline low blood pressure should avoid ADEMPAS due to risk of further hypotension.

Adhering to these contraindications is critical for patient safety.

Storage of ADEMPAS 1mg

Proper storage of ADEMPAS tablets ensures the medication’s effectiveness and safety. Follow these storage recommendations:

• Temperature: Store at room temperature, ideally between 20°C and 25°C (68°F and 77°F). Avoid exposure to excessive heat or cold.
• Humidity: Keep the tablets in their original blister packaging until use to protect from moisture and humidity.
• Light: Protect from direct sunlight and store in a dark place or container to prevent degradation.
• Handling: Keep out of reach of children and pets to prevent accidental ingestion.
• Disposal: Do not use tablets past the expiration date. Dispose of unused or expired medication safely, following local guidelines or pharmacy take-back programs.
• Transport: Avoid carrying ADEMPAS in places subject to extreme temperatures, such as cars on hot days.

Following these storage instructions helps maintain ADEMPAS's stability and therapeutic efficacy throughout the course of treatment.