ADEMPAS 0.5mg Tablets/Film-coated

What is ADEMPAS 0.5mg

ADEMPAS 0.5mg is a prescription medication containing the active ingredient Riociguat (micronized), formulated as film-coated tablets. It is primarily used to treat certain types of pulmonary hypertension, including chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH). These conditions involve high blood pressure in the arteries of the lungs, which can lead to serious heart complications if left untreated.

Key points about ADEMPAS 0.5mg:

• Active Ingredient: Riociguat, a soluble guanylate cyclase (sGC) stimulator.
• Formulation: Tablets, film-coated for ease of swallowing and better stability.
• Indications: Treatment of pulmonary hypertension, specifically CTEPH and PAH, to improve exercise capacity and delay clinical worsening.
• Packaging: Available in 42 tablets per pack, divided into 3 blister packs of 14 tablets each.
• Therapeutic Benefits: Helps relax and widen blood vessels in the lungs, improving blood flow and reducing strain on the heart.

ADEMPAS is typically prescribed by specialists experienced in managing pulmonary hypertension, and therapy involves careful dose titration and monitoring due to the complexity of the disease and the medication’s potent effects.

How to use ADEMPAS 0.5mg

Using ADEMPAS requires strict adherence to your healthcare provider’s instructions to ensure safety and efficacy. The following guidelines summarize important usage information:

• Dosage Schedule: ADEMPAS is generally taken three times a day (every 6 to 8 hours), with or without food.
• Starting Dose: Treatment usually begins with a low dose (e.g., 1 mg total daily, divided doses) which is carefully increased based on patient response and tolerance.
• Titration: Dose adjustments are made gradually, usually at intervals of 2 weeks or more, to reach the optimal dose that balances effectiveness and side effects.
• Swallowing: Take the tablet whole with water; do not crush or chew as it may affect drug release and absorption.
• Missed Dose: If you miss a dose, take it as soon as you remember unless it is close to the time of the next dose. Do not double the dose.
• Regular Monitoring: Periodic medical evaluations, including blood pressure checks and symptom assessments, are necessary during treatment.
• Avoid Alcohol: Alcohol can increase side effects such as dizziness and low blood pressure; avoid or limit consumption.
• Precautions: Inform your doctor about all other medications you take to avoid interactions.

Adhering to the prescribed regimen and attending follow-up appointments are critical to maximize the benefits of ADEMPAS and minimize risks.

Mode of Action ADEMPAS 0.5mg

ADEMPAS (Riociguat) works by targeting the nitric oxide (NO) pathway, which plays a key role in regulating vascular tone and blood pressure in the lungs.

• Soluble Guanylate Cyclase (sGC) Stimulation: Riociguat directly stimulates the enzyme sGC, which increases the production of cyclic guanosine monophosphate (cGMP).
• Enhanced cGMP Levels: Elevated cGMP leads to relaxation of vascular smooth muscle cells, causing vasodilation (widening of blood vessels).
• Improvement of Pulmonary Blood Flow: By dilating the pulmonary arteries, ADEMPAS reduces pulmonary arterial pressure and resistance, facilitating improved blood flow and oxygen exchange.
• Dual Mechanism: Riociguat sensitizes sGC to endogenous nitric oxide and also stimulates sGC independently of NO, making it effective even in conditions where NO levels are low.
• Anti-Remodeling Effects: Besides vasodilation, Riociguat may inhibit pathological remodeling of pulmonary vessels, which is common in pulmonary hypertension.

This mechanism helps alleviate symptoms such as shortness of breath and fatigue by reducing the workload on the right side of the heart and improving oxygen delivery to the body.

ADEMPAS 0.5mg Interactions ADEMPAS 0.5mg

ADEMPAS has several important drug interactions that can affect its safety and effectiveness. Always inform your healthcare provider about all medications, supplements, and herbal products you are using. Key interactions include:

• Nitrates (e.g., nitroglycerin): Combining ADEMPAS with nitrates can cause severe hypotension (dangerously low blood pressure) and is contraindicated.
• Phosphodiesterase-5 Inhibitors (e.g., sildenafil, tadalafil): Concomitant use increases the risk of hypotension and is contraindicated.
• Strong CYP450 Inducers (e.g., rifampicin, phenytoin, carbamazepine): These drugs may reduce Riociguat plasma concentrations, decreasing its effectiveness.
• CYP450 Inhibitors (e.g., ketoconazole, erythromycin): May increase Riociguat levels, potentially increasing side effects.
• Antacids: May reduce the absorption of Riociguat; spacing the doses apart by at least 1 hour is advisable.
• Antihypertensives: ADEMPAS can potentiate the effects of blood pressure-lowering agents, increasing risk of hypotension.

Careful dose adjustment and close monitoring are essential when ADEMPAS is administered alongside interacting drugs.

Dosage of ADEMPAS 0.5mg

The dosage of ADEMPAS is individualized based on patient response, tolerability, and clinical condition. General dosage guidelines include:

• Initial Dose: Typically 1 mg daily divided into three doses (0.33 mg three times daily) or 1 mg twice daily depending on clinical protocol.
• Titration: Dose may be increased in increments of 0.5 mg every 2 weeks up to a maximum of 2.5 mg three times daily (7.5 mg total daily dose).
• Adjustment Criteria: Dose adjustments depend on blood pressure, side effects, and symptom improvement.
• Renal Impairment: Dose adjustments may be necessary in moderate renal impairment; caution in severe renal impairment.
• Hepatic Impairment: Use is contraindicated or limited in severe liver dysfunction.
• Elderly Patients: Start at lower doses and titrate carefully due to increased sensitivity.
• Missed Dose: Take as soon as remembered unless close to next dose; never double up.

The goal is to achieve the highest tolerated dose that effectively controls symptoms without causing adverse effects.

Possible side effects of ADEMPAS 0.5mg

Like all medications, ADEMPAS may cause side effects, ranging from mild to severe. Patients should be aware of the potential adverse effects and report any unusual symptoms to their healthcare provider promptly.

• Common Side Effects:
  • Headache
  • Dizziness or lightheadedness, especially when standing (due to low blood pressure)
  • Nausea and vomiting
  • Indigestion or abdominal discomfort
  • Diarrhea
  • Flushing or redness of the face
  • Low blood pressure (hypotension)
• Serious Side Effects (Seek Medical Attention Immediately):
  • Severe hypotension causing fainting or falls
  • Bleeding or bruising easily
  • Severe headache or vision changes (possible signs of intracranial bleeding)
  • Signs of allergic reaction: rash, itching, swelling, difficulty breathing
  • Worsening shortness of breath or chest pain
• Other Possible Effects:
  • Anemia (low red blood cells)
  • Edema (swelling in limbs)
  • Back pain
  • Cough

Regular monitoring and communication with healthcare providers are essential to manage side effects effectively and adjust therapy as needed.

ADEMPAS 0.5mg Contraindications ADEMPAS 0.5mg

ADEMPAS should not be used in certain conditions due to risks that outweigh benefits. Contraindications include:

• Use with Nitrates or Nitric Oxide Donors: Concomitant use can cause severe hypotension.
• Concomitant use with Phosphodiesterase-5 Inhibitors: Drugs like sildenafil or tadalafil must be avoided due to risk of dangerous blood pressure drops.
• Pregnancy: ADEMPAS is contraindicated during pregnancy due to potential harm to the fetus.
• Severe Hepatic Impairment: Use is contraindicated in patients with severe liver dysfunction.
• Hypersensitivity: Known allergy to Riociguat or any tablet components.
• Hypotension: Patients with baseline low blood pressure should avoid ADEMPAS or use with extreme caution.

Always inform your healthcare provider of your complete medical history to ensure safe use of this medication.

Storage of ADEMPAS 0.5mg

Proper storage of ADEMPAS is essential to maintain its efficacy and safety. Follow these guidelines:

• Temperature: Store at room temperature, ideally between 20°C to 25°C (68°F to 77°F).
• Avoid Moisture: Keep the tablets in their original blister pack until use to protect from humidity.
• Light Protection: Store away from direct sunlight or bright light.
• Keep Out of Reach: Store the medication in a secure place away from children and pets.
• Do Not Freeze: Avoid freezing or exposing tablets to extreme cold.
• Discard Properly: Dispose of expired or unused medication safely, following local regulations or pharmacy guidance.

Following these storage instructions helps preserve the stability and potency of ADEMPAS tablets throughout their shelf life.