Adempas belong to a class of drugs called soluble guanylate cyclase activators. This type of medication helps to relax arteries, increase blood flow, and lower blood pressure.

1、 Drug name

1. Common name: Liosigua tablets

2. Product Name: Adempas

3. English name: RiociguatTables

2、 Indications

Adempas is a soluble guanylate cyclase (sGC) stimulant suitable for treating the following adult patients:

1. Chronic thromboembolic pulmonary hypertension (CTEPH): Used for patients with persistent/recurrent CTEPH or inoperable CTEPH after surgery (pulmonary endarterectomy) to improve mobility and World Health Organization (WHO) functional classification.

2. Pulmonary arterial hypertension (PAH): Used to improve exercise capacity, WHO functional classification, and delay clinical deterioration. Its effectiveness has been demonstrated in patients treated with Adempas monotherapy or in combination with endothelin receptor antagonists or prostaglandins.

3、 Specifications

1.5mg * 100 pieces/box.

4、 Main components

Active ingredient: Riociguat.

5、 Usage and dosage

1. Initial dose: The recommended initial dose is 1 milligram per dose, three times a day (approximately every 6-8 hours).

2. Dose escalation:

If the patient's systolic blood pressure remains above 95 mmHg and there are no symptoms or signs of hypotension, the dose can be increased by 0.5 milligrams per dose, three times a day.

The interval between dose escalation should not be less than 2 weeks.

It can be increased to the highest dose that the patient can tolerate, but the maximum dose three times a day should not exceed 2.5 milligrams.

3. Administration method: It can be taken with meals or on an empty stomach. For patients with swallowing difficulties, the pill can be crushed and immediately mixed with water or soft food (such as apple sauce) for consumption.

4. Maximum daily dose: Unless otherwise instructed by a doctor, the total daily dose should not exceed 7.5 milligrams.

6、 Dose adjustment

1. Patients who cannot tolerate hypotension: Consider starting with a dose of 0.5 milligrams per dose, three times a day.

2. When low blood pressure symptoms occur: If low blood pressure symptoms occur, the dose should be reduced by 0.5 milligrams each time, three times a day.

3. Smokers: Plasma drug concentrations may decrease in smokers. If the patient tolerates, titration to a dose higher than 2.5 milligrams per dose, three times a day, may be considered. If the patient quit smoking, the dosage may need to be reduced.

4. Patients using potent CYP and P-gp/BCRP inhibitors: When using potent CYP and P-gp/BCRP inhibitors (such as azole antifungal drugs, HIV protease inhibitors) at the same time, an initial dose of 0.5 milligrams per dose, three times a day, should be considered, and signs and symptoms of hypotension should be monitored.

5. After interrupting the medication: If the treatment is interrupted for 3 days or more, the dose needs to be titrated again when resuming the treatment.

7、 Medication precautions

1. Before and after meals: can be taken with food or on an empty stomach without special requirements.

2. Missed dose: If one dose is missed, the next dose should be taken at the regular time. Do not supplement the missed dose.

3. Vomiting: The instructions do not explicitly mention the treatment after vomiting. If vomiting occurs, it is recommended to consult a doctor or pharmacist.

4. Antacids: When taking antacids containing aluminum hydroxide or magnesium hydroxide, there should be at least an hour of separation from Adempas.

5. Conversion with other drugs:

Switching from Sildenafil to Adempas: Discontinue Sildenafil for at least 24 hours.

Convert from Tadalafil to Adempas: Discontinue Tadalafil for at least 48 hours.

Switching from Adempas to PDE5 inhibitors: Discontinue Adempas for at least 24 hours.

8、 Medication for special populations

1. Pregnant women: Do not use. Adempas may cause harm to the fetus and pose a risk of teratogenicity. All female patients must obtain this medication through a restricted program called the AdempasREMS program.

2. Women of childbearing age must undergo pregnancy testing before starting treatment, monthly during treatment, and one month after discontinuing medication. Effective contraceptive measures must be taken during the treatment period and within one month after discontinuation of medication.

3. Breastfeeding women: It is recommended not to breastfeed.

4. Children: Safety and efficacy have not yet been established.

5. Elderly: No need to adjust dosage, but elderly patients may have higher drug exposure.

6. Patients with renal insufficiency: Not recommended for those with creatinine clearance rate<15 mL/min or undergoing dialysis.

7. Patients with liver dysfunction: Not recommended for severe liver dysfunction (Child Pugh C grade).

9、 Adverse reactions

1. Common adverse reactions (incidence ≥ 3%, higher than placebo group): headache, indigestion/gastritis, dizziness, nausea, diarrhea, hypotension, vomiting, anemia, gastroesophageal reflux disease, constipation.

2. Other potential adverse reactions: palpitations, nasal congestion, nosebleeds, difficulty swallowing, abdominal distension, peripheral edema.

3. Serious adverse reactions:

Embryo fetal toxicity.

4. Bleeding: In clinical trials, the incidence of severe bleeding (including fatal hemoptysis) was 2.4% in the Adempas group and 0% in the placebo group.

Symptomatic hypotension.

5. Deterioration of Pulmonary Venous Occlusion Disease (PVOD): If signs of pulmonary edema appear, the possibility of PVOD should be considered, and if diagnosed, medication should be discontinued.

10、 Contraindications

1. Pregnant women.

2. Used simultaneously with any form of nitrate or nitric oxide donor (such as nitroglycerin, isoamyl nitrite).

3. Used simultaneously with phosphodiesterase (PDE) inhibitors such as sildenafil, tadalafil, vardenafil, dipyridamole, theophylline.

4. Used simultaneously with other soluble guanylate cyclase (sGC) stimulants.

5. Patients with idiopathic interstitial pneumonia associated pulmonary arterial hypertension (PH-IIP).

11、 Drug interactions

1. Prohibited combination: nitrate, nitric oxide donor, PDE5 inhibitor, other sGC stimulators.

2. Caution should be exercised when combining/adjusting dosage:

Strong CYP and P-gp/BCRP inhibitors (such as ketoconazole and ritonavir): Increasing exposure to levocetirizine may lead to hypotension, and it is necessary to consider reducing the initial dose and monitoring.

Smoking: significantly reduces plasma drug concentration, may require higher doses; After quitting smoking, it may be necessary to reduce the dosage.

Strong CYP3A inducers (such as rifampicin, phenytoin, carbamazepine, St. John's wort): may significantly reduce exposure to levocetirizine, but there are no dose adjustment guidelines available.

Antacids: Reduce absorption and should be taken at least 1 hour apart.

12、 Storage method

1. Store at room temperature of 15 ° C to 30 ° C (59 ° F to 86 ° F).

2. Please keep out of reach of children.

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