Adempas

Adempas

riociguat

Manufacturer:

Bayer

Distributor:

Zuellig
/
Four Star
Concise Prescribing Info
Contents
Riociguat
Indications/Uses
Treatment of adult patients w/ WHO functional class II-III w/ inoperable chronic thromboembolic pulmonary HTN (CTEPH), or persistent or recurrent CTEPH after surgical treatment, to improve exercise capacity. As monotherapy or in combination w/ endothelin receptor antagonists for treatment of adult patients w/ pulmonary arterial HTN (PAH) w/ WHO functional class II-III to improve exercise capacity.
Dosage/Direction for Use
Initially 1 mg tds (approx 6-8 hr apart) for 2 wk. Increase dose by 0.5 mg tds every 2 wk to a max of 2.5 mg tds if systolic BP ≥95 mmHg & patient has no signs or symptoms of hypotension. If during the up-titration phase systolic BP decreases <95 mmHg & patient shows signs & symptoms of hypotension, decrease current dose by 0.5 mg tds. Max dose: 7.5 mg daily.
Administration
May be taken with or without food. : For patients who are unable to swallow, tab may be crushed & mixed w/ water or soft foods (eg, applesauce). Antacids should be taken at least 2 hr before or 1 hr after riociguat.
Contraindications
Hypersensitivity. Systolic BP <95 mmHg at treatment initiation. Pulmonary HTN associated w/ idiopathic interstitial pneumonias. Co-administration w/ PDE5 inhibitors (eg, sildenafil, tadalafil, vardenafil); nitrates or nitric oxide donors (eg, amyl nitrite). Severe hepatic impairment (Child Pugh C). Pregnancy.
Special Precautions
Not recommended in patients w/ pulmonary veno-occlusive disease. Risk of resp tract bleeding, particularly in patients on anticoagulant therapy. Avoid in patients w/ history of serious haemoptysis or who have previously undergone bronchial arterial embolisation. Patients on antihypertensive therapy or w/ resting hypotension, hypovolaemia, severe left ventricular outflow obstruction or autonomic dysfunction. Rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption. Reduced plasma conc of riociguat in smokers; dose adjustment may be necessary in patients who start or stop smoking during treatment. Concomitant use w/ strong CYP450 & P-gp/BCRP inhibitors (eg, azole antimycotics or HIV PIs); strong CYP1A1 inhibitor (eg, erlotinib); strong P-gp/BCRP inhibitor (eg, cyclosporine A). Moderate influence on the ability to drive & use machines. Patients w/ moderate renal or hepatic impairment. Not recommended in patients w/ severe renal impairment. Women of childbearing potential must use effective contraception during therapy. Should not be used during breastfeeding. Elderly ≥65 yr. Childn & adolescents <18 yr.
Adverse Reactions
Dizziness, headache; dyspepsia, diarrhoea, nausea, vomiting; oedema peripheral. Gastroenteritis; anaemia; palpitations; hypotension; haemoptysis, epistaxis, nasal congestion; gastritis, GERD, dysphagia, GI & abdominal pains, constipation, abdominal distension.
Drug Interactions
Potentiated BP lowering effect of nitrates or nitric oxide donors (eg, amyl nitrite), including recreational drugs called 'poppers'. Additive BP lowering effect w/ PDE5 inhibitors (eg, sildenafil, tadalafil, vardenafil). Increased mean AUC & mean Cmax w/ strong CYP & P-gp/BCRP inhibitors (eg, ketoconazole, itraconazole) or HIV PIs (eg, ritonavir); strong P-gp/BCRP inhibitors (eg, cyclosporine A). Increased exposure of riociguat metabolite M1 w/ UGT 1A1 & 1A9 inhibitors. Increased exposure w/ strong CYP1A1 inhibitors (eg, erlotinib, gefitinib), especially in smokers. Potential lowered oral bioavailability w/ drugs that increase upper GI pH. Decreased mean AUC & mean Cmax w/ antacid Al/Mg hydroxide. Decreased plasma conc w/ moderate CYP3A4 inducers (eg, bosentan), strong CYP3A4 inducers (eg, phenytoin, carbamazepine, phenobarbitone, St. John's Wort). Reduced exposure w/ smoking. Potential interaction w/ CYP1A1 substrates.
MIMS Class
Other Antihypertensives
ATC Classification
C02KX05 - riociguat ; Belongs to the class of other antihypertensives. Used in the treatment of pulmonary arterial hypertension.
Presentation/Packing
Form
Adempas FC tab 1 mg
Packing/Price
42's
Form
Adempas FC tab 1.5 mg
Packing/Price
42's
Form
Adempas FC tab 2 mg
Packing/Price
42's
Form
Adempas FC tab 2.5 mg
Packing/Price
42's
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