Adempas (riociguat) is a soluble guanylate cyclase stimulator tablet for oral administration. Riociguat is methyl 4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo [3,4-b]pyridin-3-yl]-5-pyrimidinyl(methyl)carbamate with the following structural formula: C 20 H 19 FN 8 O 2 Riociguat is a white to yellowish, crystalline, non-hygroscopic substance with a molecular weight of 422.42 g/mol. In solid form it is stable to temperature, light, and humidity. The solubility at 25°C in water: 4 mg/L, in ethanol: ...

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Adempas is a soluble guanylate cyclase (sGC) stimulator indicated for the treatment of adults with: • Persistent/recurrent Chronic Thromboembolic Pulmonary Hypertension (CTEPH) (WHO Group 4) after surgical treatment or inoperable CTEPH to improve exercise capacity and WHO functional class. • Pulmonary Arterial Hypertension (PAH) (WHO Group 1) to improve exercise capacity, improve WHO functional class and to delay clinical worsening. 1.1 Chronic-Thromboembolic Pulmonary Hypertension Adempas is indi...

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Tablets: film-coated, round, bi-convex: • 0.5 mg, white, with “BAYER” cross on one side and “0.5” and “R” on the other side • 1 mg, pale-yellow, with “BAYER” cross on one side and “1” and “R” on the other side • 1.5 mg, yellow-orange, with “BAYER” cross on one side and “1.5” and “R” on the other side • 2 mg, pale orange, with “BAYER” cross on one side and “2” and “R” on the other side • 2.5 mg, red-orange, with “BAYER” cross on one side and “2.5” and “R” on the other side Tablets: 0.5 mg, 1 mg, ...

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• Initiate treatment at 1 mg taken three times a day. • For patients who may not tolerate the hypotensive effect of Adempas, consider a starting dose of 0.5 mg, three times a day. • Increase dosage by 0.5 mg at intervals of no sooner than 2-weeks as tolerated to a maximum of 2.5 mg three times a day. • Tablets may be crushed and mixed with water or soft foods for patients who have difficulty swallowing. 2.1 Recommended Dosage in Adult Patients The recommended starting dosage is 1 mg taken 3 times a ...

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• Pregnancy • Use with nitrates or nitric oxide donors in any form • Use with PDE inhibitors ( 2.6 , 4.3 , 7.1 ) • Patients with concomitant use of other soluble guanylate cyclase (sGC) stimulators. • • Pulmonary hypertension associated with idiopathic interstitial pneumonias (PH-IIP) 4.1 Pregnancy Based on data from animal reproduction studies, Adempas may cause fetal harm when administered to a pregnant woman and is contraindicated in females who are pregnant. Adempas was consistently shown to h...

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• Symptomatic hypotension • Bleeding • Pulmonary edema in patients with pulmonary veno-occlusive disease. If confirmed, discontinue treatment 5.1 Embryo-Fetal Toxicity Based on data from animal reproduction studies, Adempas may cause embryo-fetal toxicity when administered to a pregnant female and is contraindicated in females who are pregnant. Advise females of reproductive potential of the potential risk to a fetus. Obtain a pregnancy test before the start of treatment, monthly during treatment, ...

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• Strong CYP and P-gp/BCRP inhibitors: For patients receiving strong CYP and P-gp/BCRP inhibitors, consider a starting dose of 0.5 mg three times a day. Monitor for hypotension. (7.2 ) • Antacids: Separate administration by at least 1 hour. 7.1 Pharmacodynamic Interactions with Adempas Other Soluble Guanylate Cyclase Stimulators: Co-administration of Adempas is contraindicated in patients with use of other soluble guanylate cyclase (sGC) stimulators . Nitrates: Co-administration of Adempas with nitr...

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Based on data from animal reproduction studies, Adempas may cause embryo-fetal toxicity and miscarriage when administered to a pregnant woman and is contraindicated during pregnancy . There are limited available data with ADEMPAS use in pregnant women. In animal reproduction studies, oral administration of riociguat to pregnant rats during organogenesis was teratogenic and embryotoxic at exposures approximately 8 times and 2 times, respectively, the human exposure. In reproduction studies with pre...

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