Riociguat
Generic Name: riociguat
Brand Names:
Adempas
11 DESCRIPTION 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.
Overview
11 DESCRIPTION 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.
Uses
1 INDICATIONS AND USAGE 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. ( 1.1 ) • Pulmonary Arterial Hypertension (PAH) (WHO Group 1) to improve exercise capacity, improve WHO functional class and to delay clinical worsening.
Dosage
2 DOSAGE AND ADMINISTRATION • Initiate treatment at 1 mg taken three times a day. ( 2.1 ) • For patients who may not tolerate the hypotensive effect of Adempas, consider a starting dose of 0.5 mg, three times a day. ( 2.1 ) • 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. ( 2.1 ) • Tablets may be crushed and mixed with water or soft foods for patients who have difficulty swallowing. ( 2.1 ) 2.1 Recommended Dosage in Adult Patients The recommended starting dosage is 1 mg taken 3 times a day. For patients who may not tolerate the hypotensive effect of Adempas, consider a starting dose of 0.5 mg taken three times a day.
Side Effects
6 ADVERSE REACTIONS The following serious adverse reactions are discussed elsewhere in the labeling: • Embryo-Fetal Toxicity [see Warnings and Precautions ( 5.1 )] • Hypotension [see Warnings and Precautions ( 5.2 )] • Bleeding [see Warnings and Precautions ( 5.3 )] Adverse reactions occurring more frequently (≥3%) on Adempas compared to placebo are headache, dyspepsia/gastritis, dizziness, nausea, diarrhea, hypotension, vomiting, anemia, gastroesophageal reflux, and constipation. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Bayer HealthCare Pharmaceuticals Inc. at 1-888-842-2937 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
Interactions
7 DRUG INTERACTIONS • 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. ( 7.2 ) 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 [see Contraindications ( 4.4 )]. Nitrates: Co-administration of Adempas with nitrates or nitric oxide donors (such as amyl nitrite) in any form is contraindicated because of hypotension [see Contraindications ( 4.2 ) and Clinical Pharmacology ( 12.2 )] .
Warnings
WARNING: EMBRYO-FETAL TOXICITY Adempas is contraindicated for use during pregnancy because it may cause fetal harm based on animal data [see Contraindications (4.1) , Warnings and Precautions (5.1) , and Use in Specific Populations (8.1) ]. Females of reproductive potential: Confirm negative pregnancy status before the start of treatment. 5 WARNINGS AND PRECAUTIONS • Symptomatic hypotension ( 5.2 ) • Bleeding ( 5.3 ) • Pulmonary edema in patients with pulmonary veno-occlusive disease. If confirmed, discontinue treatment ( 5.4 ) 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. The available human data for sGCs do not establish the presence or absence of major birth defects related to the use of Adempas. Advise females of reproductive potential of the potential risk to a fetus. Confirm negative pregnancy status before the start of treatment. 4 CONTRAINDICATIONS • Pregnancy ( 4.1 ) • Use with nitrates or nitric oxide donors in any form ( 4.2 , 7.1 ) • Use with PDE inhibitors ( 2.6 , 4.3 , 7.1 ) • Patients with concomitant use of other soluble guanylate cyclase (sGC) stimulators.
Pregnancy
8.1 Pregnancy Risk Summary 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 [see Contraindications (4.1)] . Available data from postmarketing reports have not identified an increased risk of major birth defects; however, these data are limited. Methodological limitations of these postmarketing reports include lack of a control group; limited information regarding dose, duration, and timing of drug exposure; and missing data.
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING 16.1 How Supplied Adempas (riociguat) tablets are film-coated, round, and debossed with the "Bayer cross" on one side. Color Debossing Side 2 NDC 50419-xxx-xx Bottle of 9 Bottle of 90 Blister of 42 0.5 mg White 0.5 R 250-91 250-01 250-03 1 mg Pale yellow 1 R 251-91 251-01 251-03 1.5 mg Yellow-orange 1.5 R 252-91 252-01 252-03 2 mg Pale orange 2 R 253-91 253-01...
Frequently Asked Questions
What is Riociguat used for?▼
1 INDICATIONS AND USAGE 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. ( 1.1 ) • Pulmonary Arterial Hypertension (PAH) (WHO Group 1) to improve exercise capacity, improve WHO functional class and to delay clinical worsening.
What are the side effects of Riociguat?▼
6 ADVERSE REACTIONS The following serious adverse reactions are discussed elsewhere in the labeling: • Embryo-Fetal Toxicity [see Warnings and Precautions ( 5.1 )] • Hypotension [see Warnings and Precautions ( 5.2 )] • Bleeding [see Warnings and Precautions ( 5.3 )] Adverse reactions occurring more frequently (≥3%) on Adempas compared to placebo are headache, dyspepsia/gastritis, dizziness, nausea, diarrhea, hypotension, vomiting, anemia, gastroesophageal reflux, and constipation. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Bayer HealthCare Pharmaceuticals Inc. at 1-888-842-2937 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
Can I take Riociguat during pregnancy?▼
8.1 Pregnancy Risk Summary 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 [see Contraindications (4.1)] . Available data from postmarketing reports have not identified an increased risk of major birth defects; however, these data are limited. Methodological limitations of these postmarketing reports include lack of a control group; limited information regarding dose, duration, and timing of drug exposure; and missing data.
What are the important warnings for Riociguat?▼
WARNING: EMBRYO-FETAL TOXICITY Adempas is contraindicated for use during pregnancy because it may cause fetal harm based on animal data [see Contraindications (4.1) , Warnings and Precautions (5.1) , and Use in Specific Populations (8.1) ]. Females of reproductive potential: Confirm negative pregnancy status before the start of treatment. 5 WARNINGS AND PRECAUTIONS • Symptomatic hypotension ( 5.2 ) • Bleeding ( 5.3 ) • Pulmonary edema in patients with pulmonary veno-occlusive disease. If confirmed, discontinue treatment ( 5.4 ) 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. The available human data for sGCs do not establish the presence or absence of major birth defects related to the use of Adempas. Advise females of reproductive potential of the potential risk to a fetus. Confirm negative pregnancy status before the start of treatment. 4 CONTRAINDICATIONS • Pregnancy ( 4.1 ) • Use with nitrates or nitric oxide donors in any form ( 4.2 , 7.1 ) • Use with PDE inhibitors ( 2.6 , 4.3 , 7.1 ) • Patients with concomitant use of other soluble guanylate cyclase (sGC) stimulators.
Related Medications
Propylhexedrine
propylhexedrine
Uses Temporarily relieves nasal congestion due to a cold, hay fever, or other upper respiratory allergies (allergic rhinitis).
Geotrichum Candidum
geotrichum candidum
Dosage form: SOLUTION. Route: INTRADERMAL, PERCUTANEOUS, SUBCUTANEOUS. Active ingredients: GEOTRICHUM CANDIDUM (.001 g/mL). Category: BLA.
Cerato
cerato
INDICATIONS: For temporary relief of doubting of own judgement, and having the need to seek the confirmation of others.
Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.