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ADEMPAS is a brand name for Riociguat, supplied as a tablet. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: Pulmonary Hypertension ADEMPAS (riociguat) is indicated for the treatment of: inoperable chronic thromboembolic pulmonary hypertension (CTEPH, WHO Group 4) persistent or recurrent CTEPH after surgical treatment pulmonary arterial hypertension (PAH, WHO Group 1), as monotherapy or in combination with endothelin…
Verbatim from this product's HC label. Tap a section to expand.
1 Dosing Considerations Treatment should only be initiated and monitored under the supervision of a clinician experienced in the diagnosis and treatment of CTEPH or PAH. 2 Recommended Dose and Dosage Adjustment Treatment Initiation The recommended starting dose of ADEMPAS is 1 mg 3 times daily for 2 weeks.
Tablets should be taken 3 times daily approximately 6 to 8 hours apart, with or without food. 5 mg 3 times daily may be used at the discretion of the physician to minimize the potential of hypotensive events. 5 mg 3 times daily, if systolic blood pressure is ≥95 mmHg and the patient has no signs or symptoms of hypotension.
If systolic blood pressure falls below 95 mmHg, dosage should be maintained provided the patient does not show any signs or symptoms of hypotension. 5 mg three times daily, 24 hours later, as clinically warranted. Maintenance Dose The established individual dose should be maintained unless signs and symptoms of hypotension occur.
5 mg. If not tolerated, dose reduction might be considered at any time. Treatment Discontinuation In case treatment has to be interrupted for 3 days or more, restart treatment at the starting dose 3 times daily for 2 weeks, and continue dose titration regimen as described above.
Transitioning between PDE5 inhibitors and Riociguat Discontinue sildenafil at least 24 hours or tadalafil at least 48 hours prior to administering riociguat. 2 Recommended Dose and Dosage Adjustment – Treatment Initiation). Discontinue ADEMPAS at least 24 hours prior to administering a PDE5 inhibitor.
4 Drug-Drug Interactions). A 24-week, uncontrolled study investigated the transition from PDE5 inhibitors, sildenafil or tadalafil, to ADEMPAS, in 61 adult PAH patients stable on PDE5 inhibitors. All patients were WHO Functional Class III and 82% received background therapy with an endothelin receptor antagonist (ERA).
All patients in the study were transitioned from sildenafil (up to 80 mg tid) or tadalafil (up to 40 mg od) to 1 mg three times daily ADEMPAS (median treatment-free washout period of 1 day for sildenafil and 3 days for tadalafil). Overall, the safety profile observed in the study was comparable with that observed in the pivotal trials, with no serious adverse events reported during the transition period.
Six patients (10%) experienced at least one clinical worsening event, including 2 deaths unrelated to study drug. ADEMPAS (Riociguat Tablets) Page 6 of 46 Geriatrics (≥65 years of age) Elderly (≥65 years) patients exhibited higher plasma concentrations than younger patients.
). No specific antidote exists. In case of overdose, standard supportive measures should be adopted as required. In case of pronounced hypotension, active cardiovascular support may be required. Based on the high plasma protein binding riociguat is not expected to be dialyzable.
5” and an “R” on the other side. 1 mg pale yellow tablets marked with “1” and an “R” on the other side. 5” and an “R” on the other side. 2 mg pale orange tablets marked with “2” and an “R” on the other side. 5” and an “R” on the other side.
5 mg tablets are supplied in HDPE bottles of 42 and 90 and ADEMPAS (Riociguat Tablets) Page 8 of 46 in blisters of 42. 4 Drug-Drug Interactions), and may result in hypotension. Assess the benefit-risk for each patient individually before prescribing ADEMPAS in patients on stable doses of strong multi pathway CYP and P-gp/BCRP inhibitors.
5 mg ADEMPAS, three times a day to mitigate the risk of hypotension. 4 Drug-Drug Interactions). In patients on stable doses of ADEMPAS, the initiation of strong multi pathway CYP and P-gp/BCRP inhibitors is not recommended as no dosage recommendation can be given due to limited data.
Alternative treatments should be considered. 4 Drug-Drug Interactions). These drugs should be used with caution when co-administered with ADEMPAS. Blood pressure should be monitored and dose reduction of ADEMPAS might be considered. Drugs Affecting the NO-sGC-cGMP Pathway ADEMPAS and other drugs that result in increased levels of intracellular cGMP act as vasodilators.
Additive or synergistic effects on systemic blood pressure should be anticipated. Concomitant use of PDE5-inhibitors, nitrates or nitric oxide donors is contraindicated (see 2 CONTRAINDICATIONS). 3 Pharmacokinetics – Metabolism). Therefore patients are advised to stop smoking.
2 Recommended Dose and Dosage Adjustment). Bleeding In patients with pulmonary hypertension there is an increased likelihood of bleeding, particularly among patients receiving anticoagulation therapy. Bleeding risk should be carefully evaluated before initiating ADEMPAS therapy, and should be monitored periodically, particularly in patients taking anticoagulants.
2 Drug Interactions Overview). 5 Missed Dose If a dose is missed, the next dose should be taken as scheduled. The dose should not be doubled to make up for the missed dose. 5 OVERDOSAGE For management of suspected drug overdose, contact your regional Poison Control Centre.
Inadvertent overdosing with total daily doses of 9 to 25 mg ADEMPAS between 2 to 32 days was reported. Adverse reactions were similar to those seen at lower doses (see
10/2022 TABLE OF CONTENTS Sections or subsections that are not applicable at the time of authorization are not listed. RECENT MAJOR LABEL CHANGES .............................................................................................
2 TABLE OF CONTENTS ............................................................................................................. 2 PART I: HEALTH PROFESSIONAL INFORMATION ........................................................................
4 1 INDICATIONS...................................................................................................................... 1 Pediatrics ........................................................................................................................
2 Geriatrics......................................................................................................................... 4 2 CONTRAINDICATIONS .........................................................................................................
4 4 DOSAGE AND ADMINISTRATION........................................................................................... 1 Dosing Considerations .......................................................................................................
2 Recommended Dose and Dosage Adjustment ....................................................................... 5 Missed Dose ....................................................................................................................
7 5 OVERDOSAGE..................................................................................................................... 7 6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING...............................................
7 7 WARNINGS AND PRECAUTIONS............................................................................................ 1 Special Populations ...........................................................................................................
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
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3 Pharmacokinetics – Special Populations and Conditions: Geriatrics). Pediatrics Safety and effectiveness in pediatric patients have not been established. Therefore, Health Canada has not authorized an indication for pediatric use. 3 Pharmacokinetics, Special Populations and Conditions: Hepatic Insufficiency).
1 Special Populations). 3 Pharmacokinetics, Special Populations and Conditions: Renal Insufficiency). 1 Special Populations). Smoking Status Current smokers should be advised to stop smoking. Plasma concentrations of riociguat in smokers are reduced compared to non-smokers.
3 Pharmacokinetics – Metabolism). 2 Drug Interactions Overview). g. g. 2 Drug Interactions Overview). 5 mg, three times when initiating ADEMPAS in patients on stable doses of strong multipathway CYP and P-gp/BCRP inhibitors to mitigate risk of hypotension.
Monitor for signs and symptoms of hypotension on initiation and on treatment with strong multipathway CYP and P-gp/BCRP inhibitors. 2 Drug Interactions Overview). 5 Missed Dose If a dose is missed, the next dose should be taken as scheduled.
The dose should not be doubled to make up for the missed dose.
The risk of serious and fatal bleeding, including respiratory tract bleeding, may be further increased under treatment with ADEMPAS, especially in the presence of risk factors, such as recent episodes of serious hemoptysis including those managed by bronchial arterial embolization.
ADEMPAS should be avoided in patients with a history of serious hemoptysis or who have previously undergone bronchial arterial embolization. 4% of patients taking ADEMPAS compared to 0% of placebo patients. Serious hemoptysis occurred in 5 (1%) patients taking ADEMPAS compared to 0 placebo patients, including one event with fatal outcome.
Serious hemorrhagic events also included 2 patients with vaginal hemorrhage, 2 with catheter site hemorrhage, and 1 each with subdural hematoma, hematemesis, and intra-abdominal hemorrhage. In long-term extension studies, there was no evidence for temporal clustering of bleeding events throughout the period of treatment with ADEMPAS.
Patients should be instructed to notify the treating physician of any unexpected or excessive bleedings. Cardiovascular Hypotension As a sGC stimulator, ADEMPAS acts as a vasodilator, lowering both pulmonary and systemic blood pressure.
The demonstrated risk of hypotension should be carefully considered (see 8 ADVERSE REACTIONS), in particular in patients with concomitant or underlying conditions such as low systemic […]
1 Pregnant Women ...................................................................................................... 2 Breast-feeding ........................................................................................................
3 Pediatrics ............................................................................................................... 4 Geriatrics ...............................................................................................................
10 8 ADVERSE REACTIONS ........................................................................................................ 1 Adverse Reaction Overview..............................................................................................
2 Clinical Trial Adverse Reactions ......................................................................................... 3 Less Common Clinical Trial Adverse Reactions.....................................................................
4 Abnormal Laboratory Findings: Hematologic, Clinical Chemistry and Other Quantitative Data ... 13 9 DRUG INTERACTIONS ........................................................................................................ 1 Serious Drug Interactions.................................................................................................
2 Drug Interactions Overview.............................................................................................. 4 Drug-Drug Interactions ....................................................................................................
5 Drug-Food Interactions.................................................................................................... 6 Drug-Herb Interactions ....................................................................................................
7 Drug-Laboratory Test Interactions ..................................................................................... 20 10 CLINICAL PHARMACOLOGY ..............................................................................................
1 Mechanism of Action..................................................................................................... 2 Pharmacodynamics .......................................................................................................
3 Pharmacokinetics.......................................................................................................... 20 11 STORAGE, STABILITY AND DISPOSAL .................................................................................
22 12 SPECIAL HANDLING INSTRUCTIONS ................................................................................... 22 PART II: SCIENTIFIC INFORMATION ........................................................................................
23 13 PHARMACEUTICAL INFORMATION .................................................................................... 23 14 CLINICAL TRIALS..............................................................................................................
1 Clinical Trials by Indication ............................................................................................. 23 15 MICROBIOLOGY ..............................................................................................................
35 16 NON-CLINICAL TOXICOLOGY............................................................................................. 36 PATIENT MEDICATION INFORMATION ...................................................................................
40 ADEMPAS (Riociguat Tablets) Page 4 of 46 PART I: HEALTH PROFESSIONAL INFORMATION 1 INDICATIONS Pulmonary Hypertension ADEMPAS (riociguat) is indicated for the treatment of: inoperable chronic thromboembolic pulmonary hypertension (CTEPH, WHO Group 4) persistent or recurrent […]