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OPSYNVI is a brand name for Macitentan, supplied as a tablet. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: OPSYNVI® (macitentan and tadalafil), is indicated for: • the long-term treatment of pulmonary arterial hypertension (PAH, World Health Organization [WHO] Group 1) to reduce morbidity in patients of WHO functional class (FC) II or III whose PAH is idiopathic, heritable or associated with connective tissue disease or…
Verbatim from this product's HC label. Tap a section to expand.
1 Dosing Considerations • Renal impairment The administration of OPSYNVI® to patients with severe renal impairment is not recommended because of increased tadalafil exposure (AUC), lack of clinical experience and the lack of ability to influence clearance by dialysis.
(see 7 WARNINGS AND PRECAUTIONS, Renal). There is no experience with the use of macitentan in patients undergoing dialysis, and therefore OPSYNVI® is not recommended in this population. OPSYNVI® is recommended only for patients with mild or moderate renal impairment who tolerate macitentan 10 mg and tadalafil 40 mg once daily.
Patients with moderate renal impairment may have a higher risk of experiencing hypotension and anemia during treatment with OPSYNVI®. Therefore, monitoring of blood pressure and hemoglobin should be considered. • Hepatic impairment The administration of OPSYNVI® to patients with moderate hepatic impairment is not recommended.
OPSYNVI® must not be initiated in patients with severe hepatic impairment, with or without cirrhosis (Child-Pugh Class C), or clinically significant elevated hepatic aminotransferases greater than 3 times the Upper Limit of Normal (> 3 × ULN).
Liver enzyme tests should be obtained prior to initiation of OPSYNVI®. Subsequently, monthly testing during the first year of treatment is recommended. Testing may then be repeated less frequently during treatment as clinically indicated (see 7 WARNINGS AND PRECAUTIONS, Monitoring and Laboratory Tests).
OPSYNVI® is recommended only for patients with mild hepatic impairment who tolerate stable doses of macitentan 10 mg and tadalafil 40 mg once daily as individual components, following a careful individual benefit/risk evaluation by the prescribing physician (see 7 WARNINGS AND PRECAUTIONS, Hepatic/Biliary/Pancreatic).
2 Recommended Dose and Dosage Adjustment The recommended dose of OPSYNVI® is one tablet taken once daily. • Switch from macitentan and tadalafil as individual components to OPSYNVI® Patients who are currently treated concomitantly with stable doses of macitentan 10 mg and tadalafil 40 mg (20 mg x 2) once daily as individual components may be switched to OPSYNVI®.
0 Page 6 of 61 Unclassified / Non classifié The safety and efficacy of OPSYNVI® have not been established in children and adolescent patients <18 years of age. Health Canada has not authorized an indication for pediatric use. • Geriatrics (≥65 years of age) No dose adjustment is required in patients 65 years and older.
). Gastrointestinal OPSYNVI® contains lactose monohydrate. 0 Page 9 of 61 Unclassified / Non classifié intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicinal product. Hematologic Initiation of OPSYNVI® is not recommended in patients with severe anemia.
It is recommended that hemoglobin concentrations are measured prior to initiation of treatment, again after one month, and periodically thereafter as clinically indicated (see 7 WARNINGS AND PRECAUTIONS, Monitoring and Laboratory Tests and 8 ADVERSE REACTIONS).
Macitentan As with other endothelin receptor antagonists (ERAs), treatment with macitentan has been associated with a decrease in hemoglobin concentration. Macitentan related decreases in hemoglobin concentration occurred early, were not progressive, stabilized before 12 weeks of treatment and remained stable during chronic treatment.
Cases of anemia requiring transfusion have been reported with macitentan and other ERAs. Hepatic/Biliary/Pancreatic OPSYNVI® must not be initiated in patients with severe hepatic impairment, with or without cirrhosis (Child-Pugh Class C), or clinically significant elevated hepatic aminotransferases greater than 3 times the Upper Limit of Normal (> 3 × ULN).
1 Dosing Considerations, Hepatic Impairment). The A DUE Phase 3 clinical study for OPSYNVI® excluded patients with known severe hepatic impairment (defined as a Model for End Stage Liver Disease score ≥19). Liver enzyme tests should be obtained prior to initiation of OPSYNVI®.
Subsequently, monthly testing during the first year of treatment is recommended. Testing may then be repeated less frequently during treatment as clinically indicated (see 7 WARNINGS AND PRECAUTIONS, Monitoring and Laboratory Tests).
g. jaundice), OPSYNVI® should be discontinued. Re-initiation of OPSYNVI® may be considered following the return of hepatic enzyme levels to within the normal range in patients who have not experienced clinical symptoms of liver injury (see 8 ADVERSE REACTIONS).
). • Patients treated with guanylate cyclase stimulators, such as riociguat because coadministration of drugs containing phosphodiesterase type 5 (PDE5) inhibitors, including OPSYNVI®, with guanylate cyclase stimulators could lead to potentially life-threatening episodes of symptomatic hypotension or syncope.
1 Dosing Considerations • Renal impairment The administration of OPSYNVI® to patients with severe renal impairment is not recommended because of increased tadalafil exposure (AUC), lack of clinical experience and the lack of ability to influence clearance by dialysis.
(see 7 WARNINGS AND PRECAUTIONS, Renal). There is no experience with the use of macitentan in patients undergoing dialysis, and therefore OPSYNVI® is not recommended in this population. OPSYNVI® is recommended only for patients with mild or moderate renal impairment who tolerate macitentan 10 mg and tadalafil 40 mg once daily.
Patients with moderate renal impairment may have a higher risk of experiencing hypotension and anemia during treatment with OPSYNVI®. Therefore, monitoring of blood pressure and hemoglobin should be considered. • Hepatic impairment The administration of OPSYNVI® to patients with moderate hepatic impairment is not recommended.
OPSYNVI® must not be initiated in patients with severe hepatic impairment, with or without cirrhosis (Child-Pugh Class C), or clinically significant elevated hepatic aminotransferases greater than 3 times the Upper Limit of Normal (> 3 × ULN).
Liver enzyme tests should be obtained prior to initiation of OPSYNVI®. Subsequently, monthly testing during the first year of treatment is recommended. Testing may then be repeated less frequently during treatment as clinically indicated (see 7 WARNINGS AND PRECAUTIONS, Monitoring and Laboratory Tests).
OPSYNVI® is recommended only for patients with mild hepatic impairment who tolerate stable doses of macitentan 10 mg and tadalafil 40 mg once daily as individual components, following a careful individual benefit/risk evaluation by the prescribing physician (see 7 WARNINGS AND PRECAUTIONS, Hepatic/Biliary/Pancreatic).
OPSYNVI® is contraindicated in: • Patients who are hypersensitive to macitentan and/or tadalafil or to any ingredient in the formulation, including any non-medicinal ingredient, or component of the container. For a complete listing, see 6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING.
1 Pregnant Women). 2 Breast-feeding). g. 4 Drug-Drug Interactions, Nitrates). • Patients with previous episode of non-arteritic anterior ischaemic optic neuropathy (NAION) (see 7 WARNINGS AND PRECAUTIONS). • Patients treated with guanylate cyclase stimulators, such as riociguat because coadministration of drugs containing phosphodiesterase type 5 (PDE5) inhibitors, including OPSYNVI®, with guanylate cyclase stimulators could lead to potentially life-threatening episodes of symptomatic hypotension or syncope.
0 Page 5 of 61 Unclassified / Non classifié
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
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There is limited clinical experience in patients >75 years of age with macitentan or tadalafil, and therefore OPSYNVI® should be used with caution in this population. 4 Administration • OPSYNVI® should be taken orally once daily with or without food.
Tablets are to be swallowed whole. 5 Missed Dose If a dose of OPSYNVI® is missed, the tablet should be taken as soon as the patient remembers. Otherwise, advise the patient to skip the dose and take the next dose at the regular time.
The patient should be advised not to take 2 doses on the same day to make up for a missed dose.
Macitentan Elevations of liver aminotransferases (AST, ALT) have been associated with PAH and with ERAs. 6% in the placebo group. 0 Page 10 of 61 Unclassified / Non classifié the placebo group. 5 Post-Market Adverse Reactions, Gastrointestinal Disorders).
Monitoring and Laboratory Tests Hematologic:
It is recommended that hemoglobin concentrations are measured prior to initiation of treatment, again after one month, and periodically thereafter as clinically indicated (see 7 WARNINGS AND PRECAUTIONS, Hematologic and 8 ADVERSE REACTIONS).
Hepatic/Biliary/Pancreatic:
Liver enzyme tests should be obtained prior to initiation of OPSYNVI® and subsequently at monthly intervals during the first year of treatment. They may then be repeated less frequently during treatment as clinically indicated (see 7 WARNINGS AND PRECAUTIONS, Hepatic/Biliary/Pancreatic).
Ophthalmologic Tadalafil Physicians should advise patients to seek immediate medical attention in the event of a sudden loss of vision in one or both eyes. Such an event may be a sign of non-arteritic anterior ischemic optic neuropathy (NAION), a cause of decreased vision, including permanent loss of vision that has been reported rarely post-marketing in temporal association with the use of all PDE5 inhibitors.
An increased risk of acute NAION has been suggested from analyses of observational data in men with ED within 1 to 4 days of episodic PDE5 inhibitor use. Physicians should also discuss with patients the increased risk of NAION in individuals who have already experienced NAION in one eye, including whether such individuals could be adversely affected by use of vasodilators such as PDE5 inhibitors (see 8 ADVERSE REACTIONS).
g. crowded disc) prior to development of the condition. If physicians are concerned about the overall risk of NAION, they should consider discussing these concerns with an ophthalmologist. Patients with known hereditary degenerative retinal disorders, including retinitis pigmentosa, were not included in the clinical trials, and use in these patients is not recommended.
Renal The administration of OPSYNVI® to patients with severe renal impairment is not recommended, due to increased tadalafil exposure (AUC), limited clinical experience, and the lack of ability to influence tadalafil clearance by dialysis in patients with severe renal insufficiency.
There is no experience with the use of macitentan in patients undergoing dialysis, and therefore OPSYNVI® is not recommended in this population. Patients with moderate or severe renal impairment may run a higher risk of experiencing hypotension and anemia during treatment with macitentan.
0 Page 11 of 61 Unclassified / Non classifié pressure and hemoglobin should be considered in patients with moderate renal impairment. 1 Dosing Considerations, Renal […]
2 Recommended Dose and Dosage Adjustment The recommended dose of OPSYNVI® is one tablet taken once daily. • Switch from macitentan and tadalafil as individual components to OPSYNVI® Patients who are currently treated concomitantly with stable doses of macitentan 10 mg and tadalafil 40 mg (20 mg x 2) once daily as individual components may be switched to OPSYNVI®.
0 Page 6 of 61 Unclassified / Non classifié The safety and efficacy of OPSYNVI® have not been established in children and adolescent patients <18 years of age. Health Canada has not authorized an indication for pediatric use. • Geriatrics (≥65 years of age) No dose adjustment is required in patients 65 years and older.
There is limited clinical experience in patients >75 years of age with macitentan or tadalafil, and therefore OPSYNVI® should be used with caution in this population. 4 Administration • OPSYNVI® should be taken orally once daily with or without food.
Tablets are to be swallowed whole. 5 Missed Dose If a dose of OPSYNVI® is missed, the tablet should be taken as soon as the patient remembers. Otherwise, advise the patient to skip the dose and take the next dose at the regular time.
The patient should be advised not to take 2 doses on the same day to make up for a missed dose. 5 OVERDOSAGE There is no human experience of acute overdose with OPSYNVI®. As OPSYNVI® contains macitentan and tadalafil, the risk of overdose associated with each component should be considered.
Treatment In the event of an overdose with OPSYNVI®, standard supportive measures must be taken as required. Based on the individual component data, dialysis is unlikely to be effective. Macitentan Macitentan has been administered as a single dose of up to and including 600 mg to healthy subjects.
Adverse events of headache, nausea and vomiting were observed. Tadalafil Single doses of up to 500 mg of tadalafil have been given to healthy subjects, and multiple daily doses up to 100 mg/day for 21 days have been given to patients with erectile dysfunction (ED).
Adverse reactions were similar to those seen at lower doses. Doses greater than 40 mg have not been studied in patients with pulmonary arterial hypertension. For management of a suspected drug overdose, contact your regional poison control centre.
0 Page 7 of 61 Unclassified / Non classifié Description OPSYNVI® is available as oblong, white to almost-white, film-coated tablets debossed “MT” on one side and “1040” on the other side. Each film-coated tablet contains 10 mg macitentan and 40 mg tadalafil.
OPSYNVI® tablets are supplied as follows: 30 count film-coated tablets in high-density polyethylene bottles 7 WARNINGS AND PRECAUTIONS General As OPSYNVI® contains macitentan and tadalafil, the Warnings and Precautions associated with each component should be considered.
Cardiovascular In the double-blind portion of the A DUE study, cardiac failure events were reported within one month of treatment initiation with OPSYNVI® in 4 out of 20 patients aged 65 years or older. All four patients had not been previously treated with PAH-specific medications.
Two cases out of four resolved while on treatment, whereas treatment in the other two was discontinued due to other adverse events [a newly established diagnosis of Pulmonary Veno-Occlusive Disease (exclusionary as per study protocol) and anaemia].
Pulmonary Veno-Occlusive Disease Since there are no clinical data on administration of tadalafil to patients with veno-occlusive disease, administration of OPSYNVI® to such patients in not recommended. Cases of pulmonary […]