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OPSUMIT 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: OPSUMIT® (macitentan) is indicated for: • the long-term treatment of pulmonary arterial hypertension (PAH, WHO Group I) to reduce morbidity in adult patients of WHO Functional Class II or III whose PAH is either idiopathic or heritable, or associated with connective tissue disease or congenital heart disease. • the…
Verbatim from this product's HC label. Tap a section to expand.
1 Clinical Trials by Indication). 2 Geriatrics Geriatrics (≥ 65 years of age): Of the total number of subjects in the clinical study of OPSUMIT® for PAH, 14% were ≥65 years of age. 2 CONTRAINDICATIONS OPSUMIT® (macitentan) is contraindicated in: • patients who are hypersensitive to this drug or to any ingredient in the formulation, including any non-medicinal ingredient, or component of the container.
For a complete listing, see
). Hepatic/Biliary/Pancreatic Elevations of liver aminotransferases (AST, ALT) have been associated with PAH and with endothelin receptor antagonists (ERAs). 6% in the placebo group. 4% in the placebo group. 5 Post-Market Adverse Reactions, Gastrointestinal Disorders).
1 Dosing Considerations, Patients with Hepatic Impairment). Liver enzyme tests should be obtained prior to initiation of OPSUMIT®. Subsequently, monthly testing during the first year of treatment is recommended. They may then be repeated less frequently during treatment as clinically indicated (see 7 WARNINGS AND PRECAUTIONS, Monitoring and Laboratory Tests).
g. jaundice), OPSUMIT® treatment should be discontinued. Re-initiation of OPSUMIT® 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).
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 OPSUMIT® 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).
Pulmonary Veno-Occlusive Disease Cases of pulmonary edema have been reported with vasodilators (mainly prostacyclins) when used in patients with pulmonary veno-occlusive disease. Consequently, if signs of pulmonary edema occur when OPSUMIT® is administered in patients with PAH, the possibility of pulmonary veno-occlusive disease should be considered.
, Hepatic/Biliary/Pancreatic). No dose adjustment is required in patients with mild hepatic impairment. Patients with Renal Impairment Patients with moderate or severe renal impairment may run a higher risk of experiencing hypotension and anemia during treatment with macitentan.
Therefore, monitoring of blood pressure and hemoglobin should be considered. There is no experience with the use of OPSUMIT® in patients undergoing dialysis, and therefore OPSUMIT® is not recommended in this population (see 7 WARNINGS AND PRECAUTIONS, Renal).
2 Recommended Dose and Dosage Adjustment Adults Film-coated tablet The recommended dose of OPSUMIT® in adult patients is one 10 mg film-coated tablet taken once daily. Pediatrics (2 years to less than 18 years old) Dispersible tablets for suspension The recommended dose of OPSUMIT® in pediatric patients aged 2 years to less than 18 years is based on body weight (Table 1).
OPSUMIT® should be taken once daily. 5 mg Pediatrics (<2 years of age): The safety and efficacy of OPSUMIT® in children <2 years of age has not been established; therefore, Health Canada has not authorized an indication in this population Geriatrics (≥65 years of age) No dose adjustment is required in patients ≥65 years of age.
4 Geriatrics). 3 Reconstitution Administration by a tablespoon The prescribed daily dose of dispersible tablet(s) should be added to room temperature drinking water in a tablespoon to form a white cloudy liquid. The liquid can be gently stirred for 1 to 3 minutes using a knife tip to speed up dissolution.
Either administer the medicine to the patient right away or mix it further with a small portion of apple sauce or yogurt to aid with administration. A little more water, apple sauce or yogurt should be added to the tablespoon and administered to the patient to make sure the entire dose of medicine has been taken.
OPSUMIT® (macitentan) is contraindicated in: • patients who are hypersensitive to this drug 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).
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
Other brands of Macitentan in Canada.
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Brand names are compiled from public regulatory records for active-ingredient mapping only. Drugvu is not affiliated with any manufacturer. This is not medical advice.
Renal Patients with renal impairment:
Patients with moderate or severe renal impairment may run a higher risk of experiencing hypotension and anaemia during treatment with macitentan. Therefore, monitoring of blood pressure and hemoglobin should be considered. There is no experience with the use of OPSUMIT® in patients undergoing dialysis, and therefore OPSUMIT® is not recommended in this population.
0 Page 9 of 44 Unclassified / Non classifié Reproductive Health: Female and Male Potential Fertility Based on findings in animals, OPSUMIT® may impair fertility in males of reproductive potential. Decreases in sperm cell count have been observed in patients taking ERAs.
OPSUMIT®, like other ERAs, may have an adverse effect on spermatogenesis in men. It is not known whether the effects on fertility would be reversible. Counsel men about potential effects on fertility. In repeated-dose toxicity studies, pathologic changes in testes (tubular dilatation, tubular degeneration and/or tubular atrophy; and/or hypospermatogenesis) occurred in rats or dogs at >18-fold human exposure (see 16 NON-CLINICAL TOXICOLOGY, Reproductive toxicity).
1 Pregnant Women PAH is a contraindication to pregnancy, due to a high mortality risk to both mother and fetus. There are limited data from the use of OPSUMIT® in pregnant women. The potential risk for humans is still unknown. In animal studies, macitentan was teratogenic in rabbits and rats causing cardiovascular and mandibular arch fusion abnormalities at all dose levels tested.
Women receiving OPSUMIT® must be advised of the risk of harm to the fetus. OPSUMIT® is contraindicated during pregnancy (see 2 CONTRAINDICATIONS). OPSUMIT® treatment should only be initiated in women of child-bearing potential when the absence of pregnancy has been verified, appropriate advice on contraception provided, and reliable contraception is practiced.
Women should not become pregnant for 1 month after discontinuation of OPSUMIT®. Monthly pregnancy tests during treatment with OPSUMIT® are recommended to allow the early detection of pregnancy. 2 Breast-feeding It is not known whether macitentan is excreted into human breast milk.
In rats, macitentan and its metabolites were excreted into milk during lactation. Breast-feeding is contraindicated during treatment with OPSUMIT® (see 2 CONTRAINDICATIONS). 1 Clinical Trials by Indication).
Pediatrics (<2 years of age):
The safety and efficacy of OPSUMIT® in children <2 years of age has not been established; therefore, Health Canada has not authorized an indication in this population. 4 Geriatrics Geriatrics (≥ 65 years of age): Of the total number of subjects in the clinical study of OPSUMIT® for pulmonary arterial hypertension, 14% were ≥65 years of age.
There is limited clinical […]
Alternatively, instead of drinking water, the oral suspension can be prepared in other liquids like orange juice, apple juice or skimmed milk. Administration by a glass The prescribed daily dose of dispersible tablet(s) should be placed in a small glass containing a small volume (from 10 ml up to maximum 100 ml) of room temperature drinking water to form a white cloudy liquid.
The liquid can be gently stirred with a spoon for 1 to 2 minutes. Administer the medicine to the patient right away. A little more water (minimum 5 mL) should be added to the glass and stirred with the same spoon to re-suspend any remaining medicine.
The entire contents of the glass should be administered to the patient to make sure all the medicine has been taken. 4 Administration Film-coated tablets OPSUMIT® is to be taken orally at a dose of 10 mg once daily at about the same time, with or without food.
Tablets are to be swallowed whole. Dispersible tablets OPSUMIT® should be taken orally once a day at about the same time with or without food. OPSUMIT® dispersible tablets must be dispersed in room temperature liquid and are to be taken as an oral suspension only.
The oral suspension must be prepared and administered using either a spoon or a small glass. Care should be taken to ensure the entire dose of medicine has been taken. If not administered right away the medicine should be discarded and a new dose of medicine should be prepared.
Hands must be thoroughly washed and dried before and after preparation of the medicine. 5 Missed Dose If a dose of OPSUMIT® is missed, the tablet(s) should be taken as soon as it is remembered. 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. 0 Page 7 of 44 Unclassified / Non classifié 5 OVERDOSAGE There is currently no experience with overdosage of OPSUMIT®. In a clinical study in healthy adult subjects where macitentan was administered as a single dose up to and including 600 mg, AEs of headache, nausea and vomiting were observed.
In the event of an overdose, standard supportive measures should be taken, as required. Due to high degree of protein binding of macitentan, dialysis is unlikely to be effective. For management of a suspected drug overdose, contact your regional poison control centre.
6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING Table 1: Dosage Forms, Strengths, Composition and Packaging. 0 mg - white to off-white, round, biconvex film-coated tablet, debossed with “10” on both sides. Each film -coated tablet contains 10 mg macitentan OPSUMIT® film-coated tablets are supplied as follows: • 30 count film-coated tablets PVC/PE/PVDC aluminum foil blisters in carton.
5” on one side and with “Mn” on the other side. 5 mg of macitentan OPSUMIT® dispersible tablets for suspension are supplied as follows: • 30 count tablets in aluminum cold form film blisters with integrated desiccant and an aluminum push through lidding foil in cartons 7 WARNINGS AND PRECAUTIONS Hematologic As with other ERAs, treatment with OPSUMIT® has been associated with a decrease in hemoglobin concentration.
OPSUMIT® related decreases in hemoglobin concentration occurred early, were not progressive, stabilised before 12 weeks of treatment and remained stable during chronic treatment. Cases of anemia requiring transfusion have been reported with OPSUMIT® and […]