Consumer medicine information

Opsumit 10 mg Tablets

Macitentan

BRAND INFORMATION

Brand name

Opsumit

Active ingredient

Macitentan

Schedule

S4

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Opsumit 10 mg Tablets.

1. Why am I using OPSUMIT?


OPSUMIT contains the active ingredient macitentan. OPSUMIT is used to treat pulmonary arterial hypertension (PAH). It can be used on its own or with other drugs to treat PAH.
For more information, see Section 1. Why am I using OPSUMIT? in the full CMI.

2. What should I know before I use OPSUMIT?


Do not use if you have ever had an allergic reaction to macitentan, soya or any of the ingredients listed at the end of the CMI.
Talk to your doctor if you have any other medical conditions, take any other medicines, or are pregnant or plan to become pregnant or are breastfeeding. Women of childbearing potential must use reliable birth control (contraception) during and for at least 3 months after you stop taking it.
For more information, see Section 2. What should I know before I use OPSUMIT? in the full CMI.

3. What if I am taking other medicines?


Some medicines may interfere with OPSUMIT and affect how it works.
A list of these medicines is in Section 3. What if I am taking other medicines? in the full CMI.

4. How do I use OPSUMIT?


The recommended dose of OPSUMIT for adults and children over 12 years and weighing more than 40 kg is one 10 mg tablet once a day with or without food.
More instructions can be found in Section 4. How do I use OPSUMIT? in the full CMI.

5. What should I know while using OPSUMIT?

Things you should do
  • Remind any doctor, dentist or pharmacist you visit that you are using OPSUMIT.
  • You must use at least two reliable forms of birth control (contraception) while taking OPSUMIT and for 3 months after you stop taking it.
  • Tell your doctor immediately if you notice any of the following: become pregnant or trying to become pregnant, have signs of pulmonary oedema, such as a sudden, important increase in breathlessness and low oxygen.
Things you should not do
  • Do not stop taking this medicine unless your doctor tells you to.
  • Do not breast feed while you are taking OPSUMIT.
Driving or using machines
  • Be careful before you drive or use any machines or tools until you know how OPSUMIT affects you.
Looking after your medicine
  • Keep tablets in the original pack, in a cool, dry place where the temperature stays below 30°C.
  • Keep out of reach of children.

For more information, see Section 5. What should I know while using OPSUMIT? in the full CMI.

6. Are there any side effects?


The common but less serious side effects you may experience include low number of red blood cells (anaemia), swelling caused by fluid buildup in the body, infection of nose or throat. The serious side effects that require medical attention include severe allergic reaction.
For more information, including what to do if you have any side effects, see Section 6. Are there any side effects? in the full CMI.

BRAND INFORMATION

Brand name

Opsumit

Active ingredient

Macitentan

Schedule

S4

 

Boxed Warnings

Opsumit may cause birth defects and is contraindicated in pregnancy. See Section 4.3 Contraindications; Section 4.6 Fertility, Pregnancy and Lactation.

1 Name of Medicine

Opsumit macitentan.

2 Qualitative and Quantitative Composition

Opsumit is available as a 10 mg film-coated tablet for once daily oral administration.
Excipients with known effects. Lactose monohydrate and soya lecithin. For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Film-coated tablet.
White to off-white, round, biconvex film-coated tablet, debossed with "10" on both sides.

4 Clinical Particulars

4.9 Overdose

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. In the event of an overdose, standard supportive measures must be taken, as required. Due to the high degree of protein binding of macitentan, dialysis is unlikely to be effective.
For information on the management of overdose, contact the Poisons Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.3 Preclinical Safety Data

Genotoxicity. Macitentan was not genotoxic in a standard battery of in vitro and in vivo assays.
Carcinogenicity. Studies of 2 years duration did not reveal a carcinogenic potential at exposures 18-fold and 116-fold the human exposure in rats and mice, respectively.

6 Pharmaceutical Particulars

6.7 Physicochemical Properties

Active: macitentan.
Opsumit is the brand name for macitentan and is a dual ETA and ETB endothelin receptor antagonist. The chemical name of macitentan is N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide.
The molecular formula: C19H20Br2N6O4S.
Relative molecular mass: 588.3 g/mol, the molecule is achiral.
Chemical structure.
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSMACITE.gif CAS number. 441798-33-0.
Macitentan is a white to off white crystalline powder that is insoluble in water and slightly soluble in ethanol (approx 2 mg/mL). In the solid state macitentan is very stable, is not hygroscopic, and is not light sensitive. The melting temperature of macitentan is 135°C, Partition coefficient (1-octanol/ aqueous phosphate buffer, pH 7.4): log D = 2.9 and ionization constant pKa is 6.2.

7 Medicine Schedule (Poisons Standard)

Schedule 4 - Prescription Only Medicine.

Summary Table of Changes

https://stagingapi.mims.com/au/public/v2/images/fulltablegif/OPSUMIST.gif