Drug Detail:Macitentan (Macitentan [ ma-si-ten-tan ])
Drug Class: Agents for pulmonary hypertension
Usual Adult Dose for Pulmonary Hypertension
10 mg orally once a day
Uses: For the treatment of pulmonary arterial hypertension (PAH, WHO Group I) to delay disease progression
Renal Dose Adjustments
No adjustment recommended.
Liver Dose Adjustments
No adjustment recommended.
If hepatic dysfunction develops during treatment:
- Discontinue treatment if sustained, unexplained, clinically relevant aminotransferase elevations occur or if elevations are accompanied by an increase in bilirubin greater than 2 times the upper limit of normal, or by clinical symptoms of liver injury.
- Treatment may be reinitiated in patients who have not experienced clinical symptoms of liver injury once hepatic enzyme levels return to within normal range. Specialist advice should be sought.
Precautions
The US FDA requires a Risk Evaluation and Mitigation Strategy (REMS) for macitentan. It includes elements to assure safe use and an implementation system. For additional information: www.accessdata.fda.gov/scripts/cder/rems/index.cfm
US BOXED WARNING:
- EMBRYOFETAL TOXICITY: Do not administer this drug to a pregnant female because it may cause fetal harm. Females of reproductive potential must exclude pregnancy before the start of treatment, monthly during treatment, and 1 month after stopping treatment. Pregnancy must be prevented during treatment and for one month after stopping treatment by using acceptable methods of contraception. For all female patients, this drug is available only through a restricted program called the OPSUMIT(R) REMS.
This drug is not recommended for use in children.
Consult WARNINGS section for additional precautions.
Dialysis
No adjustment recommended.
Other Comments
Administration advice:
- Macitentan may be taken with or without food.
- Tablets should be swallowed whole (not split, crushed, or chewed).
Monitoring:
- Metabolic: Monitor for signs of fluid retention after initiation of therapy.
- Pregnancy: Females of reproductive potential are required to have pregnancy ruled out prior to initiating therapy and to use acceptable forms of birth control and undergo a pregnancy test every month for the duration of therapy and for one month following discontinuation of therapy.
Patient advice:
- Female patients are required to sign an enrolment form.
- Female patients of reproductive potential are required to comply with the pregnancy testing and contraception requirements.
- Counsel men regarding potential effects on fertility.
