macitentan

(redirected from Opsumit)

macitentan

(ma-si-ten-tan ) ,

Opsumit

(trade name)

Classification

Therapeutic: temporary class
Pharmacologic: endothelin receptor antagonists
Pregnancy Category: X

Indications

Treatment of Pulmonary Hypertension (PAH, WHO Group I) to delay disease progression.

Action

Acts as an endothelin receptor antagonist. Endothelin mediates vasocontriction, fibrosis, proliferation, hypertrophy and inflammation. Antagonizing endothelin effects delays vascular hypertrophy and organ damage.

Therapeutic effects

Delayed sequelae of progression of PAH (death, need for initiation of parenteral prostanoids, increased frequency of hospitalization, diminished exercise tolerance or need for other interventions)

Pharmacokinetics

Absorption: Absorption follows oral administration, bioavailability Unknown.
Distribution: Unknown.
Protein Binding: Macitentan—>99%; active metabolite—>99%
Metabolism and Excretion: Extensively metabolized, primarily by the CYP3A4 enzyme system with conversion to a pharmacologically active metabolite that contributes 40% of activity. 50% excreted in urine as metabolites, 24% in feces.
Half-life: Macitentan—16 hr; active metabolite—48 hr

Time/action profile (improvement in primary endpoints†)

ROUTEONSETPEAKDURATION
POwithin 6 mos12–18 mosunknown
†worsening of PAH, death, or need for other interventions

Contraindications/Precautions

Contraindicated in: Strong inhibitors or inducers of the CYP3A4 enzyme system (can significantly alter drug effectiveness/risk of toxicity) Obstetric: Causes fetal harm, should not be used during pregnancy; Lactation: Discontinue drug or breast feeding
Use Cautiously in: Females with reproductive potential (pregnancy must be excluded prior to treatment and for one mo following treatment, effective contraception must be utilized)Pulmonary veno-occlusive disease (↑ risk of pulmonary edema) Pediatric: Safe and effective use in children has not been established.

Adverse Reactions/Side Effects

Central nervous system

  • headache (most frequent)

Respiratory

  • pulmonary edema

Gastrointestinal

  • hepatotoxicity

Genitourinary

  • ↓ sperm count

Hematologic

  • anemia (most frequent)

Interactions

Drug-Drug interaction

Strong CYP3A4 inducers including rifampin ↓ blood levels and effectiveness and should be avoided Strong CYP3A4 inhibitors including ketoconazole ↑ blood levels and risk of toxicity and should be avoided

Route/Dosage

Oral (Adults) 10 mg once daily

Availability

Tablets: 10 mg

Nursing implications

Nursing assessment

  • Monitor hemodynamic parameters and exercise tolerance prior to and periodically during therapy.
  • Assess for signs and symptoms of pulmonary edema (shortness of breath). If confirmed, discontinue therapy.
  • Lab Test Considerations: Obtain a negative pregnancy test prior to beginning, monthly during therapy, and 1 mo following treatment.
    • Monitor hepatic function periodically during therapy. May cause ↑ AST, ALT, and bilirubin. If clinically relevant ↑ of AST or ALT occur, or if ↑ are accompanied by ↑ bilirubin >2 x upper limit of normal, or by clinical symptoms of hepatotoxicity, discontinue therapy. May re­ initiate therapy when hepatic enzyme levels normalize in patients who have not experienced clinical symptoms of hepatotoxicity.
    • Monitor CBC before starting and periodically during therapy. May cause ↓ hemoglobin. Avoid therapy in patients with severe anemia.

Potential Nursing Diagnoses

Activity intolerance (Indications)

Implementation

  • Only available through a restricted program, Opsumit Risk Evaluation and Mitigation Strategy (REMS). Prescribers and pharmacies must be enrolled and certified. All female patients must enroll and comply with pregnancy testing and contraception requirements. Male patients do not need to enroll.
  • Oral: Administer once daily at the same time each day. Swallow tablets whole, do not break, crush, or chew.

Patient/Family Teaching

  • Instruct patient to take macitentan as directed. Take missed doses as soon as remembered unless almost time for next dose; do not double doses.
  • Advise patients to notify health care professional if symptoms of hepatic injury (nausea, vomiting, right upper quadrant pain, fatigue, anorexia, jaundice, dark urine, fever, itching) occur.
  • Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
  • Caution female patients that macitentan may harm fetus. Instruct females to use effective contraception (intrauterine device IUD, contraceptive implants, tubal sterilization) or a combination of methods (hormone method with a barrier method or two barrier methods) during and for at least a mo following discontinuation of therapy. If a partner’s vasectomy is method of contraception, a hormone or barrier method must be used along with this method. Counsel patient on emergency contraception. May decrease sperm count in male patients. Advise female patient to notify health care professional immediately if pregnancy is suspected and avoid breastfeeding.

Evaluation/Desired Outcomes

  • Increased exercise tolerance.
References in periodicals archive ?
163/2006, divided into two separate parts, for the award of the exclusive supply of drugs: Lot 1 Opsumit A 10 mg 30 coated tablets (Macitentan) and Lot 2 Tecfidera A 120 mg 14 resistant capsules and 240 mg capsules 56 hard gastro (Dimethylfumarate) required the Company Provincial Health Services of Trento.
A drug called Opsumit, also known as Macitentan, is available for adults in England with moderate to severe pulmonary arterial hypertension (PAH).
A new drug called Opsumit - also known as Macitentan - is available for adults in England with moderate to severe pulmonary arterial hypertension (PAH).
Contract awarded for award summary one time contract opsumit 30mg (30 tbs)
Designed to delay the progression of pulmonary arterial hypertension, Oral Opsumit, is expected to enter into the market in November, said Actelion, and added that still the firm seeks regulatory approval outside the United States.
Jean-Paul Clozel said, Over the last 14 years, Actelion has worked tirelessly to first discover and then develop Opsumit in the largest, longest and first-ever outcome study of PAH.
Clinical data and the opinions of interviewed thought leaders indicate that Actelion/Nippon Shinyaku's Opsumit has advantages on this attribute over sales-leading Actelion's Tracleer.
OTC: ALIOF -Free Report) announced the launch of Opsumit 10 mg in the U.
The SERAPHIN study established the effectiveness of Opsumit in PAH patients with predominantly WHO Functional Class II-III symptoms treated for an average of 2 years.
Actelion is looking to get Opsumit approved in the EU as monotherapy or in combination, for the long-term treatment of PAH in adults of WHO functional class II to III.
Opsumit met its primary end point in the Phase III SERAPHIN study, demonstrating a significant (45 percent) risk reduction in mortality/morbidity events compared with placebo and is currently under review by the U.