Macitentan: Difference between revisions
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:* OPSUMIT may cause fetal harm when administered to a pregnant woman. OPSUMIT is contraindicated in females who are pregnant. OPSUMIT was consistently shown to have teratogenic effects when administered to animals. If OPSUMIT is used during pregnancy, apprise the patient of the potential hazard to a fetus. | |||
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Revision as of 16:05, 27 July 2014
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Gerald Chi
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Black Box Warning
WARNING: EMBRYO-FETAL TOXICITY
See full prescribing information for complete Boxed Warning.
* Do not administer OPSUMIT to a pregnant female because it may cause fetal harm.
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Overview
Macitentan is an endothelin receptor antagonist and antihypertensive that is FDA approved for the {{{indicationType}}} of pulmonary artery hypertension. There is a Black Box Warning for this drug as shown here. Common adverse reactions include anemia, influenza, headache, urinary tract infections, bronchitis, nasopharyngitis, and pharyngitis.
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
Pulmonary Arterial Hypertension
- OPSUMIT® is an endothelin receptor antagonist (ERA) indicated for the treatment of pulmonary arterial hypertension (PAH, WHO Group I) to delay disease progression. Disease progression included: death, initiation of intravenous (IV) or subcutaneous prostanoids, or clinical worsening of PAH (decreased 6-minute walk distance, worsened PAH symptoms and need for additional PAH treatment). OPSUMIT also reduced hospitalization for PAH.
- Effectiveness was established in a long-term study in PAH patients with predominantly WHO Functional Class II-III symptoms treated for an average of 2 years. Patients were treated with OPSUMIT monotherapy or in combination with phosphodiesterase-5 inhibitors or inhaled prostanoids. Patients had idiopathic and heritable PAH (57%), PAH caused by connective tissue disorders (31%), and PAH caused by congenital heart disease with repaired shunts (8%).
- Dosing Information
- The recommended dosage of OPSUMIT is 10 mg once daily for oral administration. Doses higher than 10 mg once daily have not been studied in patients with PAH and are not recommended.
- Initiate treatment with OPSUMIT in females of reproductive potential only after a negative pregnancy test. Obtain monthly pregnancy test during treatment.
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Macitentan in adult patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Macitentan in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
There is limited information regarding FDA-Labeled Use of Macitentan in pediatric patients.
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
- The safety and efficacy of OPSUMIT in children have not been established.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Macitentan in pediatric patients.
Contraindications
- Pregnancy
- OPSUMIT may cause fetal harm when administered to a pregnant woman. OPSUMIT is contraindicated in females who are pregnant. OPSUMIT was consistently shown to have teratogenic effects when administered to animals. If OPSUMIT is used during pregnancy, apprise the patient of the potential hazard to a fetus.
Warnings
WARNING: EMBRYO-FETAL TOXICITY
See full prescribing information for complete Boxed Warning.
* Do not administer OPSUMIT to a pregnant female because it may cause fetal harm.
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- Description
Precautions
- Description
Adverse Reactions
Clinical Trials Experience
There is limited information regarding Clinical Trial Experience of Macitentan in the drug label.
Body as a Whole
Cardiovascular
Digestive
Endocrine
Hematologic and Lymphatic
Metabolic and Nutritional
Musculoskeletal
Neurologic
Respiratory
Skin and Hypersensitivy Reactions
Special Senses
Urogenital
Miscellaneous
Postmarketing Experience
There is limited information regarding Postmarketing Experience of Macitentan in the drug label.
Body as a Whole
Cardiovascular
Digestive
Endocrine
Hematologic and Lymphatic
Metabolic and Nutritional
Musculoskeletal
Neurologic
Respiratory
Skin and Hypersensitivy Reactions
Special Senses
Urogenital
Miscellaneous
Drug Interactions
- Drug
- Description
Use in Specific Populations
Pregnancy
- Pregnancy Category
- Australian Drug Evaluation Committee (ADEC) Pregnancy Category
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Macitentan in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Macitentan during labor and delivery.
Nursing Mothers
There is no FDA guidance on the use of Macitentan with respect to nursing mothers.
Pediatric Use
There is no FDA guidance on the use of Macitentan with respect to pediatric patients.
Geriatic Use
There is no FDA guidance on the use of Macitentan with respect to geriatric patients.
Gender
There is no FDA guidance on the use of Macitentan with respect to specific gender populations.
Race
There is no FDA guidance on the use of Macitentan with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Macitentan in patients with renal impairment.
Hepatic Impairment
There is no FDA guidance on the use of Macitentan in patients with hepatic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Macitentan in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Macitentan in patients who are immunocompromised.
Administration and Monitoring
Administration
- Oral
- Intravenous
Monitoring
There is limited information regarding Monitoring of Macitentan in the drug label.
- Description
IV Compatibility
There is limited information regarding IV Compatibility of Macitentan in the drug label.
Overdosage
Acute Overdose
Signs and Symptoms
- Description
Management
- Description
Chronic Overdose
There is limited information regarding Chronic Overdose of Macitentan in the drug label.
Pharmacology
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Macitentan
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Systematic (IUPAC) name | |
N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide | |
Identifiers | |
CAS number | |
ATC code | C02 |
PubChem | |
Chemical data | |
Formula | Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox |
Mol. mass | 588.273 g/mol |
SMILES | & |
Synonyms | ACT-064992 |
Pharmacokinetic data | |
Bioavailability | ? |
Metabolism | Hydrolysis, oxidation (CYP3A4) |
Half life | ? |
Excretion | 2/3 urine, 1/3 faeces |
Therapeutic considerations | |
Pregnancy cat. |
X(US) |
Legal status |
[[Prescription drug|Template:Unicode-only]](US) FDA approved drug |
Routes | Oral |
Mechanism of Action
Structure
Pharmacodynamics
There is limited information regarding Pharmacodynamics of Macitentan in the drug label.
Pharmacokinetics
There is limited information regarding Pharmacokinetics of Macitentan in the drug label.
Nonclinical Toxicology
There is limited information regarding Nonclinical Toxicology of Macitentan in the drug label.
Clinical Studies
There is limited information regarding Clinical Studies of Macitentan in the drug label.
How Supplied
Storage
There is limited information regarding Macitentan Storage in the drug label.
Images
Drug Images
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Package and Label Display Panel
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Patient Counseling Information
There is limited information regarding Patient Counseling Information of Macitentan in the drug label.
Precautions with Alcohol
- Alcohol-Macitentan interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
- Opsumit®[1]
Look-Alike Drug Names
- A® — B®[2]
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.
- ↑ "OPSUMIT (macitentan) tablet, film coated".
- ↑ "http://www.ismp.org". External link in
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