Ambrisentan

Ambrisentan
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Gerald Chi

Disclaimer

WikiDoc MAKES NO GUARANTEE OF VALIDITY. WikiDoc is not a professional health care provider, nor is it a suitable replacement for a licensed healthcare provider. WikiDoc is intended to be an educational tool, not a tool for any form of healthcare delivery. The educational content on WikiDoc drug pages is based upon the FDA package insert, National Library of Medicine content and practice guidelines / consensus statements. WikiDoc does not promote the administration of any medication or device that is not consistent with its labeling. Please read our full disclaimer here.

Black Box Warning

Title See full prescribing information for complete Boxed Warning. ConditionName: Content

Overview

Ambrisentan is an endothelin receptor antagonist that is FDA approved for the {{{indicationType}}} of pulmonary arterial hypertension. There is a Black Box Warning for this drug as shown here. Common adverse reactions include edema, decreased hemoglobin, and headache.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Pulmonary Arterial Hypertension

• Letairis is indicated for the treatment of pulmonary arterial hypertension (PAH) (WHO Group 1) to improve exercise ability and delay clinical worsening. Studies establishing effectiveness included predominantly patients with WHO Functional Class II–III symptoms and etiologies of idiopathic or heritable PAH (64%) or PAH associated with connective tissue diseases (32%).

• Dosing Information

• Initiate treatment at 5 mg once daily, and consider increasing the dose to 10 mg once daily if 5 mg is tolerated.
• Tablets may be administered with or without food. Tablets should not be split, crushed, or chewed. Doses higher than 10 mg once daily have not been studied in patients with pulmonary arterial hypertension (PAH).

Pregnancy Testing in Females of Reproductive Potential

• Initiate treatment with Letairis in females of reproductive potential only after a negative pregnancy test. Obtain monthly pregnancy tests during treatment

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Ambrisentan in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Ambrisentan in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

• Safety and effectiveness of Letairis in pediatric patients have not been established.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Ambrisentan in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Ambrisentan in pediatric patients.

Contraindications

• Condition1

Warnings

Title See full prescribing information for complete Boxed Warning. ConditionName: Content

• Description

Precautions

• Description

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Clinical Trial Experience of Ambrisentan 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 Ambrisentan 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 (FDA):

• Pregnancy Category

Pregnancy Category (AUS):

• Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Ambrisentan in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Ambrisentan during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Ambrisentan with respect to nursing mothers.

Pediatric Use

There is no FDA guidance on the use of Ambrisentan with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Ambrisentan with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Ambrisentan with respect to specific gender populations.

Race

There is no FDA guidance on the use of Ambrisentan with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Ambrisentan in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Ambrisentan in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Ambrisentan in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Ambrisentan in patients who are immunocompromised.

Administration and Monitoring

Administration

• Oral

• Intravenous

Monitoring

There is limited information regarding Monitoring of Ambrisentan in the drug label.

• Description

IV Compatibility

There is limited information regarding IV Compatibility of Ambrisentan in the drug label.

Overdosage

Acute Overdose

Signs and Symptoms

• Description

Management

• xx

Chronic Overdose

There is limited information regarding Chronic Overdose of Ambrisentan in the drug label.

Pharmacology

Ambrisentan
Systematic (IUPAC) name
(2S)-2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3-methoxy- 3,3-diphenylpropanoic acid
Identifiers
CAS number	177036-94-1
ATC code	C02KX02
PubChem	6918493
Chemical data
Formula	Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox
Mol. mass	378.421 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	Undetermined
Protein binding	99%
Metabolism	?
Half life	15 hours (terminal)
Excretion	?
Therapeutic considerations
Licence data	EU, US
Pregnancy cat.	X(AU) X(US)
Legal status	Prescription Only (S4)(AU) ?(CA) POM(UK) [[Prescription drug|Template:Unicode-only]](US)
Routes	Oral

Mechanism of Action

Structure

This image is provided by the National Library of Medicine.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Ambrisentan in the drug label.

Pharmacokinetics

There is limited information regarding Pharmacokinetics of Ambrisentan in the drug label.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Ambrisentan in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Ambrisentan in the drug label.

How Supplied

Storage

There is limited information regarding Ambrisentan Storage in the drug label.

Images

Drug Images

{{#ask: Page Name::Ambrisentan |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}

Package and Label Display Panel

{{#ask: Label Page::Ambrisentan |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}

Patient Counseling Information

There is limited information regarding Patient Counseling Information of Ambrisentan in the drug label.

Precautions with Alcohol

• Alcohol-Ambrisentan interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

• Letairis®

Look-Alike Drug Names

• Letairis® — Letaris®

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

{{#subobject:

 |Page Name=Ambrisentan
 |Pill Name=No image.jpg
 |Drug Name=
 |Pill Ingred=|+sep=;
 |Pill Imprint=
 |Pill Dosage=
 |Pill Color=|+sep=;
 |Pill Shape=
 |Pill Size (mm)=
 |Pill Scoring=
 |Pill Image=
 |Drug Author=
 |NDC=

}}

{{#subobject:

 |Label Page=Ambrisentan
 |Label Name=Ambrisentan11.png

}}

{{#subobject:

 |Label Page=Ambrisentan
 |Label Name=Ambrisentan11.png

}}