Ambrisentan: Difference between revisions

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{{drugbox
{{DrugProjectFormSinglePage
| IUPAC_name        = 2-(4,6-dimethylpyrimidin-2-yl)oxy-3-methoxy-<br>3,3-diphenyl-propanoic acid
|authorTag=
| image            = Ambrisentan_svg.png
 
| CAS_number        = 177036-94-1
Gerald Chi
| ATC_prefix        = C02
 
| ATC_suffix        = KX02
<!--Overview-->
| PubChem          = 197712
 
| DrugBank          =  
|genericName=
| smiles            = COC(C(Oc1nc(C)cc(C)n1)C(O)=O)(c2ccccc2)c3ccccc3 <!-- Unique SMILES formula -->
 
| C = 22 | H = 22 | N = 2 | O = 4
 
| molecular_weight  = 378.421 g/mol
 
| bioavailability  = Undetermined
|aOrAn=
| protein_bound    = 99%
 
| metabolism        =  
a
| elimination_half-life = 15 hours (terminal)
 
| excretion        =  
|drugClass=
| pregnancy_AU      = <!-- A / B1 / B2 / B3 / C / D / X -->
 
| pregnancy_US      = X
 
| pregnancy_category= May cause harm to fetus
 
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| legal_CA          = <!--             / Schedule I, II, III, IV, V, VI, VII, VIII -->
 
| legal_UK          = <!-- GSL        / P      / POM / CD / Class A, B, C -->
 
| legal_US          = Rx-only
 
| legal_status      =  
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| routes_of_administration = Oral
 
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<!--FDA-Labeled Indications and Dosage (Pediatric)-->
 
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|postmarketing=
 
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=====Cardiovascular=====
 
 
 
=====Digestive=====
 
 
 
=====Endocrine=====
 
 
 
=====Hematologic and Lymphatic=====
 
 
 
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=====Neurologic=====
 
 
 
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|administration=
 
* Oral
 
* Intravenous
 
|monitoring=
 
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* Description
 
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|overdose=
 
===Acute Overdose===
 
====Signs and Symptoms====
 
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: [[File:{{PAGENAME}}01.png|thumb|none|600px|This image is provided by the National Library of Medicine.]]
 
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|alcohol=
 
* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
 
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|brandNames=
 
* ®<ref>{{Cite web | title =  | url =  }}</ref>
 
<!--Look-Alike Drug Names-->


==Overview==
|lookAlike=
'''Ambrisentan''' (U.S. trade name '''Letairis'''; E.U. trade name '''Volibris'''; India trade name '''pulmonext''' by MSN labs)  is a drug indicated for use in the treatment of [[pulmonary hypertension]].


It functions as an [[endothelin receptor antagonist]], and is selective for the type A [[endothelin receptor]] (ET<sub>A</sub>).<ref>{{cite journal |author=Vatter H, Seifert V |title=Ambrisentan, a non-peptide endothelin receptor antagonist |journal=Cardiovasc Drug Rev |volume=24 |issue=1 |pages=63–76 |year=2006 |pmid=16939634 |doi=10.1111/j.1527-3466.2006.00063.x}}</ref> Once daily oral ambrisentan 2.5 to 10 mg/day significantly improved exercise capacity (6-minute walk distance) compared with placebo in two double-blind, multicenter trials (ARIES-1 & ARIES-2).<ref name="test">Frampton JE. Ambrisentan. ''American Journal of Cardiovascular Drugs'' August 1, 2011; '''11''' (4): 215-226.[http://adisonline.com/cardiovascular/pages/articleviewer.aspx?year=2011&issue=11040&article=00001&type=abstract Link text] </ref>  
* A® — B®<ref name="www.ismp.org">{{Cite web  | last = | first = | title = http://www.ismp.org | url = http://www.ismp.org | publisher = | date = }}</ref>


Ambrisentan was approved for sale by the U.S. [[Food and Drug Administration]] (FDA) on June 15, 2007 for the once-daily treatment of [[pulmonary hypertension|pulmonary arterial hypertension]].<ref>
<!--Drug Shortage Status-->
{{cite news
  | last        = Pollack
  | first      = Andrew
  | title      = Gilead’s Drug Is Approved to Treat a Rare Disease
  | work        = [[New York Times]]
  | date        = 2007-06-16
  | url        = http://www.nytimes.com/2007/06/16/business/16gilead.html
  | accessdate  = 2007-05-25
| archiveurl= http://web.archive.org/web/20070620112127/http://www.nytimes.com/2007/06/16/business/16gilead.html| archivedate= 20 June 2007 <!--DASHBot-->| deadurl= no}}</ref><ref>
{{cite press release
  | title = U.S. Food and Drug Administration Approves Gilead's Letairis Treatment of Pulmonary Arterial Hypertension
  | publisher = [[Gilead Sciences]]
  | date = 2007-06-15
  | url = http://www.gilead.com/wt/sec/pr_1016053
  | accessdate = 2007-06-16
}}</ref><ref>
{{cite press release
  | title = FDA Approves New Orphan Drug for Treatment of Pulmonary Arterial Hypertension
  | publisher = [[Food and Drug Administration]]
  | date = 2007-06-15
  | url = http://www.fda.gov/bbs/topics/NEWS/2007/NEW01653.html
  | accessdate = 2007-06-22
| archiveurl= http://web.archive.org/web/20070623055608/http://www.fda.gov/bbs/topics/NEWS/2007/NEW01653.html| archivedate= 23 June 2007 <!--DASHBot-->| deadurl= no}}</ref>
It was later approved by the [[European Medicines Agency]] for use in the EU on April 2008.<ref>
{{cite press release
  | title = GlaxoSmithKline's Volibris (ambrisentan) receives authorisation from the European Commission for the treatment of Functional Class II and III Pulmonary Arterial Hypertension
  | publisher = [[GlaxoSmithKline]]
  | date = 2008-04-25
  | url = http://www.gsk.com/media/pressreleases/2008/2008_pressrelease_10033.htm
  | accessdate = 2008-04-29
| archiveurl= http://web.archive.org/web/20080430150346/http://www.gsk.com/media/pressreleases/2008/2008_pressrelease_10033.htm| archivedate= 30 April 2008 <!--DASHBot-->| deadurl= no}}</ref>
Ambrisentan had previously been designated an [[orphan drug]] by both the FDA and the European Commission, in August 2004 and May 2005 respectively.<ref>
{{cite web
  | last = Waknine
  | first = Yael
  | title = International Approvals: Ambrisentan, Oral-lyn, Risperdal
  | publisher = [[Medscape]]
  | date = 2005-05-09
  | url = http://www.medscape.com/viewarticle/504469
  | accessdate = 2007-06-16
}}</ref>


==Clinical uses==
|drugShortage=
Ambrisentan is indicated for the treatment of pulmonary arterial hypertension (WHO Group 1) in
}}
patients with WHO class II or III symptoms to improve exercise capacity and delay clinical worsening.


==The LETAIRIS Education and Access Program==
<!--Pill Image-->
The LETAIRIS Education and Access Program (LEAP) is a program to help physicians and patients learn about the risks of LETAIRIS, including the serious risks of liver injury and birth defects.


LEAP works by:
{{PillImage
|fileName=No image.jpg|This image is provided by the National Library of Medicine.
|drugName=
|NDC=
|drugAuthor=
|ingredients=
|pillImprint=
|dosageValue=
|dosageUnit=
|pillColor=
|pillShape=
|pillSize=
|pillScore=
}}


* Providing information to prescribers on the risks of LETAIRIS
<!--Label Display Image-->
* Providing comprehensive education to patients and assistance with obtaining LETAIRIS
* Requiring enrollment of both prescriber and patient in LEAP
* Controlling dispensing through a specialized distribution network (specialty pharmacies)


==External links==
{{LabelImage
* [http://www.letairis.com/ Letairis website] run by Gilead Sciences
|fileName={{PAGENAME}}11.png|This image is provided by the National Library of Medicine.
* [http://www.letairis.com/downloads/LETAIRIS_prescribing_information.pdf Prescribing information]
}}
* [http://www.letairis.com/how_to_get_letairis.html Information on the LETAIRIS Education and Access Program (LEAP)]


==References==
{{LabelImage
{{Reflist|2}}
|fileName={{PAGENAME}}11.png|This image is provided by the National Library of Medicine.
}}


{{PAH rx}}
<!--Category-->
{{Antihypertensives and diuretics}}


[[Category:Endothelin receptor antagonists]]
[[Category:Endothelin receptor antagonists]]

Revision as of 02:56, 27 July 2014

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

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Black Box Warning

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

Overview

Ambrisentan is a that is FDA approved for the {{{indicationType}}} of . There is a Black Box Warning for this drug as shown here. Common adverse reactions include .

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Condition1
  • Dosing Information
  • Dosage
Condition2
  • Dosing Information
  • Dosage
Condition3
  • Dosing Information
  • Dosage
Condition4
  • Dosing Information
  • Dosage

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

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

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

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)

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding FDA-Labeled Use of Ambrisentan in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

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

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

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

  • Description

Chronic Overdose

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

Pharmacology

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

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

Look-Alike Drug Names

Drug Shortage Status

Price

References

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

  1. ↑ Empty citation (help)
  2. ↑ "http://www.ismp.org". External link in |title= (help)


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