Phentolamine: Difference between revisions

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Gerald Chi
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==Overview==
<!--Mechanism of Action-->
 
|mechAction=
 
*


'''Phentolamine''' (Regitine) is a reversible<ref name="isbn0-7817-4266-8">{{cite book |author=Jewell, John R.; Longworth, David L.; Stoller, James K.; Casey, David |title=The Cleveland Clinic internal medicine case reviews |publisher=Lippincott Williams & Wilkins |location=Hagerstown, MD |year=2003 |isbn=0-7817-4266-8 |oclc= |doi= |accessdate= |page=32}}</ref> nonselective alpha-[[adrenergic antagonist]].<ref>{{MeshName|Phentolamine}}</ref>
<!--Structure-->


==Mechanism==
|structure=
Its primary action is [[vasodilation]] due to α<sub>1</sub> blockade.<ref>Brock G. Oral phentolamine (Vasomax). ''Drugs Today (Barcelona)''. 2000 Feb-Mar;36(2-3):121-4.</ref>


It also can lead to reflex [[tachycardia]] because of [[hypotension]] and α<sub>2</sub> inhibition, which increases sympathetic tone.<ref name=pharmnemonics>{{Cite book | author=Shen, Howard | title=Illustrated Pharmacology Memory Cards: PharMnemonics | year=2008 | publisher=Minireview | isbn=1-59541-101-1 | page=14}}</ref>
*


==Uses==
: [[File:{{PAGENAME}}01.png|thumb|none|600px|This image is provided by the National Library of Medicine.]]
The primary application for phentolamine is for the control of [[hypertensive emergency|hypertensive emergencies]], most notably due to [[pheochromocytoma]]. <ref>Tuncel M, Ram VC. Hypertensive emergencies. Etiology and management. ''American Journal of Cardiovascular Drugs''. 2003;3(1):21-31.</ref>


It also has usefulness in  the treatment of [[cocaine]]-induced cardiovascular complications, where one would generally avoid [[Beta-blocker]]s (e.g. [[metoprolol]]), as they can cause unopposed alpha-adrenergic mediated [[Coronary vasospasm|coronary vasoconstriction]], worsening myocardial ischemia and hypertension. It is important to note that phentolamine is not a first-line agent for this indication. Phentolamine should only be given to patients who do not fully respond to [[benzodiazepines]], [[nitroglycerin]], and [[calcium channel blockers]]. <ref>Hollander JE, Henry TD. Evaluation and management of the patient who has cocaine-associated chest pain. ''Cardiology Clinics''. 2006 Feb;24(1):103-14.</ref><ref>Chan GM, Sharma R, Price D, Hoffman RS, Nelson LS. Phentolamine Therapy for Cocaine-Association Acute Coronary Syndrome (CAACS). ''Journal of Medical Toxicology''. 2006 Sep;2(3):108-11.</ref>  
<!--Pharmacodynamics-->


When given by injection it causes blood vessels to expand, thereby increasing blood flow. When injected into the penis (intracavernosal), it increases blood flow to the penis, which results in an erection.<ref>Bella AJ, Brock GB. Intracavernous pharmacotherapy for erectile dysfunction. ''Endocrine''. 2004 Mar-Apr;23(2-3):149-55.</ref>
|PD=


It may be stored in [[crash cart]]s to counteract severe peripheral vasoconstriction secondary to [[extravasation]] of peripherally placed [[vasopressor]] infusions, typically of [[norepinephrine]]. [[Epinephrine]] infusions are less vasoconstrictive than norepinephrine as they primarily stimulate beta receptor more than alpha receptors, but the effect remains dose dependent.
There is limited information regarding <i>Pharmacodynamics</i> of {{PAGENAME}} in the drug label.


Phentolamine also has diagnostic and therapeutic roles in [[complex regional pain syndrome]] (reflex sympathetic dystrophy).<ref>Rowbotham MC. Pharmacologic management of complex regional pain syndrome. ''Clinical Journal of Pain''. 2006 Jun;22(5):425-9.</ref>
<!--Pharmacokinetics-->


Phentolamine has recently been introduced in the dental field as a local anesthetic reversal agent.  Distributed by Septodont, [[OraVerse]] is a Phentolamine Mesylate injection designed to reverse the local vasoconstrictor properties used in many local anesthetics to prolong anesthesia.<ref>http://www.novalar.com/oraverse-dental-specialty-pharmaceutical</ref>  OraVerse has been shown to accelerate the reversal of the lingering soft-tissue numbness associated with the widely used anesthetic-vasoconstrictor combinations.<ref>Malamed S. What's new in local anaesthesia? ''Society For The Advancement Of Anaesthesia In Dentistry Digest''. 2009 Jan;25:4-14.</ref>
|PK=


==Chemistry==
There is limited information regarding <i>Pharmacokinetics</i> of {{PAGENAME}} in the drug label.
Phentolamine can be synthesized by alkylation of 3-(4-methylanilino)phenol using 2-chloromethylimidazoline:<ref>K. Miescher, A. Marxer, E. Urech, {{US Patent|2503059}} (1950)</ref><ref>E. Urech, A. Marxer, K. Miescher, Helv. Chim. Acta, 33, 1386 (1950)</ref>


==References==
<!--Nonclinical Toxicology-->
{{reflist|2}}


{{Antihypertensives and diuretics}}
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*
 
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<!--Precautions with Alcohol-->
 
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* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
 
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* Oraverse®<ref>{{Cite web | title = Oraverse (phentolamine mesylate)  | url = http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=38be9414-87c4-4a8a-9f17-99be0d0a33fa }}</ref>
 
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* A® — B®<ref name="www.ismp.org">{{Cite web  | last =  | first =  | title = http://www.ismp.org | url = http://www.ismp.org | publisher =  | date =  }}</ref>
 
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[[Category:Antihypertensive agents]]
[[Category:Alpha blockers]]
[[Category:Diuretics]]
[[Category:Cardiovascular Drugs]]
[[Category:Cardiovascular Drugs]]
[[Category:Drug]]
[[Category:Drug]]
[[Category:Vasodilators]]
[[Category:Vasodilators]]
[[Category:Imidazolines]]
[[Category:Alpha blockers]]

Revision as of 15:10, 26 July 2014

Phentolamine
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

Phentolamine 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 Phentolamine in adult patients.

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

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

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Phentolamine 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 Phentolamine 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 Phentolamine 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 Phentolamine in women who are pregnant.

Labor and Delivery

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

Nursing Mothers

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

Pediatric Use

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

Geriatic Use

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

Gender

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

Race

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

Renal Impairment

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

Hepatic Impairment

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

Females of Reproductive Potential and Males

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

Immunocompromised Patients

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

Administration and Monitoring

Administration

  • Oral
  • Intravenous

Monitoring

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

  • Description

IV Compatibility

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

Overdosage

Acute Overdose

Signs and Symptoms

  • Description

Management

  • Description

Chronic Overdose

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

Pharmacology

Phentolamine
Clinical data
Trade namesRegitine
AHFS/Drugs.comMicromedex Detailed Consumer Information
Pregnancy
category
Routes of
administration		Usually IV or IM
ATC code
Pharmacokinetic data
MetabolismHepatic
Elimination half-life19 minutes
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC17H19N3O
Molar mass281.352 g/mol
3D model (JSmol)
 ☒N☑Y (what is this?)  (verify)

Mechanism of Action

Structure

This image is provided by the National Library of Medicine.

Pharmacodynamics

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

Pharmacokinetics

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

Nonclinical Toxicology

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

Clinical Studies

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

How Supplied

Storage

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

Images

Drug Images

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

Patient Counseling Information

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

Precautions with Alcohol

  • Alcohol-Phentolamine 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. ↑ "Oraverse (phentolamine mesylate)".
  2. ↑ "http://www.ismp.org". External link in |title= (help)


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