Phentolamine: Difference between revisions

Phentolamine
Clinical data
Trade names	Regitine
AHFS/Drugs.com	Micromedex Detailed Consumer Information
Pregnancy; category	C (U.S.);
Routes of; administration	Usually IV or IM
ATC code	C04AB01 (WHO) V03AB36 (WHO);
Pharmacokinetic data
Metabolism	Hepatic
Elimination half-life	19 minutes
Identifiers
	IUPAC name 3-[(4,5-dihydro-1H-imidazol-2-ylmethyl)(4-methylphenyl)amino]phenol;
CAS Number	50-60-2 ;
PubChem CID	5775;
IUPHAR/BPS	502;
DrugBank	DB00692 ;
ChemSpider	5571 ;
UNII	Z468598HBV;
KEGG	D08362 ;
ChEBI	CHEBI:8081 ;
ChEMBL	ChEMBL597 ;
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
Formula	C17H19N3O
Molar mass	281.352 g/mol
3D model (JSmol)	Interactive image;
	SMILES Oc3cc(N(c1ccc(cc1)C)CC/2=N/CCN\2)ccc3;
	InChI InChI=1S/C17H19N3O/c1-13-5-7-14(8-6-13)20(12-17-18-9-10-19-17)15-3-2-4-16(21)11-15/h2-8,11,21H,9-10,12H2,1H3,(H,18,19) ; Key:MRBDMNSDAVCSSF-UHFFFAOYSA-N ;
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Phentolamine
	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

VisualWikitext

Revision as of 15:25, 26 July 2014

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

Disclaimer

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Overview

Phentolamine is a vasodilator and alpha-adrenergic blocker that is FDA approved for the {{{indicationType}}} of reversal of the soft-tissue anesthesia. Common adverse reactions include injection site pain, diarrhea, and nasal congestion.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Reversal of the Soft-Tissue Anesthesia

OraVerse is indicated for reversal of the soft-tissue anesthesia, i.e., anesthesia of the lip and tongue, and the associated functional deficits resulting from an intraoral submucosal injection of a local anesthetic containing a vasoconstrictor. OraVerse is not recommended for use in children less than 6 years of age or weighing less than 15 kg (33 lbs).

Dosing Information

The recommended dose of OraVerse is based on the number of cartridges of local anesthetic with vasoconstrictor administered:

This image is provided by the National Library of Medicine.

OraVerse should be administered following the dental procedure using the same location(s) and technique(s) (infiltration or block injection) employed for the administration of the local anesthetic.
Note: Do not administer OraVerse if the product is discolored or contains particulate matter.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

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

Non–Guideline-Supported Use

Hypertension

Dosing Information

Intravenous phentolamine 5 to 20 milligrams is effective for treating hypertensive crises induced by high levels of circulating catecholamines. conditions which phentolamine may by effective for include pheochromocytoma, clonidine withdrawal, and monoamine oxidase inhibitor interactions.^[1]

Sympathetically Maintained Pain

Phentolamine (1 to 10 milligrams, increasing at 3- to 8-minute intervals up to 25 milligrams) is effective for determining if pain is sympathetically maintained.^[2]

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Reversal of the Soft-Tissue Anesthesia

Dosing Information

In pediatric patients weighing 15-30 kg, the maximum dose of OraVerse recommended is 1/2 cartridge (0.2 mg).
Note: Use in pediatric patients under 6 years of age or weighing less than 15 kg (33 lbs) is not recommended. A dose of more than 1 cartridge [0.4 mg] of OraVerse has not been studied in children less than 12 years of age.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

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

Non–Guideline-Supported Use

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

Contraindications

None (phentolamine mesylate solution for submucosal use)

Warnings

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

Submucosal use

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

Mechanism of Action

Structure

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

Regitine®
Oraverse®^[3]

Look-Alike Drug Names

A® — B®^[4]

Drug Shortage Status

Price

References

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

↑ Kincaid-Smith, P. (1985-04-15). "Vasodilator drugs in the treatment of hypertension". The Medical Journal of Australia. 142 (8): 450–453. ISSN 0025-729X. PMID 3884988.
↑ Raja, S. N. (1991-04). "Systemic alpha-adrenergic blockade with phentolamine: a diagnostic test for sympathetically maintained pain". Anesthesiology. 74 (4): 691–698. ISSN 0003-3022. PMID 1848966. Unknown parameter |coauthors= ignored (help); Check date values in: |date= (help)
↑ "Oraverse (phentolamine mesylate)".
↑ "http://www.ismp.org". External link in |title= (help)

{{#subobject:

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 |Pill Name=No image.jpg
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{{#subobject:

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{{#subobject:

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[1] Kincaid-Smith, P. (1985-04-15). "Vasodilator drugs in the treatment of hypertension". The Medical Journal of Australia. 142 (8): 450–453. ISSN 0025-729X. PMID 3884988.

[2] Raja, S. N. (1991-04). "Systemic alpha-adrenergic blockade with phentolamine: a diagnostic test for sympathetically maintained pain". Anesthesiology. 74 (4): 691–698. ISSN 0003-3022. PMID 1848966. Unknown parameter |coauthors= ignored (help); Check date values in: |date= (help)

[3] "Oraverse (phentolamine mesylate)".

[www.ismp.org-4] "http://www.ismp.org". External link in |title= (help)

[1]

[2]

[3]

[4]

@@ Line 68: / Line 68: @@
 |offLabelAdultNoGuideSupport=
-=====Condition1=====
+=====Hypertension=====
 * Dosing Information
-:* Dosage
+:* Intravenous phentolamine 5 to 20 milligrams is effective for treating hypertensive crises induced by high levels of circulating catecholamines. conditions which phentolamine may by effective for include pheochromocytoma, clonidine withdrawal, and monoamine oxidase inhibitor interactions.<ref>{{Cite journal | issn = 0025-729X | volume = 142 | issue = 8 | pages = 450–453 | last = Kincaid-Smith | first = P. | title = Vasodilator drugs in the treatment of hypertension | journal = The Medical Journal of Australia | date = 1985-04-15 | pmid = 3884988 }}</ref>
-=====Condition2=====
+=====Sympathetically Maintained Pain=====
-There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.
+* Phentolamine (1 to 10 milligrams, increasing at 3- to 8-minute intervals up to 25 milligrams) is effective for determining if pain is sympathetically maintained.<ref>{{Cite journal | issn = 0003-3022 | volume = 74 | issue = 4 | pages = 691–698 | last = Raja | first = S. N. | coauthors = R. D. Treede, K. D. Davis, J. N. Campbell | title = Systemic alpha-adrenergic blockade with phentolamine: a diagnostic test for sympathetically maintained pain | journal = Anesthesiology | date = 1991-04 | pmid = 1848966 }}</ref>
 <!--Pediatric Indications and Dosage-->
@@ Line 84: / Line 84: @@
 |fdaLIADPed=
-=====Condition1=====
+=====Reversal of the Soft-Tissue Anesthesia=====
 * Dosing Information
-:* Dosage
+:* In pediatric patients weighing 15-30 kg, the maximum dose of OraVerse recommended is 1/2 cartridge (0.2 mg).
+:* Note: Use in pediatric patients under 6 years of age or weighing less than 15 kg (33 lbs) is not recommended. A dose of more than 1 cartridge [0.4 mg] of OraVerse has not been studied in children less than 12 years of age.
-=====Condition2=====
-There is limited information regarding <i>FDA-Labeled Use</i> of {{PAGENAME}} in pediatric patients.
 <!--Off-Label Use and Dosage (Pediatric)-->
@@ Line 99: / Line 96: @@
 |offLabelPedGuideSupport=
-=====Condition1=====
-* Developed by:
-* Class of Recommendation:
-* Strength of Evidence:
-* Dosing Information
-:* Dosage
-=====Condition2=====
 There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
@@ Line 119: / Line 102: @@
 |offLabelPedNoGuideSupport=
-=====Condition1=====
-* Dosing Information
-:* Dosage
-=====Condition2=====
 There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
@@ Line 134: / Line 109: @@
 |contraindications=
-* Condition1
+* None (phentolamine mesylate solution for submucosal use)
 <!--Warnings-->
@@ Line 327: / Line 302: @@
 |administration=
-* Oral
+* Submucosal use
-* Intravenous
 |monitoring=