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{{Drugbox|
{{DrugProjectFormSinglePage
|IUPAC_name = 2-(1-naphthylmethyl)-4,5-dihydro-1 ''H''-imidazole
|authorTag={{RB}}
| image=
|genericName=Naphazoline
| width=220px
|aOrAn=a
| CAS_number=835-31-4  
|drugClass=Alpha-Adrenergic Agonist
| ATC_prefix=R01
|indicationType=treatment
| ATC_suffix=AA08  
|indication=as a topical [[ocular vasoconstrictor]]
| ATC_supplemental=
|adverseReactions=[[Mydriasis]], increased redness, [[increased intraocular pressure]], [[irritation]]
| PubChem=4436
 
| DrugBank=
 
| C=14|H=14|N=2
<!--Black Box Warning-->
| molecular_weight = 210.274  
|blackBoxWarningTitle=<span style="color:#FF0000;">ConditionName: </span>
| bioavailability=  
|blackBoxWarningBody=<i><span style="color:#FF0000;">ConditionName: </span></i>
| metabolism =  
 
| elimination_half-life=
 
| excretion =
 
| pregnancy_category =  
<!--Adult Indications and Dosage-->
| legal_status =  
 
| routes_of_administration=Topical
<!--FDA-Labeled Indications and Dosage (Adult)-->
|fdaLIADAdult=====Indication====
* Naphazoline Hydrochloride Ophthalmic Solution is indicated for use as a topical [[ocular vasoconstrictor.]]
 
====Dosage====
* Instill one or two drops in the conjunctival sac(s) every three to four hours as needed.
|offLabelAdultGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.
 
<!--Non–Guideline-Supported Use (Adult)-->
|offLabelAdultNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.
 
<!--Pediatric Indications and Dosage-->
 
<!--FDA-Labeled Indications and Dosage (Pediatric)-->
|fdaLIADPed=There is limited information regarding <i>FDA-Labeled Use</i> of {{PAGENAME}} in pediatric patients.
 
<!--Off-Label Use and Dosage (Pediatric)-->
 
<!--Guideline-Supported Use (Pediatric)-->
|offLabelPedGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
 
<!--Non–Guideline-Supported Use (Pediatric)-->
|offLabelPedNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
 
<!--Contraindications-->
|contraindications=* Contraindicated in the presence of an anatomically narrow angle or in narrow angle glaucoma or in persons who have shown hypersensitivity to any component of this preparation.
 
<!--Warnings-->
|warnings=* Patients under therapy with MAO inhibitors may experience a severe [[hypertensive crisis]] if given a [[sympathomimetic]] drug. Use in children, especially infants, may result in CNS depression leading to coma and marked reduction in body temperature.
 
====Precautions====
 
* For topical ophthalmic use only. Use with caution in presence of [[hypertension]], cardiovascular abnormalities, [[hyperglycemia]] ([[diabetes]]), [[hyperthyroidism]], infection or injury.
 
<!--Adverse Reactions-->
 
<!--Clinical Trials Experience-->
|clinicalTrials======Ocular=====
* [[Mydriasis]], increased redness, [[irritation]], [[discomfort]], [[blurring]], [[punctate keratitis]], [[lacrimation]], [[increased intraocular pressure]].
 
=====Systemic=====
* [[Dizziness]], [[headache]], [[nausea]], [[sweating]], [[nervousness]], [[drowsiness]], [[weakness]], [[hypertension]], [[cardiac irregularities]], and [[hyperglycemia]].
|postmarketing=There is limited information regarding <i>Postmarketing Experience</i> of {{PAGENAME}} in the drug label.
 
 
 
<!--Drug Interactions-->
|drugInteractions=* Concurrent use of [[maprotiline]] or [[tricyclic antidepressants]] and naphazoline may also potentiate the pressor effect of naphazoline. Patients under therapy with [[MAO inhibitors]] may experience a severe hypertensive crisis if given a sympathomimetic drug.
 
<!--Use in Specific Populations-->
|FDAPregCat=C
|useInPregnancyFDA=* Animal reproduction studies have not been conducted with naphazoline. It is also not known whether naphazoline can cause harm when administered to a pregnant women or can affect reproduction capacity. Naphazoline should be given to a pregnant women only if clearly needed.
|useInPregnancyAUS=* '''Australian Drug Evaluation Committee (ADEC) Pregnancy Category'''
 
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of {{PAGENAME}} in women who are pregnant.
|useInLaborDelivery=There is no FDA guidance on use of {{PAGENAME}} during labor and delivery.
|useInNursing=* It is not known whether naphazoline is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when naphazoline is administered to a nursing women.
|useInPed=* Safety and effectiveness in the pediatric population have not been established
|useInGeri=There is no FDA guidance on the use of {{PAGENAME}} with respect to geriatric patients.
|useInGender=There is no FDA guidance on the use of {{PAGENAME}} with respect to specific gender populations.
|useInRace=There is no FDA guidance on the use of {{PAGENAME}} with respect to specific racial populations.
|useInRenalImpair=There is no FDA guidance on the use of {{PAGENAME}} in patients with renal impairment.
|useInHepaticImpair=There is no FDA guidance on the use of {{PAGENAME}} in patients with hepatic impairment.
|useInReproPotential=There is no FDA guidance on the use of {{PAGENAME}} in women of reproductive potentials and males.
|useInImmunocomp=There is no FDA guidance one the use of {{PAGENAME}} in patients who are immunocompromised.
 
<!--Administration and Monitoring-->
|administration=* Instill one or two drops in the conjunctival sac(s) every three to four hours as needed.
|monitoring=There is limited information regarding <i>Monitoring</i> of {{PAGENAME}} in the drug label.
 
* Description
 
<!--IV Compatibility-->
|IVCompat=There is limited information regarding <i>IV Compatibility</i> of {{PAGENAME}} in the drug label.
 
<!--Overdosage-->
|overdose=There is limited information regarding <i>Overdose</i> of {{PAGENAME}} in the drug label.
 
<!--Pharmacology-->
 
<!--Drug box 2-->
|drugBox={{Drugbox2
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 462258437
| IUPAC_name = 2-(naphthalen-1-ylmethyl)-4,5-dihydro-1''H''-imidazole
| image = Naphazoline wiki str.png
| width = 200px
| image2 = Naphazoline wiki str 2.png
 
<!--Clinical data-->
| tradename = Naphcon-a
| Drugs.com = {{drugs.com|monograph|naphazoline-hydrochloride}}
| pregnancy_category = 
| legal_status = 
| routes_of_administration = Topical
 
<!--Pharmacokinetic data-->
| bioavailability = 
| metabolism = 
| excretion =
 
<!--Identifiers-->
| CAS_number_Ref = {{cascite|changed|??}}
| CAS_number = 835-31-4
| ATC_prefix = R01
| ATC_suffix = AA08
| ATC_supplemental = {{ATC|S01|GA01}}
| PubChem = 4436
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB06711
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 4283
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = H231GF11BV
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D08253
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 761
 
<!--Chemical data-->
| C=14 | H=14 | N=2  
| molecular_weight = 210.274
| smiles = N\1=C(\NCC/1)Cc2cccc3c2cccc3
| InChI = 1/C14H14N2/c1-2-7-13-11(4-1)5-3-6-12(13)10-14-15-8-9-16-14/h1-7H,8-10H2,(H,15,16)
| InChIKey = CNIIGCLFLJGOGP-UHFFFAOYAL
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C14H14N2/c1-2-7-13-11(4-1)5-3-6-12(13)10-14-15-8-9-16-14/h1-7H,8-10H2,(H,15,16)
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = CNIIGCLFLJGOGP-UHFFFAOYSA-N
}}
 
 
 
 
<!--Mechanism of Action-->
|mechAction=* Naphazoline constricts the vascular system of the conjunctiva. It is presumed that this effect is due to direct stimulation of the drug upon the alpha adrenergic receptors in the arterioles of the conjunctiva resulting in decreased conjunctival congestion. Naphazoline belongs to the imidazoline class of sympathomimetics.
 
<!--Structure-->
|structure=* Naphazoline Hydrochloride, an ocular vasoconstrictor, is an imidazoline derivative sympathomimetic amine. It occurs as a white, odorless crystalline powder having a bitter taste and is freely soluble in water and in alcohol. The active ingredient is represented by the structural formula:
 
: [[File:Naphazolin Str.png|thumb|none|500px|This image is provided by the National Library of Medicine.]]
 
* Chemical Name:
 
: 2-(1-naphthylmethyl)-2-imidazole monohydrochloride
 
* Each mL contains:
 
: Active: Naphazoline Hydrochloride 1 mg (0.1%).
 
: Inactives: Boric Acid, Edetate Disodium, Sodium Carbonate, Sodium Chloride and Hydrochloric Acid may be added to adjust pH (5.5 to 7.0), and Purified Water USP.
 
: Preservative: Benzalkonium Chloride 0.1 mg (0.01%). Naphazoline Hydrochloride Ophthalmic Solution, USP, 0.1% is a sterile solution with a pH between 5.5 and 7.0.
 
<!--Pharmacodynamics-->
|PD=There is limited information regarding <i>Pharmacodynamics</i> of {{PAGENAME}} in the drug label.
 
<!--Pharmacokinetics-->
|PK=There is limited information regarding <i>Pharmacokinetics</i> of {{PAGENAME}} in the drug label.
 
<!--Nonclinical Toxicology-->
|nonClinToxic=There is limited information regarding <i>Nonclinical Toxicology</i> of {{PAGENAME}} in the drug label.
 
<!--Clinical Studies-->
|clinicalStudies=There is limited information regarding <i>Clinical Studies</i> of {{PAGENAME}} in the drug label.
 
<!--How Supplied-->
|howSupplied=* Naphazoline Hydrochloride Ophthalmic Solution, USP, is supplied as a sterile 0.1% solution in 15 mL plastic dropper bottles.
 
: 15mL dropper bottle - 68788-0446-1
|storage=* Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature].
 
Keep container tightly closed.
|packLabel=====PRINCIPAL DISPLAY PANEL====
 
Principal Display Panel Text for Container Label:
 
Naphazoline Hydrochloride Ophthalmic Solution, USP 0.1%
 
15 mL
 
Sterile
 
Rx only
 
: [[File:Naphazolin PDP.png|thumb|none|500px|This image is provided by the National Library of Medicine.]]
 
====Ingredients and Appearance====
 
: [[File:Naphazolin Ing and App.png|thumb|none|600px|This image is provided by the National Library of Medicine.]]
 
<!--Patient Counseling Information-->
|fdaPatientInfo=* Patients should be advised to discontinue the drug and consult the physician if relief is not obtained within 48 hours of therapy, if irritation, blurring or redness persists or increases, or if symptoms of systemic absorption occur, i.e., dizziness, headache, nausea, decrease in body temperature, or drowsiness.
 
* To prevent contaminating the dropper tip and solution, do not touch any surface, the eyelids or the surrounding area with the dropper tip of the bottle. If solution changes color or becomes cloudy, do not use.
 
<!--Precautions with Alcohol-->
|alcohol=* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
 
<!--Brand Names-->
|brandNames=* AK-Con®<ref>{{Cite web | title = Naphazoline | url = http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8d353143-cd29-4a5f-9d67-293a6322e088}}</ref>
 
<!--Look-Alike Drug Names-->
|lookAlike=<!--Drug Shortage Status-->
|drugShortage=
}}
}}
{{CMG}}
<!--Pill Image-->


{{EH}}


==Overview==
'''Naphazoline''' (in the hydrochloride form) is the common name for 2-(1-Naphthylmethyl)-2-imidazoline hydrochloride, It is a [[sympathomimetic]] agent with marked alpha adrenergic activity. It is a [[vasoconstrictor]]  with a rapid action in reducing swelling when applied to mucous membrane. It acts on alpha-receptors in the [[arterioles]] of the [[conjunctiva]] to produce constriction, resulting in decreased congestion. It is an active ingredient in [[Naphcon-A]] and Clearine eye drops.
It has the molecular formula C<sub>14</sub>H<sub>14</sub>N<sub>2</sub>.HCl and a molecular weight of 246.73 g/mol.


==Warnings and contraindications==
<!--Label Display Image-->


These apply to all naphazoline-containing substances intended for medicinal use. A few warnings and [[contraindications]] are:-


1.Hypersensitivity to Naphazoline.<br />
2.Patients taking MAO inhibitors can experience a severe hypertensive (see [[hypertension]]) crisis if given a [[sympathomimetic]] drug such as naphazoline HCl.<br />
3.Use in infants and children can result in CNS depression, leading to coma and marked reduction in body temperature.<br />
4.Should be used with caution in patients with severe [[cardiovascular disease]] including [[cardiac arrythmia]] and in patients with [[diabetes]], especially those with a tendency toward diabetic [[ketoacidosis]].<br />
5 Drug interactions can occur with [[anaesthetics]] that sensitize the [[myocardium]] to sympathomimetics (e.g [[cyclopropane]] or [[halothane]] cautiously.<br />
6.Exercise caution when applying prior to use of [[phenylephrine]].


[[Category:Decongestants]]
[[Category:Imidazolines]]


{{Nasal preparations}}
<br>
[[ja:塩酸ナファゾリン]]
[[ru:Нафтизин]]
{{SIB}}


{{WH}}
<!--Category-->


{{WikiDoc Sources}}
[[Category:Drug]]

Latest revision as of 14:32, 25 February 2015

Naphazoline
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: Rabin Bista, M.B.B.S. [2]

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.

Overview

Naphazoline is a Alpha-Adrenergic Agonist that is FDA approved for the treatment of as a topical ocular vasoconstrictor. Common adverse reactions include Mydriasis, increased redness, increased intraocular pressure, irritation.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Indication

Dosage

  • Instill one or two drops in the conjunctival sac(s) every three to four hours as needed.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

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

Non–Guideline-Supported Use

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

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

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

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

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

Non–Guideline-Supported Use

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

Contraindications

  • Contraindicated in the presence of an anatomically narrow angle or in narrow angle glaucoma or in persons who have shown hypersensitivity to any component of this preparation.

Warnings

  • Patients under therapy with MAO inhibitors may experience a severe hypertensive crisis if given a sympathomimetic drug. Use in children, especially infants, may result in CNS depression leading to coma and marked reduction in body temperature.

Precautions

Adverse Reactions

Clinical Trials Experience

Ocular
Systemic

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Naphazoline in the drug label.

Drug Interactions

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): C

  • Animal reproduction studies have not been conducted with naphazoline. It is also not known whether naphazoline can cause harm when administered to a pregnant women or can affect reproduction capacity. Naphazoline should be given to a pregnant women only if clearly needed.


Pregnancy Category (AUS):

  • Australian Drug Evaluation Committee (ADEC) Pregnancy Category

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

Labor and Delivery

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

Nursing Mothers

  • It is not known whether naphazoline is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when naphazoline is administered to a nursing women.

Pediatric Use

  • Safety and effectiveness in the pediatric population have not been established

Geriatic Use

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

Gender

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

Race

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

Renal Impairment

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

Hepatic Impairment

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

Females of Reproductive Potential and Males

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

Immunocompromised Patients

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

Administration and Monitoring

Administration

  • Instill one or two drops in the conjunctival sac(s) every three to four hours as needed.

Monitoring

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

  • Description

IV Compatibility

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

Overdosage

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

Pharmacology

Template:Px
Template:Px
Naphazoline
Systematic (IUPAC) name
2-(naphthalen-1-ylmethyl)-4,5-dihydro-1H-imidazole
Identifiers
CAS number 835-31-4
ATC code R01AA08 S01GA01 (WHO)
PubChem 4436
DrugBank DB06711
Chemical data
Formula Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox 
Mol. mass 210.274
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability ?
Metabolism ?
Half life ?
Excretion ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes Topical

Mechanism of Action

  • Naphazoline constricts the vascular system of the conjunctiva. It is presumed that this effect is due to direct stimulation of the drug upon the alpha adrenergic receptors in the arterioles of the conjunctiva resulting in decreased conjunctival congestion. Naphazoline belongs to the imidazoline class of sympathomimetics.

Structure

  • Naphazoline Hydrochloride, an ocular vasoconstrictor, is an imidazoline derivative sympathomimetic amine. It occurs as a white, odorless crystalline powder having a bitter taste and is freely soluble in water and in alcohol. The active ingredient is represented by the structural formula:
This image is provided by the National Library of Medicine.
  • Chemical Name:
2-(1-naphthylmethyl)-2-imidazole monohydrochloride
  • Each mL contains:
Active: Naphazoline Hydrochloride 1 mg (0.1%).
Inactives: Boric Acid, Edetate Disodium, Sodium Carbonate, Sodium Chloride and Hydrochloric Acid may be added to adjust pH (5.5 to 7.0), and Purified Water USP.
Preservative: Benzalkonium Chloride 0.1 mg (0.01%). Naphazoline Hydrochloride Ophthalmic Solution, USP, 0.1% is a sterile solution with a pH between 5.5 and 7.0.

Pharmacodynamics

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

Pharmacokinetics

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

Nonclinical Toxicology

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

Clinical Studies

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

How Supplied

  • Naphazoline Hydrochloride Ophthalmic Solution, USP, is supplied as a sterile 0.1% solution in 15 mL plastic dropper bottles.
15mL dropper bottle - 68788-0446-1

Storage

  • Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature].

Keep container tightly closed.

Images

Drug Images

{{#ask: Page Name::Naphazoline |?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

PRINCIPAL DISPLAY PANEL

Principal Display Panel Text for Container Label:

Naphazoline Hydrochloride Ophthalmic Solution, USP 0.1%

15 mL

Sterile

Rx only

This image is provided by the National Library of Medicine.

Ingredients and Appearance

This image is provided by the National Library of Medicine.

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

Patient Counseling Information

  • Patients should be advised to discontinue the drug and consult the physician if relief is not obtained within 48 hours of therapy, if irritation, blurring or redness persists or increases, or if symptoms of systemic absorption occur, i.e., dizziness, headache, nausea, decrease in body temperature, or drowsiness.
  • To prevent contaminating the dropper tip and solution, do not touch any surface, the eyelids or the surrounding area with the dropper tip of the bottle. If solution changes color or becomes cloudy, do not use.

Precautions with Alcohol

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

Brand Names

Look-Alike Drug Names

There is limited information regarding Naphazoline Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

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

  1. ↑ "Naphazoline".
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