Azelastine (ophthalmic): Difference between revisions

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|genericName=azelastine hydrochloride
|genericName=azelastine hydrochloride
|aOrAn=a
|aOrAn=a
|drugClass=ophthalmologic agent
|indicationType=treatment
|indicationType=treatment
|adverseReactions=<!--Black Box Warning-->
|indication=[[allergy|allergic]] [[conjunctivitis]]
|adverseReactions=[[asthma]], [[conjunctivitis]], [[dyspnea]], [[eye pain]], [[fatigue]], [[influenza-like symptoms]], [[pharyngitis]], [[pruritus]], [[rhinitis]], [[burning]], [[stinging]], and [[headache]]
|blackBoxWarningTitle=<span style="color:#FF0000;">ConditionName: </span>
|blackBoxWarningTitle=<span style="color:#FF0000;">ConditionName: </span>
|blackBoxWarningBody=<i><span style="color:#FF0000;">ConditionName: </span></i>
|blackBoxWarningBody=<i><span style="color:#FF0000;">ConditionName: </span></i>
Line 13: Line 15:


<!--FDA-Labeled Indications and Dosage (Adult)-->
<!--FDA-Labeled Indications and Dosage (Adult)-->
|fdaLIADAdult===Indications==
|fdaLIADAdult=====Indications====
For the treatment of [[itch|itching]] of the eye associated with allergic [[conjunctivitis]].
For the treatment of [[itch]] of the eye associated with [[allergy|allergic]] [[conjunctivitis]].


==Dosage==
====Dosage====


* The recommended dose is one drop instilled into each affected eye twice a day.
The recommended dose is one drop instilled into each affected eye twice a day.
|offLabelAdultGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.
|offLabelAdultGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.
|offLabelAdultNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.
|offLabelAdultNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.


<!--FDA-Labeled Indications and Dosage (Pediatric)-->
<!--FDA-Labeled Indications and Dosage (Pediatric)-->
|fdaLIADPed=There is limited information regarding <i>FDA-Labeled Use</i> of {{PAGENAME}} in pediatric patients.
|fdaLIADPed=There is limited information regarding <i>FDA-Labeled Use</i> of {{PAGENAME}} in pediatric patients.
|offLabelPedGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
|offLabelPedGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
|offLabelPedNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
|offLabelPedNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
|contraindications=* Azelastine hydrochloride ophthalmic solution is contraindicated in persons with known or suspected [[hypersensitivity]] to any of its components.
|contraindications=* Azelastine hydrochloride ophthalmic solution is contraindicated in persons with known or suspected [[hypersensitivity]] to any of its components.
|warnings=* Azelastine hydrochloride ophthalmic solution is for ocular use only and not for injection or oral use.
|warnings=* Azelastine hydrochloride ophthalmic solution is for ocular use only and not for injection or oral use.
|clinicalTrials=There is limited information regarding <i>Clinical Trial Experience</i> of {{PAGENAME}} in the drug label.
|clinicalTrials=* In controlled multiple-dose studies where patients were treated for up to 56 days, the most frequently reported adverse reactions were transient eye [[burning]]/[[stinging]] (approximately 30%), headaches (approximately 15%) and bitter taste (approximately 10%). The occurrence of these events was generally mild.
 


* The following events were reported in 1 - 10% of patients: [[asthma]], [[conjunctivitis]], [[dyspnea]], [[eye pain]], [[fatigue]], [[influenza-like symptoms]], [[pharyngitis]], [[pruritus]], [[rhinitis]] and temporary blurring. Some of these events were similar to the underlying disease being studied.
|postmarketing=There is limited information regarding <i>Postmarketing Experience</i> of {{PAGENAME}} in the drug label.
|postmarketing=There is limited information regarding <i>Postmarketing Experience</i> of {{PAGENAME}} in the drug label.
|drugInteractions=There is limited information regarding <i>Drug Interactions</i> of {{PAGENAME}} in the drug label.
|useInPregnancyFDA='''Teratogenic Effects: Pregnancy Category C'''.


* Azelastine hydrochloride has been shown to be embryotoxic, fetotoxic, and teratogenic (external and skeletal abnormalities) in mice at an oral dose of 68.6 mg/kg/day (57,000 times the recommended ocular human use level). At an oral dose of 30 mg/kg/day (25,000 times the recommended ocular human use level), delayed ossification (undeveloped metacarpus), and the incidence of 14th rib were increased in rats. At 68.6 mg/kg/day (57,000 times the maximum recommended ocular human use level) azelastine hydrochloride caused resorption and fetotoxic effects in rats. The relevance to humans of these skeletal findings noted at only high drug exposure levels in unknown.


 
* There are no adequate and well-controlled studies in pregnant women. Azelastine hydrochloride ophthalmic solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
 
 
 
|useInPregnancyAUS=* '''Australian Drug Evaluation Committee (ADEC) Pregnancy Category'''
|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.
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.
|useInLaborDelivery=There is no FDA guidance on use of {{PAGENAME}} during labor and delivery.
|useInNursing=There is no FDA guidance on the use of {{PAGENAME}} with respect to nursing mothers.
|useInNursing=* It is not known whether azelastine hydrochloride is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when azelastine hydrochloride ophthalmic solution is administered to a nursing woman.
|useInPed=There is no FDA guidance on the use of {{PAGENAME}} with respect to pediatric patients.
|useInPed=* Safety and effectiveness in pediatric patients below the age of 3 years have not been established.
|useInGeri=There is no FDA guidance on the use of {{PAGENAME}} with respect to geriatric patients.
|useInGeri=* No overall differences in safety or effectiveness have been observed between elderly and younger adult patients.
|useInGender=There is no FDA guidance on the use of {{PAGENAME}} with respect to specific gender populations.
|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.
|useInRace=There is no FDA guidance on the use of {{PAGENAME}} with respect to specific racial populations.
Line 62: Line 53:
|useInReproPotential=There is no FDA guidance on the use of {{PAGENAME}} in women of reproductive potentials and males.
|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.
|useInImmunocomp=There is no FDA guidance one the use of {{PAGENAME}} in patients who are immunocompromised.
 
|administration=* Ophthalmologic
<!--Administration and Monitoring-->
|administration=* Oral
 
* Intravenous
|monitoring=There is limited information regarding <i>Monitoring</i> of {{PAGENAME}} in the drug label.
|monitoring=There is limited information regarding <i>Monitoring</i> of {{PAGENAME}} in the drug label.
|IVCompat=There is limited information regarding <i>IV Compatibility</i> of {{PAGENAME}} in the drug label.
|IVCompat=There is limited information regarding <i>IV Compatibility</i> of {{PAGENAME}} in the drug label.
 
|overdose=There is limited information regarding <i>Chronic Overdose</i> of {{PAGENAME}} in the drug label.
 
|overdose====Acute Overdose===
 
====Signs and Symptoms====
 
* Description
 
====Management====
 
* Description
 
===Chronic Overdose===
 
There is limited information regarding <i>Chronic Overdose</i> of {{PAGENAME}} in the drug label.
 
<!--Pharmacology-->
 
<!--Drug box 2-->
|drugBox={{Drugbox2
|drugBox={{Drugbox2
| verifiedrevid = 458613328
| verifiedrevid = 458613328
Line 137: Line 106:
| StdInChIKey = MBUVEWMHONZEQD-UHFFFAOYSA-N
| StdInChIKey = MBUVEWMHONZEQD-UHFFFAOYSA-N
}}
}}
|mechAction=*
|structure=Azelastine Hydrochloride Ophthalmic Solution, 0.05% is a sterile ophthalmic solution containing azelastine hydrochloride, a relatively selective H1-receptor antagonist for topical administration to the eyes. Azelastine hydrochloride is a white crystalline powder with a molecular weight of 418.37. Azelastine hydrochloride is sparingly soluble in water, methanol and propylene glycol, and slightly soluble in ethanol, octanol, and glycerine. Azelastine hydrochloride is a racemic mixture with a melting point of 225°C. The chemical name for azelastine hydrochloride is (±)-1-(2H)-phthalazinone,4-[(4-chlorophenyl) methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-, monohydrochloride and is represented by the following chemical structure:


<!--Structure-->
[[File:Azelastine ophthalmic structure.png|thumb|none|600px|This image is provided by the National Library of Medicine.]]
|structure=*


: [[File:{{PAGENAME}}01.png|thumb|none|600px|This image is provided by the National Library of Medicine.]]
* Each mL of azelastine hydrochloride ophthalmic solution contains: Active: 0.5 mg azelastine hydrochloride, equivalent to 0.457 mg of azelastine base; Preservative: 0.125 mg benzalkonium chloride; Inactives: disodium edetate dihydrate, hydroxypropylmethylcellulose, sodium hydroxide, sorbitol solution and water for injection. It has a pH of approximately 5.0 to 6.5 and an osmolality of approximately 271 to 312 mOsmol/L.
|PD=There is limited information regarding <i>Pharmacodynamics</i> of {{PAGENAME}} in the drug label.
|PK=* Absorption of azelastine following ocular administration was relatively low. A study in symptomatic patients receiving one drop of azelastine hydrochloride ophthalmic solution in each eye two to four times a day (0.06 to 0.12 mg azelastine hydrochloride) demonstrated plasma concentrations of azelastine hydrochloride to generally be between 0.02 and 0.25 ng/mL after 56 days of treatment. Three of nineteen patients had quantifiable amounts of N-desmethylazelastine that ranged from 0.25 - 0.87 ng/mL at Day 56.


<!--Pharmacodynamics-->
* Based on intravenous and oral administration, the elimination half-life, steady-state volume of distribution and plasma clearance were 22 hours, 14.5 L/kg and 0.5 L/h/kg, respectively. Approximately 75% of an oral dose of radiolabeled azelastine hydrochloride was excreted in the feces with less than 10% as unchanged azelastine. Azelastine hydrochloride is oxidatively metabolized to the principal metabolite, N-desmethylazelastine, by the cytochrome P450 enzyme system. In vitro studies in human plasma indicate that the plasma protein binding of azelastine and N-desmethylazelastine are approximately 88% and 97% respectively.
|PD=There is limited information regarding <i>Pharmacodynamics</i> of {{PAGENAME}} in the drug label.
|nonClinToxic='''Carcinogenesis, Mutagenesis, Impairment of Fertility'''


<!--Pharmacokinetics-->
* Azelastine hydrochloride administered orally for 24 months was not carcinogenic in rats and mice at doses up to 30 mg/kg/day and 25 mg/kg/day, respectively. Based on a 30 µL drop size, these doses were approximately 25,000 and 21,000 times higher than the maximum recommended ocular human use level of 0.001 mg/kg/day for a 50 kg adult.
|PK=There is limited information regarding <i>Pharmacokinetics</i> of {{PAGENAME}} in the drug label.


<!--Nonclinical Toxicology-->
* Azelastine hydrochloride showed no genotoxic effects in the Ames test, DNA repair test, mouse lymphoma forward mutation assay, mouse micronucleus test, or chromosomal aberration test in rat bone marrow. Reproduction and fertility studies in rats showed no effects on male or female fertility at oral doses of up to 25,000 times the maximum recommended ocular human use level. At 68.6 mg/kg/day (57,000 times the maximum recommended ocular human use level), the duration of the estrous cycle was prolonged and copulatory activity and the number of pregnancies were decreased. The numbers of corpora lutea and implantations were decreased; however, the implantation ratio was not affected.
|nonClinToxic=There is limited information regarding <i>Nonclinical Toxicology</i> of {{PAGENAME}} in the drug label.
|clinicalStudies=* In a conjunctival antigen challenge study, azelastine hydrochloride ophthalmic solution was more effective than its vehicle in preventing itching associated with allergic conjunctivitis. Azelastine hydrochloride ophthalmic solution had a rapid (within 3 minutes) onset of effect and a duration of effect of approximately 8 hours for the prevention of itching.


<!--Clinical Studies-->
* In environmental studies, adult and pediatric, patients with seasonal allergic conjunctivitis were treated with azelastine hydrochloride ophthalmic solution for two to eight weeks. In these studies, azelastine hydrochloride ophthalmic solution was more effective than its vehicle in relieving itching associated with allergic [[conjunctivitis]].
|clinicalStudies=There is limited information regarding <i>Clinical Studies</i> of {{PAGENAME}} in the drug label.
|howSupplied=* Azelastine Hydrochloride Ophthalmic Solution, 0.05% is supplied as follows: 6 mL (NDC# 60505-0578-4) solution in a translucent 11 mL HDPE container with a LDPE dropper tip, and a white HDPE screw cap.
|howSupplied=* Azelastine Hydrochloride Ophthalmic Solution, 0.05% is supplied as follows: 6 mL (NDC# 60505-0578-4) solution in a translucent 11 mL HDPE container with a LDPE dropper tip, and a white HDPE screw cap.
|storage=* Store UPRIGHT at 20º-25ºC (68º-77ºF).
|storage=* Store UPRIGHT at 20º-25ºC (68º-77ºF).
|packLabel=<!--Patient Counseling Information-->
|packLabel=[[File:Azelastine ophthalmic image.jpg|thumb|none|600px|This image is provided by the National Library of Medicine.]]
|fdaPatientInfo=There is limited information regarding <i>Patient Counseling Information</i> of {{PAGENAME}} in the drug label.
 
[[File:Azelastine ophthalmic ingredients and appearance.png|thumb|none|600px|This image is provided by the National Library of Medicine.]]
|fdaPatientInfo='''Information for Patients'''


* To prevent contaminating the dropper tip and solution, care should be taken not to touch any surface, the eyelids, or surrounding areas with the dropper tip of the bottle. Keep bottle tightly closed when not in use. This product is sterile when packaged.


* Patients should be advised not to wear a contact lens if their eye is red. Azelastine hydrochloride ophthalmic solution should not be used to treat contact lens related irritation. The preservative in azelastine hydrochloride ophthalmic solution, benzalkonium chloride, may be absorbed by soft contact lenses. Patients who wear soft contact lenses and whose eyes are not red, should be instructed to wait at least ten minutes after instilling azelastine hydrochloride ophthalmic solution before they insert their contact lenses.
|alcohol=* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
|alcohol=* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
|brandNames=* AZELASTINE HYDROCHLORIDE®<ref>{{Cite web | title=azelastine hydrochloride solution/ drops|url =http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=77a33738-ffcf-221c-1562-780418882e5d }}</ref>
|brandNames=* AZELASTINE HYDROCHLORIDE®<ref>{{Cite web | title=azelastine hydrochloride solution/ drops|url =http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=77a33738-ffcf-221c-1562-780418882e5d }}</ref>
|lookAlike=* A® — B®<ref name="www.ismp.org">{{Cite web  | last =  | first =  | title = http://www.ismp.org | url = http://www.ismp.org | publisher =  | date =  }}</ref>
|lookAlike=* A® — B®<ref name="www.ismp.org">{{Cite web  | last =  | first =  | title = http://www.ismp.org | url = http://www.ismp.org | publisher =  | date =  }}</ref>
<!--Drug Shortage Status-->
|drugShortage=
|drugShortage=
}}
}}

Latest revision as of 17:51, 18 August 2015

Azelastine (ophthalmic)
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: Kiran Singh, M.D. [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

Azelastine (ophthalmic) is a ophthalmologic agent that is FDA approved for the treatment of allergic conjunctivitis. Common adverse reactions include asthma, conjunctivitis, dyspnea, eye pain, fatigue, influenza-like symptoms, pharyngitis, pruritus, rhinitis, burning, stinging, and headache.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Indications

For the treatment of itch of the eye associated with allergic conjunctivitis.

Dosage

The recommended dose is one drop instilled into each affected eye twice a day.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Azelastine (ophthalmic) in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Azelastine (ophthalmic) in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding FDA-Labeled Use of Azelastine (ophthalmic) in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Azelastine (ophthalmic) in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Azelastine (ophthalmic) in pediatric patients.

Contraindications

  • Azelastine hydrochloride ophthalmic solution is contraindicated in persons with known or suspected hypersensitivity to any of its components.

Warnings

  • Azelastine hydrochloride ophthalmic solution is for ocular use only and not for injection or oral use.

Adverse Reactions

Clinical Trials Experience

  • In controlled multiple-dose studies where patients were treated for up to 56 days, the most frequently reported adverse reactions were transient eye burning/stinging (approximately 30%), headaches (approximately 15%) and bitter taste (approximately 10%). The occurrence of these events was generally mild.

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Azelastine (ophthalmic) in the drug label.

Drug Interactions

There is limited information regarding Drug Interactions of Azelastine (ophthalmic) in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): Teratogenic Effects: Pregnancy Category C.

  • Azelastine hydrochloride has been shown to be embryotoxic, fetotoxic, and teratogenic (external and skeletal abnormalities) in mice at an oral dose of 68.6 mg/kg/day (57,000 times the recommended ocular human use level). At an oral dose of 30 mg/kg/day (25,000 times the recommended ocular human use level), delayed ossification (undeveloped metacarpus), and the incidence of 14th rib were increased in rats. At 68.6 mg/kg/day (57,000 times the maximum recommended ocular human use level) azelastine hydrochloride caused resorption and fetotoxic effects in rats. The relevance to humans of these skeletal findings noted at only high drug exposure levels in unknown.
  • There are no adequate and well-controlled studies in pregnant women. Azelastine hydrochloride ophthalmic solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.


Pregnancy Category (AUS):

  • Australian Drug Evaluation Committee (ADEC) Pregnancy Category

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

Labor and Delivery

There is no FDA guidance on use of Azelastine (ophthalmic) during labor and delivery.

Nursing Mothers

  • It is not known whether azelastine hydrochloride is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when azelastine hydrochloride ophthalmic solution is administered to a nursing woman.

Pediatric Use

  • Safety and effectiveness in pediatric patients below the age of 3 years have not been established.

Geriatic Use

  • No overall differences in safety or effectiveness have been observed between elderly and younger adult patients.

Gender

There is no FDA guidance on the use of Azelastine (ophthalmic) with respect to specific gender populations.

Race

There is no FDA guidance on the use of Azelastine (ophthalmic) with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Azelastine (ophthalmic) in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Azelastine (ophthalmic) in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Azelastine (ophthalmic) in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Azelastine (ophthalmic) in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Ophthalmologic

Monitoring

There is limited information regarding Monitoring of Azelastine (ophthalmic) in the drug label.

IV Compatibility

There is limited information regarding IV Compatibility of Azelastine (ophthalmic) in the drug label.

Overdosage

There is limited information regarding Chronic Overdose of Azelastine (ophthalmic) in the drug label.

Pharmacology

Template:Px
Azelastine (ophthalmic)
Systematic (IUPAC) name
(RS)-4-[(4-chlorophenyl)methyl]-2- (1-methylazepan-4-yl)-phthalazin-1-one
Identifiers
CAS number 58581-89-8
ATC code R01AC03 R06AX19 (WHO), S01GX07 (WHO)
PubChem 2267
DrugBank DB00972
Chemical data
Formula Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox 
Mol. mass 381.898 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 40% (intranasal)
Metabolism ?
Half life 22 hours
Excretion ?
Therapeutic considerations
Pregnancy cat.

C(US)

Legal status

Rx Only (US)

Routes intranasal, ocular

Mechanism of Action

There is limited information regarding Azelastine (ophthalmic) Mechanism of Action in the drug label.

Structure

Azelastine Hydrochloride Ophthalmic Solution, 0.05% is a sterile ophthalmic solution containing azelastine hydrochloride, a relatively selective H1-receptor antagonist for topical administration to the eyes. Azelastine hydrochloride is a white crystalline powder with a molecular weight of 418.37. Azelastine hydrochloride is sparingly soluble in water, methanol and propylene glycol, and slightly soluble in ethanol, octanol, and glycerine. Azelastine hydrochloride is a racemic mixture with a melting point of 225°C. The chemical name for azelastine hydrochloride is (±)-1-(2H)-phthalazinone,4-[(4-chlorophenyl) methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-, monohydrochloride and is represented by the following chemical structure:

This image is provided by the National Library of Medicine.
  • Each mL of azelastine hydrochloride ophthalmic solution contains: Active: 0.5 mg azelastine hydrochloride, equivalent to 0.457 mg of azelastine base; Preservative: 0.125 mg benzalkonium chloride; Inactives: disodium edetate dihydrate, hydroxypropylmethylcellulose, sodium hydroxide, sorbitol solution and water for injection. It has a pH of approximately 5.0 to 6.5 and an osmolality of approximately 271 to 312 mOsmol/L.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Azelastine (ophthalmic) in the drug label.

Pharmacokinetics

  • Absorption of azelastine following ocular administration was relatively low. A study in symptomatic patients receiving one drop of azelastine hydrochloride ophthalmic solution in each eye two to four times a day (0.06 to 0.12 mg azelastine hydrochloride) demonstrated plasma concentrations of azelastine hydrochloride to generally be between 0.02 and 0.25 ng/mL after 56 days of treatment. Three of nineteen patients had quantifiable amounts of N-desmethylazelastine that ranged from 0.25 - 0.87 ng/mL at Day 56.
  • Based on intravenous and oral administration, the elimination half-life, steady-state volume of distribution and plasma clearance were 22 hours, 14.5 L/kg and 0.5 L/h/kg, respectively. Approximately 75% of an oral dose of radiolabeled azelastine hydrochloride was excreted in the feces with less than 10% as unchanged azelastine. Azelastine hydrochloride is oxidatively metabolized to the principal metabolite, N-desmethylazelastine, by the cytochrome P450 enzyme system. In vitro studies in human plasma indicate that the plasma protein binding of azelastine and N-desmethylazelastine are approximately 88% and 97% respectively.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

  • Azelastine hydrochloride administered orally for 24 months was not carcinogenic in rats and mice at doses up to 30 mg/kg/day and 25 mg/kg/day, respectively. Based on a 30 µL drop size, these doses were approximately 25,000 and 21,000 times higher than the maximum recommended ocular human use level of 0.001 mg/kg/day for a 50 kg adult.
  • Azelastine hydrochloride showed no genotoxic effects in the Ames test, DNA repair test, mouse lymphoma forward mutation assay, mouse micronucleus test, or chromosomal aberration test in rat bone marrow. Reproduction and fertility studies in rats showed no effects on male or female fertility at oral doses of up to 25,000 times the maximum recommended ocular human use level. At 68.6 mg/kg/day (57,000 times the maximum recommended ocular human use level), the duration of the estrous cycle was prolonged and copulatory activity and the number of pregnancies were decreased. The numbers of corpora lutea and implantations were decreased; however, the implantation ratio was not affected.

Clinical Studies

  • In a conjunctival antigen challenge study, azelastine hydrochloride ophthalmic solution was more effective than its vehicle in preventing itching associated with allergic conjunctivitis. Azelastine hydrochloride ophthalmic solution had a rapid (within 3 minutes) onset of effect and a duration of effect of approximately 8 hours for the prevention of itching.
  • In environmental studies, adult and pediatric, patients with seasonal allergic conjunctivitis were treated with azelastine hydrochloride ophthalmic solution for two to eight weeks. In these studies, azelastine hydrochloride ophthalmic solution was more effective than its vehicle in relieving itching associated with allergic conjunctivitis.

How Supplied

  • Azelastine Hydrochloride Ophthalmic Solution, 0.05% is supplied as follows: 6 mL (NDC# 60505-0578-4) solution in a translucent 11 mL HDPE container with a LDPE dropper tip, and a white HDPE screw cap.

Storage

  • Store UPRIGHT at 20º-25ºC (68º-77ºF).

Images

Drug Images

{{#ask: Page Name::Azelastine (ophthalmic) |?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

This image is provided by the National Library of Medicine.
This image is provided by the National Library of Medicine.

{{#ask: Label Page::Azelastine (ophthalmic) |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}

Patient Counseling Information

Information for Patients

  • To prevent contaminating the dropper tip and solution, care should be taken not to touch any surface, the eyelids, or surrounding areas with the dropper tip of the bottle. Keep bottle tightly closed when not in use. This product is sterile when packaged.
  • Patients should be advised not to wear a contact lens if their eye is red. Azelastine hydrochloride ophthalmic solution should not be used to treat contact lens related irritation. The preservative in azelastine hydrochloride ophthalmic solution, benzalkonium chloride, may be absorbed by soft contact lenses. Patients who wear soft contact lenses and whose eyes are not red, should be instructed to wait at least ten minutes after instilling azelastine hydrochloride ophthalmic solution before they insert their contact lenses.

Precautions with Alcohol

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

Brand Names

  • AZELASTINE HYDROCHLORIDE®[1]

Look-Alike Drug Names

Drug Shortage Status

Price

References

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

  1. ↑ "azelastine hydrochloride solution/ drops".
  2. ↑ "http://www.ismp.org". External link in |title= (help)

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