Azelastine (ophthalmic)

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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]

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Overview

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Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Indications

For the treatment of itching 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 Azelastine (ophthalmic) Drug Interactions 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

  • Oral
  • Intravenous

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

Acute Overdose

Signs and Symptoms

  • Description

Management

  • Description

Chronic Overdose

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

Structure

File:Azelastine (ophthalmic)01.png
This image is provided by the National Library of Medicine.

Pharmacodynamics

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

Pharmacokinetics

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

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

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Package and Label Display Panel

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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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