Azelastine Ophthalmic Solution

Name: Azelastine Ophthalmic Solution

Azelastine Ophthalmic Solution - Clinical Pharmacology


Azelastine hydrochloride is a relatively selective histamine H1 antagonist and an inhibitor of the release of histamine and other mediators from cells (e.g., mast cells) involved in the allergic response. Based on in-vitro studies using human cell lines, inhibition of other mediators involved in allergic reactions (e.g., leukotrienes and PAF) has been demonstrated with azelastine hydrochloride. Decreased chemotaxis and activation of eosinophils has also been demonstrated.

Pharmacokinetics and Metabolism


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 to 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.

Clinical Trials


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.

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.

Package label.principal display panel - carton

NDC 47335-938-90
Azelastine Hydrochloride Ophthalmic Solution, 0.05%
6 mL - Sterile
For the Eye Only
Rx only
SUN PHARMA


AZELASTINE HYDROCHLORIDE 
azelastine hydrochloride solution/ drops
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:47335-938
Route of Administration INTRAOCULAR DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
AZELASTINE HYDROCHLORIDE (AZELASTINE) AZELASTINE HYDROCHLORIDE 0.5 mg  in 1 mL
Inactive Ingredients
Ingredient Name Strength
BENZALKONIUM CHLORIDE  
EDETATE DISODIUM  
HYPROMELLOSES  
SORBITOL  
SODIUM HYDROXIDE  
WATER  
Packaging
# Item Code Package Description
1 NDC:47335-938-90 1 BOTTLE, PLASTIC in 1 BOX
1 6 mL in 1 BOTTLE, PLASTIC
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA078738 05/31/2010
Labeler - Sun Pharma Global FZE (864347344)
Establishment
Name Address ID/FEI Operations
Sun Pharmaceutical Industries Limited 725959238 ANALYSIS(47335-938), MANUFACTURE(47335-938)
Revised: 07/2017   Sun Pharma Global FZE

Azelastine Side Effects

More Common Side Effects

The more common side effects of azelastine eye drops can include:

  • burning or stinging in the eye(s)

  • headache

  • bitter taste in the mouth

If these effects are mild, they may go away within a few days or a couple of weeks. If they’re more severe or don’t go away, talk to your doctor or pharmacist.

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this information includes all possible side effects. This information is not a substitute for medical advice. Always discuss possible side effects with a healthcare provider who knows your medical history.

How to Take azelastine (Dosage)

What are you taking this medication for?

Allergic conjunctivitis (eye allergies)

Generic: azelastine eye drops

Form: Ophthalmic solution 0.5% Adult dosage (ages 18 years years and older)

Typical dosage: One drop of 0.05% eye drops in each affected eye, 2 times per day.

Child dosage (ages 3–17 years)

Typical dosage: One drop of 0.05% eye drops in each affected eye, 2 times per day.

Child dosage (ages 0–2 years)

It hasn’t been confirmed that azelastine eye drops are safe and effective for use in people younger than 3 years.

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this list includes all possible dosages. This information is not a substitute for medical advice. Always to speak with your doctor or pharmacist about dosages that are right for you. Important considerations for taking azelastine

Take this drug at the time(s) recommended by your doctor

Store this drug carefully

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A prescription for this medication is refillable

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Travel

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Self-management

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Not every pharmacy stocks this drug. When filling your prescription, be sure to call ahead.

Are there any alternatives?

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