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Azelastine (ophthalmic): Drug information

Azelastine (ophthalmic): Drug information
(For additional information see "Azelastine (ophthalmic): Patient drug information" and see "Azelastine (ophthalmic): Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Pharmacologic Category
  • Histamine H1 Antagonist;
  • Histamine H1 Antagonist, Second Generation
Dosing: Adult
Allergic conjunctivitis

Allergic conjunctivitis: Ophthalmic: Instill 1 drop into affected eye(s) twice daily.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Pediatric

(For additional information see "Azelastine (ophthalmic): Pediatric drug information")

Seasonal allergic conjunctivitis

Seasonal allergic conjunctivitis: Children ≥3 years and Adolescents: Ophthalmic: Instill 1 drop into affected eye(s) twice daily

Dosing: Kidney Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling; however, dosage adjustment unlikely needed due to low systemic absorption.

Dosing: Hepatic Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling; however, dosage adjustment unlikely needed due to low systemic absorption.

Dosing: Older Adult

Refer to adult dosing.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Ophthalmic, as hydrochloride:

Generic: 0.05% (6 mL)

Generic Equivalent Available: US

Yes

Administration: Adult

For topical ophthalmic use only. Wash hands prior to use. Do not touch tip of container to any surface, the eyelids, or surrounding areas. After instilling drops, wait at least 10 minutes before inserting contact lenses. Do not insert contacts if eyes are red.

Administration: Pediatric

For topical ophthalmic use only. Do not allow the bottle tip to touch any surface, the eyelids, or surrounding areas. Apply gentle pressure to lacrimal sac during and immediately following instillation (1 minute) or instruct patient to gently close eyelid after administration, to decrease systemic absorption of ophthalmic drops (Urtti 1993; Zimmerman 1984). Patients should not wear contact lenses if their eye is red. For contact lens users whose eyes are not red, wait at least 10 minutes after instilling medication to insert contact lenses.

Use: Labeled Indications

Allergic conjunctivitis: Treatment of itching of the eye associated with allergic conjunctivitis

Medication Safety Issues
Sound-alike/look-alike issues:

Optivar may be confused with Optiray, Optive

International issues:

Optivar [US] may be confused with Opthavir brand name for acyclovir [Mexico]

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%:

Central nervous system: Headache (15%)

Ocular: Transient burning/stinging (30%)

1% to 10%:

Central nervous system: Fatigue

Dermatologic: Pruritus

Gastrointestinal: Bitter taste (10%)

Ocular: Conjunctivitis, eye pain, blurred vision (temporary)

Respiratory: Asthma, dyspnea, pharyngitis, rhinitis

Miscellaneous: Flu-like syndrome

Contraindications

Hypersensitivity to azelastine or any component of the formulation

Warnings/Precautions

Dosage form specific issues:

• Solution contains benzalkonium chloride; remove lens prior to administration and wait at least 10 minutes before reinserting. Do not use contact lenses if eyes are red.

Metabolism/Transport Effects

None known.

Drug Interactions

There are no known significant interactions.

Pregnancy Considerations

Animal reproduction studies have shown toxic effects to the fetus at maternally toxic doses.

Breastfeeding Considerations

It is not known if azelastine (ophthalmic) is excreted in breast milk. The manufacturer recommends that caution be exercised when administering azelastine (ophthalmic) to nursing women.

Mechanism of Action

Competes with histamine for H1-receptor sites on effector cells and inhibits the release of histamine and other mediators involved in the allergic response

Pharmacokinetics

Onset of action: Peak effect: 3 minutes

Duration: 8 hours

Absorption: Plasma concentrations following ocular administration are low for azelastine (0.02-0.25 ng/mL) and n-desmethylazelastine (0.25-0.87 ng/mL)

Pricing: US

Solution (Azelastine HCl Ophthalmic)

0.05% (per mL): $1.80 - $17.35

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Brand Names: International
  • Afluon (ES);
  • Alager (AR);
  • Alergot (VE);
  • Allergodil (AR, AT, BE, CH, CZ, DE, DK, EE, FR, HR, IT, LT, LU, NL, PT, RO, RU, SK, UA);
  • Az Ofteno (CL, CR, DO, GT, HN, NI, PA, SV, VE);
  • Azel (CO);
  • Azela-Vision (AT);
  • Azelan (KR);
  • Azep Eye Drops (HK);
  • Brixia (AR, CL, PY, UY);
  • Eyezep (AU, KR);
  • Itapleno (MX);
  • Laasticom (IT);
  • Lastin (FI, SE);
  • New Azelan (VN);
  • Oculast (IN);
  • Opthazel (PE);
  • Optilast (IL, UA);
  • Rapilastin (EG);
  • Xanaes (AR)


For country code abbreviations (show table)
  1. Azelastine hydrochloride [prescribing information]. Somerset, NJ: Somerset Therapeutics, LLC; April 2019.
  2. Urtti A, Salminen L. Minimizing systemic absorption of topically administered ophthalmic drugs. Surv Ophthalmol. 1993;37(6):435-456. [PubMed 8100087]
  3. Zimmerman TJ, Kooner KS, Kandarakis AS, Ziegler LP. Improving the therapeutic index of topically applied ocular drugs. Arch Ophthalmol. 1984;102(4):551-553. [PubMed 6704011]
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