Azelastine Hcl (azelastine HCl)
Ophthalmic Antiallergic Agents Nasal Aerosol, Spray With Pump (Ml); Ophthalmic (Eye) Drops
Last reviewed · Source: First Databank (FDB) drug data
Overview
Azelastine is a histamine H1-receptor antagonist.
Azelastine is a histamine H1-receptor antagonist. Azelastine, a phthalazinone derivative, is structurally unrelated to other currently available antihistamines and has been characterized a selective H1-receptor antagonist. Although azelastine has been referred to as a second generation (''nonsedating'') antihistamine, adverse CNS effects (e.g., drowsiness) may occur with the drug, particularly at relatively high doses or when administered with CNS depressants (e.g., alcohol).
The desmethyl metabolite also possesses antihistaminic activity. In addition, azelastine inhibits other mediators (e.g., leukotrienes, platelet activating factor (PAF)) involved in allergic reactions. Azelastine may inhibit the accumulation of eosinophils at the site of allergic inflammation and prevent eosinophil degranulation.
Azelastine currently is commercially available in the US as azelastine hydrochloride nasal spray preparation, having a pH of approximately 6.8. When administered intranasally, approximately 40% of a dose reaches systemic circulation.
Azelastine also is commercially available as azelastine hydrochloride ophthalmic solution. Azelastine hydrochloride ophthalmic solution is a sterile solution of the drug in water for injection; the solution contains benzalkonium chloride as a preservative and also contains edetate disodium, hydroxypropyl methylcellulose, sorbitol, and sodium hydroxide. Azelastine hydrochloride ophthalmic solution has a pH of approximately 5-6.5 and an osmolarity of approximately 271-312 mOsml/L.
The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer's labeling should be consulted for more detailed information.
The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.
USES: This medication is used to treat itching eyes caused by allergies (allergic conjunctivitis). Azelastine belongs to a class of drugs known as antihistamines. It works by blocking certain natural substances called histamines that are responsible for allergic symptoms.
Do not use this medication to treat redness and irritation due to wearing contact lenses.
Generic name: azelastine HCl
Pronunciation: (AY-ze-LAS-teen)
Drug class: Ophthalmic Antiallergic Agents
Therapeutic class: Respiratory Therapy Agents
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Azelastine Hcl
Indications
The following indications are listed for Azelastine Hcl:
- Allergic Conjunctivitis
Also known as: Allergy Eye Itch, Atopic Conjunctivitis, Itchy Eyes Due To Allergies, Ocular Itching Due To Allergies.
Dosing
The manufacturer preferentially labels the dosage and concentration of azelastine hydrochloride in terms of the hydrochloride salt.
No dosing information is available for this tab.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Azelastine Hcl 0.05% Drops | Maintenance | Instill 1 drop into affected eye(s) by ophthalmic route 2 times per day. |
| Azelastine 0.1% (137 Mcg) Spry | Maintenance | Spray 2 sprays (274 mcg) in each nostril by intranasal route 2 times per day. |
| Drug label | Dosing type | Instructions |
|---|---|---|
| Azelastine 0.1% (137 Mcg) Spry | Maintenance | Spray 2 sprays (274 mcg) in each nostril by intranasal route 2 times per day. |
| Azelastine Hcl 0.05% Drops | Maintenance | Instill 1 drop into affected eye(s) by ophthalmic route 2 times per day. |
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
Agents That Affect Iodide/Radioactive Iodide
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Many compounds can affect iodide protein binding and alter iodide pharmacokinetics and pharmacodynamics.(1)
CLINICAL EFFECTS: Compounds that affect iodide pharmacokinetics and pharmacodynamics may impact the effectiveness of radioactive iodide.(1)
PREDISPOSING FACTORS: Compounds that affect iodide pharmacokinetics and pharmacodynamics are expected to have the most impact during therapy using radioactive iodide. Diagnostic procedures would be expected to be impacted less.
PATIENT MANAGEMENT: Discuss the use of agents that affect iodide pharmacokinetics and pharmacodynamics with the patient's oncologist.(1) Because indocyanine green contains sodium iodide, the iodine-binding capacity of thyroid tissue may be reduced for at least one week following administration. Do not perform radioactive iodine uptake studies for at least one week following administration of indocyanine green.(2) The manufacturer of iopamidol states administration may interfere with thyroid uptake of radioactive iodine and decrease therapeutic and diagnostic efficacy. Avoid thyroid therapy or testing for up to 6 weeks post administration of iopamidol.(3)
DISCUSSION: Many agents interact with radioactive iodine. The average duration of effect is: anticoagulants - 1 week antihistamines - 1 week anti-thyroid drugs, e.g: carbimazole, methimazole, propylthiouracil - 3-5 days corticosteroids - 1 week iodide-containing medications, e.g: amiodarone - 1-6 months expectorants - 2 weeks Lugol solution - 3 weeks saturated solution of potassium iodine - 3 weeks vitamins - 10-14 days iodide-containing X-ray contrast agents - up to 1 year lithium - 4 weeks phenylbutazone - 1-2 weeks sulfonamides - 1 week thyroid hormones (natural or synthetic), e.g.: thyroxine - 4 weeks tri-iodothyronine - 2 weeks tolbutamide - 1 week topical iodide - 1-9 months (1)
Agents That Affect Iodide/Sodium Iodide I 131
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Many compounds can affect iodide protein binding and alter iodide pharmacokinetics and pharmacodynamics.(1,2)
CLINICAL EFFECTS: Compounds that affect iodide pharmacokinetics and pharmacodynamics may impact the effectiveness of radioactive iodide.(1,2)
PREDISPOSING FACTORS: Compounds that affect iodide pharmacokinetics and pharmacodynamics are expected to have the most impact during therapy using radioactive iodide. Diagnostic procedures would be expected to be impacted less.
PATIENT MANAGEMENT: Discuss the use of agents that affect iodide pharmacokinetics and pharmacodynamics with the patient's oncologist.(1,2) Because indocyanine green contains sodium iodide, the iodine-binding capacity of thyroid tissue may be reduced for at least one week following administration. Do not perform radioactive iodine uptake studies for at least one week following administration of indocyanine green.(3) The manufacturer of iopamidol states administration may interfere with thyroid uptake of radioactive iodine and decrease therapeutic and diagnostic efficacy. Avoid thyroid therapy or testing for up to 6 weeks post administration of iopamidol.(4)
DISCUSSION: Many agents interact with radioactive iodine. The average duration of effect is: anticoagulants - 1 week antihistamines - 1 week anti-thyroid drugs, e.g: carbimazole, methimazole, propylthiouracil - 3-5 days corticosteroids - 1 week iodide-containing medications, e.g: amiodarone - 1-6 months expectorants - 2 weeks Lugol solution - 3 weeks saturated solution of potassium iodine - 3 weeks vitamins - 10-14 days iodide-containing X-ray contrast agents - up to 1 year lithium - 4 weeks phenylbutazone - 1-2 weeks sulfonamides - 1 week thyroid hormones (natural or synthetic), e.g.: thyroxine - 4 weeks tri-iodothyronine - 2 weeks tolbutamide - 1 week topical iodide - 1-9 months (1,2)
There are no moderate interactions for this drug.
Contraindications
There is no enhanced messaging for this drug.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
- Drowsy
- Ocular irritation
Adverse reactions
There is no enhanced messaging for this drug.
Less Frequent
- Asthma
- Cough
- Dyspnea
Rare or Very Rare
- Anaphylaxis
- Atrial fibrillation
- Blurred vision
- Bronchospastic pulmonary disease
- Hematuria
- Ocular pain
- Pruritus of skin
- Skin rash
- Stomatitis
- Tachycardia
- Urinary retention
- Visual changes
More Frequent
- Drowsy
- Dysesthesia
- Dysgeusia
- Dysgeusia
- Headache disorder
- Headache disorder
- Ocular irritation
- Ocular pain
Less Frequent
- Blurred vision
- Conjunctivitis
- Conjunctivitis
- Dizziness
- Epistaxis
- Fatigue
- Fatigue
- Flu-like symptoms
- Myalgia
- Nasal passage irritation
- Nausea
- Pharyngitis
- Pharyngitis
- Pruritus of skin
- Rhinitis
- Rhinitis
- Sneezing
- Weight gain
- Xerostomia
Rare or Very Rare
- Acute cognitive impairment
- Aphthous stomatitis
- Chest pain
- Constipation
- Contact dermatitis
- Depression
- Diarrhea
- Dry eye
- Dyspnea
- Eczema
- Eye tearing
- Facial edema
- Flushing
- Folliculitis
- Furunculosis
- Gastroenteritis
- Glossitis
- Hyperkinesis
- Hypertension
- Hypoesthesia
- Increased appetite
- Lacerations
- Lesion of nasal mucosa
- Loss of sense of smell
- Nervousness
- Palpitations
- Paresthesia
- Parosmia
- Sleep disorder
- Symptoms of anxiety
- Toothache
- Vomiting
Precautions
No enhanced messaging available.
No enhanced messaging available.
No enhanced messaging available.
No enhanced messaging available.
No enhanced messaging available.
ICD codes
| Code | Type | Description |
|---|---|---|
| Allergic conjunctivitis | ||
| H10.1 | ICD10CM | Acute atopic conjunctivitis |
| H10.10 | ICD10CM | Acute atopic conjunctivitis, unspecified eye |
| H10.11 | ICD10CM | Acute atopic conjunctivitis, right eye |
| H10.12 | ICD10CM | Acute atopic conjunctivitis, left eye |
| H10.13 | ICD10CM | Acute atopic conjunctivitis, bilateral |
| H10.44 | ICD10CM | Vernal conjunctivitis |
| H10.45 | ICD10CM | Other chronic allergic conjunctivitis |
| H16.26 | ICD10CM | Vernal keratoconjunctivitis, with limbar and corneal involvement |
| H16.261 | ICD10CM | Vernal keratoconjunctivitis, with limbar and corneal involvement, right eye |
| H16.262 | ICD10CM | Vernal keratoconjunctivitis, with limbar and corneal involvement, left eye |
| H16.263 | ICD10CM | Vernal keratoconjunctivitis, with limbar and corneal involvement, bilateral |
| H16.269 | ICD10CM | Vernal keratoconjunctivitis, with limbar and corneal involvement, unspecified eye |
| Perennial allergic rhinitis | ||
| J31.0 | ICD10CM | Chronic rhinitis |
| Seasonal allergic rhinitis | ||
| J30.1 | ICD10CM | Allergic rhinitis due to pollen |
| J30.2 | ICD10CM | Other seasonal allergic rhinitis |
| Vasomotor rhinitis | ||
| J30.0 | ICD10CM | Vasomotor rhinitis |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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