Drug reference

Azelastine

Second-generation H1 antihistamine (topical) · Antihistamine; Antiallergic

Also known as Azelastine hydrochloride

START

1–2 sprays/nostril twice daily (or 1 eye drop BID)

TYPICAL MAX

2 sprays per nostril twice daily

STOP IF

Hypersensitivity or intolerable sedation

WATCH

Sedation (esp. with alcohol/CNS depressants); nasal mucosa

CDSCO approvedSchedule HATC R01AC03

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 30min · symptom relief
PEAK: 2.5h · Tmax
t½: 22h · t½
DURATION: 12h · BID

EXCRETION

Mainly faecal; small renal

route + CYP

INTERACTIONS

—

none in our sources

PREGNANCY

Limited data; use only if benefit outweighs risk.

FDA category + note

Available in India

5 branded formulations. Look up specific brands in the Drugs workspace.

Mechanism

Selective H1-receptor antagonist with mast-cell-stabilising and anti-inflammatory activity (inhibits leukotriene/PAF release), applied intranasally or ocularly for allergic symptoms.

Indications

Allergic rhinitis (seasonal/perennial)Vasomotor rhinitisAllergic conjunctivitis

Dosing

Adult: Nasal: 1–2 sprays per nostril twice daily. Ophthalmic 0.05%: 1 drop in affected eye(s) twice daily.
Pediatric: Nasal ≥6 y: 1 spray per nostril twice daily. Ophthalmic ≥3 y: 1 drop BID.
Renal adjustment: No dose adjustment (low systemic absorption).
Hepatic adjustment: No specific adjustment.
Geriatric: No specific adjustment.
Max dose: 2 sprays per nostril twice daily (nasal)

Pharmacokinetics

Onset

~15–30 min (nasal symptom relief)

Peak effect

2–3 h

Duration

~12 h

Half-life

~22 h (nasal); active metabolite ~54 h

Bioavailability

~40% (nasal); ~low (ocular)

Protein binding

~80–90%

Metabolism

Hepatic CYP (desmethylazelastine active metabolite)

Excretion

Mainly faecal; small renal

Contraindications

Hypersensitivity to azelastine

Side effects

Common

Bitter tasteNasal irritation/epistaxisHeadacheSomnolenceApplication-site discomfort

Serious

Significant sedation (rare at topical doses)
Hypersensitivity reaction

Pregnancy & lactation

Pregnancy

Limited data; use only if benefit outweighs risk.

Lactation

Unknown if excreted in milk; caution (topical exposure low).

Drug interactions

Aprepitant

Moderate

Textbook

Increased azelastine levels and potential for increased side effects.