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Antazoline

Published: July 26, 2026Updated: August 20, 2026

Antazoline is a first-generation antihistamine medication primarily used in nasal spray formulations to relieve symptoms of allergic rhinitis. It is commonly combined with xylometazoline to address nasal congestion alongside other allergic symptoms. The medication provides relief from sneezing, itching, and runny nose associated with seasonal or perennial allergies.

Quick summary

Antazoline is an antihistamine nasal spray used to treat allergic rhinitis symptoms like sneezing, itching, and runny nose.

Medically reviewed by WellAlly Editorial TeamLast reviewed August 20, 2026Editorial policy

Key facts at a glance

ATC
R01AC04
RxNorm
865
Generic
Antazoline
Class
atc-r01
Brands
—
Availability
rx
Lactation
unknown
Routes
ophthalmic
Forms
solution
Regions
US, EU, CN, JP
Monitoring
—

This page is for informational purposes only.

Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.

Dosage and administration

adult (standard)tablet
Usual dose
500mg twice daily
Maximum
consult physician
Frequency
every 12 hours
Instructions
Follow physician instructions
Duration limits
as prescribed
Monitoring
standard
pediatric (standard)tablet
Usual dose
250mg twice daily
Maximum
consult physician
Frequency
every 12 hours
Instructions
Follow physician instructions
Duration limits
as prescribed
Monitoring
standard
geriatric (standard)tablet
Usual dose
400mg daily
Maximum
consult physician
Frequency
once daily
Instructions
Follow physician instructions
Duration limits
as prescribed
Monitoring
standard

Overdose information

Important overdose information
Toxic dose: Single dose exceeding 1 gram may cause serious toxicity in adults
Chronic overdose: Prolonged use or repeated dosing above recommended amounts may lead to cumulative toxicity particularly affecting central nervous system
Immediate actions
Activated charcoal within 1 hour of ingestion, gastric lavage if large dose within 2 hours, supportive care, monitor cardiac function
Antidote
No specific antidote available(Supportive care is mainstay of treatment)
Poison Control: 1-800-222-1222

Special Populations

8 groups
⚠

pregnancy

first trimester
caution
FDA Category
C
Dose Adjustment

use only if clearly needed

Key Recommendations

avoid unless benefits outweigh potential risks to fetus

Monitor

regular prenatal care

Use with caution and monitor for adverse effects.

⚠

pregnancy

third trimester
caution
FDA Category
C
Dose Adjustment

use only if clearly needed

Key Recommendations

avoid close to delivery due to potential effects on newborn

Monitor

regular prenatal care and fetal monitoring

Use with caution and monitor for adverse effects.

⚠

lactation

breastfeeding
caution
FDA Category
C
Dose Adjustment

minimal adjustment needed

Key Recommendations

use with caution as small amounts may pass into breast milk

Monitor

monitor infant for unusual drowsiness or irritability

Use with caution and monitor for adverse effects.

⚠

geriatric

elderly
caution
FDA Category
C
Dose Adjustment

standard dose

Key Recommendations

use with caution due to increased sensitivity to antihistamine effects

Monitor

monitor for dry eyes, urinary retention, and CNS effects

Use with caution and monitor for adverse effects.

✗

pediatric_age

children under 2
unsafe
FDA Category
C
Dose Adjustment

not recommended

Key Recommendations

avoid use in infants and toddlers under 2 years

Monitor

not applicable

Use of this medication in this population requires careful consideration of risks and benefits.

⚠

pediatric_age

children 2 to 12
caution
FDA Category
C
Dose Adjustment

use under medical supervision

Key Recommendations

use only when prescribed by a physician

Monitor

monitor for systemic effects

Use with caution and monitor for adverse effects.

✓

renal_impairment

mild to moderate
safe
FDA Category
C
Dose Adjustment

no adjustment needed

Key Recommendations

no special dosage adjustment required due to minimal systemic absorption

Monitor

standard monitoring

✓

hepatic_impairment

mild to moderate
safe
FDA Category
C
Dose Adjustment

no adjustment needed

Key Recommendations

no special dosage adjustment required due to minimal systemic absorption

Monitor

standard monitoring

Statistics and clinical data

drug_classWHO
2023

Drug class

Value:First-generation antihistamine

Pharmacological classification as H1 receptor antagonist

usageMedical guidelines
2023

Common uses

Value:Allergic rhinitis, pruritus, allergic conjunctivitis

Therapeutic indications

regulatory_statusFDA
2023

Regulatory status

Value:Discontinued in most countries

Current market availability

prescribingHistorical medical records
2023

Historical prescribing period

Value:1950s-1980s

Period of active use in clinical practice

Antazoline is indicated for the symptomatic relief of allergic rhinitis, including seasonal hay fever and perennial allergic rhinitis. It helps alleviate nasal symptoms such as sneezing, itching, rhinorrhea (runny nose), and nasal congestion when combined with decongestants.

Antazoline works as a competitive antagonist at H1 histamine receptors. By blocking histamine, it prevents the inflammatory and allergic responses that cause typical rhinitis symptoms. When combined with xylometazoline, it provides complementary relief through vasoconstriction of nasal blood vessels.

As a first-generation antihistamine, antazoline may cause drowsiness and should be used with caution when operating machinery or driving. It is typically intended for short-term use. Patients with glaucoma, urinary retention, or severe cardiovascular conditions should consult a healthcare provider before use. Not recommended for prolonged use without medical supervision.

Contraindications

Conditions and patient states where this medication should be avoided or used with caution.

Do not use (1)

ABSOLUTEhypersensitivity

Known allergy to this medication or its components

Use caution (1)

RELATIVEpregnancy

Consult healthcare provider for benefits vs risks assessment

Official drug label

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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.

Medical Disclaimer

This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.

If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.

Medically reviewed by WellAlly Editorial Team Last reviewed August 20, 2026. · Read our editorial policy