Antazol0.05%

Antazol is a topical nasal decongestant indicated for:

• Established/OTC-approved use: Temporary relief of nasal congestion associated with the common cold, allergic rhinitis (hay fever), and sinusitis.
• Guideline-supported adjunct use: As a short-term adjunct, under medical supervision, to reduce nasal mucosal swelling before examination of the nasal passages, sinus drainage procedures, or to improve penetration of other intranasally administered medications (e.g., intranasal corticosteroids) in a blocked nose.
• Off-label/limited-evidence use: Occasionally used briefly to relieve eustachian tube congestion associated with otitis media, or before air travel/diving in individuals prone to barotrauma; evidence for this use is limited and it is not an approved indication.

Antazol is intended only for short-term, symptomatic relief and does not treat the underlying cause of nasal congestion.

Xylometazoline is formulated as Xylometazoline Hydrochloride, available as nasal drops or a metered nasal spray in two standard strengths:

• 0.05% w/v (0.5 mg/mL) – pediatric strength
• 0.1% w/v (1 mg/mL) – adult strength

Formulations typically also contain excipients such as benzalkonium chloride (preservative), sodium chloride, disodium edetate, and purified water used to adjust tonicity and pH.

Antazol is a topical alpha-adrenergic agonist belonging to the imidazoline class of sympathomimetic decongestants. Applied directly to the nasal mucosa as drops or spray, Antazol constricts the dilated blood vessels of the nasal passages, reducing swelling and congestion so that airflow through the nose improves.

Onset of action typically occurs within 5–10 minutes of application, with an effect that can last up to 10 hours, allowing twice-daily dosing. Antazol is widely available as an over-the-counter product for short-term symptomatic relief of nasal congestion.

Antazol belongs to the therapeutic class of Topical Nasal Decongestants, specifically the imidazoline-derivative subclass of alpha-adrenergic (sympathomimetic) agonists.

Xylometazoline acts directly on alpha-adrenergic receptors (predominantly alpha-1, with some alpha-2 activity) located in the smooth muscle of the nasal mucosal arterioles. Stimulation of these receptors produces localized vasoconstriction, which reduces blood flow to the engorged nasal turbinates, decreases mucosal edema, and reopens the nasal airway.

The decongestant effect of Xylometazoline begins within 5–10 minutes and persists for up to 10 hours per application. Systemic absorption through the nasal mucosa is normally minimal at recommended doses, but can increase significantly with excessive dosing, prolonged use, or in young children, raising the risk of systemic adrenergic effects.

For intranasal use only. Before use, gently blow the nose to clear the nasal passages.

• Nasal spray: With the head upright, insert the tip into one nostril and spray while gently inhaling; repeat in the other nostril as directed.
• Nasal drops: Tilt the head back slightly, instill the prescribed number of drops into each nostril, then remain still for a few moments.
• Avoid contact of Antazol with the eyes.
• Wipe the tip clean after each use and do not share the container with another person, to avoid spreading infection.
• Do not exceed the recommended dose or frequency, and do not use Antazol for more than 3–5 consecutive days (see Precautions and Warnings).

Antazol has the following clinically significant interactions:

• Monoamine oxidase inhibitors (MAOIs): Concurrent use, or use within 14 days of MAOI therapy, is contraindicated due to the risk of a hypertensive crisis (see Contraindications).
• Tricyclic antidepressants: May potentiate the pressor (blood pressure–raising) effect of Antazol if it is systemically absorbed; use with caution.
• Other sympathomimetic agents (e.g., other decongestants, stimulants, appetite suppressants): Concurrent use may produce additive cardiovascular effects such as increased heart rate and blood pressure.
• Antihypertensive agents: Systemic absorption of Antazol, particularly with excessive or prolonged use, may reduce the effectiveness of antihypertensive medications.

Antazol is generally well tolerated with short-term, correctly dosed use. Reported side effects include:

• Common (local): Nasal irritation, burning or stinging sensation, dryness of the nasal mucosa, sneezing, and a transient increase in nasal discharge.
• Rebound congestion (rhinitis medicamentosa): Worsening nasal congestion that recurs as the decongestant effect wears off, typically with use of Antazol beyond the recommended 3–5 days; this is a well-established and clinically important limitation of this drug class (see Precautions and Warnings).
• Uncommon/rare (systemic): Headache, palpitations, tachycardia, and elevated blood pressure, particularly with excessive or prolonged use, or in young children in whom systemic absorption is more likely.

Pregnancy: Data on the use of Antazol in pregnancy are limited. Because it is a vasoconstrictor with potential for systemic absorption, Antazol should be used during pregnancy only if clearly needed, at the lowest effective dose and for the shortest possible duration, and only after consulting a physician, as potential benefit must be weighed against potential risk to the fetus.

Lactation: It is not known whether Antazol passes into breast milk in clinically significant amounts. Given limited data, breastfeeding women should use Antazol only if clearly needed and under medical advice, limiting the dose and duration of use.

Do not use Antazol for more than 3–5 consecutive days. Prolonged or excessive use can cause rebound nasal congestion (rhinitis medicamentosa), in which the nasal passages become increasingly congested as the drug wears off, potentially leading to dependence on the decongestant. If congestion persists beyond this period, stop use and consult a physician.

• Use with caution in patients with cardiovascular disease (e.g., hypertension, coronary artery disease), hyperthyroidism, or diabetes mellitus, as systemic absorption of Antazol – especially with excessive or prolonged use – can produce sympathomimetic effects such as increased heart rate and blood pressure.
• Use with caution in patients with narrow-angle glaucoma or significant prostatic enlargement, given the potential for systemic alpha-adrenergic effects if Antazol is absorbed.
• Antazol should be used with particular caution, and generally avoided, in infants and young children because of a higher risk of serious systemic toxicity (see Use in Special Populations).
• Do not share a single container of Antazol between different users, as this can spread infection.
• Avoid concurrent use of other topical or oral decongestants unless advised by a physician.

Overdose or excessive use of Antazol, particularly in young children, can cause serious systemic toxicity. Symptoms may include drowsiness, lethargy, sweating, hypothermia, bradycardia, hypotension, and, in severe cases, respiratory depression or coma in young children; adults may instead experience stimulant-type effects such as tachycardia, hypertension, agitation, and headache.

If overdose is suspected, whether from accidental ingestion or excessive nasal use, seek immediate medical attention or contact a poison control center right away. There is no specific antidote for Antazol overdose; treatment is supportive and symptomatic and should only be provided by a healthcare professional.

Store Antazol at room temperature (below 30°C), away from light and moisture. Keep the container tightly closed and out of the reach and sight of children. Discard any remaining Antazol nasal spray or drops after the period stated on the label following opening, or after the expiry date, whichever comes first, to reduce the risk of contamination.

Children: Dosing of Antazol is strength- and age-based – 0.05% for children 2 to under 12 years, and 0.1% for those 12 years and older. Antazol is not recommended in children under 2 years of age because of a higher risk of serious systemic adverse effects (see Contraindications).

Elderly: Use with caution, particularly in those with underlying cardiovascular disease, as age-related comorbidities may increase sensitivity to any systemically absorbed Antazol.

Renal/Hepatic impairment: Specific dose adjustment has not been established; because systemic absorption of Antazol after intranasal use is normally minimal, formal adjustment is generally not required, but caution is advised with excessive or prolonged use.

Treatment with Antazol should be limited to a maximum of 3–5 consecutive days. If nasal congestion persists beyond this period, use should be stopped and a physician consulted before resuming, in order to avoid rebound congestion (rhinitis medicamentosa) (see Precautions and Warnings).

Nasal Decongestants; Sympathomimetic (Alpha-Adrenergic) Agonists; Imidazoline Derivatives.

Xylometazoline is a direct-acting alpha-adrenergic receptor agonist. When applied to the nasal mucosa, it stimulates alpha-1 (and, to a lesser extent, alpha-2) adrenergic receptors in the smooth muscle of the nasal blood vessels, causing local vasoconstriction. This reduces blood flow and fluid leakage into the nasal mucosa, decreasing swelling of the nasal turbinates and relieving congestion, typically within 5–10 minutes, with effects lasting up to 10 hours.

Use of Antazol in children follows strength- and age-based dosing:

• Children 2 to under 12 years: 0.05% strength, 1 spray/drop per nostril once or twice daily under adult supervision, for no more than 3–5 consecutive days.
• Children 12 years and older: Adult (0.1%) strength and dosing may be used.
• Children under 2 years: Antazol is not recommended; safety and efficacy have not been established in this age group, and serious systemic adverse effects (including sedation, bradycardia, and hypotension) have been reported with imidazoline decongestants in young children.