Xylometazoline

Pharmacologic Category

Alpha-Adrenergic Agonist; Decongestant; Imidazoline Derivative

Dosing: Adult

Nasal congestion: Intranasal:

Drops (0.1%): Apply 2 to 3 drops in each nostril every 8 to 10 hours

Metered dose spray (0.1%): 1 spray in each nostril every 8 to 10 hours

Spray (0.05%, 0.1%): 1 or 2 sprays in each nostril every 8 to 10 hours

Dosing: Geriatric

Refer to adult dosing.

Use: Labeled Indications

Nasal Congestion: Temporary relief of nasal and nasopharyngeal mucosal congestion

Class and Related Monographs

Nasal Decongestants

Administration: Intranasal

For intranasal use only. Blow nose to clear nostrils before use. Tilt head slightly forward (for spray) or backward (for drops) and then spray solution or apply drops into each nostril. After application of spray or drops inhale deeply. Wipe tip of container clean after each use. Some products may need to be primed prior to initial use (refer to package labeling).

Storage/Stability

Store at room temperature.

Medication Safety Issues

Sound-alike/look-alike issues:

Otrivin may be confused with Lotrimin

Contraindications

Hypersensitivity to xylometazoline or any component of the formulation; patients with transphenoidal hypophysectomy or surgery exposing the dura mater; narrow angle glaucoma; rhinitis sicca or atrophic rhinitis

Warnings/Precautions

Concerns related to adverse effects:

• Rebound nasal congestion: Frequent or prolonged use may cause nasal congestion to recur or worsen.

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with hypertension or heart disease.

• Diabetes mellitus: Use with caution in patients with diabetes mellitus.

• Thyroid disease: Use with caution in patients with thyroid disease.

• Prostatic hyperplasia/Urinary obstruction: Use with caution in patients with prostatic hyperplasia and/or GU obstruction.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Other warnings:

• Appropriate use: If symptoms persist longer than 3 days consult health care provider. Container should not be used by more than 1 individual.

Geriatric Considerations

Evaluate the patient's ability to self-administer; use with caution in patients with cardiovascular disease.

Pregnancy Considerations

According to the manufacturer, use during pregnancy is not recommended.

Breast-Feeding Considerations

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

Adverse Reactions

1% to 10%:

Central nervous system: Headache

Gastrointestinal: Nausea

Local: Application site burning

Respiratory: Dry nose, nasal discomfort

<1%, postmarketing, and/or case reports: Cardiac arrhythmia, hypersensitivity reaction, tachycardia, visual impairment (transient)

Metabolism/Transport Effects

None known.

Drug Interactions Open Interactions

Alpha1-Blockers: May diminish the vasoconstricting effect of Alpha1-Agonists. Similarly, Alpha1-Agonists may antagonize Alpha1-Blocker vasodilation. Risk C: Monitor therapy

AtoMOXetine: May enhance the hypertensive effect of Sympathomimetics. AtoMOXetine may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy

Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Exceptions: Cannabidiol. Risk C: Monitor therapy

Cocaine (Topical): May enhance the hypertensive effect of Sympathomimetics. Management: Consider alternatives to use of this combination when possible. Monitor closely for substantially increased blood pressure or heart rate and for any evidence of myocardial ischemia with concurrent use. Risk D: Consider therapy modification

Doxofylline: Sympathomimetics may enhance the adverse/toxic effect of Doxofylline. Risk C: Monitor therapy

Ergot Derivatives: May enhance the hypertensive effect of Alpha1-Agonists. Ergot Derivatives may enhance the vasoconstricting effect of Alpha1-Agonists. Exceptions: Ergoloid Mesylates; Nicergoline. Risk X: Avoid combination

Esketamine: Decongestants (Nasally Administered) may diminish the therapeutic effect of Esketamine. Management: Patients who require a nasal decongestant on an esketamine dosing day should administer the nasal decongestant at least 1 hour before esketamine. Risk D: Consider therapy modification

FentaNYL: Alpha1-Agonists may decrease the serum concentration of FentaNYL. Specifically, fentanyl nasal spray serum concentrations may decrease and onset of effect may be delayed. Risk C: Monitor therapy

Guanethidine: May enhance the arrhythmogenic effect of Sympathomimetics. Guanethidine may enhance the hypertensive effect of Sympathomimetics. Risk C: Monitor therapy

Iobenguane Radiopharmaceutical Products: Alpha1-Agonists may diminish the therapeutic effect of Iobenguane Radiopharmaceutical Products. Management: Discontinue all drugs that may inhibit or interfere with catecholamine transport or uptake for at least 5 biological half-lives before iobenguane administration. Do not administer these drugs until at least 7 days after each iobenguane dose. Risk X: Avoid combination

Linezolid: May enhance the hypertensive effect of Sympathomimetics. Management: Reduce initial doses of sympathomimetic agents, and closely monitor for enhanced pressor response, in patients receiving linezolid. Specific dose adjustment recommendations are not presently available. Risk D: Consider therapy modification

Monoamine Oxidase Inhibitors: May enhance the hypertensive effect of Alpha1-Agonists. While linezolid is expected to interact via this mechanism, management recommendations differ from other monoamine oxidase inhibitors. Refer to linezolid specific monographs for details. Exceptions: Linezolid. Risk X: Avoid combination

Ozanimod: May enhance the hypertensive effect of Sympathomimetics. Management: Concomitant use of ozanimod with sympathomimetic agents is not recommended. If combined, monitor patients closely for the development of hypertension, including hypertensive crises. Risk D: Consider therapy modification

Solriamfetol: Sympathomimetics may enhance the hypertensive effect of Solriamfetol. Sympathomimetics may enhance the tachycardic effect of Solriamfetol. Risk C: Monitor therapy

Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Risk C: Monitor therapy

Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy

Tricyclic Antidepressants: May enhance the therapeutic effect of Alpha1-Agonists. Tricyclic Antidepressants may diminish the therapeutic effect of Alpha1-Agonists. Risk C: Monitor therapy

Product Availability

Not available in the US

Dosage Forms: Canada

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

Solution, Nasal, as hydrochloride [drops]: 0.1%

Solution, Nasal, as hydrochloride [metered dose spray]: 0.1%

Solution, Nasal, as hydrochloride [spray]: 0.05%, 0.1%

Anatomic Therapeutic Chemical (ATC) Classification

• R01AA07

Pricing: US

Solution (Triaminic Nasal & Sinus Cong Nasal)

0.05% (20 mL): $4.85

Disclaimer: The pricing data provide a representative AWP and/or AAWP price from a single manufacturer of the brand and/or generic product, respectively. The pricing data should be used for benchmarking purposes only, and as such should not be used to set or adjudicate any prices for reimbursement or purchasing functions. Pricing data is updated monthly.

Mechanism of Action

Stimulates alpha-adrenergic receptors in the arterioles of the conjunctiva and the nasal mucosa to produce vasoconstriction

Pharmacodynamics/Kinetics

Onset of action: Intranasal: Local vasoconstriction: Within 2 minutes

Duration: Up to 12 hours

Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions

Effects on Dental Treatment

No significant effects or complications reported

Effects on Bleeding

No information available to require special precautions

Index Terms

Xylometazoline HCl; Xylometazoline Hydrochloride

References

Otrivin (xylometazoline). Mississauga, Ontario, Canada: Novartis Consumer Health Canada Inc. Available at: http://www.otrivin.ca/en/index.shtml. Accessed 1/20/2016.

Otrivin (xylometazoline) [product monograph]. Mississauga, Ontario, Canada: Novartis Consumer Health Canada Inc; January 2016.

Brand Names: International

Actavia (TH); Af-Care (IL); Amidrin (ES); Antazol (BD); Balkis (DE, EG, LU); Cirovin (LK); Colirio Azul (CO); Decon (LK); Decozal (BH, ET); Ezybreth (LK); Fastorik N (TZ); FLO Rapid Relief (AU); Galazolin (LV, UA); Gelonasal (DE); Hidropid (HR); Huma-Metazol (HU); Hysan (MT); Nasan (HU, LU); NasenGel ratiopharm (LU); NasenSpray ratiopharm (LU); NasenTropfen ratiopharm (LU); Nasoferm (SE); Nasolin (FI); Nasostop (EG); Nazol N (HR); Neusdruppels (NL); Novin (BD); Novorin (HU); Olynth (CH, EE, HR, LV, RU); Osco Xuzulex Nasal Spray (HK); Otrinase (RO); Otriven (DE); Otrivin (AE, AT, BG, BH, CH, CY, CZ, DK, EE, EG, ES, ET, FI, GR, HK, HN, HU, ID, IL, IN, IS, IT, JO, KR, KW, LB, LT, LV, MT, MY, NL, NO, NZ, PH, PL, QA, SA, SE, SG, SI, SK, TH, TW, UA, VN, ZW); Otrivina (AR, BR, PY, UY); Otrivine (BE, GB, IE, LU, TR); Pen Ke Tong (TW); Rhinidine (LU); Rhinozol (BD); Senziola (IE); Sinuvin (BD); Snup Stada (HK); Tezoline (RO); Tyzine (UA); Xoline (PK); Xylo-POS (IL); Xylolin (AE, KW, SA); Xylomaris (BE); Xylomet (AE, BH, KW, QA, SA); Xylovit (IL); Xymelin (LV)

Last Updated 4/8/20