Xylometazoline
Decongestant nasal spray, alpha sympathomimetic
Xylometazoline is a topical α sympathomimetic used as a decongestant nasal spray or nasal drop for short term treatment of blocked nasal breathing. The substance was developed by Ciba in 1959 and the best known brands in Germany are Otriven, Olynth and Snup, alongside numerous generics. It is available over the counter in pharmacies and is among the best selling cold remedies overall.
Xylometazoline works rapidly, reliably and locally. The use is deliberately limited to a few days because prolonged use can cause rhinitis medicamentosa, a therapy induced persistent nasal congestion. For correct self medication and medical prescription, it is therefore worth reviewing its mechanism of action, dosage and common mistakes.
Mechanism of Action
Xylometazoline is a selective agonist at α1 adrenoceptors, with lower affinity for α2 adrenoceptors, on the smooth muscle of blood vessels. In the nasal mucosa, activation of these receptors causes vasoconstriction of the precapillary arterioles and the postcapillary venous sinusoids. Mucosal volume decreases and nasal breathing improves within minutes.
Onset of action occurs after 5 to 10 minutes and the effect lasts 8 to 12 hours. Systemic absorption during correct use is low, but in infants and with excessive application it can become relevant. Through α2 receptors the substance acts centrally and can cause sedation or blood pressure effects when absorbed, especially in infants.
With prolonged use rebound congestion occurs. Sustained vasoconstriction leads to reactive vasodilation and receptor upregulation, so the nose swells shut again more and more quickly. Repeated use worsens this cycle and can end in rhinitis medicamentosa. International recommendations therefore limit use to a maximum of 7 days.
Indications
- Acute rhinitis during a cold, for short term relief of nasal obstruction
- Sinusitis as adjunct for opening of ostia and paranasal sinus drainage
- Otitis media and eustachian tube catarrh for opening of the Eustachian tube
- Before diagnostic procedures in the nose and paranasal sinuses for better visualisation
- Air travel with tubal blockage for pressure equalisation during a cold
Dosage and Administration
Adults and adolescents from 12 years: 0.1 percent solution, 1 spray or 2 to 3 drops in each nostril up to three times daily. Children 6 to 12 years: 0.05 percent solution, 1 spray or 2 to 3 drops in each nostril up to three times daily. Children 2 to 6 years: 0.05 percent solution only under medical supervision. Infants and toddlers under 2 years: special 0.025 percent preparations only after consulting a paediatrician.
Use must not exceed 5 to 7 days. Before each application, blow the nose, hold the bottle upright and aim the spray upward and outward into the nostril. Keep the head upright and do not sniff in deeply to avoid aspiration into the pharynx. After use, wipe the spray tip with a clean tissue and do not share the bottle with others.
Renal and hepatic impairment: no dose adjustment needed because systemic exposure with topical use is minimal. Pregnant and breastfeeding women should prefer the lower 0.05 percent concentration and keep the duration even shorter.
Side Effects
Common (1 to 10 percent): burning in the nose, dry nasal mucosa, sneezing, nosebleeds particularly when the mucosa is dry.
Uncommon (0.1 to 1 percent): rebound congestion with overuse, rhinitis medicamentosa with chronic use, headache, palpitations, rise in blood pressure in hypertensive patients.
Rare: allergic skin reactions, sleep disturbance, hallucinations in children, systemic effects in infants such as hypothermia, bradycardia and respiratory depression.
Important: rhinitis medicamentosa develops with weeks or months of use. It requires gradual discontinuation, sometimes with topical glucocorticoids as withdrawal therapy. In children under 2 years, xylometazoline may only be used in age appropriate concentrations and only after medical consultation.
Interactions
- Monoamine oxidase inhibitors (MAO inhibitors, tranylcypromine, moclobemide): do not use within 14 days of stopping an MAO inhibitor because hypertensive crises are possible
- Tricyclic antidepressants (amitriptyline, imipramine): enhanced sympathomimetic action, rises in blood pressure
- Beta blockers (propranolol): paradoxical rise in blood pressure theoretically possible, usually not clinically relevant
- Other blood pressure active substances: theoretical shift of blood pressure, reconsider use in treatment resistant hypertension
Special Notes
Contraindications: rhinitis sicca (dry inflammation), status after transsphenoidal pituitary surgery or other surgery that opened the dura mater, narrow angle glaucoma, severe cardiovascular disease, pheochromocytoma, severe hypertension, hyperthyroidism.
Pregnancy: possible after consulting a doctor, preferably using the lower 0.05 percent concentration and strictly limiting application to the necessary minimum. Breastfeeding: caution is advised, passage into breast milk is not precisely quantified; saline nasal rinses are a safer alternative.
Alternatives: isotonic and hypertonic saline solutions, seawater nasal sprays, steam inhalation and elevation of the head. In allergic rhinitis, antihistamines and nasal glucocorticoids are the more causal therapy. In chronic rhinosinusitis, medical evaluation is necessary; xylometazoline is not suitable.
Monitoring: record duration of use on the packaging and pause after 7 days at the latest. For persistent nasal obstruction, ENT evaluation is required. Counselling about rhinitis medicamentosa is part of every pharmacy dispensing.
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Frequently Asked Questions
How long may I use xylometazoline?
No more than 5 to 7 days of continuous use. Beyond that, rhinitis medicamentosa threatens, a therapy induced persistent congestion of the nose. If complaints do not resolve after a week, medical evaluation is required; the underlying cause may be sinusitis or another disorder.
What is rhinitis medicamentosa?
It arises from weeks or months of decongestant nasal spray use. The mucosa responds with reactive vasodilation and receptor upregulation, so each further application works less and less well. Treatment is gradual discontinuation, often combined with nasal glucocorticoids.
Can I use xylometazoline during pregnancy?
After consulting a gynaecologist or pharmacist, short term use is possible, preferably in the lower children's concentration of 0.05 percent and for as short a time as possible. Alternatives include saline nasal rinses with physiological saline or seawater sprays.
Can xylometazoline be dangerous in children?
In infants and toddlers, systemic absorption is higher; overdoses can cause hypothermia, bradycardia and respiratory depression. Age appropriate concentrations therefore exist and must be strictly observed. In children under 2 years, use only after medical consultation.
Sources
- BfArM, Federal Institute for Drugs and Medical Devices
- AWMF, S2k Guideline on Rhinosinusitis
- Gelbe Liste, Xylometazoline active substance profile
- EMA, European Medicines Agency
Legal Notice and Disclaimer
The information provided on this page is for general informational purposes only and does not constitute medical advice, diagnosis or treatment recommendation. It does not replace consultation with a licensed physician or pharmacist. Medicines should only be taken on medical prescription or via a pharmacy. All information is based on product information and recognised scientific sources published at the time of creation; the manufacturer's current summary of product characteristics is always authoritative. Sanoliste assumes no liability for the completeness, timeliness or accuracy of the information presented. In a medical emergency, call the emergency number 112 (Europe).