Products
Xylometazoline is commercially available in the form of nasal sprays and as nasal drops (Otrivin, generics, combination products, for example with dexpanthenol). It was developed at Ciba and has been approved in many countries since 1958.
Structure and properties
Xylometazoline is present in drugs as xylometazoline hydrochloride (C16H24N2 – HCl, Mr = 280.8 g/mol), a white crystalline powder that is readily soluble in water. It belongs structurally to the benzylimidazolines.
Effects
Xylometazoline (ATC R01AA07) has sympathomimetic properties. It causes vasoconstriction and decongestion of the mucosa. The effects are due to agonism at α-adrenoceptors. Xylometazoline facilitates nasal breathing and stops excessive secretions. The effect is rapid and lasts up to 12 hours.
Indications
- For the treatment of rhinitis of various causes.
- For inflammation of the sinuses.
- In case of inflammation of the middle ear.
- To facilitate a rhinoscopy (diagnosis).
Dosage
According to the professional information. The usual dosage for adults is 3 to 4 applications per day. Nasal agents should not be used for more than a maximum of 5 to 7 days because rhinitis medicamentosa may develop. Remedies without preservatives should be preferred. Infants between 1 and 2 years of age should be treated with xylometazoline only if prescribed by a physician. See also Administering nasal sprays.
Abuse
Because the nose is persistently congested, rhinitis medicamentosa leads to chronic and overuse of xylometazoline. Patients should be made aware that treatment is available. In sports, nasal medicaments are allowed. According to the doping list, no restrictions exist in or out of competition.
Contraindications
- Hypersensitivity
- After surgical procedures in which the dura mater is exposed
- Dry nasal mucosa
- Narrow-angle glaucoma
- Use in infants (< 1 year) and during pregnancy is not recommended.
Xylometazoline should be used with caution in:
- Hypertension
- Cardiovascular disease
- Hyperthyroidism
- Diabetes mellitus
Full precautions can be found in the drug label.
Interactions
At normal doses, drug-drug interactions are expected to be negligible, according to the drug label. In overdose, interactions with monoamine oxidase inhibitors, sympathomimetics, antihypertensive agents, and antidepressants, among others, are expected.
Adverse effects
The most common possible adverse effects include a burning sensation in the nasal cavity, dry nose, nasal discomfort, headache, and nausea. Prolonged use causes swelling of the nasal mucosa (see under Rhinitis medicamentosa).
