ACTION AND MECHANISM

- [NASO/PHARYNGEAL DECONGESTANT], [ADRENERGIC (ALPHA-2) AGONIST]. Xylometazoline is an imidazole derivative of clonidine with alpha agonist activity. Its pharmacology is not fully established, but its topical vasoconstrictor effects appear to be due to binding to postsynaptic alpha-2 receptors, although certain alpha-1 effects cannot be ruled out. After topical administration, it causes vasoconstriction of the mucosal capillaries, decreasing blood content and swelling of the mucosa, which produces a decongestant effect on the nasal passages. The decongestant effects of xylometazoline are longer lasting than those of alpha-1 agonists such as phenylephrine, although they are slower onset.

SENIORS

Elderly patients are more susceptible to adverse reactions after using sympathomimetics. They may also suffer from conditions that could be worsened by the administration of sympathomimetics, as well as be receiving treatment with drugs with which this active ingredient could interact. Close monitoring of patients over 60 years of age is recommended, and discontinuation of treatment at the slightest sign of significant adverse reactions may be necessary. Dosage adjustment may be necessary.

PATIENT ADVICE

PATIENT ADVICE:- The nose should be cleaned before each application.- Proper nasal and applicator hygiene is advisable.- It is recommended not to exceed the recommended daily doses or use for more than three consecutive days to avoid rebound congestion.- Treatment should be discontinued and a doctor consulted if symptoms persist, worsen, or if high fever, dizziness, insomnia, or nervousness appear.- It is common for a sensation of itching or nasal discomfort to appear after application, which disappears after several doses.

CONTRAINDICATIONS

- Hypersensitivity to any component of the medication.

PREGNANCY

No animal studies have been conducted, although other sympathomimetic amines have been shown to cause teratogenic effects in some species. A study of 207 pregnant women who had been in contact with the drug during the first three months of pregnancy found no increased risk of malformations. However, there are no adequate and well-controlled studies in humans, so it is unknown whether nasal administration of xylometazoline could lead to adverse effects, although possible systemic absorption should be taken into account. The use of this drug is only permitted in the absence of safer therapeutic alternatives, and its use should be limited to short periods of time.

PHARMACOKINETICS

Nasal route: - Absorption: The effects appear after 5-10 minutes, and last for a period of 5-6 hours, even reaching 10 hours.

INDICATIONS

- [NASAL CONGESTION]. Symptomatic treatment of nasal congestion associated with [RHINITIS], such as [SEASONAL ALLERGIC RHINITIS], [PERENNIAL ALLERGIC RHINITIS], or [VASOMOTOR RHINITIS], [COMMON COLD] and [SINUSITIS].

INTERACTIONS

No drug interactions have been reported with nasally administered xylometazoline, although this drug may be absorbed through the nasal mucosa or through oral administration. There is some controversy regarding the effects of alpha-2 vasoconstrictors, since at the systemic level, the affinity for presynaptic receptors predominates, resulting in sympatholytic effects. Despite this, and due to the possibility that this drug may also act on other adrenergic receptors, caution is advised when administering xylometazoline with drugs such as MAOI or tricyclic antidepressants, with antihypertensives such as diuretics, beta-blockers, methyldopa, or guanethidine, with thyroid hormones, with nervous system stimulants, nitrates, or with digoxin.

LACTATION

It is unknown whether xylometazoline is excreted in breast milk, nor is it known what effects it may have on newborns. Given the potential for systemic absorption, and given that young children are particularly sensitive to the adverse effects of sympathomimetic amines, it is recommended to discontinue breastfeeding or avoid administering this medication.

CHILDREN

Safety and efficacy in children under 12 years of age have not been evaluated, so its use is not recommended. Adverse reactions such as sedation are more common in children, and these reactions can be severe and require supportive treatment.

RULES FOR CORRECT ADMINISTRATION

- Nebulization: Insert the valve of the container into the nostrils in a vertical position. Press the valve, taking a deep breath at the same time to facilitate maximum penetration of the medication. Each press should be brief, that is, just long enough to press fully and then release. Once the medication has been administered, clean the end of the valve with warm water and then dry it with a clean cloth. - Drops: The patient should lie in a lateral position, applying the drops to each nostril. They should remain in this position for the time necessary to prevent the solution from escaping.

POSOLOGY

DOSAGE:- Adults, nasal: One spray or drop in each nostril, up to 3 times a day.- Children, nasal:* Children 12 years and older: One spray or drop in each nostril, up to 3 times a day.* Children under 12 years: The safety and efficacy of this medicine have not been evaluated. It is recommended to avoid treatments for more than 3 consecutive days to avoid the appearance of rebound congestion, which is usually interpreted by the patient as a lack of effects, which leads to a new administration, with the risk of overdose. The different doses should be separated by a period of 8-10 hours.

PRECAUTIONS

- Patients in whom sympathetic stimulation could worsen their pathologies. Xylometazoline administered nasally does not theoretically present a risk for these patients, although systemic absorption cannot be ruled out. Even in the event of such absorption, the effects on presynaptic alpha-2 receptors would theoretically predominate, with the consequent sympatholytic effects. However, it cannot be ruled out that this drug also has affinity for other adrenergic receptors, both alpha-1 and beta receptors, which is why most authors recommend extreme caution in the case of pathologies such as [DIABETES], [GLAUCOMA], [HEART DISEASE] ([CORONARY FAILURE], [ISCHAEMIC HEART DISEASE]), [HEART ARRHYTHMIA], [ARTERIAL HYPERTENSION], [HYPERTHYROIDISM], [PHEOCHROMOCYTOMA] or [PROSTATIC HYPERPLASIA].

- Rebound congestion. The administration of topical vasoconstrictors frequently results in rebound congestion, which is often accompanied by the patient's need to redose. This can pose a risk of overdose and worsen the congestion. It is recommended to gradually discontinue administration of xylometazoline in cases of rebound congestion, alternating doses in each nostril, until the congestion is completely eliminated.

PRECAUTIONS RELATED TO EXCIPIENTS

- Because it contains benzalkonium chloride, it may cause inflammation of the nasal mucosa, especially with long-term treatment. If persistent nasal congestion is suspected, a nasal product that does not contain this preservative should be used whenever possible.

ADVERSE REACTIONS

The adverse effects of this medicine are usually local and mild. However, systemic absorption of this medicine cannot be ruled out, with the appearance of systemic adverse effects, which may increase in intensity and severity at higher doses. The most frequent alterations are:- Local effects: The appearance of [SNEEZING], [NASAL IRRITATION], local itching and burning sensation, [NASAL DRYNESS] or [RHINORRHEA] is common. Rebound [NASAL CONGESTION] is also frequent, especially in the case of high doses or after prolonged periods of time. In case of abuse of the medicine, [RHINITIS] may appear, with the mucosa appearing edematous and with a reddish or pale gray color. These signs usually disappear after one week of discontinuing the drug. - Systemic effects: The absorption of xylometazoline may lead to [DIZZINESS], [VERTIGO], [NAUSEA], [VOMITING], [NERVOUSNESS], [PALPITATIONS], [ARTERIAL HYPERTENSION], [BRADYCARDIA] reflex, [EXCESSIVE SWEATING] or [PALENESS]. In children it may cause [DROWSINESS].

OVERDOSE

Symptoms: There is little experience with xylometazoline dosages, as the route of administration makes acute overdoses uncommon. Accidental ingestion of other drugs such as naphazoline commonly causes nervous breakdown, with sedation, intense hypothermia, bradycardia, and, in severe cases, coma. This overdose is especially serious in children. Headache, tremors, palpitations, nervousness, or excessive sweating may also occur. Treatment: Treatment should be symptomatic and supportive. In mild cases, oxygen should be administered. For shock, plasma expanders should be used, and in cases of anticholinergic symptoms, intramuscular or intravenous physostigmine should be administered by slow infusion, at a dose of 2 mg for adults or 0.5 mg for children.

COMPOSITION

XYLOMETAZOLINE: 1 MILLIGRAMS - HYDROCHLORIDE
BENZALKONIUM CHLORIDE (EXCIPIENT): 0