Xylometazoline

Xylometazoline is a sympathomimetic agent that is used in medicine as an alpha-adrenomimetic. It works by constricting blood vessels and reducing swelling of the mucous membranes.

This drug is often used topically in the form of nasal drops or spray to relieve nasal congestion caused by various respiratory conditions such as runny nose, flu, allergic rhinitis, and others. Xylometazoline may also be used in the treatment of allergic conjunctivitis to relieve swelling and redness of the eyes.

It is important to remember that xylometazoline is intended only for symptomatic treatment, alleviating the manifestations but not treating the cause of the disease. It should not be used for a long time without a doctor's prescription, as this may lead to the development of tolerance and other undesirable effects. It is recommended to consult a doctor before using xylometazoline, especially if you have other medical conditions or medications you are taking.

Indications Xylometazoline

1. Runny Nose: Used to relieve nasal congestion caused by various respiratory infections such as runny nose, flu or acute respiratory viral infections.
2. Allergic rhinitis: Used to relieve swelling and nasal congestion in allergic rhinitis caused by an allergic reaction to pollen, dust, animal droppings and other allergens.
3. Allergic Conjunctivitis: May be used to relieve swelling and redness of the eyes in allergic conjunctivitis.
4. Otitis media: Used to relieve swelling of the ear mucosa in otitis media.
5. Preparation for X-ray and endoscopic procedures: Sometimes used before X-ray and endoscopic procedures to constrict blood vessels in the nose and reduce swelling of the mucous membrane.

Release form

1. Nasal drops:

   • Xylometazoline is usually available as nasal drops that come in vials with a dispenser.
   • It is recommended to administer 2-3 drops in each nostril.
   • Application is usually no more often than every 10-12 hours.

2. Nasal sprays:

   • Similar to drops, xylometazoline can be presented as nasal sprays that also contain a dispenser.
   • It is recommended to make 1-2 sprays in each nostril.
   • The frequency of application is also usually no more than 2-3 times a day.

3. Other forms:

   • In rare cases, xylometazoline may be available as a gel or ointment for external application, but these are less common forms.

Pharmacodynamics

1. Adrenomimetic action: Xylometazoline is an agonist of α-1 type adrenoreceptors, which means that it stimulates these receptors. This leads to constriction of capillaries and arterioles, reducing blood flow and swelling in the nasal mucosa.
2. Reduction of edema: After topical application of xylometazoline, vasoconstriction of blood vessels leads to a decrease in edema of the nasal mucosa. This helps to improve breathing and reduce nasal congestion, relieving the symptoms of rhinitis and runny nose.
3. Long-acting: Xylometazoline has a long-lasting effect, which reduces the frequency of use to several times a day.
4. Minimal systemic exposure: When xylometazoline is applied topically as drops or sprays, systemic absorption is minimal, which reduces the risk of systemic side effects.

Pharmacokinetics

Xylometazoline is a sympathomimetic agent used primarily to constrict nasal mucosal vessels and relieve nasal congestion in runny nose, rhinitis, and other respiratory diseases.

After topical application, xylometazoline is practically not absorbed into the systemic bloodstream, as its action is limited by local constriction of blood vessels. If absorption occurs, it is slow and incomplete. Therefore, the pharmacokinetics of xylometazoline in the body is usually poorly understood.

Xylometazoline is mainly metabolized in the liver, and metabolites are excreted with urine.

It is also worth noting that xylometazoline can have systemic effects, especially with excessive or prolonged use, such as increased blood pressure, arrhythmias, dizziness, insomnia, and others.

Dosing and administration

1. For adults and children over 6 years of age:

   • It is usually recommended that 2-3 drops (or 1-2 sprays) of xylometazoline be administered into each nostril.
   • It is usually applied no more frequently than every 10 to 12 hours.

2. For children ages 2 to 6 years old:

   • For drops: it is usually recommended to administer 1-2 drops into each nostril.
   • For spray: 1 spray into each nostril.

3. For children under 2 years of age:

   • The use of xylometazoline in children under 2 years of age should be supervised by a physician.

Use of xylometazoline is not recommended for longer than indicated in the drug instructions or recommended by your doctor to avoid side effects such as reactive nasal congestion or irritation of the mucous membranes.

Use Xylometazoline during pregnancy

It is important to consult your doctor before using xylometazoline during pregnancy. Xylometazoline is a medicine that is commonly used to relieve nasal congestion and reduce mucus production in runny noses caused by respiratory infections or allergies.

Some studies indicate that topical use of xylometazoline in low doses as nasal drops is probably safe during pregnancy. However, systemic exposure or prolonged use of xylometazoline may be associated with risks to fetal development, so use in such cases should be under medical supervision.

Contraindications

1. Hypersensitivity: People with known hypersensitivity to xylometazoline or any other component of the drug should not use it.
2. Bradycardia: The use of xylometazoline may be undesirable in patients with bradycardia (excessively slow heartbeat).
3. Hypertension: Xylometazoline should be used with caution in patients with hypertension (high blood pressure).
4. Sick children: In children under 6 years of age, xylometazoline should be used only under medical supervision. For infants and children, it is recommended to use formulas designed specifically for children.
5. Pregnancy and lactation: The use of xylometazoline during pregnancy or lactation should be under the supervision of a physician.
6. Heart disease: In patients with cardiovascular disease such as coronary heart disease or arrhythmias, xylometazoline should be used with caution.
7. Thyroid disease: In patients with hyperthyroidism (increased thyroid function), xylometazoline should be used with caution because of possible increased side effects.

Side effects Xylometazoline

1. Dry mucous membranes: Increased dryness in the nose or throat can manifest as discomfort or irritation.
2. Reactive mucosal edema: Prolonged use of xylometazoline may cause reactive mucosal edema, which may increase nasal congestion.
3. Burning or tingling sensation: Some people may experience unpleasant sensations such as burning or tingling in the nose after using xylometazoline.
4. Feeling drowsy or dizzy: Xylometazoline may cause drowsiness or dizziness in some people.
5. Palpitations: In rare cases, palpitations or arrhythmias may occur.
6. Withdrawal runny nose: When xylometazoline is withdrawn, runny nose or increased symptoms of nasal congestion may occur temporarily.
7. Nausea or vomiting: Some people may experience stomach discomfort such as nausea or vomiting.
8. High blood pressure: Xylometazoline may temporarily increase blood pressure in some people.

Overdose

Symptoms of overdose may include:

1. Severe vasoconstriction, which leads to even more nasal congestion and difficulty breathing.
2. Increased blood pressure.
3. Heart palpitations (tachycardia) and arrhythmias.
4. Dizziness and headache.
5. Nervousness and restlessness.
6. Sleep disturbance.
7. Tremors and tremors.
8. Seizures.

Interactions with other drugs

Xylometazoline is generally used topically to constrict nasal mucosal vessels and relieve nasal congestion in runny nose and rhinitis. Since its systemic absorption is negligible, interactions with other drugs are rare.

However, caution should be exercised when using xylometazoline and concomitant use with other vasoconstrictors such as sympathomimetics should be avoided, as this may increase their effects and increase the risk of unwanted side effects, including increased blood pressure and cardiac problems.

Also, xylometazoline may interact with monoamine oxidase inhibitors (MAOIs) and antidepressants, causing high blood pressure.