Otrivin

Otrivin, containing the active substance xylometazoline, is a vasoconstrictor for topical application in the nose. It causes constriction of blood vessels in the nasal mucosa, which leads to reduced swelling and easier breathing in runny nose caused by rhinitis or sinusitis. Xylometazoline has been used for over 50 years to treat nasal congestion associated with rhinitis/sinusitis. Iota carrageenan, which has efficacy against a wide range of respiratory viruses that are the most common cause of upper respiratory tract infections, is often used as the active ingredient in antiviral nasal sprays. Recently, a nasal spray formulation containing both xylometazoline hydrochloride (0.05%) and iota-carrageenan (0.12%) has been developed that provides simultaneous disinfection and antiviral protection to the nasal mucosa. Studies have shown that xylometazoline hydrochloride and iota-carrageenan do not affect each other, allowing each to fulfill their specific clinical efficacy and effectiveness (Graf et al., 2018).

It was also found that a new formulation of xylometazoline with inactive preservatives and hyaluronic acid (HA) was studied to reduce negative effects on the mucosal defense mechanism. It has been shown that xylometazoline in this new formulation retains its decongestive activity and the HA possibly acts as an enhancer/carrier of the active principle, xylometazoline (Castellano & Mautone, 2002).

These data suggest that xylometazoline is an effective and well-tolerated treatment for relief of nasal congestion caused by colds and other conditions, and can provide long-term relief with just a single application, helping patients breathe easier for longer periods of time.

Indications Otrivina

1. Acute respiratory viral infections (ARVI) and colds: Eases breathing by reducing swelling of the nasal mucosa and decreasing mucus production.
2. Allergic Rhinitis: Helps reduce allergy symptoms including itching, sneezing and copious mucus production by constricting blood vessels in the nasal mucosa.
3. Sinusitis: Used to reduce nasal congestion in inflammation of the sinuses, helping to improve drainage and ease breathing.
4. Vasomotor rhinitis: It is used for the treatment of non-allergic rhinitis caused by changes in the vascular system of the nasal mucosa.
5. Preparation for sinus medical procedures: Otrivin may be used to reduce mucosal swelling before diagnostic procedures or sinus surgery, allowing better access and visibility.

Release form

1. Nasal spray: This is the most common form of Otrivin, designed for quick and convenient use. Sprays can come in different concentrations of xylometazoline, including special pediatric versions with a lower dosage of the active ingredient.
2. Nasal Drops: Provides the ability to accurately dose the amount of drug, which is particularly useful for use in infants and young children. Like sprays, the drops can contain different concentrations of xylometazoline.
3. Nasal Gel: This form of release is designed to provide long-lasting moisturization and relief of breathing during sleep, providing prolonged action. The gel may be preferred for use at night.

Pharmacodynamics

1. Vasoconstriction: Xylometazoline acts as an agonist of alpha-adrenoreceptors, mainly α1-adrenoreceptors located on vascular cells of the nasal mucosa. Stimulation of these receptors leads to constriction of blood vessels and reduction of nasal mucosal edema.
2. Reducing swelling: By constricting blood vessels, xylometazoline reduces the permeability of the vascular wall and reduces the release of fluid from capillaries into the surrounding tissues. This helps to reduce swelling of the nasal mucosa.
3. Improvement of breathing: Due to its vasoconstrictor action, xylometazoline is able to relieve breathing, especially in cases of nasal congestion caused by rhinitis, allergies or runny nose.
4. Prolonged action: The effect of xylometazoline begins a few minutes after administration and lasts up to several hours, which provides long-lasting relief from the symptoms of nasal congestion.

Pharmacokinetics

1. Absorption: After topical application of xylometazoline in the form of drops or spray in the nasal passage, it is rapidly absorbed through the mucous membrane.
2. Distribution: Xylometazoline can be distributed in the tissues of the nasal mucosa, where it exerts its constrictive effect on blood vessels.
3. Metabolism: After absorption, xylometazoline is metabolized in the liver, mainly by conjugation with glucuronic acid.
4. Excretion: Xylometazoline metabolites are eliminated from the body mainly with urine.
5. Half-life: The half-life of xylometazoline varies with individuals, but is usually about 3-7 hours.
6. Mechanism of Action: Xylometazoline acts by stimulating the α1-adrenoreceptors of the nasal mucosal vessels, resulting in blood vessel constriction and reduction of swelling.

Dosing and administration

The method of use and dosage of Otrivin with xylometazoline depend on the form of release of the drug and the age of the patient. Here are the general recommendations:

Nasal spray and drops for adults and children over 6 years of age:

• Spray (0.1% solution): One injection into each nasal passage every 8-10 hours, not more than 3 times a day, is usually recommended.
• Drops (0.1% solution): D rops 1-2 drops into each nasal passage every 8-10 hours, not more than 3 times a day.

For children from 2 to 6 years old:

• Spray (0.05% solution) or drops: It is usually recommended to administer one spray injection or to inject 1-2 drops into each nasal passage every 8-10 hours, not more than 3 times a day. Use a special pediatric formula with a lower concentration of xylometazoline (0.05%).

Important Notes:

• The drug is not recommended to be used for more than 5-7 consecutive days to avoid the development of reactive hyperemia and medicated rhinitis.
• The nasal passages should be cleared before applying the nasal spray or drops.
• After each use, the bottle of drops or spray should be capped to prevent contamination.
• Avoid contact of the vial tip with the surface of the nose or eyes to prevent the spread of infection.
• Before using the drug in children, pregnant and lactating women, as well as persons with chronic diseases, it is necessary to consult a doctor.

Use Otrivina during pregnancy

The use of Otrivin during pregnancy should be evaluated with caution.

Doctors generally recommend avoiding the use of vasoconstrictive nasal drops such as xylometazoline during pregnancy, especially in the first trimester. This is due to potential risks to fetal development, such as increased blood pressure in the mother and placental hypoxia in the fetus.

If a woman is pregnant and is experiencing breathing problems due to nasal congestion, it is important to discuss this with her doctor. The doctor may recommend safe alternatives or temporary strategies to relieve symptoms based on the patient's individual situation.

Contraindications

1. Hypersensitivity: People with known hypersensitivity to xylometazoline or other sympathomimetics should not use Otrivin because of the risk of allergic reactions.
2. Atherosclerosis: The use of xylometazoline may be contraindicated in patients with atherosclerosis due to possible increase in blood pressure and worsening of the condition.
3. Hypertension: Xylometazoline may cause an increase in blood pressure, therefore its use may be contraindicated in patients with hypertension.
4. Tachycardia: Otrivin may be contraindicated in patients with a fast heartbeat (tachycardia) due to possible aggravation of this condition.
5. Thyrotoxicosis: The use of xylometazoline may be contraindicated in patients with thyrotoxicosis due to possible increase in blood pressure and worsening of the condition.
6. Machroglobinemia: The use of xylometazoline may be contraindicated in patients with methemoglobinemia due to the risk of increased blood levels of methemoglobin.
7. Pediatric age: The safety and efficacy of Otrivin in children under a certain age have not been established, so its use in this age group may be limited.
8. Pregnancy and breastfeeding: The use of Otrivin during pregnancy and breastfeeding requires caution and may require consultation with a physician.

Side effects Otrivina

1. Dryness of the nasal mucosa: Xylometazoline may cause dryness in the nasal passages and mucous membranes, which may lead to discomfort and discomfort.
2. Reactive edema of the nasal mucosa: With prolonged and/or frequent use of "Otrivin" may develop so-called "reactive edema", when after discontinuation of the drug the nasal mucosa begins to swell even more, which leads to increased stuffiness.
3. Burn and irritation of the mucous membrane: If used incorrectly or in large quantities, "Otrivin" may cause irritation or burns of the nasal mucosa.
4. Increase in blood pressure: In rare cases, in some people the use of xylometazoline may lead to an increase in blood pressure or worsening of the cardiovascular system.
5. Drowsiness and dizziness: In rare cases, some people may experience side effects related to the central nervous system, such as drowsiness or dizziness.
6. Rare allergic reactions: There may be cases of allergic reactions to the drug components, manifested as skin rash, itching, skin redness or edema.

Overdose

1. Pupil dilation (mydriasis): An increase in pupil diameter can lead to blurred vision and photophobia.
2. Increased heartbeat (tachycardia): A fast heartbeat may be one of the first signs of an overdose.
3. High blood pressure (hypertension): Xylometazoline may cause an increase in blood pressure in overdose.
4. Drowsiness and somnolence: Drowsiness and even respiratory depression may occur in severe overdose.
5. Tremor and tremor: Nervous symptoms such as tremor and shaking may also be signs of overdose.
6. Dizzinessand headache: Overdose may cause dizziness and headache.
7. Changes in the vestibular apparatus: Balance and coordination of movements may be impaired.

Interactions with other drugs

1. MAO-inhibitors (monoamine oxidase inhibitors): Combining xylometazoline with MAO-inhibitors may increase their effect, resulting in high blood pressure or other undesirable effects. This is due to the fact that xylometazoline is a sympathomimetic agent.
2. Cardiovascular drugs: The use of xylometazoline in combination with other drugs that have vasoconstrictor or adrenergic stimulating effects (e.g., adrenaline, phenpropomazine) may increase these effects and increase the risk of cardiovascular adverse reactions.
3. Drugs for depression: Tricyclic antidepressants and other drugs that can increase the level of norepinephrine in the body may increase the effects of xylometazoline.
4. Beta-adrenoblockers: The use of xylometazoline in combination with beta-adrenoblockers may reduce the efficacy of both drugs, as beta-adrenoblockers block receptors responsible for vasoconstriction.
5. Other vasoconstrictors: Combination of xylometazoline with other vasoconstrictors may result in strengthening of their vasoconstrictive effect, which may increase the risk of hypertensive crises or other cardiovascular complications.

Storage conditions

Otrivin (xylometazoline) should usually be stored at room temperature, between 15 and 30 degrees Celsius. It is important to ensure dry storage conditions and avoid direct exposure to sunlight or heat. The drug should be kept out of the reach of children.

It is recommended to store Otrivin in its original packaging or container to prevent damage and maintain its effectiveness. Do not allow the drug to freeze.