Battle of drugs: xylometazoline vs naphazoline

Pharmacology can be surprising: drugs within the same pharmacological group that have a similar mechanism of action, as well as their indications and contraindications, can differ significantly from each other in a number of indicators. For pioneers, this may be especially important in the context of pharmaceutical consulting, so we decided to start a new series of articles devoted to drugs with a similar structure and radically different properties that affect their use in clinical practice. And the first “heroes” of the cycle will be alpha-adrenergic agonists, widely known to both pharmaceutical specialists and consumers - naphazoline and xylometazoline.

Compound

In 1 ml drops of 0.05% and 0.1% xylometazoline 500 mcg and 1 mg, respectively.
Sodium hydrogen phosphate, potassium dihydrogen phosphate, sodium chloride, benzalkonium chloride as auxiliary components. In 1 ml of spray 0.05% and 0.1% xylometazoline 500 mcg and 1 mg, respectively. Sodium hydrogen phosphate, benzalkonium chloride, disodium edetate dihydrate, potassium dihydrogen phosphate, eucalyptus oil, sodium chloride, macrogol glyceryl hydroxystearate, sorbitol, glycerin, water as auxiliary components.

1 g of xylometazoline 1 mg. Carbomer , glycerol , ammonia solution, propylene glycol ethanol, methylparaben, propylparaben, water as auxiliary components.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Xylometazoline is an imidazoline . Stimulates α1 and 2-adrenergic receptors of the blood vessels of the nasopharyngeal mucosa. As a result, blood vessels narrow, hyperemia, swelling of the mucous membrane and nasal discharge decrease. As a result, it is easier to breathe through the nose during rhinitis , allergic conditions and diseases of the paranasal sinuses . The spray additionally contains eucalyptus oil, which has anti-inflammatory and antibacterial effects, which has a beneficial effect on reducing swelling of the nasal mucosa. The effect appears after 10-15 minutes and lasts 8-10 hours.

Pharmacokinetics

The pharmacokinetics of the drug have not been studied in humans. Sometimes, when applied topically, absorption is sufficient to produce systemic effects.

Indications for use

• rhinitis of various etiologies ( allergic , viral, traumatic, bacterial);
• rhinopharyngitis;
• otitis media and eustachitis ;
• to facilitate the discharge of secretions during sinusitis ;
• to facilitate diagnostic manipulations in the nasal passages.

Contraindications

• hypertonic disease;
• angina pectoris;
• severe atherosclerosis ;
• tachycardia;
• thyrotoxicosis;
• chronic rhinitis and atrophic pharyngitis ;
• sensitization to the drug and hypersensitivity ;
• prostatic hyperplasia;
• glaucoma;
• diabetes.

Use with caution during pregnancy . In pediatrics, the drug with a concentration of 0.1% is not used.

Use in children

Decongestants are included by the Russian Association of Otorhinolaryngologists in federal clinical guidelines for the treatment of rhinitis and rhinosinusitis4. The FDA (Food and Drug Administration) approves their use in children over 6 years of age4. At the same time, it is important to select medications specifically intended for the treatment of young patients, strictly follow the recommendations of the attending physician and not exceed the doses and duration of therapy set out in the instructions4.

Important! For children from 2 to 6 years old, xylometazoline preparations are intended at a concentration of 0.05%; for children over 6 years old, a 0.1% solution can be used2.

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Side effects

• burning in the nose and throat;
• irritation of the mucous membrane;
• dryness of the nasopharyngeal mucosa;
• sneezing;
• headache;
• dizziness;
• swelling of the nasal mucosa;
• insomnia;
• heart rhythm disturbance;
• tachycardia;
• increased blood pressure ;
• increased excitability ;
• visual impairment;
• vomit;
• depression.

Side effects

When applied topically, the drug is practically not absorbed into the blood and is not determined in the body by analytical methods1. However, in rare cases due to xylometazoline preparations:

• the nasal mucosa swells;
• heart rhythm is disturbed;
• blood pressure increases;
• headache, vomiting, sleep disturbance and blurred vision1.

Depression can occur extremely rarely (with long-term use in high doses)1.

The listed reactions from the drug develop more often if people are predisposed to them or if xylometazoline is used incorrectly2. In most cases, its side effects are limited to local reactions to the active component2.

Xylometazoline can cause irritation and dryness of the mucous membrane, burning and tingling in the nose, which causes sneezing attacks and excessive discharge of liquid mucus from the nose2.

With prolonged and frequent use of drops or spray, the development of rebound syndrome and tachyphylaxis is possible2,3. The rebound effect may occur several hours after using the decongestant. The reason for the reaction is the activation of b-adrenergic receptors. When they are stimulated, the blood vessels dilate, swelling of the mucous membrane occurs and nasal breathing becomes difficult3.

The “rebound” syndrome encourages the patient to use the medicine more often and in larger doses, which causes addiction. Over time, the sensitivity of adrenergic receptors decreases, and this contributes to the development of tachyphylaxis - a noticeable decrease in the effectiveness of the drug3.

Frequent and long-term use of a decongestant can lead to changes in the mucous membrane of the nasal cavity - its thinning, death of ciliated epithelial cells and the development of drug-induced rhinitis2,3.

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Instructions for use of Xylometazoline (Method and dosage)

All forms of the drug are used intranasally.

Xylometazoline nasal drops 0.1% are used in adults, 1-2 drops at each turn three times a day.

The 0.1% spray is used in adults with 1 pump (corresponding to 0.1 mg) per stroke. The applicator is inserted, maintaining the vertical position of the bottle, and injected three times a day after 8-10 hours.

Gel 0.1% is used by adults, 2-3 drops of gel 3 times a day.

Considering the possibility of systemic adsorption and the occurrence of adverse reactions, the instructions for use of Xylometazoline must be strictly followed. Use the drug in any form of release for no more than 3-5 days. Should not be used for a long time or for chronic rhinitis. If crusts appear in the nose, it is better to use the drug in gel form. If a dose is missed, the next dose will not be doubled.

Literature

1. Xylometazoline. Active ingredients // Radar of Russia - https://www.rlsnet.ru/mnn_index_id_111.htm
2. Description of the drug Xylometazoline, based on the officially approved instructions for use of the drug // Vidal Directory - 2011. — https://www.vidal.ru/drugs/molecule/1121
3. Evdokimova A.I., Miroshnichenko N.A., Ovchinnikov A.Yu. Topical decongestants: myths and reality // Medical Council. - No. 12. – 2021. – pp. 40-43.
4. Karneeva O. V., Garashchenko T. I., Karpova E. P., Ryazantsev S. V., Nikiforova G. N., Geppe N. A., Gorelov A. V., Malakhov A. B., Kondurina E. G., Bakradze M.D., Kolosova N.G. Current trends and safety problems in the use of decongestants in childhood. Resolution of the expert council. Pediatrics (Appendix to the journal Consilium Medicum). 2018; 1:32-35. DOI: 10.26442/2413-8460_2018.1.32-35.
5. Instructions for medical use of the drug TIZIN® Classic.
6. Malakhov A.B. et al. Topical decongestants in the complex therapy of acute respiratory infections in children // Medical Council. - No. 14. — 2015
7. Instructions for medical use of the drug TIZIN® Expert.
8. Official website TIZIN ®, description of the drug TIZIN ® Expert.

Overdose

Manifested by symptoms: dilated pupils, cyanosis, nausea, vomiting, fever, tachycardia, arrhythmias, cardiac arrest, respiratory failure, hypertension, pulmonary edema, mental disorders. Drowsiness , bradycardia, apnea and coma indicate suppression of central nervous system function.

Treatment: gastric lavage, sorbents, artificial respiration, drugs to lower blood pressure, antipyretics and anticonvulsants.

Xylometazoline for children

For acute rhinitis in children, it is not advisable to use short-acting vasoconstrictors: Naphazoline, Tetrizoline, Ephedrine , since after their use there is recurrent swelling of the nasal mucosa. It is preferable to use long-acting drugs: Xylometazoline ( Dlyanos , Otrivin ), Oxymetazoline ( Nazivin ), Epinephrine ( Vibrocil ), which allows reducing the frequency of use.

Remember that the risk group for poisoning with imidazoline (Xylometazoline) drugs are children under 2 years of age. This drug is not recommended for use in newborns, infants, or children under 2 years of age. In rare cases, if there is no alternative, 0.05% drops are prescribed to children under 2 years of age.

For children over 2 years of age, only a 0.05% concentration of this drug is used, and it is necessary to strictly dose and observe the frequency of use.

From 2 to 6 years 0.05% drops, 1 - 2 drops per turn, twice a day, if necessary, use up to 3 times a day is acceptable. From 6 to 12 years old, you can use 0.05% drops and 0.05% spray, 2-3 drops or one injection at each turn, but no more than 3 times a day.

Children over 7 years old are prescribed 0.05% gel - placed 3-4 times a day deep into each stroke.

From 12 years old, 0.1% drops and spray are used.

It is necessary to take into account that frequent and long-term (more than 5 days, in some authors - more than 3 days) use of this drug can cause a pronounced decrease in local blood flow, as a result of which inadequate blood supply to the mucosa develops, up to its atrophy in the future. In this regard, you should not use the drug in any form of release more than 3 times a day or for more than 3-5 days.

If there is a need to use nasal drops at an earlier age, then Vibrocil is approved for use in children from infancy. Nazivin is also used , from the age of 1 year - Nazivin 0.025%.

What are xylometazoline preparations used for?

Decongestants are drugs that can eliminate swelling of the mucous membrane and nasal congestion, and restore nasal breathing4. Xylometazoline belongs to this category of drugs. It has a stimulating effect on α-adrenergic receptors, constricts the blood vessels of the nasal mucosa and limits blood flow to it, thereby helping to reduce swelling and facilitate breathing through the nose1,2.

Difficulty in nasal breathing not only affects well-being and quality of life. It can disrupt normal aeration - the natural exchange of air between the nasal cavity, paranasal sinuses and middle ear. The worse the cavities are “ventilated”, the more mucus is formed in them and the slower its outflow occurs. Stagnation of mucus, in turn, promotes the proliferation of microorganisms and often leads to inflammatory diseases - sinusitis, sinusitis and otitis media. In addition, nasal congestion and mouth breathing aggravate respiratory infections. If the air does not pass through the “nasal filter,” pathogens easily penetrate the lower respiratory tract and lungs, causing inflammation – bronchitis and pneumonia.

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Indications

The main cause of nasal congestion is rhinitis3. Proper, controlled use of decongestants prevents complications of rhinitis and speeds recovery3,4.

According to the instructions for use2, xylometazoline can help with the following diseases:

• acute respiratory infectious diseases accompanied by inflammation of the nasopharynx (runny nose);
• acute sinusitis (inflammation of the paranasal sinuses, sinusitis);
• seasonal allergic rhinitis (hay fever);
• otitis (inflammation of the middle ear).

Xylometazoline can also be prescribed by otolaryngologists before diagnostic and therapeutic procedures to reduce swelling of the nasal mucosa2.

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Application, dosage regimen

Xylometazoline preparations are intended for intranasal administration - instillation into the nose. The dose and frequency of use of the drug depend on the chosen dosage form, the concentration of the active substance and the age of the patient.

In the pharmacy chain you can find sprays and drops for the common cold containing xylometazoline in the following concentrations:

• 0.05% (500 mg of substance in 1 ml of solution);
• 0.1% (1 mg in 1 ml).

The first is more often prescribed to children, the second to adults1,2.

Before using xylometazoline drops/spray, it is necessary to clear the nasal passages of mucus and crusts. You can rinse your nose with a syringe or remove mucus with an aspirator. Then drip/inject the medicine into both nostrils.

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Standard dosage regimen

Adults and children over 6 years of age: one injection or 2-3 drops of a 0.1% xylometazoline solution into each nasal passage. To reduce nasal congestion, the procedure should be repeated 3 times during the day5.

For symptomatic treatment of children from 2 to 6 years old, a 0.05% xylometazoline solution is used. For rhinitis and other indications, the drug is injected once or instilled 1-2 drops 1-2 times a day5.

Important! The optimal dosage regimen for xylometazoline preparations is determined by the doctor. During treatment, it is necessary to follow its recommendations on the choice of dosage form, dosage and duration of use of the drug. To relieve nasal congestion and reduce the risk of side effects, the drug should be used for no more than 5-7 days in a row2,5.

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Xylometazoline analogues

Level 4 ATX code matches:
Xymelin Eco

Xymelin

Nazivin

Galazolin

Lazorin

Nazivin Sensitive for children

Otrivin

Naphthyzin

Sanorin

Knoxprey

For the nose

Lazolvan Rino

Afrin

Rhinorus

Eucazoline Aqua

Rinazolin

Grippostad Reno

Farmazolin

Nazol Advance

Nazol Baby

Analogues: Farmazolin, Farmazolin N, Galazolin, Xylo-mefa, Meralis, Otrivin, Otrivin with menthol and eucalyptus, Tizin Xylo .

Differences between Xylometazoline and Oxymetazoline

Xylometazoline and Oxymetazoline belong to the group of imidazolines, acting on α1 and 2 adrenergic receptors and have a longer effect than drugs of the phenylephrine : 10 hours of action.

For long-acting drugs, the effect does not occur immediately, but after 10–15 minutes. The long-term vasoconstrictive effect allows them to be used 1-2 times a day, provides restful sleep, but causes a greater risk of damage to the mucous membrane, including atrophy. However, if you do not exceed the period of continuous use (3-4 days), the risk is reduced.

The difference between Xylometazoline and Oxymetazoline is only in the duration of action. Xylometazoline is a drug with an average duration of action of 8-10 hours. Known preparations of xylometazoline: Xylen, Rinostop, Galazolin, Xymelin, Otrivin, Farmazolin, Dlyanos, Tizin-Xylo . Oxymetazoline is a long-acting drug - up to 12 hours. Preparations based on it: Nazivin, Rinazolin, Nazol, Noxprey . To prolong the vasoconstrictor effect, high-molecular prolongators (cellulose ethers, alginates) are added to the composition.

Features of the mechanism of action

It is known that various receptors of the sympathetic nervous system are present in the nasal cavity, and their representation and functions differ significantly. Thus, alpha2-adrenergic receptors regulate the volume of the vascular network of the nasal turbinates, and beta2-adrenergic receptors change the intensity of blood flow in the mucous membrane. The nasal mucosa also contains alpha1-adrenergic receptors, which, like alpha2-receptors, affect the width of the lumen of blood vessels [2].

Various local vasoconstrictors can act on alpha1- and alpha2-adrenergic receptors, which largely determines their properties. It is known that stimulation of the former is accompanied by a mild vasoconstrictor effect due to a predominant effect on the “obturator” throttle vessels and does not cause a significant decrease in blood flow in the nasal mucosa. Therefore, the therapeutic effect of alpha1-adrenergic agonists is less pronounced and less durable compared to alpha2-adrenergic agonists [2].

Both naphazoline and xylometazoline are stimulants primarily of alpha2-adrenergic receptors, and the severity of the vasoconstrictor effect of both drugs is comparable [2].

Reviews

Reviews about the use of the drug are mostly positive, everyone notes the effectiveness and duration of action, which is very convenient during the working day and throughout the night.

The drug in drops is difficult to dose, since part of the solution enters the pharynx, so side effects occur more often. In this regard, it is safer to use a metered spray. Many people note undesirable reactions: insomnia, neurosis, anxiety.

Another unpleasant phenomenon that is often written about in reviews is rebound congestion, the so-called “ medicinal rhinitis ”. Long-term use of the drug leads to the fact that vasoconstriction is replaced by increased blood flow and the resumption of secretions. Nasal congestion returns and cannot be treated with medication. With prolonged use, atrophy of the nasal mucosa . To avoid these side effects, it is recommended to limit the use of the drug to three days.

pharmachologic effect

The mucous membrane of the nasal cavity is penetrated by many small blood vessels. Two parts of the nervous system are responsible for their tone. Parasympathetic dilates blood vessels, increases blood flow to tissues and stimulates mucus secretion. The sympathetic part activates α(alpha)-adrenergic receptors, located in the walls of blood vessels and responding to adrenaline. When they are stimulated, vasoconstriction occurs, blood flow accelerates and nasal secretion decreases3.

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Xylometazoline price, where to buy

You can buy the drug in Moscow in pharmacies provided on the website of the Federal Information Service www.poisklekarstv.ru. Price of Xylometazoline drops 0.1% from 64 rub. up to 70 rub., in the form of a spray 0.1% from 56 rub. up to 64 rub.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine

ZdravCity

• Xylometazoline drops called.
  0.1% fl. 10ml LLC Vips-Med 28 rub. order
• Rinostop Double relief for runny nose 6+, nasal spray + xylometazoline, 15 mlPharmstandard-Leksredstva OJSC

  RUB 158 order

• Xylometazoline nasal spray. 0.1% fl. 10ml LLC Vips-Med

  64 RUR order

• Xylometazoline spray called. 0.05% fl. 10ml LLC Vips-Med

  67 RUR order

• Xylometazoline drops called. 0.05% fl. 10ml LLC Vips-Med

  26 RUR order

Pharmacy Dialogue

• Xylometazoline eucalyptus (spray called 0.1% 10ml)VIPS-Med

  59 RUR order

• Xylometazoline (spray called 0.1% 10ml)VIPS-Med

  60 rub. order

• Xylometazoline (spray called 0.1% 10ml)Ozone LLC

  81 RUR order

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Pharmacy24

• Xylometazoline 0.1% 10 ml spray Flumed-Pharm TOV, Republic of Moldova
  38 UAH.order
• Xylometazoline 0.05% 10 ml spray Flumed-Pharm TOV, Republic of Moldova

  38 UAH order

TIZIN® - xylometazoline preparation

The TIZIN® line includes several drugs. TIZIN® Classic spray in the form of a 0.05% xylometazoline solution is intended for children from 2 to 6 years old, 0.1% solution for adults5.

The drug can begin to act within 2-5 minutes5, reduces swelling of the nasal mucosa and helps fight nasal congestion for 10 hours6,8.

TIZIN® Expert spray is also available in dosages for children from 2 to 6 years old and for children over 6 years old and adults7. In addition to xylometazoline, it contains hyaluronic acid, which helps moisturize the nasal mucosa and helps it recover6,7. The drug does not contain preservatives. The spray is equipped with a special SILVER TURBO spiral with silver ions, which prevents bacteria from penetrating inside. Thanks to this, the medicinal solution remains sterile throughout the entire period of use.

The information in this article is for reference only and does not replace professional advice from a doctor. To make a diagnosis and prescribe treatment, consult a qualified specialist.

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