Metazolin what is it

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Xylometazoline

Description current as of 02/13/2015

  • Latin name: Xylometazoline
  • ATX code: R01AA07
  • Active ingredient: Xylometazoline
  • Manufacturer: Update PFK (Russia), Lance-Pharm LLC (Russia), VIPS-MED Firm (Russia), Glaxo Wellcome Poznan (Poland); Pharmacies 36.6 (Russia).

Table of contents:

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 gel contains 1 mg. Carbomer, glycerol, ammonia solution, propylene glycol ethanol, methylparaben, propylparaben, water as auxiliary components.

Release form

Drops in concentrations of 0.05% and 0.1%, nasal gel 0.1%, spray 0.05% and 0.1%.

pharmachologic effect

Pharmacodynamics and pharmacokinetics

Xylometazoline is an imidazoline derivative. 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 action appears in minutes and lasts for hours.

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.

Side effects

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

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.

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.

Interaction

Medicines that stimulate the sympathetic system enhance the effect. The drug should not be prescribed with MAO inhibitors and antidepressants, since their interaction provokes a hypertensive crisis.

Terms of sale

Available without a prescription.

Storage conditions

At temperatures below 250C.

Best before date

Xylometazoline during pregnancy

Xylometazoline can be used to reduce nasal discharge during pregnancy. Experience with the use of this drug in pregnant women is limited, but short-term use in minimal doses is allowed under strict medical supervision.

Oxymetazoline, despite the fact that it is also an imidazoline derivative, is contraindicated during pregnancy.

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 you to reduce 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 in each 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. In infants, Nazivin 0.01% is also used, from the age of 1 year - Nazivin 0.025%.

Xylometazoline analogues

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 group: 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.

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 appears. To avoid these side effects, it is recommended to limit the use of the drug to three days.

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 Russia Russia

WER.RU

ZdravZone

Education: Graduated from the Sverdlovsk Medical School (1968 - 1971) with a degree in Paramedic. He graduated from the Donetsk Medical Institute (1975 - 1981) with a degree in epidemiologist and hygienist. He completed his postgraduate studies at the Central Research Institute of Epidemiology in Moscow (1986 - 1989). Academic degree - Candidate of Medical Sciences (degree awarded in 1989, defense - Central Research Institute of Epidemiology, Moscow). Completed numerous advanced training courses in epidemiology and infectious diseases.

Work experience: Work as head of the disinfection and sterilization department 1981 - 1992. Work as head of the department of especially dangerous infections 1992 - 2010. Teaching activity at the Medical Institute 2010 - 2013

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All materials presented on the site are for reference and informational purposes only and cannot be considered a treatment method prescribed by a doctor or sufficient advice.

The site administration and the authors of the articles are not responsible for any losses and consequences that may arise when using the site materials.

Source: http://medside.ru/ksilometazolin

Xylometazoline (xylometazoline hydrochloride) – instructions for use, indications, contraindications, side effects, analogues, reviews, prices

What kind of drug is xylometazoline?

  • Purification of inhaled air. The cilia of the ciliated epithelium capture dust particles and other small particles that enter the nasal cavity with inhaled air, and then ensure their removal. This is also facilitated by the layer of mucus covering them, produced by special cells of the mucous membrane.
  • Warming the inhaled air. As the inhaled air passes through the nasal passages, it comes into close contact with the warm blood in the small blood vessels, causing it to heat up.
  • Humidification of inhaled air. This process occurs due to the contact of air with the moist surface of the mucous membrane.

If any strong irritant comes into contact with the nasal mucosa, this can cause the activation of protective reflexes ( for example, sneezing ). If viruses or bacteria act as irritants, they can penetrate into the deeper layers of the mucous membrane and infect it ( destroy its cells ). In this case, the body’s immune ( protective ) system is activated, aimed at destroying the infectious agent. One of the manifestations of the immune response is a pronounced expansion of the blood vessels of the nasal mucosa and an increase in the permeability of the vascular walls, as a result of which a certain proportion of the liquid part of the blood can exit the vascular bed into the intercellular space. All this contributes to the development of pronounced swelling of the mucous membrane ( that is, an increase in its thickness ), as a result of which it can completely block the nasal passages. Also, during infection ( especially with a viral infection ), mucus-producing cells are activated, resulting in a significant increase in its quantity. The described processes are the direct cause of nasal congestion during colds and other diseases.

Composition, release forms and analogues of xylometazoline

  • in the form of nasal drops;
  • in the form of a nasal spray;
  • in the form of a nasal ointment ( gel ).

The active component of all forms of the drug is xylometazoline hydrochloride. Auxiliary components include purified water, as well as various stabilizers.

Xylometazoline nasal drops

Xylometazoline nasal spray

Xylometazoline ointment ( gel )

Instructions for use of the drug xylometazoline

The mechanism of action of xylometazoline

  • Constriction of blood vessels. This leads to a decrease in their blood supply, as a result of which the volume ( mass ) of the mucous membrane is significantly reduced. The vasoconstrictor effect of the drug develops quite quickly, so within 2 to 4 minutes after use you can feel an improvement in nasal breathing.
  • Reduced permeability of the vascular wall. As a result of the narrowing of the blood vessel, its wall becomes denser, which prevents the liquid part of the blood from leaving the vascular bed. As a result, soon after using the drug, swelling of the mucous membrane is eliminated, which also facilitates nasal breathing.
  • Improving ventilation of the nasal passages. This is a secondary effect due to the vasoconstrictor effect of the drug. As a result of constriction of the vessels of the nasal mucosa, oxygen access to the nasal passages and to the paranasal sinuses ( intraosseous cavities located around the nose and also covered with mucous membrane ) improves, which inhibits the development of infection and promotes a speedy recovery.

The duration of action of the drug depends on the form of its release. For example, when using drops, the vasoconstrictor effect persists for 6 to 8 hours. Xylometazoline is then released from specific receptors, causing the blood vessels to dilate and fill with blood again. At the same time, the mucous membrane swells again, that is, nasal congestion resumes.

Indications for the use of xylometazoline

  • Acute rhinitis. Acute rhinitis ( inflammation of the nasal mucosa ) usually occurs when the nasal mucosa is damaged by viruses ( for example, colds, flu ) or bacteria. Rhinitis can also develop with some other infectious and inflammatory diseases ( for example, measles, scarlet fever, diphtheria, and so on ). Rhinitis manifests itself as pronounced swelling of the nasal mucosa and rhinorrhea, that is, the release of a large amount of mucus from the nasal passages.
  • Acute nasopharyngitis. This term refers to inflammation of the mucous membrane of the nasopharynx, which develops as a result of exposure to infectious ( viral, bacterial ) or non-infectious ( allergic, chemical ) factors. In addition to nasal congestion, infectious nasopharyngitis can be manifested by general weakness, headaches, cough, increased body temperature to 38 - 39 degrees, and so on.
  • Acute sinusitis. Sinusitis is inflammation of the paranasal sinuses. These include the maxillary sinuses ( when they are damaged, sinusitis develops ), the frontal ( frontal ) sinuses ( when they are damaged, frontal sinusitis develops ), the sphenoid sinus ( sphenoiditis ) or the cells of the ethmoid bone ( ethmoiditis ). The mechanism of damage to the paranasal sinuses is also associated with swelling of the mucous membrane. As a result, the entrance to the sinuses, through which their ventilation is normally carried out, is blocked. This creates favorable conditions for the development and spread of infection.
  • Hay fever ( seasonal allergic rhinoconjunctivitis ). This disease develops as a result of increased sensitivity of the body to the pollen of certain plants. The immediate cause of the development of allergic reactions is the penetration of pollen microparticles into the patient’s nasal cavity along with the inhaled air. When they come into contact with the mucous membrane, a whole complex of immune reactions is triggered, resulting in dilation of blood vessels and swelling of the mucous membrane itself. Other manifestations of hay fever may include redness of the eyes, increased tearing, and increased body temperature. Characteristic of this pathology is the fact that all signs of the disease occur at the same time of year, when certain plants bloom.
  • Other allergic rhinitis. Allergic swelling of the nasal mucosa can be caused not only by plant pollen, but also by other allergens. It could be dog hair, house dust, and so on. The mechanism of development of nasal congestion in this case is also due to swelling of its mucous membrane.
  • Otitis media Otitis media is characterized by inflammation of the mucous membrane of the middle ear ( tympanic cavity ). The cause of the development of this pathology is usually infectious and inflammatory processes in the nasopharynx or oropharynx. Through a special auditory tube ( which connects the tympanic cavity with the pharynx, ensuring the normal functioning of the hearing organ ), infectious agents ( bacteria, viruses ) can penetrate into the tympanic cavity, which will lead to the development of an inflammatory process in it. Also, the mucous membrane of the auditory tube itself swells, which further aggravates the course of the disease. The purpose of using xylometazoline in this case is to narrow the vessels of the nasopharynx. This can help relieve swelling in the area of ​​the auditory tubes and restore normal ventilation of the tympanic cavity, which is a necessary condition in the treatment of otitis media.
  • Eustachite. This is an infectious-inflammatory disease characterized by inflammation of the auditory ( Eustachian ) tube connecting the pharynx to the tympanic cavity. It manifests itself as congestion in one or both ears, sore throat, and when the nasal mucosa is involved in the pathological process – runny nose and nasal congestion.
  • Preparation for medical procedures. When performing some diagnostic measures ( for example, rhinoscopy - examination of the nasal mucosa using special instruments ), difficulties may arise due to swelling of the mucous membrane. In such cases, the use of xylometazoline allows you to temporarily narrow the blood vessels in the nasal cavity, which reduces the risk of bleeding ( which can occur as a result of accidental trauma to the mucous membrane during the examination ), and also allows the doctor to more accurately examine the areas of the nasal cavity of interest.
  • Stopping nosebleeds. The use of this drug for moderate nosebleeds ( for example, after injury ) leads to a narrowing of the blood vessels of the mucous membrane, which helps to stop the bleeding as quickly as possible.

Contraindications to the use of xylometazoline

  • In case of hypersensitivity to the drug. Hypersensitivity is characterized by the fact that when the body comes into contact with this substance, extremely pronounced allergic reactions are triggered, which can manifest as severe swelling of the mucous membrane, redness of the skin in the facial area, hives, or even anaphylactic reactions. It is important to remember that in various commercial preparations, xylometazoline is produced together with some auxiliary components, to which you may also be allergic.
  • For arterial hypertension. This disease is characterized by a persistent increase in blood pressure of more than 140 mmHg. Xylometazoline, having a vasoconstrictor effect, can aggravate the course of this pathology ( vasoconstriction at the systemic level will lead to an even greater increase in blood pressure ).
  • With tachycardia ( increased heart rate more than 90 beats per minute ). Tachycardia itself can occur under certain physiological conditions ( for example, after exercise ), which is not a contraindication to the use of xylometazoline. At the same time, in case of tachycardia combined with certain diseases of the cardiovascular system ( for example, coronary heart disease ), the use of this drug is not recommended, as this can lead to the development of complications.
  • With severe atherosclerosis. This disease is characterized by impaired elasticity of large arteries ( blood vessels through which blood flows from the heart to all organs and tissues ). In most cases, atherosclerosis is combined with increased blood pressure, and therefore the use of xylometazoline for this pathology is also not recommended.
  • With glaucoma. Glaucoma is characterized by a pronounced increase in intraocular pressure, resulting from a violation of the outflow of intraocular fluid ( normally it flows through special channels located in the anterior part of the eye at the base of the iris ). The use of xylometazoline can lead to pupil dilation, which, in turn, can contribute to blocking the outflow pathways of intraocular fluid and further increasing intraocular pressure.
  • For atrophic rhinitis. This disease is characterized by atrophy ( thinning, destruction ) of the nasal mucosa. The cause of dryness and a feeling of nasal congestion in this case is a violation of the protective functions of the mucous membrane, as a result of which hard crusts form on it, blocking the nasal passages. The use of vasoconstrictor drugs in this case is ineffective, since with atrophic rhinitis the number of vessels in the mucosa itself is significantly reduced.
  • With thyrotoxicosis. Thyrotoxicosis is characterized by a pronounced increase in the concentration of thyroid hormones in the blood. The use of alpha-agonists in this case can provoke the development of adverse reactions from the cardiovascular system.
  • For diabetes mellitus. Alpha adrenergic receptors are found not only in the walls of blood vessels, but also in some other tissues, including pancreatic cells. Their stimulation can reduce the amount of insulin produced in the gland ( a hormone necessary for the normal absorption of glucose by cells ), which can aggravate the course of diabetes.
  • For prostate adenoma. This disease is characterized by an increase in the size of the prostate gland, which in severe cases may be accompanied by difficulty urinating ( due to compression of the urethra ). The use of alpha-adrenergic agonists can aggravate this process, and therefore they should be used with extreme caution for prostate adenoma ( for short periods of time, without exceeding the dose prescribed by the doctor ).

Xylometazoline during pregnancy and breastfeeding

Dosage and method of use of xylometazoline

Directions for use and doses

Before using the drug, the patient should lie on his back or sit on a chair and tilt his head back. Then you should place the tip of the bottle above the nostril ( without inserting it into the nostril ) and lightly press on it, instilling 1 - 3 drops of the drug into each nasal passage. After administering the drug, you should hold your head in a tilted position for 2 to 3 minutes until the active substance takes effect. The medication should be used 2–4 times a day.

Before use, you need to clean the nasal passages, remove the protective cap from the bottle and insert the tip into the nasal passage to a depth of about 1 cm. After this, exhale completely and then inhale deeply ( through the nose ). While inhaling, you need to sharply press on the bottle, injecting the drug deep into the nasal passage.

For medicinal purposes, 1–2 injections should be performed in each nasal passage 2–3 times a day.

The drug is available in special bottles equipped with a dispenser. Before use, remove the protective cap from the tip and press the dispenser several times until the gel appears. After this, you should insert the tip into the nasal passage ( to a depth of about 1 - 1.5 cm ) and press the dispenser one more time. Then you should insert the tip into the other nostril and also press the dispenser only 1 time.

The duration of action of the drug is 8–10 hours, so it should be used no more than 2 times a day.

It is important to note that when using xylometazoline, the drug should be injected into both nostrils, even if the nose is blocked on only one side. This is explained by the fact that when the drug is administered only into the blocked nasal passages, the vessels in them will narrow, but this will result in a reflex vasodilation and swelling of the mucous membrane on the other side, as a result of which the nasal passages will also be blocked.

Xylometazoline for children

  • Children under 6 years old - only 0.05% solution in the form of drops or spray, and the frequency and duration of use are determined by the severity of the disease.
  • Children from 6 to 12 years old - 0.05% or 0.1% solution in the form of drops, spray or gel.
  • Children over 12 years of age and adults – 0.1% solution in any form.

Side effects of xylometazoline

  • Dryness of the nasal mucosa. As a result of the narrowing of blood vessels, the amount of mucus produced may decrease, causing the mucous membrane to “dry out.”
  • Irritation of the nasal mucosa. This effect may manifest itself as itching or burning in the nasal cavity. The development of these reactions is associated with dryness of the nasal mucosa, as well as ( possibly ) with the irritating effect of xylometazoline itself.
  • Paresthesia in the area of ​​the nasal mucosa. Paresthesia is an unpleasant sensation of tingling, coldness or crawling. The development of this phenomenon when using xylometazoline may be associated with damage to the sensitive nerve fibers of the nasal cavity as a result of disruption of their blood supply.
  • Increased mucus secretion. This is an abnormal ( atypical ) reaction that is sometimes observed with xylometazoline.
  • Sneezing. This is a protective reflex aimed at removing any foreign particles from the nasal cavity. When using xylometazoline, its microparticles can irritate sensitive nerve endings, triggering the sneeze reflex.
  • Development of tolerance. This phenomenon is characterized by a decrease in the sensitivity of the nasal mucosa to the vasoconstrictor effect of the drug. This is due to the fact that with prolonged stimulation of alpha-adrenergic receptors, their total number decreases. As a result, in order to achieve the same therapeutic effect, it is necessary to constantly increase the dose of the medication.
  • The phenomenon of cancellation ( ricochet ). The essence of this phenomenon is as follows. If, after prolonged use of xylometazoline, its use is abruptly stopped, this will lead to even more pronounced swelling of the mucous membrane, which will persist for several days.

Systemic side effects of xylometazoline may include:

  • Increased blood pressure. May occur in patients with arterial hypertension with prolonged or too frequent use of the drug.
  • Arrhythmia ( abnormal heart rate ). Rapid heartbeat can also occur when taking too large doses of the drug.
  • Headache. Headaches may be associated with impaired blood supply to the brain, which may be due to the effect of the medication on the blood vessels.
  • Visual impairment. Using the drug for severe glaucoma can lead to a critical increase in intraocular pressure, which will cause damage to the retina ( the layer of photosensitive nerve cells that perceive light rays ).
  • Vomiting. Vomiting is a rare side effect that develops with long-term use of the medication.
  • Depression ( persistent decrease in mood ). Depression can develop with prolonged and frequent use of the drug in large doses.

Xylometazoline addiction

Xylometazoline overdose

  • increased heart rate;
  • increased blood pressure;
  • drowsiness;
  • disturbance of consciousness;
  • breathing problems ( rare ).

The development of the described reactions is more typical for children, since when the same amount of solution is swallowed, the final concentration of xylometazoline in the child’s blood will be higher than in the blood of an adult ( due to the smaller volume of circulating blood ).

Price of the drug xylometazoline

Average cost of the drug

Xylometazoline nasal drops

Xylometazoline nasal spray

Galazolin ( xylometazoline ) nasal gel

Reviews of xylometazoline

Nasal drops are the most common and accessible form of the drug, due to its relatively low cost ( 3 times cheaper than a spray and 6 times cheaper than a gel ). However, despite the low price, the effectiveness of the vasoconstrictor effect of xylometazoline in the form of drops is not inferior to other forms of the drug, which is noted by almost everyone who has used it.

The spray is also quite affordable in terms of price, but is significantly superior to nasal drops in terms of ease of use. Most people note that applying the spray using a special spray nozzle is much more convenient than throwing back your head and putting drops into your nose, while trying to count their number.

Reviews about this ointment are mostly positive, since the drug has a quick and pronounced effect in cases where drops or spray do not help. Negative reviews are mainly associated with the high cost of the medication.

What is the difference between xylometazoline and oxymetazoline?

Drops, spray and ointment.

Only for application to the nasal mucosa.

There are nasal drops, as well as eye drops, that can be instilled into the conjunctival sac for swelling and inflammation of the conjunctiva ( that is, conjunctivitis ). The drug is indicated for use in conjunctivitis caused by allergic reactions, exposure to smoke or dust in the eyes, exposure to strong winds, prolonged exposure to direct sunlight, and so on.

Rapid development of the vasoconstrictor effect

Not recommended for use in children under 2 years of age.

Nasal drops are contraindicated in children under 1 year of age, while nasal spray can only be used after 6 years of age. Eye drops can also be used to treat children over 6 years of age.

Use during pregnancy and breastfeeding

Possible if a large amount of the drug is swallowed ( especially in children ).

Develops with long-term use of the drug.

Based on the above, it follows that to eliminate nasal congestion it is better to use xylometazoline, as it ensures a faster restoration of nasal breathing. In terms of effectiveness, indications, contraindications and adverse reactions, these drugs are similar.

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Metronidazole - instructions, use, reviews

Metronidazole (lat. Metronidazolum) is a broad-spectrum antimicrobial drug. According to its chemical structure, it belongs to the group of 5-nitroimidazole derivatives.

Shows activity against anaerobic bacteria and some protozoa. Available in the form of tablets, injections, suppositories and external gels. Used to treat bacterial and protozoal infections caused by microflora sensitive to its action.

Areas of application include surgery, gynecology, urology, gastroenterology and dermatology. The prescription of metronidazole for alcoholism leads to the formation of an aversion to alcoholic beverages.

Story

The prerequisites for the creation of the drug were exploratory studies in a number of imidazole compounds, begun by medical scientists in the 1950s. During the experiments, it turned out that some derivatives of 5-nitroimidazole (5-NIM) have antimicrobial properties.

In 1957, specialists from the French company Rhone Poulenc (now Sanofi) obtained a formula for metronidazole, for which high trichomanadocidal activity was established. In 1960, after a series of clinical trials, the drug entered the pharmaceutical market under the trade name Flagyl.

For a long time, metronidazole was considered exclusively as a treatment for trichomaniasis and a number of other protozoal diseases. However, in the 70s. Its antibacterial properties were accidentally discovered. It turned out that the compound is also highly effective against anaerobic bacteria. The drug began to be used to treat bacterial infections of the urinary tract, respiratory organs, skin and gastrointestinal tract.

After the expiration of patent protection, various pharmaceutical companies received the right to produce metronidazole. Its numerous generics have become available to patients: Trichopolum, Metronidazole, Metrogyl, Klion, etc.

In the 2000s. The list of indications for antimicrobial agents was expanded to include peptic ulcer of the digestive tract. It is believed that the bacterium Helicobater pylori, which is adversely affected by metronidazole, plays an important role in the development of this disease.

Properties

International nonproprietary name: metronidazole.

Chemical name according to IUPAC nomenclature: 2-(2-methyl-5-nitro-1H-imidazol-1-yl)-ethanol.

Molecular weight: 171.154

Metronidazole is a white or white with a greenish tint crystalline powder, poorly soluble in water and ethanol. Sparingly soluble in dimethylformamide. Stable in air. Melting point -ºС. Density - 1.45 g/cu. cm.

Carcinogenicity information

In 1985, the American FDA added metronidazole to the National Toxicology Program list as a drug of probable carcinogenicity to humans. The reason was a number of studies in which the drug demonstrated the ability to cause cancer in experimental animals.

Taking metronidazole with food provoked the development of lung carcinoma in mice of both sexes, lymphoma in female mice (Rustia and Shubik 1972, IARC 1977), as well as malignant tumors of the liver and pituitary gland in male rats (IARC 1982).

However, the connection between the use of metronidazole and the occurrence of cancer in humans remains unconfirmed. One of the studies (Beard et al. 1988) provided evidence that long-term use of the drug increases the risk of developing lung cancer in women. However, other studies (IARC 1987, Thapa et al. 1998) found no danger.

Despite conflicting information, in 2010 the International Agency for Research on Cancer, part of the World Health Organization, also included metronidazole in the List of Possible Human Carcinogens.

Application in different countries

Currently, metronidazole remains one of the most used antimicrobial drugs. It is included in international recommendations for the treatment of trichomoniasis, amebiasis, giardiasis and a number of anaerobic infections. The product is widely used in all countries of the world.

At the end of the 80s. Metronidazole has been added to the WHO List of Essential Medicines. In Russia it is included in the List of vital and essential medicines.

In the USA, the drug has been used since 1963. As of 2015, the FDA has approved 42 medications for sale, the active compound of which is metronidazole.

Due to potential carcinogenic properties, the drug is prohibited from being added to the feed of farm animals in the United States (Ordinance 21CFR530.41), Canada, Australia and the European Union. In Russia, the residual concentration of metronidazole in livestock products is subject to control.

Composition and release forms

The following dosage forms of metronidazole are registered in the Russian Federation:

  • 0.5% solution for infusion,
  • tablets containing the active substance 200, 250, 400, 500 or 600 mg,
  • film-coated tablets containing 200, 250, 400 or 500 mg of active substance,
  • suspension for oral administration with a concentration of the active component of 200 mg/5 ml,
  • vaginal suppositories 125, 250 and 500 mg,
  • vaginal tablets 250 and 500 mg,
  • 1% vaginal gel,
  • 1% gel for external use,
  • 1% cream for external use.

In pharmacies in other countries you can also find 0.75% gel for external use and 0.75% lotion.

Mechanism of action

Metronidazole has bactericidal and protistocidal effects. Once in the cells of bacteria and protozoa, the drug is exposed to special enzymes - nitroreductases. As a result of a series of chemical transformations, active metabolites are formed that block the synthesis of microbial DNA. This process leads to the death of pathogenic organisms.

Nitroreductases are present only in anaerobic bacteria and some protozoa, therefore metronidazole does not have a negative effect on aerobes and human cells. It has been established that the severity of the antimicrobial effect directly depends on the concentration of the drug in the blood.

The use of metronidazole for alcoholism is due to its ability to block the enzyme acetaldehyde dehyrogenase, which is involved in the breakdown of ethyl alcohol. This leads to an increase in the concentration of toxic metabolites of ethanol in the blood and the development of such unpleasant sensations as nausea, vomiting, rapid heartbeat, and heat in the face. As a result, the patient develops a conditioned reflex aversion to drinking alcoholic beverages.

There is also evidence that metronidazole stimulates regenerative processes in the body and increases the sensitivity of malignant tumors to radiation.

Spectrum of antimicrobial activity

The spectrum of action of the drug against pathogens of protozoal infections includes:

  • trichomonas (Trichomonas spp., Trichomonas vaginalis),
  • lamblia (Lamblia intestinalis),
  • amoebas (Entamoeba hystolytica),
  • balantidium (Balantidium coli),
  • leishmania (Leishmania spp.).

Among the bacteria that are sensitive to metronidazole are anaerobes:

  • clostridia (Clostridium spp.),
  • fusobacterium (Fusobacterium spp.),
  • bacteroides (Bacteroides spp.),
  • veillonella (Veillonela spp.),
  • prevotella (Prevotella spp.),
  • peptococci (Peptococcus spp.).

In terms of its antibacterial properties, metronidazole is comparable to clindamycin.

In combination with amoxicillin, the drug is detrimental to Helicobacter pylori (the antibiotic suppresses the development of resistance to metronidazole).

Metabolism and excretion

When administered internally, the drug is almost completely absorbed through the intestinal mucous membranes. Up to% of the dose taken enters the bloodstream. Maximum plasma concentration is achieved 1-2 hours after administration. Some metronidazole is slightly bound to blood proteins (no more than 20%).

The product is quickly distributed throughout the body, creating high concentrations in saliva, bile, vaginal mucus, skin, lungs, liver, brain and kidneys. Penetrates through the blood-brain and placental barriers.

When used vaginally and rectally, the drug is also well absorbed from the mucous membranes, providing both local and systemic effects.

Metabolized in the liver to hydroxy derivatives. Metabolites exhibit similar antimicrobial activity.

Up to 80% of metronidazole is excreted in the urine, the rest through the intestines. The half-life is 6-10 hours, in newborns - up to 24 hours.

With long-term treatment, the drug may accumulate in tissues.

Indications

Metronidazole is effective against various protozoal and bacterial infections:

  • intestinal and extraintestinal amebiasis,
  • giardiasis,
  • trichomoniasis in men and women (including asymptomatic forms),
  • balantidiaze,
  • cutaneous leishmaniasis,
  • anaerobic skin infections (including acne vulgaris),
  • infections of soft tissues and joints,
  • infections of the pelvic organs (endometritis, infected abortion, etc.),
  • bacterial vaginosis,
  • abdominal infections (peritonitis),
  • endocarditis,
  • respiratory infections (lung abscess, aspiration pneumonia),
  • meningitis,
  • oral infections,
  • pseudomembranous and necrotizing colitis.

The drug is also used for peptic ulcers of the digestive tract and alcoholism.

Contraindications

Metronidazole is not prescribed for the following conditions:

  • allergic reactions to 5-nitroimidazole derivatives,
  • organic lesions of the central nervous system,
  • severe liver failure,
  • leukopenia.

Use during pregnancy and breastfeeding

There have been no adequate studies on the use of metronidazole in pregnant women. Under the strict supervision of a doctor, therapy is permissible in the 2nd and 3rd trimesters of pregnancy. The drug is absolutely contraindicated in the 1st trimester. When treating during lactation, breastfeeding is recommended to be interrupted.

In the USA, the drug was assigned safety category B (meaning that no negative effects on the fetus were found when tested on animals).

Impact on the ability to drive vehicles and other complex mechanisms

The drug may reduce the speed of mental reactions, so during treatment you should avoid driving a car and engaging in potentially hazardous activities.

Directions for use and doses

Metronidazole is used orally, parenterally, intravaginally, rectally and externally.

For trichomoniasis, adults are prescribed 0.25-0.5 g of the drug orally 2-3 times a day. The course of treatment is 5-7 days. Children are recommended 0.25-0.5 g per day, divided into 3 doses. Vaginal tablets are administered once a day for a week. To avoid reinfection, partners are treated simultaneously.

For giardiasis, adults are prescribed 0.75-2 g of the drug per day orally, children - 0.5-1.2 g. The daily dose is divided into 2-3 doses. The duration of treatment is 5-7 days.

To treat amebiasis, tablets or infusions are used. Adults are recommended 0.75-2.25 g of metronidazole per day, children - 0.25-0.5 g. The course of treatment is 10 days.

For cutaneous leishmaniasis, it is enough for adults to take 0.2 g of the drug orally 4 times a day, for children - 0.1-0.2 g 3 times a day for 7 days. After this, a one-week break is taken and therapy is continued for another 14 days.

For aerobic infections, doses range from 1.2 to 1.8 g per day for adults and from 0.25 to 1.2 g for children. If necessary, the drug is prescribed rectally (in the form of suppositories) or parenterally.

For bacterial vaginosis, suppositories or vaginal tablets are prescribed - 1 suppository/tablet at night for 10 days.

For skin diseases, external gels and creams are applied no more than 2 times a day.

For alcoholism, tablets are taken at a dose of 0.5-0.75 g per day after meals for 3 days. If well tolerated, the dose is increased to 1.5 g and therapy is continued for another 10 days. Then the daily amount of the drug is again reduced to 0.5 g and treatment is continued for up to six months.

Side effects

When used in therapeutic doses, metronidazole is well tolerated by most patients. Adverse reactions occur in no more than 1-10 cases out of 1000.

When used internally, the following may be observed:

  • nausea,
  • diarrhea,
  • a metallic taste or dry mouth,
  • stomach ache,
  • headache,
  • dizziness,
  • convulsive states,
  • lethargy,
  • sleep disorders,
  • impaired coordination of movements,
  • allergic reactions (in the form of rash, redness of the skin, nasal congestion, joint pain),
  • decrease in the level of leukocytes and neutrophils in the blood,
  • urinary incontinence,
  • cystitis,
  • dark coloration of urine.

In combination with amoxicillin, the drug can provoke:

When used parenterally, the following are possible:

  • phlebitis,
  • pain and redness at the injection site.

External forms sometimes provoke:

With intravaginal administration the following may be observed:

  • swelling of the vulva,
  • itching in the vagina,
  • increased frequency of urination,
  • increased secretions.

Negative phenomena disappear after completion of the course of therapy.

Overdose information

If recommended doses are exceeded, poisoning with internal forms of metronidazole is possible. The condition is manifested by nausea, abdominal pain, vomiting, convulsive reactions, and weakness. There are no specific antidotes. Treatment is carried out symptomatically.

special instructions

When treating trichomoniasis, it is necessary to abstain from sexual intercourse. Simultaneous therapy of both partners is required.

When taking metronidazole for a long time, blood counts should be monitored.

A month after completion of treatment for giardiasis, it is necessary to take 3 stool tests at intervals of 3-4 days.

If dizziness or muscle weakness occurs, the drug should be discontinued.

During treatment, the development of candidiasis is possible, therefore, for prevention purposes, simultaneous use of antifungal drugs is recommended.

Metronidazole is not prescribed in combination with amoxicillin to children under 18 years of age.

Alcohol intake is prohibited during therapy.

When using external gels and creams, avoid contact with the eyes.

Therapy should be carried out under strict medical supervision in patients taking corticosteroids.

Interaction with other drugs

Metronidazole potentiates the effects of sulfonamides and indirect anticoagulants (warfarin, etc.).

Cimetidine increases the adverse reactions of the drug.

Phenobarbital and other agents that activate microsomal enzymes in the liver accelerate the elimination of metronidazole from the body.

Combination therapy with disulfiram (“Teturam”, etc.) leads to increased negative neurological reactions.

It is not recommended to take the drug simultaneously with muscle relaxants and lithium preparations.

Vacation conditions

All dosage forms of metronidazole, with the exception of cream and gel for external use, are available with a prescription.

Storage

In a dry place, protected from light, at a temperature not exceeding 25ºС. Keep away from children.

Internal forms in pharmacies and medical institutions are stored according to the conditions of List B.

Best before date

For tablets - 3-5 years (depending on the manufacturer).

For infusion solutions - 2-3 years.

For suppositories and vaginal tablets - 2-3 years.

For external dosage forms - 2-3 years.

Manufacturers

Metronidazole preparations are manufactured by various foreign and Russian enterprises. In total, there are more than 300 of its manufacturers in the world.

Various companies produce medicines under the brands “Metronidazole”, “Metronidazole hemisuccinate” or under brand names (“Flagil”, “Trichopol”, “Medazol”, “Metrobak”, etc.).

Some metronidazole drugs registered in the Russian Federation:

OJSC Uralbiopharm (Russia)

JSC Biokhimik (Russia)

Borisov Pharmaceutical Plant (Republic of Belarus)

Aquarius Enterprises (India), etc.

Other 5-nitroimidazole derivatives have effects similar to metronidazole:

All these drugs have the same mechanism of action, but differ in pharmacokinetic parameters and safety profile.

In comparison with its analogues, metronidazole is characterized by lower activity against protozoan microorganisms and a wide range of adverse reactions. However, despite this, according to WHO recommendations, it remains the drug of choice for the treatment of protozoal and anaerobic bacterial infections. All other representatives of the class are considered as reserve drugs, which should be used only if metronidazole is ineffective.

The main factor limiting the use of modern 5-NIM derivatives is the high risk of cross-resistance in pathogens. Failure to comply with international recommendations risks the loss of therapeutic alternatives for patients with protozoal diseases.

Comparative characteristics of metronidazole and some of its analogues (using the example of oral forms):

Source: http://farmamir.ru/2015/07/metronidazol-instrukciya-primenenie-otzyvy/