Pharmacological properties

Pharmacodynamics. xylomethazolinum is derivative imidazoline, a α-adrenergic sympathomimetic. directly excites α-adrenoceptors and narrows vessels. at topical administration reduces hypostasis of a mucous membrane of a nasopharynx and hyperaemia. restores passability of nasal ways and facilitates nasal breath by a dekongestation of a mucous membrane and improvement of a drainage of a secret.

Drug begins to work with

in 5–10 min., and the effect remains within several hours (on average 6–8 h).

At intranasal application the quantity of means which is absorbed can sometimes be sufficient for development of system effects, for example, from central nervous system and a cardiovascular system.

Pharmacokinetics. At topical administration xylomethazolinum in blood plasma is practically not defined (concentration in blood plasma below a limit definition).

Indication

Rhinedema in case of cold and a rhinorrhea with a large amount of liquid slime (vasomotorial rhinitis), allergic rhinitis.

Use Grippostad Rino is intended to

by

for nasal application.

Grippostad Rino of 0.05% nasal drops. To children aged from 1 up to 5 years (under supervision of adults) on 1–2 drops in each nasal course up to 1–2 times a day in case of need, but no more than 3 times a day.

to Children aged from 6 up to 11 years (under supervision of adults) on 2–4 drops in each nasal course up to 2–3 times a day in case of need, but no more than 3 times a day.

Grippostad Rino of 0.1% nasal drops, Grippostad Rino of 0.1% nasal spray. To adults and children 6 years are aged more senior — on 1 drop (on 1 injection) in each nasal course to 3 times a day as necessary.

Dose is defined by

depending on individual sensitivity and symptoms of a disease. Grippostad Rino is not recommended to apply more than 5 days. Before a new course of treatment it is necessary to take a break for several days.

not to exceed the recommended dose.

concerning duration of treatment needs to see a doctor.

treatment should be carried out by

in case of chronic rhinitises under medical control in view of risk of thinning of a mucous membrane of a nose.

Contraindication

Hypersensitivity to medicine components. "dry" inflammation of a mucous membrane of a nose with a korkoobrazovaniye (dry rhinitis). transsphenoidal hypophysectomy or existence in the anamnesis of transsphenoidal hypophysectomy and also surgical interventions with exposure of a firm meninx. closed-angle glaucoma. simultaneous treatment by Mao's inhibitors and during 2 weeks after the termination of their application. sharp coronary diseases, cardiac asthma. hyperthyroidism.

Due to the application a chloride benzalkoniya as preservative as a part of the medicine Grippostad of Rino cannot be applied at the known hypersensitivity to this substance.

Side effects

from heart: cardiopalmus, arrhythmia.

from nervous system: a headache, spasms (mainly at children), insomnia, increased fatigue, dizziness.

Respiratory, thoracic and mediastinal violations: burning and xeromycteria, sneezing, short wind, increase in a rhinedema (after medicamentous influence decreases), nasal bleeding.

from a cardiovascular system: AG.

General violations and condition of the injection site of medicine: increased fatigue, drowsiness.

from an organ of sight: disorder of vision.

from a digestive tract: nausea.

from the immune system: hypersensitivity reactions (Quincke's disease, skin rash, itch).

from mentality: excitement, a sleep disorder, hallucinations (mainly at children).

Special instructions

At medicament treatment the emergence of some side effects is possible

(especially asthmas). not to allow overdose.

Preserving means which contains in medicament (a benzalkoniya chloride), maybe, especially at prolonged use to cause a rhinedema. If such reaction is supposed (for example a continuous accumulation of slime in the nasal courses), it is necessary to use nasal medicaments which do not contain preservatives.

Grippostad Rino can be applied, having carefully weighed advantages of the expected advantage over possible development of undesirable effects in the following cases:

• at the patients treated by MAO inhibitors or other medicines with expected hypertensive effect;
• increased intraocular pressure, especially closed-angle glaucoma;
• some cardiovascular diseases (for example IBS, AG);
• pheochromocytoma;
• metabolic violations (for example hyperthyroidism, diabetes);
• porphyria;
• prostate hyperplasia.

Patients who often have a cold can apply

Grippostad Rino only under medical control because of risk of thinning of a mucous membrane of a nose.

At prolonged use or overdose can arise a reactive hyperemia and a repeated accumulation of slime in the nasal courses that causes narrowing of airways, in case of constant use of medicine can lead to a chronic accumulation of slime in a nose (medicamentous rhinitis) and even to a nose mucosal atrophy.

In mild cases can stop application of a sympathomimetic in one nasal course before disappearance of the above-stated symptoms to support a part of nasal breath.

Use during pregnancy and feeding by a breast. Drug should not be used during pregnancy.

In view of lack of data on whether active substance in breast milk is emitted, it is impossible to use medicament when feeding by a breast.

Children. Grippostad Rino of 0.05% not to apply nasal drops at children aged till 1 year. It is recommended to apply at children aged from 1 up to 11 years only under observation of adults.

Grippostad Rino of 0.1% nasal drops and Grippostad Rino of 0.1% nasal spray at children aged up to 12 years not to apply

.

Ability to influence speed of response at control of vehicles or work with other mechanisms. Prolonged use or application in high doses of the means for cold containing xylomethazolinum does not exclude influence on a cardiovascular system. In this case the ability to steer vehicles and to work with precision instruments also decreases.

action of sympathomimetics Can strengthen

Interaction and reduce influence of the medicines suppressing sympathetic nerves. at application with blockers of β-adrenoceptors hell can cause a bronchial spasm or decrease. when using together with tricyclic or tetracyclic antidepressants strengthening of systemic action xylomethazolinum is not excluded. application in parallel with Mao's inhibitors is contraindicated.

Overdose

Overdose or accidental oral administration can lead

to the following symptoms: expansion of pupils (mydriasis), nausea, cyanosis, fever, increased fatigue, the increased sweating, pallor, narrowing of peripheral vessels, spasms, violations from a cardiovascular system (tachycardia, arrhythmia, ag), an asystolia, dysfunction of lungs (fluid lungs, respiratory violations), intellectual violations, drowsiness, decrease in body temperature, a pokholodeniye of extremities, decrease chss, shocklike decrease hell, an apnoea.

At heavy overdose, especially at children (for example at accidental ingestion of high doses of medicine), stages of stimulation and oppression of central nervous system and a cardiovascular system can alternate. The concern, excitement, hallucinations and in hard cases — spasms can be symptoms of stimulation of central nervous system. Decrease in body temperature, slackness, drowsiness and in hard cases — development of a coma can be symptoms of oppression of central nervous system.

Treatment: at the complications arising at overdose, patients should carry out intensive care: to urgently apply activated carbon (absorbent), sodium sulfate (depletive) or to carry out gastric lavage, ventilation of the lungs.

Storage conditions

At a temperature up to 25 °C. an expiration date after opening of a bottle — 6 months

Relevant information

Grippostad Rino — plain single-component medicine which is intended for simplification of a state at catarrhal diseases, in particular at congestion of a nose or cold. it belongs to the category of decongestants, that is antiedematouses. therefore the basic principle of its action comes down to reduction of a rhinedema and amount of the cosecreted slime at the expense of a local spasm of submucosal vessels and decrease in a capillary blood-groove (wight r.g., 1989).

Grippostad Rino is issued as in the form of drops, and spray that does it convenient for application for various categories of patients. As active ingredient in medicament the hydrochloride in number of 0.5 mg on 1 ml is used xylomethazolinum that corresponds to concentration of solution of 0.05% (instruction of MZ of Ukraine) or 1 mg on 1 ml — according to 0.1%. Such dosage of medicine (0.5 mg on 1 ml) allows to apply it both at children aged from 1 year, and at adults with hypersensitivity to active ingredient.

Pharmacodynamics

Ksilometazolin a hydrochloride belongs to alpha and adrenergic sympathomimetics, imidazole derivatives. Its vasoconstrictive action is implemented via the mechanism of direct excitement of alpha adrenoceptors which 6 subtypes are known today. Xylomethazolinum the hydrochloride has big affinity to these receptors, than adrenaline and noradrenaline therefore is more effective at local drawing (Haenish B., 2010). At the same time hypostasis of a mucous membrane of a nasopharynx noticeably decreases, the passability of the upper airways is restored and the slime/exudate drainage improves. Due to reduction of hypostasis of a mucous membrane in paranasal sinuses the irritation of local baroreceptors decreases that promotes subjective reduction of severity of a headache and weight in a forehead and cheekbones (Eccles R., 2010). Restoration of nasal breath contributes to gas exchange normalization. Thus, Grippostad Rino , as well as other decongestants, can will be applied to symptomatic monotherapy of acute respiratory diseases (Deckx L., 2016). Xylomethazolinum the hydrochloride has property to slow down the frequency of peristaltic movements of a ciliate epithelium which covers a nasal cavity (Curtis L.N., 1992).

Pharmacokinetics

Effect of medicine develops in 5–10 min. after drawing on a mucous membrane of a nose and proceeds during 6–8 h. At strong inflammatory process in the upper airways duration of effect can decrease.

Drug is soaked up by

from a mucous membrane of a nasopharynx and has systemic action, however at strict observance of a dose and frequency of the use the hydrochloride xylomethazolinum level in blood is practically not defined.

Indications

Grippostad Rino is used for simplification of such symptoms of cold as cold and congestion of a nose (Eccles R., 2008). Besides, medicament can be used:

• in combination with lubricants and local anesthetics for carrying out a rigid rinoskopiya (McCluney N.A., 2009). For preparation for inspection medicament is used in the corresponding therapeutic dose not less than in 10 min. prior to the procedure;

• in combination with anesthetics for carrying out transnasal gastroscopy or a nazogastralny intubation in the absence of an anesthesia or a medicamentous sedation (Cheung J., 2010);

• for carrying out a nazotrakhealny intubation at operations in maxillofacial surgery. At the same time active ingredient Grippostad Rino interferes with hypostasis of a mucous membrane and narrowing of a nasal cavity (Han J.S., 2013);

• for conservative treatment of the not allergic rhinitis connected with a hypertrophy of a mucous membrane of a nose (Cingi C., 2014);

• for decrease in intensity of nasal bleeding in couples traumatizing a mucous membrane, for example after extraction of a foreign body from a nose. At the same time Grippostad Rino in the form of spray is much more convenient for application, than introduction of tampons with adrenaline solution (Song J., 2017);

• for preoperative preparation — before bougieurage of the plaintive channel or removal of his cysts (Joganathan V., 2018);

• for symptomatic treatment of vasomotorial rhinitis which arises after physical activity or owing to existence of other provocative factors;

• in combination with antihistaminic medicines for treatment of allergic rhinitis (Barnes M.L., 2005);

• in complex therapy of a frontal sinusitis/antritises/sphenoidites for improvement of a drainage of adnexal bosoms of a nose (Falck B., 1990);

• as supportive application in treatment of otitis (eliminates hypostasis of an Eustachian tube) (with Meyer M.F., 2015).

Route of administration and a dosage

Grippostad Rino in the form of nasal drops or spray with concentration of active ingredient of 0.1% can be applied at children aged from 12 years and adults. At the same time on one application there is enough 1–2 drops (1–2 injections) in each nasal course. It is necessary to repeat such dose in 8 h (3 r / days).

by

To children aged from 1 year or to adults with hypersensitivity to xylomethazolinum to a hydrochloride applies 0.05% solution in the form of drops. The total amount of medicine and frequency of application are similar to 0.01% to solution.

needs to clean with

For the maximum effect before application Grippostad Rino a nasal cavity (to wash out, then to remove slime). If the child cannot independently blow the nose, then excess slime is removed by means of the soft syringe or a special suction. For introduction of drops the head should be thrown back, and for spray of rather usual situation. The best result of symptomatic treatment will be achieved if to use vasoconstrictive medicament in the evening before going to bed, and during the day to wash a nose with saline solutions.

does not recommend to prolong the general duration of a course of treatment more than 10 days as the tolerance to decongestants with the further need for increase in a dose and a withdrawal can develop (that is shown by a rhinedema and excess mucifying).

Contraindications

Drug is not used at individual intolerance of its components. At the same time similar reactions can arise both in response to the main active ingredient, and on preservative — a benzalkoniya chloride.

Besides, considering the expressed local action, medicine is categorically contraindicated to people to whom neurosurgical operations as a result of which the firm meninx was bared were performed earlier (for example transsphenoidal hypophysectomy).

As side effect Grippostad Rino is reduction of secretion of a mucous membrane, medicine is not shown for treatment of dry rhinitis with a korkoobrazovaniye.

Resorptive effect of xylomethazolinum of a hydrochloride on a cardiovascular system causes inadmissibility of its application at substantial increase of arterial blood pressure or stenocardia.

Also should not use medicament at diseases which can become aggravated at stimulation of alpha adrenoceptors (thyrotoxicosis, closed-angle glaucoma, a pheochromocytoma).

Grippostad Rino , as well as other sympathomimetics, it is not necessary to apply at patients at whom the expressed reactions to adrenergic medicines (such as dizziness, insomnia, cardiopalmus, etc.) are noted.

Besides, it is necessary to treat with care use of medicine for patients with a porphyria, diabetes, prostate adenoma.

Side effects and overdose

All side effects Grippostad Rino , both local, and system, are connected with considerable exceeding a dose, frequency of application or duration of a course. If the patient exceeds the recommended frequency and a dose of medicine, manifestation of rebaund-effect is possible — when effect of medicine comes to an end, initial symptoms are shown more intensively. In case of Grippostada Rino rebaund-effect can be shown by a reactive hyperemia and an excess accumulation of slime in the nasal courses that can be regarded as medicamentous rhinitis. Besides, during active effect of medicine there can be a dryness, burning sensation in a nose, sneezing. Exceeding the recommended duration of a course of treatment is fraught with development of medicamentous dependence. It is rather easy to overcome it if completely to refuse use of any decongestants at least on 1 week. The rinitopodobny symptoms arising at this time can be eliminated by means of frequent washing of a nose with saline solutions or any distracting actions (for example inhalations with broths of herbs, respiratory gymnastics).

Considering

that active ingredient Grippostad Rino can be soaked up by a mucous membrane of a nasopharynx and get to blood, at its short-term application the system side effects connected with stimulation of alpha adrenoceptors are possible: increase in arterial blood pressure, cardiopalmus, headache and tremor. Allergic reactions as an acute anaphylaxis are a rarity (Haldar R., 2017). Also cases of the cardiomyopathy connected with prolonged use of xylomethazolinum of a hydrochloride are recorded, however pathology was reversible (Figueiras-Graillet L.M., 2013).

by

At prolonged use of xylomethazolinum of a hydrochloride (more than 3 weeks) note such changes in a mucous membrane of a nose as aseptic inflammation, fibrosis and an epithelial metaplasia (Nikolaidis E., 2010). it Is noted by

p that if the dose of xylomethazolinum of a hydrochloride does not exceed 0.4 mg/kg of body weight, then no more than at 6% of patients the serious conditions demanding hospitalization develop (Agnes G. van Velzen, 2005).

needs to be considered that the overdose or consuming (intended or accidental) are shown by such symptoms: nausea, pallor with cyanosis, the increased sweating, a mydriasis (expansion of pupils), violations of cardiac performance (tachycardia, arrhythmia, syncopal states), drowsiness, violations of breath up to its stop. Hallucinations, spasms can sometimes be observed. A characteristic symptom of overdose is decrease in body temperature. At treatment of small children it is necessary to consider that they are more sensitive to toxic effect of xylomethazolinum of a hydrochloride, than adults. And also if several adults participate in treatment of the child, then it is necessary to coordinate the mode of administration of medicine strictly.

by

For treatment use gastric lavage and enterosorbents, support of function of external respiration (up to IVL). In case of extremely heavy overdose the resuscitation actions have to last not less than 60 min. in connection with hydrochloride xylomethazolinum metabolism.

Features of use of medicine

At absorption of a large amount of xylomethazolinum in blood can be observed block, drowsiness. It is necessary to consider such effect Grippostad Rino and during its application to refuse the driving of the car or other types of activity demanding good reaction.

Resorptive effects of medicine limit its application during pregnancy or feeding to a breast as researches of its excretion in milk or its actions on a fruit were not conducted.

Interaction with other medicines

Grippostad Rino at absorption in blood can strengthen action of sympathomimetics and act as the antagonist of simpatoblokator. At simultaneous application with blockers of beta adrenoceptors such effects as a bronchospasm or arterial hypotension can be observed. It is necessary to consider that during reception three - and tetracyclic antidepressants, MAO inhibitors and within 14 days after their cancellation the systemic action of xylomethazolinum of a hydrochloride considerably amplifies.

Conclusion

Thus, Grippostad Rino perfectly is suitable for symptomatic treatment of catarrhal diseases around the world, especially is issued in different concentration and doses for more convenient application. Besides, it is widely applied to simplification of the medical manipulations touching a nose and a nasopharynx. But it is suitable only for short-term application. If cold symptoms, such as cold, congestion of a nose and headache, proceed more than a week, then it is necessary to see a doctor.