Sinoflurin
Sinoflurin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Sinoflurin
ATX code: R01AD08
Active ingredient: fluticasone (Fluticasone)
Manufacturer: Sava Medica, Ltd. (Sava Medica, Ltd.) (India)
Description and photo update: 2020-09-01
Sinoflurin - GCS (glucocorticosteroid) for topical use.
Release form and composition
Dosage form - dosed nasal spray, which is a suspension of white or almost white color [120 doses (12 ml) each in a dark glass bottle equipped with a dispensing device, adapter and protective cap; in a cardboard box 1 bottle in a plastic tray and instructions for use of Sinoflurin].
One spray dose contains:
- active ingredient: fluticasone propionate (micronized) - 50 μg;
- additional ingredients: anhydrous dextrose - 5000 μg, Avicel RC-591 (sodium carmellose, microcrystalline cellulose) - 1250 μg, phenylethanol - 250 μg, polysorbate-80 - 100 μg, benzalkonium chloride - 10 μg, purified water - 0.1 ml.
Pharmacological properties
Pharmacodynamics
The active ingredient in Sinoflurin, fluticasone propionate, has a strong anti-inflammatory effect. With the introduction of a suspension of intranasally expressed systemic action and inhibition of the hypothalamic-pituitary-adrenal system was not recorded.
The introduction of fluticasone propionate in a daily dose of 200 mcg does not significantly change the AUC (area according to the pharmacokinetic curve "concentration-time") of serum cortisol for 24 hours, compared with placebo [ratio is 1.01; 90% CI (confidence interval) ranged from 0.9 to 1.14].
The anti-inflammatory effect of Sinoflurin is due to its interaction with GCS receptors. The substance during the early and late phase of an allergic reaction reduces the production of inflammatory mediators and other biological active substances, such as cytokines, prostaglandins, leukotrienes, histamine; inhibits the proliferation of mast cells, macrophages, eosinophils, neutrophils, lymphocytes.
The anti-inflammatory effect of fluticasone propionate on the nasal mucosa manifests itself quickly, and already after 2-4 hours from the moment of the first application, the antiallergic effect of the drug is also noticeable. Symptoms such as nasal congestion, runny nose, sneezing, itchy nose, sinus discomfort, and pressure around the nose and eyes are reduced. It also helps to relieve eye symptoms associated with allergic rhinitis.
The severity of the symptoms of allergic rhinitis, especially nasal congestion, remains reduced throughout the day from the moment of a single injection of a spray at a dose of 200 μg.
Thanks to the action of Sinoflurin, the quality of life of patients improves, their physical and social activity increases.
Pharmacokinetics
Pharmacokinetic parameters of fluticasone propionate:
- absorption: the intranasal method of administration of the drug does not allow quantitative determination of the maximum equilibrium concentration of the active substance (Css max). In most patients, after the administration of a daily dose of fluticasone propionate (200 μg) Css maxis less than 0.01 ng / ml. The highest recorded plasma concentration was 0.017 ng / ml. Absorption of fluticasone propionate directly from the nasal cavity is unlikely due to its low water solubility, and also due to the fact that when injected through the nose, most of the drug is swallowed. The combination of active metabolism during the first passage through the liver and partial absorption from the gastrointestinal tract (gastrointestinal tract) causes a low absolute bioavailability of the substance (less than 1%) and, as a result, a very low total systemic absorption;
- distribution: V d (volume of distribution) in equilibrium is ~ 318 liters. Plasma protein binding is 91%;
- metabolism: the rapid elimination of fluticasone propionate from the systemic circulation is provided mainly due to metabolic processes in the liver, during which an inactive metabolite, carboxylic acid, is formed through the isoenzyme of the cytochrome P450 CYP3A4 system. Similarly, during the first passage through the liver, the swallowed fraction of fluticasone propionate is biotransformed;
- excretion: is linear in the dose range of 250–1000 mcg and has a high plasma clearance (1.1 l / min). C max (maximum concentration) in plasma within 3-4 hours decreases to ~ 98%, the final T 1/2 (half-life) is 7.8 hours (observed only at very low plasma concentrations). The renal clearance of fluticasone propionate does not exceed 0.2%, carboxylic acid (an inactive metabolite of the substance) - 5%. Both the main substance and its metabolites are excreted mainly with bile through the intestines.
Indications for use
Sinoflurin is used for the treatment and prevention of allergic rhinitis, which manifests itself at a certain time of the year (seasonal rhinitis) or all year round (chronic rhinitis).
Contraindications
Absolute:
- children under 4 years of age;
- hypersensitivity to the active component of Sinoflurin or additional substances in its composition.
Relative (use the spray with caution):
- infections of the nasal cavity or paranasal sinuses (it is not a contraindication to the use of the spray, but the patient in the presence of such an infectious disease must undergo appropriate treatment);
- a recent nasal injury or ulceration of the nasal mucosa;
- combined intake of other corticosteroids (in other dosage forms);
- the simultaneous use of drugs that are strong inhibitors of the CYP3A4 isoenzyme (for example, ketoconazole and ritonavir), as this can lead to an increase in the plasma concentration of fluticasone propionate.
Sinoflurin, instructions for use: method and dosage
Spray Sinoflurin is used exclusively intranasally.
The full therapeutic effect of the drug is ensured by its regular use, the maximum is achieved after 3-4 days of therapy.
Patients, depending on age, are advised to adhere to the following dosage regimen:
- adults and children over 12 years old: for the treatment and prevention of year-round / seasonal allergic rhinitis - once a day (preferably in the morning), 2 injections into each nostril. This dosing regimen provides the patient with a daily dose of Sinoflurin - 200 μg. In hotel patients, doubling the daily dose (up to 400 mcg) may be justified to achieve symptom control. In this case, the frequency of use is doubled. An increased dose should be used for a short time; upon reaching the desired effect, it must be reduced to the recommended dose (200 mcg per day). The maximum dose for adult patients and children over 12 years old should not exceed 400 mcg per day (no more than 4 injections into each nostril);
- children aged 4 to 12 years: for the treatment and prevention of year-round / seasonal allergic rhinitis - once a day (preferably in the morning), 1 injection (50 μg) in each nostril. In hotel patients, in order to achieve control over symptoms, it can be justified to double the daily dose (up to 200 μg), in which case the frequency of use is doubled. The maximum daily dose for children aged 4-12 years should not exceed 200 mcg (no more than 2 injections into each nostril).
Elderly patients are prescribed the usual adult dose of Sinoflurin.
Using the inhaler:
- Take the bottle, placing your index and middle fingers on either side of the tip, and your thumb under the bottom, and gently shake it.
- If the drug is used for the first time, or more than 7 days have passed since its last use, it is necessary to check the operability of the nebulizer: by directing the tip away from you, press several times until a small cloud appears from the tip.
- Clear the nasal passages. Close one nostril and insert the tip into the other.
- While holding the bottle in an upright position, tilt your head slightly forward and, while inhaling through the nose, inject the agent by pressing the dispenser of the bottle once. Exhale through your mouth.
- If a second spray into the same nostril is required, repeat the procedure.
- Follow the above procedure for the other nostril.
After using Sinoflurin, you should close the tip with a cap after blotting it with a clean cloth. The sprayer is cleaned once a week (at least). For this, the tip is carefully removed and washed in warm water. Further, shaking off excess water, it is left to dry in a warm place. It is important to avoid overheating. After drying, the tip is installed in its original place in the upper part of the bottle and a protective cap is put on. If the hole is clogged, the tip must be removed as described above and left in warm water for a while. Then place under running cold water, dry and put on the bottle again. It is strictly forbidden to clean the clogged hole of the tip with a pin or any other sharp objects.
Side effects
The side effects of Sinoflurin listed below are grouped according to the anatomical and physiological classification and frequency of occurrence, defined as follows: very often - more than 1/10; often - from 1/100 to 1/10; infrequently - from 1/1000 to 1/100; rarely - from 1/10 000 to 1/1000; extremely rare - less than 1/10 000, including isolated cases.
The frequency of side effects that occur infrequently, often and very often, is established mainly on the basis of information obtained during clinical trials. The frequency of the rare and extremely rare occurrences is based on spontaneous reporting data. The baseline values in the placebo group were not taken into account in the formation of the incidence of adverse events, since, in general, they were comparable with the active treatment group.
Side effects from systems and organs that can occur when using Sinoflurin spray:
- respiratory system, chest and mediastinal organs: very often - nosebleeds; often - irritation / dryness of the mucous membrane of the nasal cavity and pharynx (there are reports of the development of similar side effects when using other intranasal drugs); extremely rarely - perforation of the nasal septum (there is information about cases of the development of this undesirable phenomenon when taking intranasal corticosteroids);
- nervous system: often - a feeling of unpleasant taste and smell, headache (similar side effects have also been reported with other nasal sprays);
- immune system: extremely rarely - anaphylactoid reactions, hypersensitivity (including anaphylactic reactions, swelling of the face and tongue, bronchospasm, rash);
- organ of vision: extremely rarely - cataract, increased intraocular pressure, glaucoma (in the course of clinical studies lasting up to 1 year, a causal relationship between these phenomena and intranasal intake of fluticasone propionate could not be identified).
Overdose
There is no information on chronic or acute overdose of Sinoflurin.
When intranasally administered to healthy volunteers, 2 mg of fluticasone propionate (a dose 20 times higher than the therapeutic dose) twice a day for a week, no effect on the function of the hypothalamic-pituitary-adrenal system was recorded.
Exceeding the dose of Sinoflurin for a long period can cause temporary suppression of adrenal function. In these patients, fluticasone propionate therapy should be continued at doses necessary to control symptoms; recovery of adrenal function takes several days and is monitored by measuring plasma cortisol levels.
special instructions
Spray Sinoflurin is used exclusively intranasally.
Continuous use of the nasal spray without medical supervision should not exceed 6 months.
Long-term therapy with fluticasone requires regular monitoring of the function of the adrenal cortex.
The use of high doses of nasal corticosteroids for a long time can lead to the manifestation of systemic effects, which, however, occur much less frequently than with the use of oral forms of corticosteroids. The variability in the development of these effects is permissible both with the use of various glucocorticosteroid drugs, and in individual patients.
Potential systemic effects may include glaucoma, cataracts, suppression of adrenal function, Itsenko-Cushing's syndrome, and in extremely rare cases, mental or behavioral disorders (including anxiety, psychomotor hyperactivity, aggression, depression, sleep disturbances).
In children who received intranasal GCS, a decrease in the growth rate was noted. In this regard, as a maintenance dose, they were prescribed the lowest dose that could provide adequate control of the symptoms of the disease.
The full effect of the use of the nasal spray occurs only after several days of treatment.
The maximum therapeutic effect is due to the regular use of Sinoflurin according to the scheme recommended in this instruction.
Transfer of patients from systemic GCS therapy to treatment with a nasal spray containing fluticasone propionate should be carried out with extreme caution if there are suspicions of adrenal dysfunction.
Sinoflurin Nasal Spray relieves symptoms of seasonal allergic rhinitis in most patients. However, in cases where the concentration of airborne allergens is very high, additional therapy may be required. Complex treatment may also be required for the relief of ophthalmic manifestations against the background of successful treatment of seasonal allergic rhinitis.
Post-registration observations revealed episodes of systemic effects of corticosteroids, namely, inhibition of adrenal function and Itsenko-Cushing syndrome, as a result of the combined use of ritonavir and fluticasone propionate. For this reason, the combined use of these funds should be avoided. An exception may be cases where the potential benefit to the patient outweighs the possible risk of developing side systemic effects of corticosteroids.
Influence on the ability to drive vehicles and complex mechanisms
There is no information on the effect of Sinoflurin on human cognitive functions. However, when driving and performing work associated with an increased risk of injury, it is necessary to take into account the side effects that may occur during the use of the drug.
Application during pregnancy and lactation
The use of Sinoflurin during pregnancy and breastfeeding is allowed, but only after assessing the expected benefits to the mother and possible risks to the fetus and baby.
Pediatric use
In pediatrics, Sinoflurin is used according to the recommended dosage regimen:
- children over 12 years old: once a day (preferably in the morning), 2 sprays into each nostril. In some patients, in order to achieve control over symptoms, it can be justified to double the daily dose (up to 400 μg), in which case the frequency of use is doubled. The maximum daily dose is not more than 400 mcg;
- children aged 4–12 years: once a day (preferably in the morning), 1 injection (50 mcg) in each nostril. In some patients, in order to achieve control over symptoms, it can be justified to double the daily dose (up to 200 μg), in which case the frequency of use is doubled. The maximum daily dose is not more than 200 mcg.
Sinoflurin spray is contraindicated in children under 4 years of age.
With impaired renal function
There are no special instructions for the use of the drug in patients with impaired renal function.
For violations of liver function
There are no special instructions for the use of Sinoflurin in patients with impaired liver function.
Use in the elderly
Elderly persons are prescribed Sinoflurin in doses usual for adult patients.
Drug interactions
Clinically significant interactions of fluticasone propionate with other substances are unlikely, since after the use of a nasal spray, the plasma concentration of the active substance is very low.
Ritonavir, being a highly active inhibitor of the coenzyme CYP3A4 of the cytochrome P450 enzyme system, can significantly increase plasma concentrations of fluticasone propionate, which causes a sharp decrease in serum cortisol levels and the occurrence of systemic side effects, in particular adrenal suppression and Itsenko-Cushing's syndrome. For this reason, the combined use of these funds should be avoided, with the exception of cases where the potential benefit to the patient outweighs the possible risk of developing side systemic effects of corticosteroids.
Erythromycin, ketoconazole and other inhibitors of the CYP3A4 isoenzyme of the cytochrome P450 enzyme system cause such an insignificant increase in plasma concentrations of fluticasone propionate that no noticeable decrease in serum cortisol concentrations is noted. Nevertheless, with the combined use of drugs of this group (for example, ketoconazole) and fluticasone propionate, care must be taken due to a possible increase in the plasma concentration of the latter.
Analogs
The analogues of Sinoflurin are Avamis, Dezrinit, Nazarel, Nazonex, Nasobek, FeniVeit, Flixotide, Fliksonase, etc.
Terms and conditions of storage
Keep out of the reach of children.
The temperature at the storage location should not exceed 25 ° C. The drug must not be frozen.
The shelf life is 3 years.
It is prohibited to use the spray after the recommended shelf life.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Sinoflurin
At the moment, reviews about Sinoflurin are rarely left. In them, users characterize the drug as a more affordable, but no less effective substitute for other means of similar action. The use of the spray can significantly improve the quality of life of patients. It gives them the opportunity to do their usual things, not paying attention to the disease. Among the positive aspects, the convenience of using Sinoflurin and a small list of side effects are also noted. There are no complaints on the network about the development of negative phenomena during drug therapy.
Some patients consider the cost of the product to be overpriced, but they are ready to purchase it, because they are sure of its effectiveness.
Price for Sinoflurin in pharmacies
In pharmacy chains, the price of Sinoflurin, a dosed nasal spray, for 1 bottle of 12 ml (120 doses) varies within 398-417 rubles.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
