Composition, form of production and packaging
Spray nasal dosed in the form of a white or almost white, opaque, homogeneous suspension.
1 dose
fluticasone propionate 50 Ојg
Auxiliary substances: polysorbate-80 - 0.005 mg, microcrystalline cellulose + carmellose sodium (dispersive cellulose) - 1.55 mg, dextrose-5 mg, benzalkonium chloride (50% solution) - 0.04 mg, phenylethanol 0.25 mg, water qs
120 doses - bottles of dark glass with a dispensing device and protective cap (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
PHARMACHOLOGIC EFFECT
GCS for topical application. In recommended doses, it has a pronounced anti-inflammatory, anti-edematous and anti-allergic effect.
The anti-inflammatory effect is due to the interaction of the drug with the GCS receptors. Suppresses the proliferation of mast cells, eosinophils, lymphocytes, macrophages, neutrophils, reduces the production and release of inflammatory mediators and other biologically active substances (including histamine, prostaglandins, leukotrienes, cytokines) during the early and late phases of an allergic reaction.
Antiallergic effect manifests itself 2-4 hours after the first application. It reduces itching in the nose, sneezing, rhinitis, nasal congestion, discomfort in the sinuses and a feeling of pressure around the nose and eyes. It alleviates eye symptoms associated with allergic rhinitis.
When used in therapeutic doses of fluticasone, propionate shows no systemic effect and has virtually no effect on the hypothalamic-pituitary-adrenal system.
The effect of the drug is maintained for 24 hours after a single application.
PHARMACOKINETICS
Suction
After intranasal administration of fluticasone propionate at a dose of 200 Ојg / day C max in blood plasma in most patients below the detection level (<0.01 ng / ml).Absorption from the mucous membrane of the nasal cavity is extremely small due to the low solubility of the drug in the water (as a result, most of the dose is swallowed). With oral administration of fluticasone propionate, less than 1% of the dose is delivered to the blood due to low absorption and presystemic metabolism.These reasons cause an extremely low total absorption of the drug from the nasal mucosa and gastrointestinal tract.
Distribution
Fluticasone propionate in a stable state has a significant V d of about 318 liters. Binding to plasma proteins is 91%.
Metabolism
Exposed to the effect of "first passage" through the liver. Metabolised in the liver with the participation of the isoenzyme CYP3A4 with the formation of an inactive carboxyl metabolite.
Excretion
T 1/2 is 3 hours. It is excreted mainly through the intestine. Renal clearance of fluticasone propionate is less than 0.2%, the renal clearance of a metabolite containing a carboxyl group is less than 5%.
INDICATIONS
- prevention and treatment of seasonal and all-year-round allergic rhinitis.
DOSING MODE
The drug is administered intranasally.
Adults and children 12 years of age and older are prescribed 2 doses (100 Ојg) in each nasal passage 1 time / day, preferably in the morning. In some cases it is necessary to administer 2 doses in each nasal passage 2 times / day (the maximum daily dose is 400 mcg). After achieving the therapeutic effect, a maintenance dose of 50 Ојg / day can be administered to each nasal passage (100 Ојg). The maximum daily dose should not exceed 400 mcg (4 doses per each nasal passage).
Older patients do not need a dose adjustment.
Children aged 4 to 12 years are prescribed 1 dose (50 Ојg) 1 time / day in each nasal passage, preferably in the morning. The maximum daily dose should not exceed 200 mcg in each nasal passage. It is necessary to apply the minimum dosage, which ensures effective elimination of symptoms.
To achieve full therapeutic effect the drug should be used regularly.
Terms of use
The bottle with nasal spray is equipped with a protective cap, which protects the tip from getting dust and pollution.
At the first application it is necessary to prepare the bottle by pressing the dispenser 6 times. The spraying mechanism is unlocked. If the drug has not been used for more than one week, you should again prepare the vial and unlock the spraying mechanism.
Then you need:
- clean the nasal cavity;
- close one nasal passage and insert the tip into the other nasal passage;
- tilt the head slightly forward, continuing to hold the bottle vertically;
- start breathing in through your nose and, continuing to inhale, make a single tap with your fingers;
exhale through the mouth.
Then, in the same way, inject the drug into the other nasal passage.
After use, the tip should be soaked with a clean cloth or a handkerchief and cover it with a cap. The sprayer should be washed at least once a week. To do this, remove the tip, rinse it in warm water, dry it and then gently place it on the top of the bottle. Put the protective cap on. If the tip of the tip is clogged, the tip should be removed and left for a while in warm water. Then rinse under the stream, dry and re-put on the bottle. Do not clean the hole with a pin or other sharp objects.
After opening the package, the drug can be used until the expiration date.
SIDE EFFECT
Determination of the frequency of adverse reactions (according to WHO recommendations): very often (? 10%), often (? 1%, but <10%), infrequently (≤ 0.1%, but <1%), rarely (≥ 0.01%, but < 0.1%), very rarely, including isolated cases (<0.01%).
On the part of the immune system: rarely - bronchospasm, anaphylactic reaction; very rarely - the reaction of skin hypersensitivity, angioedema.
From the nervous system: often - headache, a violation of taste, a violation of the sense of smell.
From the side of the organ of vision: very rarely - increased intraocular pressure, glaucoma, cataract.
On the part of the respiratory system: very often - nosebleeds; often - dryness and irritation of the mucous membrane of the nasopharynx; very rarely - perforation of the nasal septum.
From the skin and subcutaneous tissues: very rarely - ulceration of the subcutaneous-mucous layer.
Other: very rarely - stunted growth in children, decreased function of the adrenal cortex, osteoporosis.
CONTRAINDICATIONS
- Children's age up to 4 years;
- Hypersensitivity to the components of the drug.
Caution should be applied to the drug with concomitant herpes, bacterial infections of the upper respiratory tract (in such cases, antibiotics and / or antiviral agents should additionally be prescribed); after surgery in the nasal cavity or nose trauma, as well as in the presence of ulcerative lesions of the nasal mucosa; simultaneously with other forms of corticosteroids (including tablets, creams, ointments, asthma medications, analogous nasal or ophthalmic sprays and nasal drops).
PREGNANCY AND LACTATION
It is not recommended to prescribe the drug during pregnancy. If necessary, consider the expected benefit of therapy for the mother and the potential risk to the fetus.
It is unlikely that fluticasone propionate excreted in breast milk. Nevertheless, it is recommended to stop breastfeeding while the drug is being used.
APPLICATION FOR CHILDREN
Contraindicated in childhood up to 4 years. Children aged 4 to 12 years are prescribed 1 dose (50 Ојg) 1 time / day in each nasal passage, preferably in the morning.The maximum daily dose should not exceed 200 mcg in each nasal passage. It is necessary to apply the minimum dosage, which ensures effective elimination of symptoms.
Because GCS for intranasal use even when used in therapeutic doses can cause a slowdown in the growth of children with prolonged therapy, it is necessary to regularly monitor the growth of the child and timely adjust the dose of the drug Nazarel.
APPLICATION IN ELDERLY PATIENTS
Older patients do not need a dose adjustment.
SPECIAL INSTRUCTIONS
Simultaneous use with inhibitors of the isoenzyme CYP3A4 (ritonavir, ketonazole) requires careful monitoring of the patients' condition, as these drugs can cause an increase in the concentration of fluticasone propionate in the plasma.
In the appointment of GCS for intranasal use in high doses for a long time increases the risk of systemic effects of GCS. With prolonged use of the drug Nazarel, regular monitoring of the function of the adrenal cortex is necessary.
Because GCS for intranasal use even when used in therapeutic doses can cause a slowdown in the growth of children with prolonged therapy, it is necessary to regularly monitor the growth of the child and timely adjust the dose of the drug Nazarel.
In the treatment of seasonal allergic rhinitis, Nazarel is quite effective, but in the case of an especially high concentration in the air in the summer, allergens may require additional treatment.
When prescribing Nazarel to patients with tuberculosis, the infectious process, herpetic keratitis, and also recently undergone surgical intervention in the oral cavity and nose, the relationship between possible risk and the expected benefit should be carefully evaluated.
OVERDOSE
Symptoms of acute and chronic overdose have not been reported. With intranasal administration of 2 mg of fluticasone propionate 2 times / day for volunteers, no effect on the hypothalamic-pituitary-adrenal system was observed for 7 days.
DRUG INTERACTION
Interaction with other drugs is unlikely, because with intranasal administration of the concentration of fluticasone in the plasma is very low.
When used simultaneously with strong inhibitors of the isoenzyme CYP3A4 (ritonavir), the systemic effect of fluticasone and the development of side effects (Cushing's syndrome, suppression of adrenal cortex function) are possible.
When used simultaneously with other inhibitors of the cytochrome P450 system (erythromycin, ketoconazole), a slight increase in the concentration of fluticasone propionate in the blood is observed, which practically does not affect the cortisol content.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of the reach of children at a temperature of no higher than 25 В° C. Shelf life - 3 years.
