Nazarel, spray 50 mcg/dose 120 doses

Pharmacotherapeutic group: glucocorticosteroid for topical use
ATC code: R01AD08

Pharmacological properties

Pharmacodynamics
Mechanism of action. Fluticasone propionate is a substance with strong anti-inflammatory action. When administered intranasally no marked systemic action and suppression of hypothalamic-pituitary-adrenal system is noted.
No significant changes of the daily area under the pharmacokinetic curve of serum cortisol after administration of fluticasone propionate at a dose of 200 mcg/day compared to placebo (ratio: 1.01, 90% CI – confidence interval 0.9 to 1.14).
Fluticasone propionate has anti-inflammatory effect due to its interaction with glucocorticosteroid receptors. It suppresses proliferation of mast cells, eosinophils, lymphocytes, macrophages, neutrophils, reduces the production of inflammatory mediators and other biologically active substances (histamine, prostaglandins, leukotrienes, cytokines) during the early and late phase of the allergic reaction. Fluticasone propionate has a rapid anti-inflammatory effect on the nasal mucosa, and its anti-allergic effect is seen as early as 2-4 hours after the first use. It relieves sneezing, nasal itching, runny nose, nasal congestion, nasal sinus discomfort and feeling of pressure around the nose and eyes. Also relieves eye symptoms associated with allergic rhinitis. Reduction of symptoms (especially nasal congestion) persists for 24 hours after a single administration of 200 mcg spray. Fluticasone propionate improves patients’ quality of life, including physical and social activity.

Pharmacokinetics

Intake. After intranasal administration of fluticasone propionate at a dose of 200 mcg/day, maximum equilibrium plasma concentrations are not quantifiable in most patients (less than 0.01 ng/ml). The highest plasma concentration was recorded at 0.017 ng/ml. Direct nasal absorption is unlikely due to low water solubility and swallowing most of the drug. Absolute oral bioavailability is low (less than 1%) due to a combination of incomplete absorption from the gastrointestinal tract and active metabolism during first passage through the liver. Total systemic absorption is thus extremely low.
Distribution. Fluticasone propionate has a large volume of distribution in the equilibrium state (approximately 318 l). The binding to plasma proteins is high (91%).
Metabolism. Fluticasone propionate is rapidly eliminated from the systemic bloodstream primarily by metabolism in the liver to form inactive carboxylic acid via CYP3A4 isoenzyme of cytochrome P450 system. Metabolism of the swallowed fraction of fluticasone propionate on first passage through the liver occurs in the same manner.
Excretion. Excretion of fluticasone propionate is linear in the dose range from 250 to 1000 µg and is characterized by high plasma clearance (1.1 L/min). Maximum plasma concentrations are reduced by approximately 98% within 3-4 hours, and only at very low plasma concentrations was a final half-life of 7.8 hours observed. Renal clearance of fluticasone propionate is insignificant (less than 0.2%) and of the inactive metabolite, carboxylic acid, less than 5%. Fluticasone propionate and its metabolites are mainly excreted with the bile through the intestine.

Indications

Active ingredient

Composition

How to take, the dosage

Intranasal only.

The drug should be used regularly to achieve the full therapeutic effect. Maximum therapeutic effect may be achieved after 3-4 days of therapy.

Adults and children over 12 years

Week 1: 2 injections in each nostril once daily (200 mcg per day).

From 2nd week to 3 months: 1 or 2 injections in each nostril once daily (100-200 mcg per day).

The maximum daily dose is 200 mcg per day (no more than 2 injections in each nostril).

Special patient groups

Patients.Elderly patients

The usual dose for adults.

Children 4 to 12 years

1 injection in each nostril once daily (100 mcg per day). Do not exceed the recommended dose (100 mcg per day). Children aged 4 to 12 years should use the drug for the shortest time necessary to achieve symptom control. You should talk to your doctor if your child needs to use the drug for more than 2 months out of the year.

The maximum daily dose is 100 mcg (no more than 1 injection in each nostril).

Consult a physician if there is no effect of the drug in all age groups of patients.

Instructions for Use

Shake the bottle gently before use by placing the index and middle fingers on either side of the tip and the thumb under the bottom.

The first time the product is used, or if the product is not used for more than 1 week, the atomizer should be checked to make sure it is working properly: point the tip away from yourself and perform 6 squeezes until a small cloud emerges from the tip. Then you need to clean your nose (blow your nose). Close one nostril and insert the tip in the other. Tilt your head slightly forward, continuing to hold the vial vertically. Then start breathing in through your nose and while continuing to inhale, press once with your fingers to atomize the medicine. Exhale through the mouth. Repeat the procedure for a second spray in the same nostril, if necessary. Then repeat the entire procedure, inserting the tip in the other nostril. After use, wipe the tip with a clean cloth or handkerchief and cap it.

The nebulizer should be rinsed at least once a week. To do this, gently remove the tip and rinse it in warm water. Shake off excess water and leave to dry in a warm place. Avoid overheating. Then carefully reinstall the tip in its original position at the top of the bottle. Put on the protective cap. If the tip hole is clogged, remove the tip as described above and leave it in warm water for a while. Then rinse under cold water, dry and put back on the bottle. Do not use a pin or other sharp object to clean the tip hole.

Interaction

Ritonavir (a highly active inhibitor of the CYP3A4 isoenzyme of the cytochrome P450 enzyme system) can significantly increase plasma concentrations of fluticasone propionate, resulting in a sharp decrease in serum cortisol concentrations.

The use of fluticasone propionate (inhaled or intranasally) and ritonavir leads to the development of systemic glucocorticoid effects, including Icenko-Cushing syndrome and suppression of adrenal cortical function. Therefore, concomitant use of fluticasone propionate and ritonavir should be avoided unless the possible benefits exceed the risks of systemic effects.

The concomitant use of fluticasone propionate for inhaled use and less potent CYP3A isoenzyme inhibitors such as ketoconazole and itraconazole leads to increased exposure of fluticasone propionate and increased risk of systemic side effects. Caution is recommended and long-term co-administration of these drugs should be avoided if possible.

The CYP3A4 isoenzyme inhibitors of the cytochrome P450 enzyme system cause negligible (erythromycin) or slight (ketoconazole) increase in plasma concentrations of fluticasone propionate, which do not result in any significant decrease in serum cortisol concentrations. However, caution should be exercised when using CYP3A4 isoenzyme inhibitors of cytochrome P450 enzyme system (e.g., ketoconazole) and fluticasone propionate concomitantly due to possible increase of plasma concentration of the latter.

Concomitant use of fluticasone propionate with cobicistat-containing drugs increases the risk of systemic side effects. Concomitant use should be avoided unless the potential benefit to the patient outweighs the possible risk of developing systemic side effects of glucocorticosteroids. In case of concomitant use, the development of systemic side effects in patients should be monitored.

Special Instructions

The drug is indicated for intranasal use only.

For adults and children from 12 years of age: Do not use Nazarel Nasal Spray for more than 3 months. If it is necessary to use the drug for more than 3 months, a physician’s consultation is required.

For children from 4 to 12 years of age: Do not use Nazarel nasal spray for more than 2 months.

If the drug must be used for more than 2 months, a physician’s consultation is required. Continuous use requires regular monitoring of adrenal function.

Systemic effects may occur with nasal glucocorticosteroids, particularly when high doses are used over an extended period of time. These effects are much less likely to occur than with oral glucocorticosteroids, and they can vary between patients and between different glucocorticosteroid products.

Possible systemic effects may include Icenko-Cushing’s syndrome, characteristic signs of cushingoid, suppression of adrenal function, growth retardation in children and adolescents, cataracts, glaucoma, and less commonly, a number of psychological or behavioral effects, including psychomotor hyperactivity, sleep disturbances, anxiety, depression or aggression (especially in children).

In children receiving therapy with some intranasal glucocorticosteroids at approved doses, a decrease in growth rate has been observed. It is recommended that the growth rate of children receiving long-term treatment with intranasal glucocorticosteroids be monitored regularly. If growth rate decreases, treatment should be reconsidered to reduce the intranasal glucocorticosteroid dose, if possible, to the lowest dose that maintains effective symptom control and contact the pediatrician.

The concomitant use of ritonavir and fluticasone propionate should be avoided unless the potential benefit to the patient exceeds the possible risk of systemic side effects of the glucocorticosteroids (see section “Interaction with other drugs”).

The full effect of fluticasone propionate in nasal spray can only be seen after 3-4 days of treatment.

We recommend stopping the product and consulting a physician if there is no improvement within 4 days. Your physician should also be consulted if you have any new symptoms, such as significant facial pain or thick nasal discharge, which could indicate an infection and are not due to an allergy.

Infections of the nasal cavity or sinuses require appropriate treatment, but are not contraindications to the use of Nazarel Nasal Spray.

In most patients, fluticasone propionate nasal spray resolves symptoms of seasonal allergic rhinitis, but in some cases, additional therapy may be necessary if there are very high levels of airborne allergens.

Additional therapy may be necessary to relieve eye symptoms with successful therapy of seasonal allergic rhinitis.

To achieve maximum therapeutic benefit, it is necessary to adhere to a regular regimen of use.

Caution should be used when converting patients from systemic glucocorticosteroid therapy to treatment with fluticasone propionate nasal spray, especially if there is impaired adrenal function with regular monitoring.

Nasarel, a nasal water spray, contains benzalkonium chloride, which can cause bronchospasm.

In case of contact with patients with chickenpox, measles, and changes in vision, we recommend stopping treatment and seeing a doctor.

Influence on driving and operating ability

In clinical trials no data have been obtained on the effect of the drug on the ability to drive vehicles and other mechanisms, but side effects that may be caused by the drug should be considered.

Synopsis

Contraindications

– Hypersensitivity to fluticasone propionate or any other component of the drug.
– Children under 4 years of age.
– Recent nasal trauma or surgery in the nasal cavity.

With caution
Before using the drug, you should consult your doctor if you are taking:
– medications to treat HIV infection, such as ritonavir;
– glucocorticosteroids to treat bronchial asthma, allergies, skin rash;
– medications to treat fungal infections, such as ketoconazole;
– other potent CYP3A isoenzyme inhibitors, such as itraconazole.
Also consult your doctor if you have glaucoma or cataracts.

Take with caution if you have infections of the nasal cavity or sinuses. Note that nasal infections require appropriate treatment, but are not a contraindication to the use of Nazarel Nasal Spray.

Side effects

The undesired reactions presented below are listed according to organ and organ system involvement and frequency of occurrence. The frequency is defined as follows: very frequent (≥1/10), frequent (≥1/100 and < 1/10), infrequent (≥1/1000 and < 1/100), rare (≥1/10000 and < 1/1000), very rare (< 1/10000, including individual cases). Very common, frequent, and infrequent adverse reactions are mainly established on the basis of data from clinical trials. Rare and very rare reactions are mainly determined from spontaneous reports. In forming the incidence of adverse reactions, baseline rates in the placebo group were not taken into account because they were generally comparable to the active treatment group.

Immune system disorders: very rare – hypersensitivity reactions, including bronchospasm, rash, facial and tongue swelling, anaphylactic reactions, anaphylactoid reactions.

Nervous system disorders:often – headache, sensation of unpleasant taste and smell.

The occurrence of headache, unpleasant taste and odor have also been reported with other nasal sprays.

Visual disorders:very rarely, glaucoma, increased intraocular pressure, cataracts. A small number of spontaneous reports have been associated with long-term therapy with the drug.

Disorders of the respiratory system, thorax and mediastinum:

very often – nasal bleeding; often – dryness and irritation of the mucous membrane in the nasal cavity and pharynx.

These adverse reactions, as well as nasal bleeding, have also been observed with other intranasal medications.

Very rarely, nasal septal perforation (also reported with other intranasal glucocorticosteroids).

Some intranasal glucocorticosteroids may develop systemic effects, especially when administered in high doses over a long period of time (see also section on “Special Precautions”).

Overdose

Pregnancy use

Similarities