Universal reference book for medicines
Name of the preparation: AVAMIS (AVAMYS)

Active substance: fluticasone furoate

Type: GCS for intranasal administration

Manufacturer: GlaxoSmithKline Trading (Russia) manufactured by Glaxo Operations UK (UK)
Composition, form of production and packaging
Spray nasal dosed
in the form of a homogeneous suspension of white color.

1 dose

fluticasone furoate micronized 27.5 μg

Excipients: dextrose - 2750 μg / dose, cellulose dispersible * - 825 μg / dose, polysorbate 80 - 13.75 μg / dose, benzalkonium chloride solution ** - 16.5 μg ***, disodium edetate - 8.25 μg / dose, purified water - up to 50 μl.

30 doses - bottles of orange glass, equipped with a spraying device (1) - plastic case with indicator window, pressure valve and cap with elastomer stop (1) - cardboard packs.

60 doses - bottles of orange glass, equipped with a spraying device (1) - plastic case with indicator window, pressure valve and cap with elastomer stop (1) - cardboard packs.

120 doses - bottles of orange glass, equipped with a spraying device (1) - plastic case with indicator window, pressure valve and cap with elastomer stop (1) - cardboard packs.

* viscosity 65 cP, contains 11% carmellose sodium;

** contains 50% benzalkonium chloride;

*** the content of benzalkonium chloride is 8.25 μg / dose or 0.015% (w / w) in the suspension.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2017.

PHARMACHOLOGIC EFFECT

GCS for topical application.
Fluticasone furoate - synthetic trifluorinated glucocorticosteroids with high affinity for glucocorticoid receptors, has a pronounced anti-inflammatory effect.
PHARMACOKINETICS

Suction

Fluticasone furoate is not completely absorbed, undergoing primary metabolism in the liver and intestines, which leads to a slight systemic exposure.
Intranasal administration at a dose of 110 μg 1 time / day usually does not lead to the achievement of detectable concentrations in plasma (<10 pg / ml). Absolute bioavailability of fluticasone furoate with intranasal administration at a dose of 880 μg 3 times / day (daily dose of 2640 μg) is 0.5%.
Distribution

Fluticasone furoate binds to plasma proteins more than 99%.
When the equilibrium concentration V d of fluticasone furoate is reached, an average of 608 liters.
Metabolism

Fluticasone furoate is rapidly excreted from the systemic blood flow (total plasma clearance 58.7 L), mainly by metabolism in the liver with the formation of an inactive 17? -carboxylic metabolite (GW694301X) with the participation of the CYP3A4 isoenzyme of the cytochrome P450 system.
The main pathway of metabolism is the hydrolysis of the S-fluoromethylcarbothioate group with the formation of a 17? -carboxylic acid metabolite. In vivo studies have shown that splitting of fluticasone furoate to fluticasone does not occur.
Excretion

With oral administration and / or introduction, the excretion of fluticasone furoate and its metabolites is mainly through the intestine by excretion with bile.
When I / in the introduction of T 1/2 is 15.1 hours. About 1% and 2% is excreted by the kidneys by oral and intravenous administration, respectively.
Special patient groups

Patients of advanced age.
Pharmacokinetic data are presented only for a small number of elderly patients (n = 23/872, 2.6%). There is no evidence that quantifiable concentrations of fluticasone furoate in elderly patients are higher than in young patients.
Children.
In children with intranasal use at a dose of 110 μg 1 time / day fluticasone furoate is usually not found in concentrations that can be quantified (<10 pg / ml).Concentrations determined quantitatively are recorded in less than 16% of children with intranasal use at a dose of 110 μg 1 time / day and less than 7% of children, with intranasal application at a dose of 55 μg 1 time / day. There is no evidence that an increase in the concentration of fluticasone furoate is more common in children younger than 6 years of age.
Patients with impaired renal function.
Fluticasone furoate was not detected in urine in healthy volunteers with intranasal administration. Less than 1% of metabolites are excreted by the kidneys, thus, it is not expected that renal dysfunction may affect the pharmacokinetics of fluticasone furoate.
Patients with impaired liver function.
In a study in patients with moderate impaired hepatic function, with an inhalation application of fluticasone furoate at a dose of 400 μg, a C max increase of 42% and an increase in AUC of 0-? on 172%, in comparison with healthy volunteers. Based on the results of the study, it is not expected that the average expected exposure of fluticasone furoate at a dose of 110 μg when administered intranasally in this group of patients will not lead to suppression of cortisol. Therefore, it is not expected that moderate liver dysfunction likely will not lead to clinically significant effects in prescribing a standard dose for adults.
Thus, dose adjustments in patients with mild and moderate impairment of liver function (Class A and B by Chaydd-Pyo) are not required.
There is no data on patients with severe impairment of liver function (Child-Pugh class C). Caution should be exercised when determining the dose for patients with severe impairment of liver function. such patients may be more at risk of systemic adverse reactions associated with the use of GCS (see section "Dosage regimen" and "Special instructions").
Other pharmacokinetic parameters

The concentrations of fluticasone furoate are usually not determined (<10 pg / ml) with intranasal administration at a dose of 110 μg 1 time / day.
The defined concentrations were observed only in less than 31% of patients aged 12 years and older and less than 16% of patients younger than 12 years of age when administered at a dose of 110 μg 1 time / day intranasally. Dependence on sex, age (including children's age), race was not observed in cases where concentrations were above or below the detection threshold.
INDICATIONS

Adults and adolescents (aged 12 years and over)

- treatment of nasal and eye symptoms of seasonal allergic rhinitis;

- treatment of nasal symptoms of year-round allergic rhinitis.

Children (aged 2 to 11 years)

- treatment of nasal symptoms of seasonal and year-round allergic rhinitis.

DOSING MODE

The drug Avamis is intended only for intranasal use.

To achieve the maximum therapeutic effect, you must adhere to a regular scheme of application.
The onset of action can be observed within 8 hours after the first administration. To achieve maximum effect, it may take several days. Care should be given to explaining to the patient the reason for the absence of an immediate effect.
Treatment of nasal and ocular symptoms of seasonal allergic rhinitis, nasal symptoms of year-round allergic rhinitis in adults and adolescents (ages 12 and older)

The recommended initial dose is 2 sprays (27.5 μg fluticasone furoate in one spray) in each nostril 1 time / day (110 μg / day).

When adequate control of symptoms is achieved, reducing the dose to 1 spray into each nostril 1 time / day (55 μg / day) can be effective for maintenance treatment.

Treatment of nasal symptoms of seasonal and year-round allergic rhinitis in children aged 2 to 11 years

The recommended initial dose is 27.5 μg (1 spray) in each nostril 1 time / day (55 μg / day).

If there is no desired effect at a dose of 27.5 μg (1 sputtering), a dose increase up to 55 μg (2 sprays) per nostril 1 time / day (110 μg / day) is possible in each nostril 1 time / day.
When adequate symptom control is achieved, it is recommended to reduce the dose to 27.5 μg (1 spray) in each nostril 1 time / day (55 μg / day).
Children under 2 years of age

There is no evidence to recommend the use of fluticasone furoate intranasally as a treatment for seasonal and allergic allergic rhinitis in children under 2 years of age.

Elderly patients

Correction of the dose is not required (see the section "Pharmacokinetics").

Patients with impaired renal function

Correction of the dose is not required (see section "Pharmacokinetics").

Patients with impaired hepatic function

Dose adjustments in patients with mild and moderate impairment of liver function (Child-Pugh class A and B) do not require dose adjustment.
There is no data for patients with severe impairment of liver function (Child-Pugh class C). Caution should be exercised when determining the dose for patients with severe impairment of liver function.such patients may be more at risk of systemic adverse reactions associated with the use of GCS (see section "Pharmacokinetics" and section "Special instructions").
Rules of use and handling of the drug

The indicator window in the plastic package allows you to monitor the level of the drug in the vial.
In vials for 30 or 60 doses, the level of the drug will be visible immediately, and in bottles for 120 doses the initial level of the drug is above the upper boundary of the viewing window. Nasal spray is available in orange glass vials that are in plastic cases. To check the level of the drug in the vial, you need to look at it in the light. The level will be visible in the viewing window.
Preparation for use should be carried out with the use of a spray for the first time, and also if the bottle has been left open.
Proper preparation for use will ensure the injection of the required dose of the drug.
1. Without removing the cap, shake the bottle well for 10 seconds.
The drug is a fairly thick suspension and becomes more liquid when shaken. Spraying is possible only after shaking.
2. Remove the cap by gently pulling it with your thumb and forefinger.

3. Hold the bottle vertically and point the tip away from yourself.

4. Press the button hard, press several times (at least 6) until a small cloud appears from the tip (if you can not press the button with one thumb, then press it with your thumbs).

5. The spray is ready for use.

Use of nasal spray

1. Thoroughly shake the vial.

2. Remove the cap.

3. Clean the nose and tilt the head slightly forward.

4.
Insert the tip into one nostril, continuing to hold the bottle vertically.
5. Guide the tip of the nebulizer to the outer wall of the nose, not to the nasal septum.
This will ensure the correct injection of the drug.
6. Start breathing in through the nose and make a single finger tap to spray the drug.

7. Remove the nebulizer from the nasal spray and exhale through the mouth.

8.
If it is necessary to make two injections into each nostril (as directed by the doctor), repeat steps 4-6.
9. Repeat the procedure for the other nostril.

10. Close the bottle with a cap.

11. Avoid contact with eyes.
If the product gets into the eyes, rinse thoroughly with water.
Care of the sprayer

After each use:

1. Soak the tip and inner surface of the cap with a dry clean cloth.
Avoid getting water.
2. Do not attempt to clean the tip of the tip with a pin or other sharp objects.

3. Always close the vial and keep it closed.
The cap protects the spray gun from dust and clogging, seals the bottle, prevents accidental pressing of the button.
In case the spray gun does not work:

1. Check the remaining drug level in the vial through the inspection window.
If only a small amount of liquid is left, it may not be enough to operate the nebulizer.
2. Check the bottle for damage.

3. Check that the tip of the tip is not clogged.
Do not attempt to clean the tip of the tip with a pin or other sharp objects.
4. Attempt to activate the device by repeating the procedure for preparing a nasal spray for use.

SIDE EFFECT

The adverse events presented below are listed in accordance with the damage to organs and organ systems and frequency of occurrence.
Frequency of occurrence is defined as follows: very often (? 1/10); often (? 1/100, <1/10); infrequently (? 1/1000, <1/100); rarely (? 1/10 000, <1/1000); very rarely (<1/10 000, including individual cases).
Undesirable effects observed in clinical trials

On the part of the respiratory system, the organs of the thorax and the mediastinum: very often - nosebleeds.
In adults and adolescents, cases of epistaxis were observed more often with prolonged use (more than 6 weeks) than with a short course (up to 6 weeks). Studies in children with a duration of therapy up to 12 weeks, the number of cases of nasal bleeding was similar in the fluticasone furoate group and placebo. Often - ulceration of the mucous membrane of the nasal cavity.
From the musculoskeletal system and connective tissue: the frequency is unknown - growth retardation in children.

The results of a study conducted during the year in pre-pubertal children who received fluticasone

furoate at a dose of 110 μg 1 time / day, do not allow to determine the statistical frequency of this undesirable phenomenon, as it is impossible to calculate the effect of the drug on the final growth rates of the children participating in the study.

The delay in the growth of the skeleton in children refers to systemic undesirable phenomena characteristic of SCS with prolonged oral or parenteral administration.

Undesirable phenomena observed during post-registration observation

On the part of the immune system, rarely - hypersensitivity reactions, including anaphylaxis, Quincke's edema, rash, hives.

From the nervous system: often - a headache.

On the part of the respiratory system, chest and mediastinum: infrequently - rinalgia, discomfort in the nose (including burning, irritation in the nose and soreness), dryness in the nose;
very rarely - perforation of the nasal septum.
From the side of the organ of vision: frequencies unknown - transient visual impairment.
Possible occurrence of systemic side effects, characteristic for GCS (see section "Special instructions").
CONTRAINDICATIONS

- hypersensitivity to fluticasone furoate and other components of the drug.

With caution should be used in patients with severe impairment of liver function, t.
the pharmacokinetics of fluticasone furoate may vary.
PREGNANCY AND LACTATION

Data on the use of fluticasone furoate in pregnancy and during breastfeeding is not enough.

Fertility

There is no data on the effect of the drug on human fertility.

Pregnancy

There is no data on the use of fluticasone furoate in pregnant women.
As shown in animal studies, GCS caused malformations, including cleft palate and intrauterine growth retardation.
It is unlikely that these data are relevant for people receiving SCS intranasally at the recommended therapeutic doses (see subsection "Pharmacokinetics").

Fluticasone furoate can be used during pregnancy only in cases where the expected benefit of therapy for the mother exceeds the potential risk to the fetus.

Breastfeeding period

Excretion of fluticasone furoate with human breast milk has not been studied.
Fluticasone furoate may be used in lactating women only if the expected benefit to the mother exceeds the potential risk to the child.
APPLICATION FOR FUNCTIONS OF THE LIVER

Patients with renal dysfunction do not need dose adjustment.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

In patients with mild and moderate impairment of liver function, dose adjustment is not required.
There is no data on the use in patients with severe impairment of liver function .
APPLICATION FOR CHILDREN

For children from 2 to 11 years of age, the recommended initial dose is 27.5 μg (1 spray) in each nostril 1 time / day (55 μg / day).

If there is no desired effect at a dose of 27.5 μg (1 sputtering), a dose increase up to 55 μg (2 sprays) per nostril 1 time / day (110 μg / day) is possible in each nostril 1 time / day.
When adequate control of symptoms is achieved, it is recommended to reduce the dose to 27.5 μg (1 spray) in each nostril 1 time / day (55 μg / day).
There is insufficient data to recommend the application of fluticasone furoate intranasally for the treatment of seasonal and year-round allergic rhinitis in children under 2 years of age .

APPLICATION IN ELDERLY PATIENTS

Older patients are not required to adjust the dose.

SPECIAL INSTRUCTIONS

The drug Avamis is intended only for intranasal use.

Fluticasone furoate undergoes metabolism at the "first passage" through the liver with the participation of the CYP3A4 isoenzyme of the cytochrome P450 system.
Therefore, in patients with severe impairment of liver function, the pharmacokinetics of fluticasone furoate may vary (see "Drug Interactions" and "Pharmacokinetics" section). Dose adjustments in patients with mild and moderate impairment of liver function (Child-Pugh class A and B) are not required. There is no data for patients with severe impairment of liver function (Child-Pugh class C). Caution should be exercised when determining the dose for patients with severe impairment of liver function. such patients may be more at risk of systemic adverse reactions associated with the use of GCS (see section "Dosage regimen" and section "Pharmacokinetics").
Based on the application of other glucocorticosteroids, which is metabolized by isoenzyme SYR3A4 cytochrome P450, with ritonavir, combined use of ritonavir with fluticasone furoate is not recommended due to the possible risk of increased systemic exposure fluticasone furoate (see. The section "Patient interaction" and to "Pharmacokinetics" ).
Systemic effects characteristic of corticosteroids (such as Cushing's syndrome, adrenal suppression, growth retardation in children and adolescents, cataract, glaucoma) as well as a number of psychological or behavioral effects including psychomotor hyperactivity, sleep disturbance, anxiety, depression or aggression (especially in children), can occur in the application of intranasal corticosteroids. The likelihood of such effects is much lower than with oral dosage forms of corticosteroids and oral and intranasal combined SCS. The effects may vary in individual patients, and also for different glucocorticosteroids. If there is any reason to believe possible violations of
adrenal function, caution should be exercised when switching patients from systemic steroid therapy to fluticasone furoate.
In children who received 110 micrograms of fluticasone furoate daily for one year, there was a decrease of growth rate. However, the results of this study do not allow us to determine the statistical frequency of manifestations of this undesirable phenomenon, since s is possible to calculate the effect of the drug on the final figures of growth in children (see. Section "Side effects"). As a maintenance dose to be used in children lowest dose that provides adequate control of symptoms (see. The section "metering mode").
It is recommended to regularly monitor the growth of children receiving long-term therapy with corticosteroids intranasally. If growth is slowed, if possible therapy should be reviewed in order to reduce intranasal doses of corticosteroids to the lowest dose at which it is maintained effective control of symptoms. In addition, should pay attention to the direction of the patient to the pediatrician.
As with other intranasal corticosteroids, physicians must be alert for possible systemic effects of corticosteroids, including changes in the organ of vision. Therefore, close monitoring is warranted in patients with deteriorating vision or increased intraocular pressure, glaucoma and / or cataracts in history.
Impact on the ability to drive vehicles and manage mechanisms

Based on the pharmacological properties of fluticasone furoate and other corticosteroids for topical application, the impact on the capacity for road management or other mechanisms are envisaged.
OVERDOSE

Symptoms in the bioavailability study drug dose applied intranasally with 24 times higher than the recommended doses for adults for more than 3 days, the undesirable systemic reactions were observed.
Treatment: it is unlikely that acute overdose require other treatment besides medical supervision.
DRUG INTERACTION

Fluticasone furoate is rapidly excreted, subjected to primary metabolism in liver involving CYP3A4 isoenzyme of cytochrome P450. The study drug interaction fluticasone furoate and highly active inhibitor of isozyme CYP3A4 - ketoconazole was observed more cases of determining plasma concentrations of fluticasone furoate, which values ​​are above the threshold, in patients treated with ketoconazole (6 of 20 patients) compared to placebo (1 out of 20 patients ). This slight increase does not result in a statistically significant difference in plasma cortisol for 24 hours between the two groups.
On the basis of theoretical data is not intended any drug interactions fluticasone furoate applied intranasally, according to the instructions for use, with other drugs that are metabolized by the participation of cytochrome P450 isoenzymes. Therefore, clinical trials to study the interaction between fluticasone furoate and other drugs have not been conducted (see. Section "Special instructions").
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be kept out of reach of children at a temperature not higher than 30 ° C; Do not freeze.
Shelf life - 3 years.

Alphabetical index of medicines:
A  B  V  G  D  E  J
Z  I  Y  K  L  M  N
O  P  R  S  T  U  F
H  C  CH  SH  E  U  Y
Rambler's Top100
Privacy policy:
Copyright 2009 - 2017. Universal reference book of medicines. All rights reserved.
When using site materials, an active hyperlink is required!