Avamys nasal spray 27.5 ug dose 120dose N1
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Active ingredients
Fluticasone Furoate
Release form
Spray
Composition
In 1 dose: fluticasone furoate micronized 27.5 mcg. Excipients: dextrose - 2750 mcg / dose, dispersible cellulose * - 825 mcg / dose, polysorbate 80 - 13.75 mcg / dose, benzalkonium chloride solution ** - 16.5 mcg ***, disodium edetate - 8.25 mcg / dose, purified water - up to 50 mcl. * viscosity 65 cPz, contains 11% carmellose sodium; ** contains 50% benzalkonium chloride; *** the content of benzalkonium chloride is 8.25 mcg / dose or 0.015% (w / w) in suspension.
Pharmacological effect
GCS for local use. Fluticasone furoate is a synthetic trifluorinated corticosteroids with high affinity for glucocorticoid receptors, it has a pronounced anti-inflammatory effect.
Pharmacokinetics
The absorption of Fluticasone furoate is not completely absorbed, undergoing primary metabolism in the liver and intestines, which leads to a slight systemic effect. Intranasal administration in a dose of 110 μg 1 time / day usually does not lead to the achievement of detectable plasma concentrations (less than 10 pg / ml). The absolute bioavailability of fluticasone furoate when administered intranasally at a dose of 880 mcg 3 times / day (daily dose of 2640 mcg) is 0.5%. The distribution of Fluticasone furoate is associated with blood plasma proteins of more than 99%. When the equilibrium Vd concentration of fluticasone furoate is reached, on average, 608 l. Metabolism Fluticasone furoate is rapidly eliminated from the systemic blood flow (total plasma clearance of 58.7 l), mainly through metabolism in the liver with the formation of an inactive 17β-carboxyl metabolite (GW694301X) with isoenzyme CYP3A4 cytochrome P450 system. The main pathway of metabolism is the hydrolysis of the S-fluoromethylcarbioate group to form a metabolite of 17β-carboxylic acid. In vivo studies have shown that splitting of fluticasone furoate to fluticasone does not occur. Exception When administered orally and in / in the administration, fluticasone furoate and its metabolites are eliminated mainly through the intestine by excretion with bile. With on / in the introduction of T1 / 2 is 15.1 h. About 1% and 2% is excreted by the kidneys by oral administration and in / in the introduction, respectively. Special groups of patients Elderly patients. Pharmacokinetic data are presented only for a small number of elderly patients (n = 23/872; 2.6%). There is no evidence that fluticasone furoate concentrations, which are quantifiable, are higher in elderly patients than in younger patients. Children.In children with intranasal use in a dose of 110 mcg 1 time per day, fluticasone furoate is usually not detected in concentrations that can be quantified (less than 10 pg / ml). Concentrations determined quantitatively were registered in less than 16% of children with intranasal administration at a dose of 110 mcg 1 time / day and less than 7% of children, with intranasal administration at a dose of 55 mcg 1 time / day. There is no evidence that children under 6 years of age are more likely to have an increase in the concentration of fluticasone furoate. Patients with impaired renal function. Fluticasone furoate was not detected in the urine of healthy volunteers by intranasal administration. Less than 1% of metabolites are excreted by the kidneys, so it is not expected that impaired renal function can affect the pharmacokinetics of fluticasone furoate. Patients with impaired liver function. In a study in patients with moderately impaired liver function, with inhalation use of fluticasone furoate at a dose of 400 mcg, Cmax increased by 42% and AUC0-∞ increased by 172%, compared 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 mcg for intranasal use in this group of patients will not lead to the suppression of cortisol. Therefore, it is not expected that moderate liver dysfunction will probably not lead to clinically significant effects when prescribing a standard dose for adults. Thus, dose adjustment in patients with mild and moderate liver dysfunction (class A and B according to Chidd-Pyo) does not required. There is no data on patients with severely impaired liver function (Child-Pugh class C). Caution should be exercised in determining the dose for patients with severely impaired liver function, since such patients may be more at risk of systemic adverse reactions associated with the use of corticosteroids (see sections Dosage regimen and Special Instructions). Other pharmacokinetic parameters Concentration of fluticasone furoate is usually not determined (less than 10 pg / ml) when administered intranasally at a dose of 110 mcg 1 time per day Determined concentrations were observed only in less than 31% of patients aged 12 years and older and less than in 16% of patients under 12 years of age with a dose of 110 mcg administered 1 time / day intranasally. Depending on gender, age (including childhood), race was not observed in cases where concentrations were above or below the threshold of determination.
Indications
Adults and teenagers (aged 12 years and older) - treatment of nasal and ocular 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.
Contraindications
Hypersensitivity to fluticasone furoate and other components of the drug.
Precautionary measures
The drug should be used with caution in patients with severely impaired liver function, since The pharmacokinetics of fluticasone furoate may vary.
Use during pregnancy and lactation
Data on the use of fluticasone furoate during 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 was shown in animal studies, GCS caused malformations, including cleft palate and intrauterine growth retardation. It is unlikely that this data is relevant for people receiving GCS intranasally at recommended therapeutic doses (see Pharmacokinetics). Fluticasone furoate can be used during pregnancy only in cases where the expected benefit of therapy for the mother outweighs the potential risk to the fetus. The period of breastfeeding Excretion of fluticasone furoate with female breast milk has not been studied. Fluticasone furoate can be used in lactating women only if the expected benefit to the mother outweighs the potential risk to the baby.
Dosage and administration
The drug Avamis is intended only for intranasal use. In order to achieve the maximum therapeutic effect, it is necessary to adhere to a regular regimen of administration. Onset of action can be observed within 8 hours after the first injection. It may take several days to achieve the maximum effect. The reason for the lack of immediate effect should be carefully explained to the patient. Treatment of nasal and ocular symptoms of seasonal allergic rhinitis, nasal symptoms of year-round allergic rhinitis in adults and adolescents (aged 12 years and older). The recommended initial dose is 2 sprays (27.5 mcg of fluticasone furoate in one spraying) in each nostril 1 time / day (110mcg / day). If the symptoms are adequately controlled, reducing the dose to 1 spray in each nostril 1 time / day (55 mcg / day) may be effective for maintenance treatment. Treatment of nasal symptoms of seasonal and year-round allergic rhinitis in children aged 2 to 11 yearsRecommended initial dose - 27.5 mcg (1 spray) in each nostril 1 time / day (55 mcg / day). In the absence of the desired effect at a dose of 27.5 mcg (1 spray) in each nostril 1 time / day, you can increase the dose to 55 mcg (2 sprays) in each nostril 1 time / day (110 mcg / day). When adequate symptom control is achieved, it is recommended to reduce the dose to 27.5 mcg (1 spray) in each nostril 1 time / day (55 mcg / day). Children younger than 2 yearsThere are no data to recommend the use of fluticasone furoate intranasally as a treatment for seasonal and year-round allergic Rhinitis in children under the age of 2 years. Elderly patients Dose adjustment is not required (see Pharmacokinetics section). Patients with impaired renal function Dose adjustment is not required (see Pharmacokinetics section). Patients with impaired pecheniKorrektsii function of dose in patients with mild to moderate hepatic impairment (class A and B Child-Pugh) dose adjustment is required. There is no data on patients with severely impaired liver function (Child-Pugh class C). Caution should be exercised in determining the dose for patients with severely impaired liver function, since such patients may be more at risk of systemic adverse reactions associated with the use of corticosteroids (see Pharmacokinetics and Special Instructions section). Usage and treatment rules The indicator window in plastic packaging allows you to control the level of the drug in the vial. In bottles of 30 or 60 doses, the level of the drug will be visible immediately, and in bottles of 120 doses, the initial level of the drug is above the upper border 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 see it in the light. The level will be visible in the viewing window. Preparation for use should be carried out when using the 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. Without removing the cap, shake the bottle well for 10 seconds. The drug is a rather thick suspension and becomes thinner when shaken. Spraying is possible only after shaking. Remove the cap by gently pulling it with your thumb and forefinger. Hold the bottle vertically and direct the tip away from you. Press the button with force, make a few clicks (at least 6) until a small cloud emerges from the tip (if you cannot press the button with one thumb, you should press it with the thumbs of both hands) .5. The spray is ready to use. Application of nasal spray1. Shake the vial thoroughly. Remove cap.3. Clear your nose and tilt your head slightly forward. Insert the tip into one nostril while continuing to hold the bottle vertically.5. Point the tip of the nebulizer on the outer wall of the nose, not on the nasal septum. This will ensure the correct injection of the drug. Begin to inhale through the nose and press once with your fingers to spray the preparation. Remove the nebulizer from the nostrils and exhale through the mouth. If it is necessary to make two injections into each nostril (as prescribed by a physician), paragraphs 4-6.9 should be repeated. Repeat the procedure for the other nostril. Close the bottle cap.11. Avoid spraying the eyes. If the product gets into the eyes, rinse them thoroughly with water. Care of the sprayer After each use: 1. Blot the tip and the inside of the cap with a dry, clean cloth. Avoid ingress of water. Do not attempt to clean the tip opening with a pin or other sharp objects. Always close the vial and keep it closed. The cap protects the sprayer from dust and clogging, seals the bottle, prevents accidental pressing of the button. In case the sprayer does not work: 1. Check the level of the remaining drug in the vial through the viewing window. If only a very small amount of liquid remains, it may not be enough for the sprayer to work. Check the bottle for damage. Check if the tip hole is clogged. Do not attempt to clean the tip opening with a pin or other sharp objects.4.Try to power the device by repeating the procedure for preparing the nasal spray for use.
Side effects
The adverse events listed below are listed in accordance with the damage to organs and organ systems and the frequency of occurrence. The frequency of occurrence is determined as follows: very often (≥1 / 10); often (≥1 / 100, less than 1/10); infrequently (≥1 / 1000, less than 1/100); rarely (≥1 / 10,000, less than 1/1000); very rarely (less than 1 / 10,000, including isolated cases). Adverse events observed in clinical studies From the respiratory system, chest organs and mediastinum: very often - nosebleeds. In adults and adolescents, cases of nasal bleeding were noted 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 treatment up to 12 weeks, the number of cases of nasal bleeding was similar in the group of fluticasone furoate and placebo. Often, ulceration of the nasal mucosa. From the side of the musculoskeletal system and connective tissue: frequency unknown do not allow to determine the statistical frequency of manifestation of this adverse event, since it is impossible to calculate the effect of the drug on the final growth rates in children who participated in the study. Skeleton growth delay in children, it is a systemic adverse event characteristic of GCS with prolonged oral or parenteral administration. Adverse events observed during post-registration monitoring - headache. On the part of the respiratory system, organs of the chest and mediastinum: infrequently - rhinalgia, discomfort in the nose (including burning, irritation in the nose and soreness), dryness in nose; very rarely - perforation of the nasal septum. On the part of the organ of vision: frequencies unknown - transient visual disturbances. You may experience systemic side effects characteristic of corticosteroids (see section Special instructions).
Overdose
Symptoms: In the study of the bioavailability of the drug, doses 24 times higher than the recommended dose for adults for more than 3 days were used intranasally, and no undesirable systemic reactions were observed. Treatment: it is unlikely that acute overdose will require other treatment than medical supervision.
Interaction with other drugs
Fluticasone furoate is rapidly excreted by undergoing primary metabolism in the liver with the participation of the cytochrome P450 isoenzyme CYP3A4. In the study of drug interaction of fluticasone furoate and a highly active inhibitor of the CYP3A4 isoenzyme - ketoconazole, there were more cases of determining plasma concentrations of fluticasone furoate, which values were higher than the threshold, in the group of patients treated with ketoconazole (6 out of 20 patients) compared to placebo (1 out of 20 patients ). This small increase does not lead to a statistically significant difference in plasma cortisol content within 24 hours between the two groups. Based on theoretical data, no drug interaction of fluticonone furoate is used intranasally, according to the instructions for use, with other drugs that are metabolized by participation of cytochrome P450 isoenzymes. Therefore, clinical studies to study the interaction of fluticasone furoate and other drugs were not conducted.
special instructions
The drug Avamis is intended only for intranasal use. Fluticasone furoate is metabolized during the first passage through the liver with the participation of the CYP3A4 isoenzyme of the cytochrome P450 system. Therefore, in patients with severely impaired liver function, the pharmacokinetics of fluticasone furoate may change (see the Drug Interaction section and the Pharmacokinetics section). Dose adjustment in patients with mild and moderate hepatic impairment (class A and B on Child-Pugh) is not required. There is no data on patients with severely impaired liver function (Child-Pugh class C). Caution should be exercised in determining the dose for patients with severely impaired liver function, since such patients may be more at risk of systemic adverse reactions associated with the use of corticosteroids (seesection Dosage regimen and Pharmacokinetics section. Based on data from another GCS, which is metabolized by the cytochrome P450 system CYP3A4 isoenzyme, with ritonavir, co-administration of ritonavir with fluticasone furoate is not recommended because of the possible risk of increased systemic fluticonone furoate (see the section on fluticonone furoicone) interaction and Pharmacokinetics section). Systemic effects characteristic of GCS (such as Itsenko-Cushing syndrome, adrenal suppression, growth retardation in children and sprouts, cataracts, glaucoma), as well as a range of psychological or behavioral effects including psychomotor hyperactivity, sleep disorders, anxiety, depression or aggression (particularly in children), can occur in the application of intranasal corticosteroids. The probability of occurrence of such effects is much lower than with the use of oral forms of GCS and the combination of oral and intranasal GCS. Effects may vary in individual patients, as well as for different corticosteroids. If there is any reason to suggest possible dysfunction of the adrenal glands, care must be taken when switching patients from systemic steroids to fluticasone furoate. Children who received 110 mcg of fluticasone furoate daily for one year experienced a decrease in growth rate. However, the results of this study do not allow to determine the statistical frequency of manifestations of this adverse event, since it is not possible to calculate the effect of the drug on the final growth rates in children (see section Side Effects). As a maintenance dose in children, the smallest dose should be used to adequately control the symptoms of the disease (see section Dosage regimen). It is recommended to regularly monitor the growth of children receiving long-term GCS therapy intranasally. If growth slows down, therapy should, if possible, be revised to reduce the intranasal dose of GCS to the lowest dose at which effective symptom control is maintained. In addition, attention should be paid to the issue of referral of the patient to the pediatrician. As with the use of other intranasal GCS, physicians should be vigilant about the possible systemic effects of GCS, including changes on the part of the organ of vision.Therefore, careful monitoring is justified in patients with visual impairment or with increased intraocular pressure, glaucoma and / or cataracts in history. Effect on ability to drive vehicles and control mechanisms Based on the pharmacological properties of fluticasone furoate and other GCS for local use, the effect on the ability to control motor transport or other mechanisms are not supposed.