2010/06/05

AVAMIS

Pharmacological properties: Pharmacodynamics. Flyutikazona furoate - a synthetic fluorinated corticosteroid with a very high affinity for glucocorticoid receptors and a strong anti-inflammatory action.
Pharmacokinetics. Flyutikazona furoate undergoes extensive first pass metabolism and incomplete absorption in the liver and intestines, resulting in very little systemic effects of the drug. Typically, intranasal application of 110 mg 1 time per day achieved this concentration of the drug in plasma, which can not be measured (≤ 10 pg / ml). Absolute bioavailability flyutikazona furoate applying 880 mg 3 times daily (total daily dose - 2640 mg) is 0,5%.
Level flyutikazona furoate binding to proteins in blood plasma of 99%. The drug is widely distributed, volume of distribution is approximately 608 liters.
Flyutikazona furoate is rapidly excreted (total plasmatic clearance - 58 l / h) from the systemic circulation, mainly through hepatic metabolism involving CYP 3A4 enzyme cytochrome P450 to the inactive carboxyl metabolite (GW694301X). The primary mechanism of metabolism is the hydrolysis of S-flyuorometilkarbotionata to metabolite 17β-carboxylic acid. Is derived after oral and / in use, mainly in the faeces with signs of excretion flyutikazona furoate and its metabolites with bile. After i / v use half-life - 15,1 hours Excretion in the urine is approximately 1 and 2% after oral and / in the application accordingly.

INDICATIONS: Allergic rhinitis (as a symptomatic therapy).

APPLICATION: Avamis intranasal use only.
Adults and children over the age of 12 years: The recommended starting dose - 2 injection (27.5 micrograms per 1 injection) in each nasal passage 1 time per day (total daily dose - 110 micrograms).
After achieving control of symptoms of rhinitis maintenance dose can be reduced to 1 injection into each nasal passage 1 time per day (total daily dose - 55 micrograms).
Children aged 6-11 years: The recommended starting dose - 1 injection each nasal passage 1 time per day (total daily dose - 55 micrograms). In case of inadequate control of symptoms of rhinitis when injected into each nasal passage 1 time per day (total daily dose - 55 mg) dose may be increased to 2 injections into each nasal passage 1 time per day (total daily dose - 110 micrograms). After achieving control of symptoms of rhinitis dose reduced to 1 injection into each nasal passage 1 time per day (total daily dose - 55 micrograms).
Elderly patients using the same dose as in adults.
In renal insufficiency, dosage adjustment is not needed.
Hepatic insufficiency of mild to moderate severity does not require dose adjustment. Data on severe liver failure there.
To achieve the full therapeutic effect of the drug should be used regularly, that should inform the patient. Onset of action occurs within 8 h after the first application, maximum therapeutic effect after a few days of starting treatment. Duration of treatment should be limited to the period of influence allergen.
Terms of Use nasal sprays
Nasal metered dose spray consists of a glass bottle, placed in a plastic housing with a protective cap, which closes the tip of the sprayer (a special device at the upper end of the spray). In the lower part of the body are small holes through which the visible presence of the drug in a glass vial. At one of the sides of the plastic casing is a large dosing button, when clicked, which is fed through spray atomizer.
Before the first application (and if the drug is not used within 1 month) should check the device:
Shake the closed bottle (without removing the protective cap);
remove the cap, pulling it up, lightly pressing his fingers on both sides;
strongly press the dispensing button (not less than 6 times) for the release of a sufficient number of spray into the air.
Before each application must clear nasal passages, a little shake and spray the following steps:
slightly tilt your head forward;
holding the spray upright and gently place the dispenser in one nasal passage;
send a spray nozzle in the opposite direction from the nose to the drug is uniformly distributed in the nasal cavity;
inhale nose and simultaneously press the dispensing button on a plastic housing for spraying a spray in the nasal cavity;
Avoid getting spray into the eyes, and if this happens, rinse eyes with water;
, remove the spray from the nose and exhale mouth.
For the introduction of spray in the other nasal passage procedure is repeated in the same sequence.
Always close the device after the application of a protective cap.
After each use of a spray nozzle and cap is wiped clean, dry cloth.

CONTRAINDICATIONS: Hypersensitivity to the drug's components.

SIDE EFFECTS: very often (≥ 1 / 10), often (≥ 1 / 100 and ≤ 1 / 10), rare (≥ 1 / 1000 ≤ 1 / 100), sometimes (≥ 1 / 10 000 and ≤ 1 / 1000 ), isolated cases (≤ 1 / 10 000).
On the part of the respiratory system: very often - nosebleeds, often - sores on the mucous membrane of the nose. Epistaxis were usually mild or moderate degree. In adults and adolescents nasal bleeding occurred more frequently with prolonged use (6 weeks) than in the application of up to 6 weeks. In the pediatric clinical trials of up to 12 weeks, cases of nasal bleeding were similar in the group, which applied flyutikazona furoate and placebo.
On the part of the immune system: sometimes - hypersensitivity reactions, including anaphylaxis, angioedema, rash, and urticaria.

Cautions: flyutikazona furoate undergoes extensive first pass metabolism in the liver, so systemic effects intranasal flyutikazona furoate with severe liver disease may increase, which in turn may increase the risk of systemic side effects. Therefore, use in patients with severe hepatic insufficiency should be cautious.
Do not recommend the use of the drug combined with ritonavir due to the increased risk of systemic effects flyutikazona furoate.
Exceeding the recommended dose of intranasal GCS can cause clinically significant adrenal suppression. In times of stress or elective surgical intervention need to take into account the additional use of systemic GCS in the presence of signs of exceeding the recommended dose of GCS. Application of 110 mg / day flyutikazona furoate is not associated with the suppression of the hypothalamic-pituitary-adrenal system in adults and children. However, the dose intranasal flyutikazona furoate reduced to the minimum effective. As with the application of other intranasal GCS in the case of concomitant use of any other types of corticosteroid therapy take into account their overall systemic impact.
When treating children intranasal GCS in recommended doses, there were instances of stunted growth. Therefore, we recommend regularly measuring the growth of children with long-term therapy intranasal GCS. If you delay your child grows, treatment should be reviewed to reduce the dose, if possible - to the minimum effective.
In the case of signs of adrenal suppression function to transfer a patient with systemic use of steroids on the intranasal application flyutikazona furoate should be cautious.
Avamis contains benzalkonium chloride, which can cause irritation of the nasal mucosa.
During pregnancy and lactation. Flyutikazona furoate is used in this period, if the expected benefit to the mother exceeds potential risk to the fetus / child.
For children aged under 6 years old to apply Avamis not recommended, since the experience of the drug in pediatric practice is not enough.
Ability to influence the reaction rate on driving or using machinery is unlikely.

INTERACTION: flyutikazona furoate is rapidly excreted by the extensive first pass metabolism in the liver by cytochrome P450 3A4.
According to the results of other SCS - flyutikazona propionate, which is also metabolized by CYP 3A4, is not recommended the combined use with ritonavir due to increased systemic impact flyutikazona furoate.
Apply flyutikazona furoate in combination with strong CYP 3A4 inhibitors should be cautious due to the increasing influence of systemic flyutikazona furoate. In a clinical study drug interaction flyutikazona furoate with strong CYP 3A4 inhibitor ketoconazole number of persons whose concentration flyutikazona furoate in plasma can be measured, it was greater in the group using ketoconazole (6 to 20) compared with placebo (1 to 20). This is a slight strengthening of systemic effects caused no statistically significant difference in 24-hour levels of cortisol in the blood plasma in these 2 groups.
Data for the study of enzyme induction and inhibition suggest that there is no reason to expect the metabolic interaction between flyutikazona furoate and other neurotransmitters metabolism of cytochrome P450 in the relevant intranasal dosages for clinical application. Therefore, clinical studies on the interaction flyutikazona furoate and other drugs was not performed.

OVERDOSE: According to clinical studies with intranasal application of up to 2,640 micrograms of the drug per day for 3 days, side effects were observed. In applying the drug in high doses necessary to monitor the condition of the patient. In case of overdose Treatment is symptomatic.

Storage conditions: at temperatures below 30 ° C. Do not store in the refrigerator. Do not freeze. Before use, stir.