At recommended doses, has a pronounced anti-inflammatory, anti-edema and anti-allergic effect. Anti-inflammatory effect is realized by the interaction of the drug with the receptors glucocorticosteroids. Inhibits proliferation of mast cells, eosinophils, lymphocytes, macrophages, neutrophils, reduces the production and release of mediators of inflammation and other testosterone cypionate vs enanthate biologically active agents (including histamine, prostaglandins, leukotrienes, cytokines) during the early and late phase allergic reactions. Allergy effect occurs within 2-4 hours after the first application.Reduces itchy nose, sneezing, runny nose, nasal congestion, discomfort in the sinuses and feeling of pressure around the nose and eyes. It eases eye symptoms associated with allergic rhinitis. Effect of the drug is maintained for 24 hours after a single application. When used in therapeutic doses fluticasone not show systemic action and almost no effect on the hypothalamic-pituitary-adrenal axis.
Pharmacokinetics Absorption: Following intranasal fluticasone (200 mcg / day), the maximum plasma concentration in the majority of patients following detection level (<0.01 ng / ml). Immediate absorption from the nasal mucosa is very low due to the low solubility of the drug in water and therefore most of the ingested dose. When taken orally, it enters into the blood fluticasone less than 1% of the dose due to the low absorption and first-pass metabolism. These reasons due to the extremely low total absorption of the drug with the mucous membranes of the nasal cavity and gastrointestinal tract. Distribution:
Fluticasone steady state volume of distribution is significant – about 318 liters. Plasma protein binding is 91%.
Has the effect of “first pass” through the liver. It is metabolized in the liver, with the participation of CYP3A4 cytochrome P450 system to produce an inactive carboxyl metabolite. Excretion:
The half-life (T1 / 2) was 3 h. Write mainly through the intestine. Renal clearance of less than 0.2% fluticasone, renal clearance metabolite containing a carboxylic group, less than 5%.
- prevention and treatment of seasonal and perennial allergic rhinitis.
- Hypersensitivity to fluticasone and other ingredients;
- Children under 4 years of age.
- concomitant use with herpes simplex, and bacterial infections of the upper respiratory tract. In such cases, in addition to prescribe antibiotics and / or antiviral agents;
- after surgery testosterone cypionate vs enanthate in the nasal cavity or the nasal injury, and in the presence of ulcerative lesions of the nasal mucosa;
- concurrently with other corticosteroids dosage forms, including tablets, creams, ointments for treating asthma, nasal or similar eye drops and nasal sprays.
Pregnancy and lactation
is not recommended to prescribe during pregnancy. If necessary, take into account the expected benefits of therapy for the mother and the potential risk to the fetus.
The penetration of fluticasone in breast milk is unlikely. However, at the time of the drug is recommended to stop breastfeeding.
DOSAGE AND ADMINISTRATION:
Adults and children 12 years and older: 2 doses (100 micrograms) in each nasal passage 1 time per day, preferably in the morning. In some cases, you must enter the 2 doses in each nostril 2 times a day (maximum daily dose 400 mg). After a therapeutic effect can be administered to a maintenance dose of 50 mg per day in each nostril (100 mcg). The maximum daily dose should not exceed 400 micrograms (4 doses in each nostril).
Elderly patients do not require dose adjustment. Children aged 4 to 12 years of age: one dose (50 mg) once a day in each nostril, preferably in the morning. The maximum daily dose should not exceed 200 micrograms in each nostril. It is necessary to use the minimum dosage that provides effective removal of symptoms.
the drug should be used regularly to achieve full therapeutic effect.
DIRECTIONS FOR USE
bottle of nasal spray is equipped with a protective cap, which protects the tip from dust and dirt.
The first application is necessary to prepare a bottle: press the dispenser 6 times. Nozzle mechanism is unlocked. If you have not used the drug for more than one week, you should prepare spray bottle and unlock the mechanism again. Next, you need:
- clean the nose;
- close one nostril and put the tip into the other nostril;
- Tilt your head forward slightly, still holding a spray bottle vertically;
- begin to inhale through the nose and by continuing to inhale, to produce a single touch of a finger to spray;
- exhale through the mouth.
Next, in the same way to inject the drug into the other nostril. After use, the tip should be wet with a clean cloth or handkerchief and close the cap. The sprayer should be washed at least 1 time per week. To do this, remove the tip, wash it in warm water, dry and then carefully set at the top of the vial. Wear protective cap. If clogged nozzle hole, the tip should be removed and leave for some time in the warm water. Then rinse under the tap, dry and put on a bottle again. You can not clean the hole with a pin or other sharp objects.
Use for a maximum of 3 months after the first application of spray.
. Local reactions are often observed headaches, dryness and irritation of the nose and throat, unpleasant taste and smell, a burning sensation, stuffy nose, bleeding from the nose; rarely perforation of the nasal septum (usually in patients who had previously had surgery in the nasal cavity).
Allergic reactions. There are skin rash, very rare anaphylactic reactions and bronchospasm, angioedema (mainly facial edema, oral cavity and pharynx).
With prolonged use at high doses, concomitant or prior use of systemic effects of glucocorticosteroids are rarely observed decrease in adrenocortical function, osteoporosis, growth testosterone cypionate vs enanthate retardation in children, cataracts, increased intraocular pressure.
symptoms of acute and chronic overdose has been reported. When administered intranasally volunteers fluticasone 2 mg 2 times a day for 7 days did not found any effect on the hypothalamic-pituitary-adrenal axis.
INTERACTION WITH OTHER DRUGS
interaction with other drugs is unlikely, since the intranasal route of administration of fluticasone plasma concentrations are very low. In an application with strong inhibitors of CYP3A4 cytochrome P450 system (ritonavir) may increase fluticasone systemic effects and the development of side effects (Cushing’s syndrome, depression of adrenocortical function). While the use of other inhibitors of cytochrome P450 (erythromycin, ketoconazole) observed a slight increase in the blood concentration of fluticasone that virtually no effect on cortisol.
Interactions with inhibitors of the CYP3A4 isoenzyme of cytochrome P450 (ritonavir, ketoconazole) requires careful monitoring of the patient, as these drugs may cause an increase in plasma fluticasone concentrations.
Occurrence of the systemic effects of nasal corticosteroids, especially if they are assigned for a long period of time and in large doses. Therefore, long-term use of the drug requires regular monitoring of adrenocortical function. Since nasal steroids, even when used in approved doses may cause slowing of growth in children with long-term treatment, it is necessary to regularly monitor the growth of the child and in a timely manner to adjust the dose of the drug.
In the treatment of seasonal allergic rhinitis Nazarel quite effective, but in the case of particularly high concentration in the air in the summer allergens may require additional treatment. geneza pharmaceuticals arnold bodybuilder tramadol 100mg female bodybuilding diet plan