Following intranasal administration at a dose of fluticasone propionate 200mkg / day. maximum plasma concentration equilibrium is not quantitatively defined in the majority of patients (up less than 0.01 ng / ml). The highest plasma concentration was recorded at 0,017 ng / ml. The direct absorption from the nasal cavity is unlikely due to the low water solubility and most of drug ingestion.
Absolute oral bioavailability is low (less than 1%) by a combination of incomplete absorption from the gastrointestinal tract and the active first-pass metabolism through the liver. Total systemic absorption, thus, extremely low. Distribution Fluticasone propionate has a high volume of distribution at steady state (approximately 318 L). Communication to plasma proteins is high (91%). MetabolismFluticasone propionate is displayed rapidly from the systemic circulation predominantly by hepatic metabolism to form inactive carboxylic acid by oxandrolone cycle isoenzyme of cytochrome P450. The metabolism of ingested fraction fluticasone propionate in the first pass through the liver in the same manner. Excretion Excretion fluticasone propionate is linear over a dose range of from 250 to 1000 g and characterized by a high plasma clearance. Maximum plasma concentration is reduced by approximately 98% within 3-4 hours, and only at very low concentrations in plasma terminal half-life was observed 7,8 h Renal clearance of fluticasone propionate is negligible (less than 0.2%), and an inactive metabolite. – carboxylic acid – less than 5%. Fluticasone propionate and its metabolites are mostly excreted in bile via the intestine. Indications for prevention and treatment of seasonal and perennial allergic rhinitis.
Contraindications for use
Hypersensitivity to fluticasone propionate or any other component of the drug; Children under 4 years old.
- Simultaneous treatment with strong inhibitors isoenzyme, such as ketoconazole and ritonavir may cause increasing concentration of fluticasone propionate in plasma.
- When applied simultaneously with other dosage forms of corticosteroids.
- If you have infection of the nasal cavity or paranasal sinuses. Thus infectious diseases of the nose requires appropriate treatment, but are not a contraindication to the use of a nasal .
- After recently undergone surgery or injury to the nose to the nasal cavity or in the presence of ulceration of the nasal mucosa.
Pregnancy and lactation
Pregnant and lactating women drug oxandrolone cycle can be given only in cases where the expected benefit to the patient is greater than any possible risk to the fetus or child.
Dosing and Administration
You need to use the drug on a regular basis to achieve full therapeutic effect. The maximum therapeutic effect may be achieved after 3-4 days of treatment.
Adults and children over 12 years old for prophylaxis and treatment of seasonal and perennial allergic rhinitis 2 injections into each nostril once a day 1, preferably in the morning (200 mg per day). In some cases it is possible to apply to 2 injections into each nostril two times daily (400 mg per day) for a short time to achieve control of symptoms, after which the dose can be reduced. The maximum daily dose – 400 g (not more than four injections in each nostril).
Specific patient groups elderly The usual adult dose. Children from 4 to 12 years for the prevention and treatment of seasonal and perennial allergic rhinitis by injection of 1 s (50 mcg) in each nostril 1 times a day, preferably in the morning. In some cases, it may require the appointment of 1 injection into each nostril 2 times a day. The maximum daily dose -. 200 g (not more than 2 injections in each nostril) The use of the inhaler before use should be carefully shake the bottle, take it, placing the index and middle fingers . on both sides of the tip, and the thumb – a bedplate for the first use of a drug or a break in its use of more than 1 week, check the serviceability sprayer: send a tip by itself, produce a few clicks, until the tip of a small cloud appears not. Next, you need to clean the nose (blow your nose).Close one nostril and put the tip into the other nostril. Tilt oxandrolone cycle your head slightly forward while holding the vial upright. Then. should begin to breathe in through the nose and by continuing to inhale, to produce a single finger tap to spray the drug. Exhale through the mouth. Repeat the procedure for a second spray into the same nostril, if necessary. Next, repeat the above procedure completely, insert the tip 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, carefully remove the tip and rinse it in warm water. Shake off excess water and leave to dry in a warm place. Avoid overheating. Then gently install the tip into place at the top of the vial. Wear protective cap. If clogged nozzle hole, the tip should be removed in the manner described above and leave for some time in the warm water. Then rinse under cold water, dry and put on a bottle again. You can not clean the hole with a pin or other sharp object tip.
Adverse events reported below are listed according to the anatomical and physiological classification and frequency of occurrence. Very often, frequently and infrequently occurring adverse events were mainly established on the basis of the clinical study.
The phenomena that occur rarely and very rarely, mostly identified from spontaneous reports. In the formation of the incidence of adverse events, the background rates in the placebo group were not taken into account, as they were generally comparable with the group of active treatment. Immune system : very rarely – hypersensitivity reactions (including bronchospasm, rash, swelling of face and tongue , anaphylactic reactions), anaphylactoid reactions. nervous system : often . – headache, a feeling of unpleasant taste and odor The appearance of headache, unpleasant taste and smell have also been reported with other nasal sprays. From a sight organ : very rarely – glaucoma , increased intraocular pressure, cataract. The causal relationship between intranasal receiving fluticasone propionate and these events in clinical trials lasting up to 1 year has not been revealed. The respiratory system, organs, thoracic and mediastinal disorders : very often – nosebleeds, often – dryness in the nasal cavity and pharynx, irritation of the nasal cavity and pharynx (reported as with other oxandrolone cycle nasal preparations); very seldom – nasal septum perforation (reported when receiving intranasal corticosteroids).