Fluticasone: instructions for use, price

Fluticasone is a synthetic drug from the group of glucocorticoids. It was first authorized in Switzerland in 1993.

Fluticasone is a synthetic and fluorinated glucocorticoid. Esters of fluticasone propionate and fluticasone furoate are used as medicines. Fluticasone propionate is a colorless solid that is present as a white or off-white powder. The molecule is very lipophilic. Therefore, fluticasone is almost insoluble in water, but quickly reaches cells and binds to cytosolic glucocorticoid receptors. The active substance is metabolized through the enzyme CYP3A4.

Chemical properties

Fluticasone furoate - what kind of medicine is it? This chemical compound is a fluorinated synthetic corticosteroid . In medications, the substance is most often found in combination with almeterol and is part of the most important and vital drugs.

Derived from this chemical. compounds - Fluticasone furoate ( C27H29F3O6S ) is used as a local anti-inflammatory agent. Fluticasone furoate preparations are not intended for systemic use. The chemical compound is a white fine powder that is practically insoluble in water. Molecular mass = 538.6 grams per mole. The price of Fluticasone furoate depends on the manufacturer and the content of the active ingredient in the medicine. Preparations containing this substance are produced in the form of nasal sprays, creams, inhalers, ointments, etc. The medicine also contains fluticasone propionate .

Fluticasone prescription in Latin

Fluticasone in aerosol form.

The fluticasone prescription in Latin will be written depending on the dosage form to be prescribed. Fluticasone is available as a nasal spray, inhalation powder, inhalation suspension (metered dose inhaler), cream, and ointment. Read more about the rules for extracting in our article: recipe in Latin.

Fluticasone nasal spray prescription:

Rp.: Fluticazoni propionatis 120 doses DS In the nose, 2 doses in each nostril 1 time per day.

Fluticasone aerosol prescription:

Rp.: Aer. Fluticazoni propionatis N 1 DS 2 breaths 2 times a day

Recipe for fluticasone in ointment form - more details about the ointment recipe in Latin.

Rp.: Ung. Fluticazoni propionatis 0.05 – 15.0 DS Apply to affected skin areas 2 times a day.

Trade names

You can also write out a prescription for fluticasone by a trade name, for example, let’s write out a prescription for nasophane in Latin:

Rp.: “Nasofan” 120 doses DS Into the nose, 2 breaths 1 time per day.

Fluticasone is available in the world in the form of a single drug: Axotide (CH), Avamys (EU), Flutide (D), Nasofan (CH), Cutivate (AT, CH). And in the form of a combination drug:

with salmeterol: Atmadisc (D), Rolenium (D), Seretide (D, CH, A), Viani (D, A), Airflusal (D, A);
with formoterol: Flutiform (D);
with azelastine: Dymista (D, USA, LT) – more about azelastine.
with vilanterol: Relvar (D, CH)

Pharmacodynamics and pharmacokinetics

Fluticasone, upon contact with specific glucocorticosteroid receptors, inhibits the proliferation of eosinophils , lymphocytes , mast cells , neutrophils and macrophages . The substance reduces the intensity of the formation and release of inflammatory mediators ( prostaglandins , cytokines , histamine and leukotrienes ). The effect of the medicine appears within 180 minutes after the first use. When used intranasally, the product eliminates unpleasant sensations in the nose, sneezing, rhinitis , and nasal congestion. Redness in the eyes also goes away and tearfulness decreases. The duration of action of the substance after the first use is one day.

If you do not exceed the recommended therapeutic dosages, the medicine does not penetrate the systemic circulation and does not affect the hypothalamic-pituitary-adrenal system. The drug is very poorly soluble in water, so most of it flows down the back wall of the larynx and enters the stomach. Less than 1% of the dose taken penetrates into the blood.

The bioavailability of the drug after inhalation administration ranges from 10 to 30%. However, the drug has a fairly high degree of binding to plasma proteins - 91%. The substance undergoes a first-pass effect through the liver, where it is metabolized with the participation of the CYP3A4 cytochrome P450 (a negative carboxyl metabolite is formed). The half-life of the drug is approximately 3 hours for intranasal administration and 8 for inhalation administration. Fluticasone is excreted through the intestines and via the kidneys.

FeniVate, 1 piece, 15 g, 0.005%, ointment for external use

Manifestations of hypercorticism (Cushing's syndrome) and reversible inhibition of the HPA axis, leading to glucocorticoid insufficiency, in some cases occur due to increased systemic absorption of GCS for external use. In such cases, it is necessary to gradually stop treatment, reducing the frequency of applications, or replace the drug FeniVate with a less active GCS. Sudden cessation of treatment may lead to glucocorticoid insufficiency.

Risk factors for severe systemic reactions include the following:

activity and dosage form of GCS for external use;
duration of treatment;
application to large areas of the skin;
increased hydration of the stratum corneum of the dermis;
application to areas with thin skin such as the face;
damaged skin or other conditions potentially accompanied by damage to the skin barrier;
Compared to adults, children are likely to absorb more corticosteroids for external use, thereby increasing the risk of developing systemic adverse reactions. This is due to the immaturity of the skin barrier and the higher body surface area to body weight ratio in children compared to adults.

In children from 10 to 12 years of age, long-term continuous therapy with GCS for external use should be avoided if possible, as there is a possibility of suppression of adrenal function.

Cases of visual impairment have been reported with the use of systemic and local corticosteroids, resulting from increased systemic availability and direct eye contact. Therefore, if a patient has symptoms such as blurred vision or other visual disturbances, consideration should be given to referring the patient to an ophthalmologist to evaluate possible causes, which may include cataracts, glaucoma, or rare diseases such as central serous chorioretinopathy (CSCR).

Long-term application of FeniVate cream to the face area is undesirable, since the skin in this area is more susceptible to atrophic changes. When applying FeniVate cream to the eyelids, it is necessary to ensure that the drug does not get into the eyes, since repeated contact of the drug with the mucous membrane of the eye can lead to the development of cataracts and glaucoma.

In case of secondary infection of skin lesions, appropriate antibacterial therapy must be prescribed. If signs of infection spread, GCS for external use should be discontinued and appropriate antibacterial therapy should be prescribed.

Topical corticosteroid therapy is sometimes used to treat dermatitis that develops around chronic leg ulcers. However, this may be associated with a higher incidence of local hypersensitivity reactions and infectious complications. Obvious inhibition of HPA axis function (morning plasma cortisol level less than 5 mcg/dL) in adults is unlikely when using PheniVate in recommended doses, except when the drug is applied to more than 50% of the body surface area and in an amount of more than 20 g per day.

Indications for use

Fluticasone furoate is prescribed in the form of inhalations for basic anti-inflammatory therapy of bronchial asthma , chronic bronchitis , emphysema , etc.

The substance is prescribed intranasally as a prophylactic agent or as part of a complex treatment for allergic rhinitis .

The drug is used externally:

for atopic , discoid , childhood and other types of eczema ;
for the treatment of nodular prurigo , lichen planus ;
for neurodermatoses ;
in patients with psoriasis (except plaque);
for contact dermatitis ;
in patients with discoid lupus erythematosus ;
as an additional remedy for generalized erythroderma ;
to relieve unpleasant symptoms from insect bites;
for seborrheic dermatitis ;
in patients with miliaria erythematosus .

Contraindications

The medicine is not prescribed intranasally if you are allergic to Fluticasone.

GCS is not recommended for external use:

patients with rosacea ;
for acne ;
patients with perioral dermatitis ;
for primary viral infections, chickenpox , herpes ;
patients with genital and perianal itching;
if the skin is affected by bacteria or fungi;
in children under 6 months (cream) or 1 year (ointment);
if you are allergic to the drug.

Side effects

Fluticasone inhalation may cause:

candidiasis of the oral cavity or pharynx;
paradoxical bronchospasm ;
hoarseness and hoarseness of voice;
decreased function of the adrenal cortex, osteoporosis , growth retardation in children, glaucoma (rare if systemic glucocorticosteroids ).

When administered intranasally, the substance is most often well tolerated. Rarely develop: irritation and dryness in the nasopharynx, unpleasant odor and distortion of taste, perforation of the nasal septum (the likelihood is higher if surgical interventions in the nasal cavity have previously been performed).

The use of Fluticasone-based creams and ointments may cause:

itching, burning and dry skin at the site of application;
stretch marks , thinning of the skin, dilation of blood vessels on the surface;
activation of hair growth, hypopigmentation ;
development of secondary infections and allergic contact dermatitis .

In infants, with prolonged use of high dosages, the drug may undergo systemic absorption and develop symptomatic hypercortisolism .

Side effects of fluticasone

The main side effect is candidal infection of the oral and/or pharyngeal mucosa. Also common are upper respiratory tract infections, hoarseness, pneumonia in patients with COPD (chronic obstructive bronchitis), headaches, weakness, and bruising of the skin.

In order to prevent infection of the mucous membranes of the mouth and pharynx, it is necessary to rinse your mouth with water or eat something after inhalation.

Very rare side effects include angioedema, allergic reactions, Cushing's syndrome, adrenal insufficiency, growth retardation in children and adolescents, anxiety, hyperglycemia, sleep disorders, glaucoma, decreased bone density, behavioral changes, and paradoxical bronchospasm.

Fluticasone, instructions for use (Method and dosage)

Depending on the dosage form and indications, various treatment regimens and methods of using the drug are used. The drug is prescribed externally, intranasally and in the form of inhalations.

Fluticasone, instructions for use of ointment and cream

The product is applied in a thin layer to the affected area of the skin, 1 or 2 times a day, depending on the recommendations of the attending physician. The course of treatment is no more than 14 days.

As a preventative measure, the medicine is used once every 3-4 days, without applying an occlusive dressing, in areas that were previously affected by the disease.

Intranasally. Children over 12 years of age and adults are prescribed 2 doses (100 mcg) of the drug in each nasal passage, once a day, preferably in the morning. If necessary, you can administer 2 doses into each nostril, twice a day. The maximum amount of medication that can be used per day is 400 mcg. Maintenance dosage of Fluticasone = a total of 100 mcg per day.

For children from 4 to 12 years of age, dosage adjustment is required. As a rule, 50 mcg of the drug is prescribed in each nostril. Maximum daily dosage for children = 200 mcg.

Fluticasone inhalation

For bronchial asthma, 100 to 1000 mcg of the substance is prescribed, 2 times a day, depending on how the disease progresses. The dosage is adjusted depending on the response to therapy. For children over 4 years of age, the recommended dosage is 50 to 100 mcg, twice daily. Children aged 12 months to 4 years are recommended to use 200 mcg of the drug per day.

The drug is administered using a special inhaler. For the treatment of chronic obstructive pulmonary disease, 500 mcg of the substance is used 2 times a day.

Fluticasone

INSTRUCTIONS for use of Fluticasone
Code ATX: R01AD08 (Fluticasone)
Active substance:

fluticasone

Dosage form Nasal spray dosed 50 mcg/dose: 12 ml (120 doses) vial.

Release form, composition and packaging Dosed nasal spray in the form of a white or almost white suspension. 1 dose - fluticasone propionate (micronized) 50 mcg Excipients: benzalkonium chloride - 10 mcg, phenylethanol - 250 mcg, polysorbate 80 - 100 mcg, Avicel RC-591 - 1250 mcg, anhydrous dextrose - 5000 mcg, purified water - 0.1 ml. 12 ml (120 doses) - dark glass bottles (1) with a dosing device - plastic trays (1) - cardboard packs.

Clinical and pharmacological group: GCS for inhalation

Pharmacotherapeutic group: Glucocorticosteroid for local use

Pharmacological action Mechanism of action Fluticasone propionate is a substance with a strong anti-inflammatory effect. With intranasal administration, no pronounced systemic effect or inhibition of the hypothalamic-pituitary-adrenal system is observed. No significant changes in the daily area according to the pharmacokinetic curve of serum cortisol were detected after the administration of fluticasone propionate at a dose of 200 mcg/day. compared with placebo (ratio: 1.01, 90% CI 0.9 to 1.14). Fluticasone propionate has an anti-inflammatory effect due to interaction with glucocorticosteroid receptors. Suppresses the proliferation of mast cells, eosinophils, lymphocytes, macrophages, neutrophils; reduces the production of inflammatory mediators and other biological active substances (histamine, prostaglandins, leukotrienes, cytokines) during the early and late phases of the allergic reaction. Fluticasone propionate has a rapid anti-inflammatory effect on the nasal mucosa, and its antiallergic effect appears within 2-4 hours after the first application. Reduces sneezing, itchy nose, runny nose, nasal congestion, discomfort in the sinuses and pressure around the nose and eyes. In addition, it relieves eye symptoms associated with allergic rhinitis. A decrease in the severity of symptoms (especially nasal congestion) persists for 24 hours after a single administration of a spray at a dose of 200 mcg. Fluticasone propionate improves the quality of life of patients, including physical and social activity.

Pharmacokinetics Absorption After intranasal administration of fluticasone propionate at a dose of 200 mcg/day. maximum steady-state plasma concentrations are not quantifiable in most patients (less than 0.01 ng/ml). The highest plasma concentration was recorded at 0.017 ng/mL. Direct absorption from the nasal cavity is unlikely due to low water solubility and ingestion of most of the drug. Absolute oral bioavailability is low (less than 1%) as a result of a combination of incomplete absorption from the gastrointestinal tract and extensive first-pass metabolism through the liver. The total systemic absorption is therefore extremely low. Distribution Fluticasone propionate has a large volume of distribution at steady state (approximately 318 L). The connection with blood plasma proteins is high (91%). Metabolism Fluticasone propionate is rapidly eliminated from the systemic circulation mainly due to metabolism in the liver with the formation of inactive carboxylic acid through the CYP3A4 isoenzyme of the cytochrome P450 system. The metabolism of the ingested fraction of fluticasone propionate during its first passage through the liver occurs in the same way. Elimination The elimination of fluticasone propionate is linear in the dose range from 250 to 1000 mcg and is characterized by a high plasma clearance (1.1 l/min). The maximum plasma concentration decreases to approximately 98% within 3-4 hours, and only at very low plasma concentrations a terminal half-life of 7.8 hours was observed. The renal clearance of fluticasone propionate is negligible (less than 0.2%), and the inactive metabolite is negligible. carboxylic acid - less than 5%. Fluticasone propionate and its metabolites are mainly excreted in bile through the intestines.

Indications Prevention and treatment of seasonal and year-round allergic rhinitis.

Dosage regimen Intranasal only. To achieve the full therapeutic effect, it is necessary to use the drug regularly. The maximum therapeutic effect can be achieved after 3-4 days of therapy. Adults and children over 12 years of age For the prevention and treatment of seasonal and year-round allergic rhinitis, 2 injections into each nostril once a day, preferably in the morning (200 mcg per day). In some cases, you can use 2 sprays in each nostril 2 times a day (400 mcg per day) for a short time to achieve control of symptoms, after which the dose can be reduced. The maximum daily dose is 400 mcg (no more than 4 injections into each nostril). Special groups of patients Elderly patients Usual dose for adults. Children from 4 to 12 years old For the prevention and treatment of seasonal and year-round allergic rhinitis, 1 injection (50 mcg) into each nostril 1 time per day, preferably in the morning. In some cases, it may be necessary to administer 1 spray into each nostril 2 times a day. The maximum daily dose is 200 mcg (no more than 2 injections into each nostril). Using the inhaler Before use, you should carefully shake the bottle, take it by placing your index and middle fingers on either side of the tip, and your thumb under the bottom. When using the drug for the first time or a break in its use for more than 1 week, you should check the serviceability of the sprayer: point the tip away from you, make several presses until a small cloud appears from the tip. Next, you need to clear your nose (blow your nose). Close one nostril and insert the tip into the other nostril. Tilt your head slightly forward while continuing to hold the bottle vertically. Then you should begin to inhale through your nose and, continuing to inhale, press once with your fingers to spray the drug. Exhale through your mouth. Repeat the procedure for a second spray in the same nostril, if necessary. Next, repeat the described procedure completely, inserting the tip into the other nostril. After use, blot the tip with a clean napkin or handkerchief and close it with the cap. The sprayer should be washed at least once a 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 carefully place the tip in its original place at the top of the bottle. Put on the protective cap. If the hole in the tip is clogged, the tip should be removed as described above and left in warm water for a while. Then rinse under running cold water, dry and put back on the bottle. Do not clean the tip hole with a pin or other sharp objects.

Side effects The adverse events presented below are listed depending on the anatomical and physiological classification and frequency of occurrence. The frequency of occurrence is defined as follows: very common (≥ 1/10), common (≥ 1/100 and < 1/10), uncommon (≥ 1/1,000 and < 1/100), rare (≥ 1/10,000 and < 1/1,000), very rare (≥ 1/10,000, including isolated cases). Very common, common and infrequent adverse events are mainly established on the basis of clinical trial data. Rare and very rare phenomena are mainly identified from spontaneous reports. When generating the incidence of adverse events, background rates in the placebo group were not taken into account because they were generally comparable to the active treatment group. From the immune system: Very rarely: hypersensitivity reactions (including bronchospasm, rash, swelling of the face and tongue, anaphylactic reactions), anaphylactoid reactions. From the nervous system: Often: headache, unpleasant taste and smell. Headache and unpleasant taste and odor have also been reported with other nasal sprays. From the organ of vision: Very rarely: glaucoma, increased intraocular pressure, cataracts. A cause-and-effect relationship between intranasal fluticasone propionate and these events was not identified in clinical studies lasting up to a year. From the respiratory system, chest and mediastinal organs: Very often: nosebleeds. Common: dryness in the nasal cavity and pharynx, irritation of the nasal cavity and pharynx (reported as with other intranasal drugs). Very rare: perforation of the nasal septum (reported when taking intranasal corticosteroids).

Contraindications for use : hypersensitivity to fluticasone propionate or any other component of the drug; - children under 4 years of age.

With caution: - simultaneous use with strong inhibitors of the CYP3A4 isoenzyme, such as ritonavir and ketoconazole, may cause an increase in the concentration of fluticasone propionate in plasma; - when used simultaneously with other dosage forms of glucocorticosteroids; - if you have infections of the nasal cavity or paranasal sinuses. In this case, infectious diseases of the nose require appropriate treatment, but are not a contraindication to the use of nasal spray; - after a recent injury to the nose or surgery in the nasal cavity, or in the presence of ulcerations of the nasal mucosa.

Use during pregnancy and breastfeeding Pregnant and lactating women can only prescribe the drug in cases where the expected benefit to the patient outweighs any possible risk to the fetus or child.

Use in children For the prevention and treatment of seasonal and year-round allergic rhinitis, 1 injection (50 mcg) into each nostril 1 time per day, preferably in the morning. In some cases, it may be necessary to administer 1 spray into each nostril 2 times a day. The maximum daily dose is 200 mcg (no more than 2 injections into each nostril). Contraindicated for children under 4 years of age. Use in Elderly Patients Usual dosage for adults.

Special instructions The drug is indicated for intranasal use only. Without medical supervision, the nasal spray should not be used continuously for more than 6 months. With long-term use, regular monitoring of the function of the adrenal cortex is necessary. There are reports of systemic effects when using nasal corticosteroids in very high doses for a long time. These effects are much less likely to occur than with oral corticosteroids and may vary in individual patients and between different corticosteroid medications. Possible systemic effects may include Cushing's syndrome, adrenal suppression, cataracts, glaucoma, and, in even rarer cases, mental or behavioral disorders including psychomotor hyperactivity, sleep disturbance, anxiety, depression, or aggression. In children receiving intranasal glucocorticosteroids, a decrease in growth rate was observed. Therefore, the lowest dose that provides adequate control of disease symptoms should be used as a maintenance dose in children. The full effect of fluticasone propionate nasal spray may not appear until after a few days of treatment. To achieve maximum therapeutic effect, it is necessary to adhere to a regular regimen of use. Caution should be exercised when transferring patients from systemic corticosteroid therapy to treatment with fluticasone propionate nasal spray if there is reason to suspect adrenal dysfunction. For most patients, fluticasone propionate nasal spray relieves the symptoms of seasonal allergic rhinitis, but in some cases, when the concentration of allergens in the air is very high, additional therapy may be necessary. To relieve ophthalmological manifestations against the background of successful treatment of seasonal allergic rhinitis, additional therapy may be required. During post-marketing surveillance, cases of systemic corticosteroid effects, such as Cushing's syndrome and adrenal suppression, have been reported with the combined use of fluticasone propionate and ritonavir. Therefore, concomitant use of ritonavir and fluticasone propionate should be avoided unless the potential benefit to the patient outweighs the possible risk of systemic corticosteroid side effects. Effect on the ability to drive vehicles and machinery No data have been obtained on the effect of the drug on the ability to drive vehicles, however, the side effects that the drug may cause should be taken into account.

Overdose There is no evidence of acute or chronic overdose of fluticasone propionate. In healthy volunteers, intranasal administration of 2 mg fluticasone propionate twice daily for 7 days had no effect on the function of the hypothalamic-pituitary-adrenal axis (doses 20 times higher than the therapeutic dose). Use of the drug in doses higher than recommended for a long period of time may lead to temporary suppression of adrenal function. In such patients, treatment with fluticasone propionate should be continued at doses necessary to control symptoms; Recovery of adrenal function takes several days and is monitored by measuring plasma cortisol levels. Drug Interactions Due to the very low plasma concentrations of fluticasone propionate following use of the nasal spray, clinically significant interactions are unlikely. Ritonavir (a highly active inhibitor of the coenzyme CYP3A4 of the cytochrome P450 enzyme system) is capable of significantly increasing plasma concentrations of fluticasone propionate, resulting in a sharp decrease in serum cortisol levels and systemic side effects, including Cushing's syndrome and adrenal suppression. Inhibitors of the CYP3A4 isoenzyme of the cytochrome P450 enzyme system cause a negligible (erythromycin) or insignificant (ketoconazole) increase in plasma fluticasone propionate concentrations, which do not entail any noticeable decrease in serum cortisol concentrations. However, caution should be exercised when combining inhibitors of the CYP3A4 isoenzyme of the cytochrome P450 enzyme system (for example, ketoconazole) and fluticasone propionate due to a possible increase in the plasma concentration of the latter. During post-marketing surveillance, cases of systemic corticosteroid effects, such as Cushing's syndrome and adrenal suppression, have been reported with the combined use of fluticasone propionate and ritonavir. Therefore, concomitant use of ritonavir and fluticasone propionate should be avoided unless the potential benefit to the patient outweighs the possible risk of systemic corticosteroid side effects.

Storage conditions and periods Store in a dry place at a temperature not exceeding 25°C. Do not freeze. Keep out of the reach of children. Shelf life: 3 years.

Conditions for dispensing from pharmacies By prescription.

Registration certificate holder: SAVAPHARM, LLC (Russia).

Manufactured by: SAVA MEDICA (India).

special instructions

Intranasal administration of the drug is carried out with extreme caution after systemic use of glucocorticosteroids .

Treatment of children is carried out under the supervision of the attending physician. It is necessary to carefully monitor the growth dynamics of children if therapy with the drug is carried out over a long period of time.

Inhalation of the substance is used with caution for pulmonary tuberculosis . Treatment with the drug is stopped, gradually reducing the dose.

When using a cream or ointment based on this medicine, you must avoid getting the drug on the mucous membranes of the eyes. Systemic absorption is most likely to occur in small infants.

Most likely, the drug does not affect the patient’s ability to operate machinery or drive a car.

Drugs containing (Analogs)

Level 4 ATC code matches:
Gistan-N

Sinalar

Avecourt

Mesoderm

Momederm

Betazon

Silkaren

Elokom

Flucinar

Sinaflan

Celestoderm

Cutivate

Advantan

Betamethasone

Beloderm

Mometasone Furoate

Uniderm

Momat

Trade names of this GCS: Cutivate , Flixonase , Fluticasone , Nazarel , Flixotide , Fluticasone Propionate .

The substance is also often used in combination Fluticasone + Salmeterol : Salticasone-native , Seretide , Tevacomb , Salmecort , Seretide Multidisk .