Pharmacodynamics
Beclomethasone dipropionate, a synthetic corticosteroid for topical use, has anti-inflammatory, antiallergic and immunosuppressive effects. Increases the production of lipomodulin, which is an inhibitor of phospholipase A, inhibits the release of arachidonic acid. Prevents the marginal accumulation of neutrophils, reduces inflammatory exudation and the production of lymphokines, inhibits the migration of macrophages, reduces the intensity of the processes of infiltration and granulation, and the formation of a chemotaxis substance. Reduces swelling of the nasal mucosa and mucus production. Improves mucociliary transport. It is well tolerated during long-term treatment, does not have mineralocorticoid activity, and has virtually no resorptive effect.
The therapeutic effect of Nasobek, unlike local vasoconstrictors for the treatment of rhinitis, does not appear immediately when administered intranasally. Relief from rhinitis symptoms usually becomes noticeable within a few days of starting treatment.
Nasobek nasal spray doses 50 mcg/dose 200 DOZES
Compound
Active substance: beclomethasone dipropionate - 50 mcg. Excipients: benzalkonium chloride (50% solution) - 0.04 µl, phenylethanol - 250 µg, polysorbate 80 - 5 µg, anhydrous dextrose - 5 mg, microcrystalline cellulose + carmellose sodium (dispersed cellulose) - 1 mg, hydrochloric acid 35% - qs , purified water - up to 0.1 g.
Pharmacokinetics
Absorption and distribution
When administered by inhalation in recommended doses, it does not have significant systemic activity.
After intranasal use, it is quickly absorbed through the nasal mucosa. Part of the administered drug is swallowed. Absorption from the gastrointestinal tract is low. Plasma protein binding - 87%.
Metabolism and excretion
Most of the drug that enters the gastrointestinal tract is metabolized during the “first pass” through the liver. T1/2 – 15 hours. The main part of the drug (35-76%), regardless of the route of administration, is excreted within 96 hours with feces, mainly in the form of polar metabolites; 10-15% is excreted by the kidneys.
Indications for use
Seasonal and year-round allergic rhinitis, vasomotor rhinitis.
Contraindications
Hypersensitivity to beclomethasone and other components of the drug; hemorrhagic diathesis, frequent nosebleeds, pulmonary tuberculosis, children under 6 years of age, pregnancy (first trimester), viral, fungal diseases.
With caution: Amebiasis, glaucoma, severe liver failure, hypothyroidism, recent myocardial infarction, ulceration of the nasal septum, recent surgical interventions in the nasal cavity, recent trauma to the nose, pregnancy (P-3 trimesters), breastfeeding period.
Directions for use and doses
Intranasally.
Adults and children over 12 years old
1-2 doses (50-100 mcg) in each nasal passage 2 times a day (200-400 mcg/day). The maximum daily dose is 400 mcg/day. The daily dose can be divided into 2-4 doses. Children from 6 to 12 years old
The initial dose is 50 mcg (1 dose) in each nasal passage 2 times a day, if necessary - 100 mcg (2 doses) in each nasal passage 2 times a day. The maximum daily dose is 400 mcg/day. The daily dose can be divided into 2-4 doses.
When a therapeutic effect is achieved, the drug is discontinued, gradually reducing the dose.
Elderly patients do not require dose adjustment.
Recommendations for patients on the use of the drug.
Before using the drug, it is necessary to clean the nasal passages.
When using for the first time, you should unlock the spray mechanism: press the dispenser several times until a cloud of aerosol appears. If the drug has not been used for several days, the spray mechanism should be unlocked again.
Before using the drug for the first time, remove the plastic protective half-ring located between the screw-on part and the dosing nasal applicator (see Fig. 1).
1. Before use, shake the bottle slightly, then remove the cap of the nasal applicator.
2. Position the bottle between your thumb and forefinger so that the bottom of the bottle rests on your thumb and your index and middle fingers rest on either opposite side of the bottom of the applicator (see Figure 2).
3. Before the first use of the drug, or in case of a long break in use, the first dose should be sprayed into the air.
4. Exhale lightly through your nose.
5. The nasal passage into which the drug will not be injected should be clamped with a finger, and the applicator should be inserted into the free nasal passage. Then tilt your head slightly so that the bottle is in a perpendicular position (see Fig. 3).
6. Inhale lightly through the open nasal passage and at the same time press the nasal applicator and inject a dose of the aerosol.
7. Exhale through your mouth.
8. When re-introducing the drug into the same nasal passage, repeat the operations described in paragraphs 6 and 7.
9. When introducing the drug into the other nasal passage, repeat the operations described in paragraphs 5, 6, 7, 8.
After finishing using the drug, you should clean the end (upper) part of the applicator with a clean cloth and return the cap to its place.
Cleaning the applicator:
The nasal applicator should be cleaned at least once a week to prevent the possibility of clogging.
To do this, lightly press the bottom of the applicator and remove the nasal applicator (see Fig. 4).
Rinse the applicator and cap with warm water and allow to dry.
After this, put the applicator and cap back on the bottle.
Storage conditions
At a temperature not exceeding 25°C, in a place protected from light.
Do not freeze. Keep out of the reach of children.
Best before date
4 years.
Do not use the drug after the expiration date. After opening the bottle for the first time, the drug must be used within 6 months.
special instructions
Care should be taken to avoid getting Nasobek into the eyes.
The therapeutic effect of the drug Nasobek, unlike local vasoconstrictors for the treatment of rhinitis, does not appear immediately when administered intranasally. Relief of rhinitis symptoms usually becomes noticeable after 5-7 days from the start of use of the drug.
When a therapeutic effect is achieved, the dose of Nasobek should be reduced to the minimum effective dose that controls the course of the disease. Patients at high risk of developing adrenal insufficiency should be under the supervision of a physician.
With long-term use of the drug Nasobek in children, it is necessary to monitor the dynamics of their growth.
Since the drug slows down wound healing, patients with ulceration of the nasal septum, after surgery in the nasal cavity, or nasal injuries should not use Nasobek until the wounds have completely healed.
Infectious diseases of the nasal cavity and paranasal sinuses require appropriate therapy, but are not contraindications to the use of the drug Nasobek.
Benzalkonium chloride contained in the drug Nasobek, with long-term use, increases the risk of swelling of the nasal mucosa. If such a reaction occurs, it is necessary to adjust the dose of Nasobek or use a drug that does not contain benzalkonium chloride.
Description
Glucocorticosteroid for local use.
Dosage form
White opaque suspension, without visible foreign inclusions.
Use in children
Contraindication: children under 6 years of age.
Pharmacodynamics
Beclomethasone is a synthetic glucocorticosteroid (GCS) for topical use that has anti-inflammatory, antiallergic and immunosuppressive effects. Increases the production of lipomodulin, which is an inhibitor of phospholipase A, and inhibits the release of arachidonic acid. Prevents the marginal accumulation of neutrophils, reduces inflammatory exudation and the production of lymphokines, inhibits the migration of macrophages, reduces the intensity of the processes of infiltration and granulation, and the formation of a chemotaxis substance. Reduces swelling of the nasal mucosa and mucus production. Improves mucociliary transport. It is well tolerated during long-term treatment, does not have mineralocorticoid activity, and has virtually no resorptive effect.
Side effects
The incidence of side effects is classified according to the recommendations of the World Health Organization: very often - at least 10%;
often - at least 1%, but less than 10%; infrequently - not less than 0.1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rare (including isolated cases); unknown - insufficient data to estimate the frequency of the phenomenon in the population - less than 0.01%. From the immune system: rarely - skin rash, urticaria, angioedema.
From the nervous system: rarely - disturbance of olfactory and taste sensations, drowsiness, headache, dizziness.
On the part of the organ of vision: unknown - increased intraocular pressure, including glaucoma, cataracts (with long-term use), conjunctival hyperemia, decreased vision.
From the respiratory system, chest and mediastinal organs: rarely - dryness and irritation of the nasopharynx, sneezing, burning, nasal congestion, nosebleeds, atrophy of the nasal mucosa, cough, rhinorrhea; very rarely - ulceration of the nasal mucosa, perforation of the nasal septum (usually in patients who have previously undergone surgery in the nasal cavity).
Other: rarely - myalgia, candidiasis of the oral cavity and upper respiratory tract (with long-term use and/or in high doses (more than 400 mcg/day)); unknown - with long-term use, the development of adrenal insufficiency, a decrease in growth rate in children, and a decrease in bone mineral density are possible.
Use during pregnancy and breastfeeding
The use of the drug Nasobek is contraindicated in the first trimester of pregnancy; the use of the drug Nasobek in the second to third trimester of pregnancy is allowed only if the expected benefit to the mother outweighs the possible risk to the fetus.
When treating with Nasobek during breastfeeding, caution should be exercised.
Interaction
When used simultaneously, phenobarbital, phenytoin, and rifampicin reduce the effectiveness of beclomethasone due to the induction of microsomal oxidation enzymes.
With simultaneous use, methandrostenolone, estrogens, beta2-adrenergic stimulants, theophylline, and corticosteroids for oral administration enhance the effect of beclomethasone. Beclomethasone, when used simultaneously, increases the effect of beta-agonists.
Overdose
With prolonged use of high doses, as well as with simultaneous use of other systemic corticosteroids, symptoms of hypercortisolism may appear. In this case, the drug should be discontinued and the dose gradually reduced.
Release form
Nasal spray dosed 50 µg/dose 200 DOZES.
Impact on the ability to drive vehicles and operate machinery
Due to the fact that drowsiness and dizziness may develop when using the drug Nasobek, caution should be exercised when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Pharmacokinetics
When administered by inhalation in recommended doses, it does not have significant systemic activity. After intranasal use, it is quickly absorbed into the nasal mucosa. Part of the administered drug is swallowed. Most of the drug that enters the gastrointestinal tract is inactivated during its first passage through the liver.
Absorption from the gastrointestinal tract is low. T1/2 - 15 hours. Communication with plasma proteins - 87%.
The main part of the drug (35–76%), regardless of the route of administration, is excreted within 96 hours in the feces, mainly in the form of polar metabolites, 10–15% by the kidneys.
Side effects
When used in therapeutic doses, side effects are rare, including: sneezing, irritation, burning, dry nose; rash, urticaria, angioedema and nasopharyngeal infections caused by fungal flora, rhinorrhea, headache.
In rare cases - nosebleeds, conjunctival hyperemia, increased intraocular pressure, myalgia, drowsiness, cough, decreased sense of taste, atrophy of the nasal mucosa. Extremely rarely - ulceration of the nasal mucosa, perforation of the nasal septum.
With long-term use in doses of more than 1500 mcg/day - systemic side effects (including adrenal insufficiency).
Directions for use and doses
Intranasally.
Before using Nasobek, the nasal passages must be free. Adults and children over 6 years of age: 1 dose (50 mcg) in each nasal passage 2–4 times a day (200–400 mcg). The dose is then reduced depending on the patient's response. The maximum daily dose is 400 mcg.
Directions for correct use:
Before using the spray for the first time, remove the plastic strip between the bottle cap and the nasal applicator.
1. Before use, shake the bottle slightly and then remove the cap of the nasal applicator.
2. Hold the bottle between your thumb and index finger so that the bottom of the bottle rests on your thumb and your index and middle fingers rest on either opposite side of the bottom of the applicator.
3. Before the first use of the drug or in case of a week-long break in use, the first dose should be released into the free space.
4. Exhale lightly through your nose.
5. The nasal passage into which the drug will not be injected should be clamped with a finger, and the end part of the applicator should be inserted into the free nasal passage. Then tilt your head slightly so that the bubble is in a perpendicular position.
6. After this, inhale lightly through the open nasal passage and at the same time press the nasal applicator and administer the dose.
7. Exhale through your mouth.
8. When re-introducing the drug into the same nasal passage, repeat the operations described in paragraphs 6 and 7.
9. When introducing the drug into the other nasal passage, repeat the operations described in paragraphs 4, 5, 6 and 7.
After finishing using the drug, you should clean the end of the applicator with a clean cloth and return the cap to its place.
Cleaning the nasal applicator:
The nasal applicator should be cleaned at least once a week to prevent the possibility of clogging.
To do this, lightly press the bottom of the bottle and remove the nasal applicator from the bottle.
The applicator and cap are rinsed with warm water and allowed to dry. After this, the applicator and cap are placed on the bottle.
Nasobek nasal spray 50 µg/dose 200 doses No. 1
Name
Nasobek
Description
Opaque suspension of white color, does not contain visible foreign particles.
Main active ingredient
Beclomethasone
Release form
Nasal spray dosed 50 mcg/dose in a bottle of 200 doses. Suspension in a 30 ml polyethylene bottle, nominally containing 200 doses. The bottle is equipped with a dosing valve. 1 bottle with instructions for use per cardboard box.
Dosage
50 mcg / 1 dose 200 doses
Pharmacodynamics
Beclomethasone dipropionate (BDP) is a diester of beclomethasone, a synthetic glucocorticoid that has anti-inflammatory and immunosuppressive effects. At recommended doses, the drug has a local effect on the lungs without significant systemic effects, although the mechanism of this action is not yet known. When applied topically, beclomethasone 17,21-dipropionate (BDP) produces potent anti-inflammatory and vasoconstrictor effects. BDP is a prodrug with weak binding affinity for corticosteroid receptors. It is hydrolyzed by esterases to the highly active metabolite beclomethasone -17-monopropionate (B-17-MP), which has high local anti-inflammatory activity. Beclomethasone dipropionate is used for the preventive treatment of hay fever before exposure to an allergen. Regular use of BDP is then continued to prevent recurrence of allergy symptoms.
Pharmacokinetics
Absorption Following intranasal administration of BDP to healthy male volunteers, systemic absorption was assessed by measuring the plasma concentration of its active metabolite B-17-MP. Its absolute bioavailability after intranasal administration is 44% (95% CI 28%, 70%). After intranasal administration, 1% of the dose is absorbed by the nasal mucosa. The rest of the drug is eliminated from the nose by drainage or mucociliary clearance, and absorption from the gastrointestinal tract is possible. The B-17-MP metabolite that reaches the plasma is formed by the conversion of BDP absorbed from the ingested portion of the dose. After oral administration of BDP, systemic absorption was also assessed by measuring the plasma concentration of its active metabolite B-17-MP. Its absolute bioavailability after oral administration was 41% (95% CI 27%, 62%). After an oral dose, B-17-MR is absorbed slowly, with peak plasma concentrations reached after 3-5 hours. Metabolism After oral and intranasal administration, BDP is rapidly cleared from the bloodstream and plasma concentrations are undetectable (50 pg/ml). The majority of an ingested dose of BDP is metabolized during the first pass through the liver. The main product of metabolism is the active metabolite B-17-MR. The minimally active metabolites beclomethasone-21-monopropionate (B-21-MP) and beclomethasone (BON) are also formed, but they have little systemic effect. Distribution BDP is moderately distributed in tissues (201); B-17-MR is distributed more intensively (4241). Plasma protein binding of BDP is moderately high (87%). Elimination Elimination of BDP and B-17-MP is characterized by high plasma clearance (150 and 120 L/h, terminal half-lives are 0.5 hours and 2.7 hours, respectively. After oral administration of BDP, approximately 60% of the dose is excreted in the feces within 96 hours, primarily as free and conjugated polar metabolites.Approximately 12% of the dose is excreted as free and conjugated polar metabolites in the urine.
Indications for use
Nasobek is indicated for the prevention and treatment of: seasonal and year-round allergic rhinitis, including rhinitis due to hay fever (hay fever); vasomotor rhinitis.
Directions for use and doses
Adults and children over 6 years of age: 2 doses in each nostril twice daily (400 mcg beclomethasone per day) are recommended. For some patients, it is preferable to use one dose in each nasal passage three or four times a day. Once symptom control is achieved, the dose is reduced to one dose twice daily in each nostril (200 mcg beclomethasone per day). To maintain effective control of symptoms, the minimum dose should be used. If symptoms recur, patients should return to the recommended dosage of two doses in each nostril in the morning and evening. The full therapeutic effect is achieved after several days of treatment. The maximum recommended daily dose of beclomethasone should not exceed 400 mcg. Elderly patients: adult dose. Children under 6 years of age: Nasobek is not indicated for the treatment of children under 6 years of age due to a lack of clinical data.
Use during pregnancy and lactation
Use during pregnancy The safety of the drug in humans during pregnancy has not been established. Early animal studies demonstrated an increased incidence of cleft palate and decreased fetal growth when maternal oral corticosteroids were administered. There is a very small risk of these effects occurring in the human fetus. It should be noted that similar changes in fetal animals were noted after exposure to relatively high systemic doses. Intranasal use in recommended doses has minimal systemic effect. The use of beclomethasone dipropionate should be avoided during pregnancy. Nasobek is contraindicated in the first trimester of pregnancy. In the next two trimesters, the benefit/risk ratio for the mother and fetus should be weighed. Use during lactation No special studies have been conducted on the penetration of beclomethasone dipropionate into the breast milk of lactating animals. It is likely that beclomethasone dipropionate is excreted in breast milk. But with relatively low doses administered intranasally, levels in breast milk are likely to be low. Before using the drug in nursing mothers, it is necessary to weigh the balance of benefit for the mother and risk for the child. Nasobek should not be used during lactation without consulting a doctor.
Precautionary measures
Systemic effects of nasal corticosteroids may occur, particularly when high doses are used for long periods of time. These effects occur less frequently than with oral corticosteroids and may vary between patients and between different corticosteroid medications. Potential systemic effects may include Cushing's syndrome, Cushingoid features, adrenal suppression, growth retardation in children and adolescents, cataracts, glaucoma, and more rarely, a range of psychological and behavioral effects including psychomotor hyperactivity, sleep disturbance, fear, depression, and aggression (particularly , in children). Continuous monitoring of the growth of children receiving treatment with nasal corticosteroids for a long time is recommended. When children's growth slows, therapy should be reconsidered to reduce the dose of nasal corticosteroids, if possible, the lowest dose that provides effective control of symptoms should be prescribed. Additionally, the decision of the pediatrician is made in relation to the patient. Treatment with doses higher than recommended may result in clinically significant adrenal suppression. Caution is required when transferring patients from systemic corticosterol therapy to Nasobek, as hypothalamic disorders are possible. In most cases, Nasobek controls seasonal allergic rhinitis, but concomitant therapy for ocular symptoms may be needed for severe allergies. Proper treatment of infections of the nasal passages and paranasal sinuses should be carried out, but this should not create a specific contraindication to treatment with Nasobek. Patients with glaucoma, a recent wound, surgery, or ulceration in the nasal area should consult a physician before using Nasobek. Influence on the ability to drive a car and other mechanisms Nasobek does not affect the ability to drive a car or other mechanisms.
Interaction with other drugs
Not known.
Contraindications
Hypersensitivity to beclomethasone dipropionate or to the excipients of the drug, bleeding diathesis, frequent nosebleeds, viral or fungal infections, pulmonary tuberculosis, children under 6 years of age, first trimester of pregnancy.
Compound
25 g of the drug contains: beclomethasone dipropionate 0.01250 g; excipients: benzalkonium chloride, phenylethyl alcohol, polysorbate 80, glucose, dispersed cellulose (a mixture of microcrystalline cellulose and sodium carboxymethylcellulose), hydrochloric acid 3594, purified water. One dose contains 50 mcg of beclomethasone dipropionate.
Overdose
Symptoms: When large amounts of beclomethasone dipropionate are taken over a short period of time, the only harmful effect is suppression of the function of the hypothalamic-pituitary-adrenal axis. Treatment: no emergency measures are taken, and treatment with Nasobek should continue at the recommended dose. The function of the hypothalamic-pituitary-adrenal system returns to normal within one to two days.
Side effect
Systemic effects of nasal corticosteroids are possible only when used in high doses for a long time. In rare cases, nasal septal perforation may develop after the use of intranasal corticosteroids. Dryness and irritation of the nasal mucosa and the formation of blood-stained crusts in the nose may occur when using intranasal sprays, but these conditions do not progress and rarely cause concern. Changes in olfactory and gustatory perception, epistachys, have rarely been reported. Rare cases of increased intraocular pressure, glaucoma, and cataracts have been reported with intranasal use of beclomethasone dipropionate. Widespread use of beclomethasone dipropionate over decades has shown no serious local damage to the nasal mucosa. Very rarely, cases of hypersensitivity reactions have been reported, including urticaria, itching and erythema, swelling of the eyes, face, lips and pharynx, anaphylactoid/anaphylactic reactions, dyspnea and/or bronchospasm. Cases of growth retardation have been reported in children receiving intranasal corticosteroids.
Storage conditions
Store at a temperature not exceeding 25 0 C. Do not freeze. Keep out of the reach of children. Shelf life: 4 years in unopened original packaging; 6 months after first opening the package. Do not use after expiration date.
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