Pharmacological properties of the drug Tafen nasal
Budesonide is a synthetic corticosteroid with pronounced anti-inflammatory and antiallergic effects. When used in therapeutic doses, it is almost not resorbed. Does not exhibit mineralocorticoid activity and is well tolerated with long-term treatment. The drug inhibits the release of mediators of the inflammatory response, increases the synthesis of anti-inflammatory proteins, reduces the number of mast cells and eosinophilic granulocytes. Budesonide reduces the release of toxic proteins from eosinophilic granulocytes, free radicals from macrophages and lymphokines from lymphocytes. It also reduces the binding of adhesion molecules to endothelial cells, and thus reduces the number of white blood cells at the site of allergic inflammation. Budesonide increases the number of beta-adrenergic receptors in smooth muscle. The drug inhibits the activity of phospholipase A2, which slows down the synthesis of prostaglandins, leukotrienes and PAF, which induce an inflammatory response. Budesonide also inhibits histamine synthesis, which leads to a decrease in histamine levels in mast cells. Tafen nasal reduces the severity of symptoms in allergic rhinitis, suppressing the late and early phases of the allergic reaction and reduces the severity of inflammation in the upper respiratory tract. Improvement in condition is noted 2–3 days after the start of treatment. Budesonide is a mixture of two epimers in a 1:1 ratio. The 22R epimer has 2–3 times more activity than the 22S epimer. After inhalation of 400 mcg of budesonide through the nose, the maximum concentration is reached after 0.7 hours and is 1 nmol/l in blood plasma. After inhalation through the nose, about 20% of the administered budesonide enters the systemic circulation. The systemic bioavailability of budesonide is low, since about 90% of the portion that is absorbed is inactivated during one-step metabolism in the liver. The 22R and 22S epimers are biotransformed into beta-hydroxybudesonide and alpha-hydroxyprednisolone, respectively. Metabolites exhibit less than 1% glucocorticoid activity; excreted by the kidneys (70%) and through the intestines. The half-life is 2–3 hours.
Tafen nasal 50mcg/dose 200doses 10ml dosed nasal spray
pharmachologic effect
Glucocorticosteroid for local use.
Composition and release form Tafen nasal 50 µg/dose 200 doses 10 ml dosed nasal spray
Spray - 1 dose:
- Active substance: Budesonide - 50.0 mcg;
- Excipients: Methyl parahydroxybenzoate - 50.0 mcg; Propyl parahydroxybenzoate - 10.00 mcg; Microcrystalline cellulose and carmellose sodium - 550.0 mcg; Polysorbate-80 - 50.0 mcg; Simethicone emulsion - 50.0 mcg; Propylene glycol - 5,000 mg; Sucrose - 15,000 mg; Disodium edetate - 5.0 mcg; Hydrochloric acid - 10.0 mg; Water - 35.725 mg.
10 ml in a dark glass bottle with a mechanical dispensing device with a nasal nozzle with a tip closed with a protective cap.
One bottle with instructions for medical use is placed in a cardboard box.
Description of the dosage form
White or almost white homogeneous suspension.
Directions for use and doses
Adults and children over 6 years of age: Initially, 2 doses of 50 mcg of budesonide in each nasal passage 2 times a day. The usual maintenance dose is 1 dose in each nasal passage 2 times a day or 2 doses in each nasal passage 1 time per day, in the morning. The maintenance dose should be the lowest effective dose to relieve rhinitis symptoms.
The maximum single dose is 200 mcg (100 mcg in each nasal passage), the maximum daily dose is 400 mcg for no more than 3 months.
For full therapeutic effect, regular and correct use is required.
If a dose is missed, it should be taken as soon as possible, but at least 1 hour before the next regular dose.
Pharmacodynamics
Budesonide is a synthetic glucocorticosteroid drug with a pronounced anti-inflammatory and antiallergic effect.
When used in therapeutic doses, it has virtually no resorptive effect. It does not have mineralocorticoid activity and is well tolerated during long-term treatment. The drug has an inhibitory effect on the release of mediators of the inflammatory reaction, increases the synthesis of anti-inflammatory proteins, reduces the number of mast cells and eosinophilic granulocytes, prevents the marginal standing of neutrophils, reduces inflammatory exudation and the production of cytokines. Budesonide reduces the release of toxic proteins from eosinophils, free radicals from macrophages and lymphokines from lymphocytes. It also reduces the binding of adhesion molecules to endothelial cells, thus reducing the flow of leukocytes to the site of allergic inflammation. Budesonide increases the number of alpha-adrenergic receptors on the surface of the membrane of vascular smooth muscle cells, thereby increasing sensitivity to decongestants.
The drug inhibits the activity of phospholipase A2, which leads to inhibition of the synthesis of prostaglandins, leukotrienes and platelet activating factor, which induce an inflammatory response. Budesonide also inhibits histamine synthesis, which leads to a decrease in histamine levels in mast cells. Improvement in condition is observed on the second or third day after the start of treatment.
Tafen® nasal reduces the severity of symptoms in allergic rhinitis, suppresses the late and early phases of the allergic reaction and reduces inflammation in the upper respiratory tract.
Pharmacokinetics
After topical application of 400 mcg of budesonide, the maximum concentration of Cmax in the blood plasma is reached after approximately 30 minutes and is 1 nmol/l.
Only about 20% of the administered dose of Tafen® nasal enters the systemic circulation. Due to good distribution in tissues and binding to blood plasma proteins, the volume of distribution is 301 liters. Binding to plasma proteins, mainly albumin, is 86 - 90%.
The systemic bioavailability of budesonide is low, since more than 90% of the absorbed drug is inactivated during the “first pass” through the liver. Glucocorticoid activity of metabolites does not exceed 1%. Metabolites are excreted mainly by the kidneys (70%) and through the intestines (10%). The half-life (T1/2) is 2 hours.
Indications for use Tafen nasal 50 µg/dose 200 doses 10 ml dosed nasal spray
Prevention and treatment of seasonal and year-round allergic rhinitis.
Prevention and treatment of vasomotor rhinitis.
Nasal polyps.
Contraindications
Hypersensitivity to budesonide or excipients of the drug.
Active form of pulmonary tuberculosis.
Lactation period.
Children's age up to 6 years.
With caution: fungal, bacterial and viral infections of the respiratory tract (necessarily under constant monitoring of the patient’s condition and specific therapy), recent surgical interventions in the nasal cavity, recent trauma to the nose, neurotropic viral infections (shingles, herpes), pregnancy, cirrhosis of the liver , glaucoma, hypothyroidism.
Application of Tafen nasal 50mcg/dose 200doses 10ml nasal spray dosed during pregnancy and breastfeeding
The use of Tafen® nasal during pregnancy is allowed only if the expected benefit to the mother outweighs the possible risk to the fetus. The drug can pass into breast milk, therefore, when treated with this drug, nursing mothers are advised to stop breastfeeding.
special instructions
It is recommended to avoid getting Tafen® nasal in the eyes!
When switching from treatment with systemic glucocorticosteroids to treatment with a nasal spray, due to the risk of developing adrenal insufficiency, caution is required during the period of restoration of the function of the hypothalamic-pituitary-adrenal axis (HPA). The drug should be discontinued by gradually reducing the dose until the HPA axis function is normalized. During the dose reduction phase, some patients may experience symptoms of systemic glucocorticosteroid withdrawal, such as muscle and/or joint pain, apathy and depression. If such symptoms are detected, a temporary increase in the dose of systemic glucocorticosteroids may be required, and subsequently further withdrawal at a slower pace. Since glucocorticosteroids slow down wound healing, caution should be exercised when prescribing Tafen® nasal to patients who have recently undergone trauma or surgery of the nose. For a full therapeutic effect for allergic rhinitis, the drug must be used regularly. During long-term therapy with Tafen® nasal, it is necessary to assess the condition of the nasal mucosa at least once a year. Cases of growth retardation have been reported in children receiving nasal glucocorticosteroids in therapeutic doses. With long-term use of glucocorticosteroids for nasal administration in children, dynamic growth monitoring is recommended. If growth slows, the pediatrician should reconsider the method of use of the drug in order to reduce the dose and switch to the minimum therapeutic dose at which control of the symptoms of the disease is possible.
The use of glucocorticosteroids for nasal administration in doses exceeding the recommended ones can lead to significant suppression of adrenal function. When identifying the use of glucocorticosteroids for nasal administration in doses exceeding the recommended ones, the need for additional use of systemic glucocorticosteroids during the period of decreased adrenal function or elective surgery should be taken into account.
Special precautions when disposing of unused medicinal product
There is no need for special precautions when disposing of unused Tafen® nasal.
Impact on the ability to drive vehicles and operate machinery
Due to the possibility of developing psychoneurological symptoms during therapy with Tafen® nasal, caution should be exercised when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Overdose
Accidental overdose of the drug Tafen® nasal in the dosage form of a nasal spray dosage does not cause any obvious symptoms.
Acute overdose is unlikely.
With prolonged use of high doses, as well as with simultaneous use of other glucocorticosteroids, symptoms of hypercortisolism may appear. In this case, the drug should be stopped, gradually reducing its dose.
Side effects Tafen nasal 50mcg/dose 200doses 10ml dosed nasal spray
The drug Tafen® nasal in dosage form is a dosed nasal spray, which very rarely has side effects. According to the World Health Organization (WHO), adverse reactions are classified according to their frequency of development as follows: very often (> 1/10), often (> 1/100, 1/1000, 1/10000,
From the respiratory system - very often: irritation of the nasal mucosa. At the beginning of therapy, the following phenomena may be observed for a short period of time: rhinorrhea and crusting on the mucous membrane, nosebleeds; often: sneezing after the first use of the drug, dyspnea, hoarseness, wheezing, pain in the nasal cavity, bloody discharge from the nose.
From the immune system - very rarely: anaphylactic reactions.
From the gastrointestinal tract (GIT) - often: dry mucous membrane of the throat.
From the skin and subcutaneous tissue system - rarely: immediate and delayed hypersensitivity reactions (including urticaria, rash, dermatitis, itching, angioedema).
General disorders and changes at the site of drug administration - infrequently: candidiasis of the nasal cavity and upper respiratory tract, with long-term use - atrophy of the nasal mucosa, especially with long-term therapy; very rarely: ulceration of the nasal mucosa, perforation of the nasal septum.
Some ENT symptoms may be masked due to the use of glucocorticosteroids. With long-term administration of high doses of budesonide, the risk of systemic effects cannot be excluded, including Cushing's syndrome, Cushingoid signs, adrenal suppression, growth retardation in children and adolescents, decreased bone mineral density, symptoms of hypo- or hypercortipism, cataracts and glaucoma.
Also possible: nausea, changes in taste, difficulty swallowing, anosmia, palpitations, nasal congestion, dizziness, headache, sore throat, conjunctival hyperemia, myalgia, drowsiness, cough.
Less commonly, psychological and behavioral abnormalities may occur, including psychomotor hyperactivity, sleep disturbances, anxiety, depression or aggression (especially in children).
Drug interactions
The simultaneous use of Tafen® nasal with inducers of microsomal oxidation (phenobarbital, phenytoin, rifampicin) may reduce the effectiveness of the former.
Methandienone, estrogens, and ketoconazole enhance the effect of budesonide. Itracoiazole may cause an increase in plasma concentrations of budesonide.
Use of the drug Tafen nasal
adults and children aged 6 years and older. The initial dose is 400 mcg of budesonide per day: 2 doses (100 mcg of budesonide) in each nostril 2 times a day. The usual maintenance dose is 200 mcg of budesonide per day: 1 dose (50 mcg of budesonide) in each nostril 2 times a day or 2 doses in each nostril once a day in the morning. Maintenance therapy should be at the lowest dose level that eliminates the symptoms of rhinitis. If a dose is missed, it should be taken as soon as possible, but not less than 1 hour before the next dose. When stopping the use of the drug, the dose is reduced gradually. When used correctly, Tafen nasal reduces the frequency of adverse reactions and improves the therapeutic effect:
- Clean the nasal passages (if possible with sodium chloride solution).
- Remove the cap from the bottle.
- Shake the bottle.
- When using the bottle for the first time, release some spray into the air. Press the nasal adapter down several times until a light mist appears. The same procedure must be repeated if the drug has not been used for several days. If the adapter is blocked, you need to gently press it and clean it.
- Tilt your head forward (so that you can see your toes). Insert the nozzle from the right side into the left nostril and point it towards the outer wall.
- Press the adapter down to release one dose of spray and inhale it.
- Insert the nozzle from the left side into the right nostril and point it towards the outer wall; Squeeze out one dose of the spray and inhale it.
- After use, wipe the adapter with a clean cloth and replace the cap. Store the bottle in an upright position with the cap facing up.
Tafen nasal spray naz 50 mcg/dose cor 200 doses x1
Tafen nasal spray naz 50 mcg/dose 200 doses x1, ATX code: R01AD05 (Budesonide) Active substance: budesonide Rec.INN registered by WHO
Dosage form
TAFEN® NASAL
dosed nasal spray 50 mcg/1 dose: vial. 200 doses per dosage. devicereg. No.: P N014740/01 dated 12/19/08 - Indefinitely
Release form, composition and packaging
Nasal spray dosed in the form of a homogeneous suspension of white or almost white color.
1 dose
budesonide 50 mcg
Excipients: methyl parahydroxybenzoate - 50 mcg, propyl parahydroxybenzoate - 10 mcg, microcrystalline cellulose and carmellose sodium - 550 mcg, polysorbate 80 - 50 mcg, simethicone emulsion - 50 mcg, propylene glycol - 5 mg, sucrose - 15 mg, disodium edetate - 5 mcg, hydrochloric acid - 10 mg, water - 35.725 mg.
Clinical-pharmacological group: GCS for local use Pharmaco-therapeutic group: Glucocorticosteroid for local use
pharmachologic effect
GCS for intranasal use. It has a pronounced anti-inflammatory and antiallergic effect. When used in therapeutic doses, it has virtually no resorptive effect. It does not have mineralocorticoid activity and is well tolerated during long-term treatment. The drug has an inhibitory effect on the release of mediators of the inflammatory response, increases the synthesis of anti-inflammatory proteins, reduces the number of mast cells and eosinophilic granulocytes. Budesonide reduces the release of toxic proteins from eosinophils, free radicals from macrophages and lymphokines from lymphocytes. It also reduces the binding of adhesion molecules to endothelial cells, thus reducing the flow of leukocytes to the site of allergic inflammation. Budesonide increases the number of β-adrenergic receptors in smooth muscle. The drug inhibits the activity of phospholipase 2A, which leads to inhibition of the synthesis of prostaglandins, leukotrienes and PAF, which induce an inflammatory response. Budesonide also inhibits histamine synthesis, which leads to a decrease in histamine levels in mast cells.
Tafen® nasal reduces the severity of symptoms in allergic rhinitis, suppresses the late and early phases of the allergic reaction and reduces inflammation in the upper respiratory tract. Improvement in condition is observed 2-3 days after the start of treatment.
Pharmacokinetics
Suction
After inhalation of 400 mcg of budesonide, Cmax in plasma is achieved within 0.7 hours and is 1 nmol/l.
Only about 20% of the intranasally administered dose enters the systemic circulation.
Distribution
Due to good distribution in tissues and binding to plasma proteins, Vd is 301 l.
Metabolism
Systemic bioavailability of budesonide is low because more than 90% of the absorbed drug is inactivated in the process of one-step metabolism in the liver. Glucocorticoid activity of metabolites does not exceed 1%.
Removal
Metabolites are excreted mainly in urine (70%) and feces. T1/2 is 2-3 hours.
Indications
– prevention and treatment of seasonal and year-round allergic rhinitis,
- non-allergic rhinitis,
- nasal polyps.
ICD-10 codes
Dosage regimen
At the beginning of therapy, adults and children over 6 years of age are prescribed 2 doses (50 mcg of budesonide) in each nostril 2 times a day. The usual maintenance dose is 1 dose in each nostril 2 times a day or 2 doses in each nostril 1 time a day, in the morning. The maintenance dose should be the lowest effective dose to relieve rhinitis symptoms.
The maximum single dose is 200 mcg (100 mcg in each nostril), the maximum daily dose is 400 mcg for no more than 3 months.
For full therapeutic effect, regular and correct use is required.
If a dose is missed, it should be taken as soon as possible, but not less than 1 hour before taking the next regular dose.
Side effect
From the respiratory system: irritation of the mucous membrane of the nose and throat, nosebleeds, cough, less often dry nasal mucosa, sneezing.
Dermatological reactions: dermatitis, urticaria, rash are noted.
Other: fatigue, dizziness.
In exceptional cases, when using nasal corticosteroids, perforation of the nasal septum, angioedema, loss of smell, tachycardia, and growth retardation were observed.
When using the drug, side effects develop very rarely and are transient.
Contraindications for use
- fungal, bacterial and viral infections of the respiratory tract,
- active form of pulmonary tuberculosis,
- hypersensitivity to budesonide or any other component of the drug.
Use during pregnancy and breastfeeding
The use of Tafen® nasal during pregnancy is allowed only if the expected benefit to the mother outweighs the possible risk to the fetus.
If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.
Use in children
The drug is prescribed to children over 6 years of age.
special instructions
When switching from treatment with systemic corticosteroids to treatment with a nasal spray, due to the risk of developing adrenal insufficiency, caution is required during the period of restoration of the function of the hypothalamic-pituitary-adrenal system.
Since corticosteroids slow down wound healing, caution should be exercised when prescribing Tafen® nasal to patients who have recently undergone trauma or nasal surgery.
For a full therapeutic effect for allergic rhinitis, you need to take the drug regularly.
It is recommended to avoid contact with eyes.
Impact on the ability to drive vehicles and operate machinery
Tafen® nasal does not affect the ability to drive a car or operate machinery.
Overdose
Accidental overdose of Tafen® nasal does not cause any obvious symptoms. Acute overdose is unlikely.
With prolonged use of high doses, as well as with simultaneous use of other corticosteroids, symptoms of hypercortisolism may appear.
In this case, the drug should be stopped, gradually reducing its dose.
Drug interactions
The simultaneous use of Tafen® Nasal with inducers of microsomal oxidation (phenobarbital, phenytoin, rifampicin) may reduce the effectiveness of the former.
Methandrostenolone, estrogens, and ketoconazole enhance the effect of budesonide.
Storage conditions and periods
The drug should be stored out of the reach of children at a temperature not exceeding 25°C. Shelf life – 2 years.
Conditions for dispensing from pharmacies
The drug is available with a prescription.
Special instructions for the use of the drug Tafen nasal
Be careful when switching from the use of systemic corticosteroids to treatment with Tafen nasal due to the risk of developing adrenal insufficiency. Rapid reduction of the dose of corticosteroids in patients with asthma can provoke a serious deterioration of the disease. Discontinuation of the drug Tafen nasal should be gradual. GCS may mask signs of infection, and new infections may develop during their use. Patients with untreated fungal, bacterial or viral infections (transmitted by airborne droplets) require special attention. Sometimes, to prevent the appearance of pathological symptoms of the organ of vision caused by allergic rhinitis, concomitant treatment may be necessary. With prolonged use of the drug, it is recommended to examine the mucous membrane of the nasal cavity 1-2 times a year to determine the possible development of atrophic rhinitis or pharyngeal candidiasis. In patients with liver cirrhosis or hypothyroidism, the systemic effect of budesonide may be increased. Due to the inhibitory effect of GCS on wound healing, Tafen nasal should be used with caution in patients with recent surgery or trauma to the nasal cavity. Use during pregnancy and breastfeeding is only possible if absolutely necessary. In infants and nursing mothers who have used budesonide, it is necessary to exclude the presence of hypofunction of the adrenal glands. Impact on psychophysical abilities. The drug does not affect the ability to drive vehicles and other machinery.
