Pharmacological properties
Budesonide is a synthetic corticosteroid with a pronounced anti-inflammatory and antiallergic effect.
when used in therapeutic doses, it almost does not resorb. 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 nasal spray 50 µg/dose 200 doses bottle 1 pc. in Moscow
Pharmacological action: Glucocorticosteroid with pronounced glucocorticoid and weak mineralocorticoid activity. In standard in vitro
and animal models have shown that the affinity of budesonide for specific glucocorticoid receptors exceeds that of cortisol by 200 times, and the local anti-inflammatory effect of budesonide is 1000 times higher than that of cortisol. When studying the systemic activity of budesonide in animal experiments, it was shown that when administered subcutaneously, the effect of budesonide was 40 times stronger than that of cortisol, and when administered orally, it was 25 times stronger.
Inhibits the synthesis of leukotrienes and PGs, inhibits the production of cytokines, prevents the migration and activation of inflammatory cells.
Increases the number of active beta-adrenergic receptors, restores the body's response to beta-adrenergic bronchodilators after their long-term use.
Rapidly absorbed from the lungs and gastrointestinal tract. When administered intranasally, very little is absorbed from the nasal mucosa (only 20% enters the systemic circulation). After inhalation, about 25% of the dose enters the alveoli. The part that enters the gastrointestinal tract is almost completely (90%) destroyed (inactive metabolites are formed) during the “first pass” through the liver. Bioavailability is 10% of the amount that enters the stomach; 25–30% of budesonide that enters the alveoli is absorbed. Cmax in the blood is reached 15–45 minutes after inhalation and intranasal administration. Plasma protein binding is 88%. Has high systemic clearance (84 l/h). T1/2 from plasma - 2.8 hours. Excreted in urine, partially in bile in the form of metabolites.
After oral administration, Cmax and Tmax values are variable (Tmax in individual patients - from 30 to 600 minutes). Systemic availability after a single dose is higher in patients with Crohn's disease compared to healthy volunteers (21% and 9%, respectively), but approaches that of healthy volunteers after repeated doses. About 90% of absorbed budesonide is metabolized during the “first pass” through the liver with the participation of microsomal enzymes (mainly CYP3A4) to 2 main metabolites - 6-beta-hydroxy-budesonide and 16-alpha-hydroxyprednisolone (the glucocorticoid activity of the metabolites is less than 1/100 of the activity of budesonide , of the remaining amount, about 90% binds to albumin and is in an inactive state.
The effectiveness of budesonide (oral dosage form) has been shown for inflammatory bowel diseases, incl. with collagenous colitis.
The intranasal form is effective in the treatment of non-infectious inflammatory processes in the nasal cavity, to prevent the recurrence of polyps in the nasal cavity after their surgical removal and complete healing of the mucous membrane.
Carcinogenicity, mutagenicity, effect on fertility
The potential carcinogenicity of budesonide was assessed in long-term studies in rats and mice. No carcinogenic effect of budesonide was detected in mice when administered orally for 91 weeks at doses up to 200 mcg/kg/day (600 mcg/m2/day, approximately 0.1 MRDC based on body surface area).
A two-year study in Sprague-Dawley rats revealed a statistically significant increase in the incidence of gliomas in male rats receiving an oral dose of budesonide 50 mcg/kg/day (300 mcg/m2/day); similar changes were not observed in males at doses of 10 and 25 μg/kg/day (60 and 150 μg/m2/day) and in females at all doses tested. In 2 additional two-year studies in male Fischer and Sprague-Dawley rats at doses of 50 μg/kg/day (less than the MRV when converted to body surface area), there was no increase in the incidence of gliomas compared with other glucocorticoids (prednisolone and triamcinolone). However, with all 3 glucocorticoids studied, a statistically significant increase in the incidence of hepatocellular tumors in rats was observed.
No mutagenic or clastogenic properties of budesonide were detected in a number of standard tests.
With subcutaneous administration of budesonide to rats in doses up to 80 mcg/kg/day (less than the MRDC when calculated per body surface area), no adverse effects on fertility were recorded, but a decrease in weight gain in females was noted along with a decrease in the viability of pups in the prenatal period, at birth and during the lactation period. At doses of 5 mcg/kg/day (30 mcg/m2/day), similar effects were not observed.
Pregnancy
Like other corticosteroids, budesonide was teratogenic and embryotoxic in rabbits and rats. Experimental studies on animals (rats, rabbits) have shown that subcutaneous administration of budesonide leads to congenital malformations in the fetus (mainly skeletal defects).
Application
Adults and children aged 6 years and older. initial dose - 400 mcg budesonide per day: 2 doses (100 mcg 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:
1. Clean the nasal passages (if possible with sodium chloride solution).
2. Remove the cap from the bottle.
3. Shake the bottle.
4. 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.
5. 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.
6. Press the adapter down to deliver one dose of spray and inhale it.
7. 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.
8. After use, wipe the adapter with a clean cloth and put on the cap. Store the bottle in an upright position with the cap facing up.
Tafen nasal
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
Be careful when switching from the use of systemic corticosteroids to treatment with tafen nasal due to the risk of developing adrenal insufficiency. A rapid reduction in 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 adrenal hypofunction.
Impact on psychophysical abilities. The drug does not affect the ability to drive vehicles and other machinery.
Note!
Description of the drug Tafen Nasal spray nasal. susp. 50mcg/dose vial. 10 ml, 200 doses on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
