Tafen nasal, 1 piece, 10 ml, 50 mcg/dose, metered nasal spray
Intranasally.
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 that eliminates symptoms of rhinitis.
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 not less than 1 hour before taking the next regular dose.
Directions for use of the drug Tafen® nasal
When the drug is used correctly, its therapeutic effect is fully manifested, and undesirable effects are less pronounced.
1. Thoroughly clean the nasal passages of mucus, best with saline solution.
2. Remove the dustproof cap from the bottle.
3. Shake the bottle.
4. When using Tafen® nasal for the first time, release a small amount of the drug into the air by pressing the nozzle several times, while placing your index and middle fingers on the side bars of the bottle and supporting the bottom with your thumb (the bottle should be in a vertical position).
A small cloud of spray will be visible.
This procedure must be repeated if the patient has not used the drug for several days. If dried drug has accumulated in the nozzle hole, you must remove the nozzle and rinse it (as indicated in the “Cleaning” section).
5. Tilt your head forward and down. With your right hand, insert the nozzle into the left nasal passage towards its outer wall.
6. Press the nozzle, thereby releasing the measured dose of the drug, and at the same time inhale through the nose.
7. With your left hand, insert the nozzle into the right nasal passage towards its outer wall, press the nozzle and at the same time inhale through the nose.
8. After using the drug, wipe the nozzle with a clean napkin and close the bottle with the cap. The bottle should be stored in an upright position, tightly closed.
Cleaning
1. The nozzle and cap should be cleaned regularly.
2. Carefully remove the nozzle and cap, rinse with warm water and rinse with cold water, allow to air dry. Carefully place the nozzle in its original place and close the cap.
If dried product has accumulated in the hole, keep the nozzle in a vessel with warm water and then rinse as described above. Do not clean the nozzle hole with a needle or other sharp objects.
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).
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.
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.
