Tafen^® Nasal (Spray) Instructions for Use

Marketing Authorization Holder

Sandoz, d.d. (Slovenia)

Manufactured By

Lek d.d. (Slovenia)

ATC Code

R01AD05 (Budesonide)

Active Substance

Budesonide (Rec.INN registered by WHO)

Dosage Form

Tafen® Nasal

Dosage nasal spray 50 mcg/1 dose: 200 dose bottle with dosing device

Dosage Form, Packaging, and Composition

Dosage nasal spray in the form of a homogeneous suspension of white or almost white color.

Excipients : methylparahydroxybenzoate – 50 mcg, propylparahydroxybenzoate – 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.

200 doses (10 ml) – dark glass bottles (1) with a mechanical dosing device with a nasal applicator tip, closed with a protective cap – cardboard packs.

Clinical-Pharmacological Group

Topical corticosteroids

Pharmacotherapeutic Group

Topical glucocorticosteroid

Pharmacological Action

Glucocorticosteroid for intranasal use. It has a pronounced anti-inflammatory and anti-allergic effect. When used in therapeutic doses, it has practically no resorptive effect. It does not possess mineralocorticoid activity and is well tolerated during long-term treatment. It has an inhibitory effect on the release of inflammatory reaction mediators, increases the synthesis of anti-inflammatory proteins, and 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 influx of leukocytes to the site of allergic inflammation. Budesonide increases the number of β-adrenergic receptors in smooth muscle. It inhibits the activity of phospholipase 2A, which leads to inhibition of the synthesis of prostaglandins, leukotrienes, and PAF, which induce the inflammatory reaction.

Budesonide also inhibits the synthesis of histamine, leading to a decrease in its level in mast cells.

When used intranasally, Budesonide 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 is noted on days 2-3 after the start of treatment.

Pharmacokinetics

After inhalation of 400 mcg of budesonide, C_max in plasma is reached within 0.7 hours and is 1 nmol/L. Only about 20% of the intranasally administered dose enters the systemic circulation. Due to good tissue distribution and binding to plasma proteins, V_d is 301 L.

The systemic bioavailability of budesonide is low because more than 90% of the absorbed drug is inactivated during first-pass metabolism in the liver. The glucocorticoid activity of metabolites does not exceed 1%. Metabolites are excreted mainly in the urine (70%) and in the feces. T_1/2 is 2-3 hours.

Indications

Prophylaxis and treatment of seasonal and perennial allergic rhinitis; non-allergic rhinitis; nasal polyps.

ICD codes

Dosage Regimen

Adults and children over 6 years of age are prescribed 2 doses (50 mcg of budesonide each) in each nostril 2 times/day at the beginning of therapy. The usual maintenance dose is 1 dose in each nostril 2 times/day or 2 doses in each nostril 1 time/day, in the morning. The maintenance dose should be the lowest effective dose that relieves the symptoms of rhinitis.

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.

Regular and correct use is required for the full therapeutic effect.

Adverse Reactions

Respiratory system irritation of the nasal and throat mucosa, nosebleed, cough; less commonly, dryness of the nasal mucosa, sneezing are noted.

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 have been noted.

Contraindications

Hypersensitivity to budesonide; fungal, bacterial and viral respiratory tract infections; active form of pulmonary tuberculosis; children under 6 years of age; some dosage forms for intranasal use are contraindicated in children and adolescents under 18 years of age.

With caution

Fungal, viral or bacterial respiratory tract infections, pulmonary tuberculosis (active or inactive form), recent surgical interventions in the nasal cavity, recent nasal trauma, neurotropic viral infections (herpetic infections, including herpes zoster), liver cirrhosis, glaucoma, hypothyroidism, pregnancy, breastfeeding period.

Use in Pregnancy and Lactation

Use with caution during pregnancy and breastfeeding.

Use in Hepatic Impairment

Impaired liver function may lead to reduced elimination of glucocorticosteroids, which increases the likelihood of systemic exposure.

Pediatric Use

Used in children over 6 years of age.

Special Precautions

When switching from treatment with systemic glucocorticosteroids to treatment with intranasal dosage forms, caution is required during the recovery period of the hypothalamic-pituitary-adrenal system function due to the risk of adrenal insufficiency.

Since glucocorticosteroids slow down wound healing, caution should be exercised when using in patients who have recently undergone nasal trauma or surgery.

Impaired liver function may lead to reduced elimination of glucocorticosteroids, which increases the likelihood of systemic exposure.

In children and adolescents with long-term use in high doses, the risk of systemic side effects, including growth retardation, increases.

Drug Interactions

Concomitant use with inducers of microsomal oxidation (phenobarbital, phenytoin, rifampicin) may reduce the effectiveness of budesonide.

Methandrostenolone, estrogens, ketoconazole enhance the effect of budesonide.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.