Zodacort (Spray) Instructions for Use

Marketing Authorization Holder

Opella Healthcare, LLC (Russia)

Manufactured By

Recipharm HC, Limited (United Kingdom)

ATC Code

R01AD11 (Triamcinolone)

Active Substance

Triamcinolone acetonide (BAN)

Dosage Form

Zodacort

Nasal spray, metered 55 mcg/1 dose: 16.5 g bottle (120 doses)

Dosage Form, Packaging, and Composition

Metered nasal spray as a white or almost white suspension.

Excipients: disodium edetate dihydrate, dextrose, microcrystalline cellulose/sodium carboxymethylcellulose, polysorbate 80, benzalkonium chloride 50%, hydrochloric acid*, sodium hydroxide*, purified water.

* 10% hydrochloric acid and 0.1M sodium hydroxide are used as technological additives to adjust the pH of the final solution.

16.5 g (not less than 120 doses) – HDPE bottles (1) with a pump dosing device with a sprayer – cardboard packs.

Clinical-Pharmacological Group

Intranasal corticosteroids

Pharmacotherapeutic Group

Drugs for the treatment of nasal diseases; decongestants and other preparations for topical use; corticosteroids

Pharmacological Action

Corticosteroid. Suppresses the functions of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of inflammation. Impairs the ability of macrophages to phagocytose and to form interleukin-1. Promotes the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of inflammation. Reduces capillary permeability caused by the release of histamine. Suppresses fibroblast activity and collagen formation.

Inhibits the activity of phospholipase A₂, which leads to the suppression of prostaglandin and leukotriene synthesis. Suppresses the release of COX (mainly COX-2), which also contributes to the reduction of prostaglandin production.

Reduces the number of circulating lymphocytes (T- and B-cells), monocytes, eosinophils, and basophils due to their movement from the vascular bed into the lymphoid tissue; suppresses antibody formation.

Suppresses the release of ACTH and β-lipotropin by the pituitary gland but does not reduce the level of circulating β-endorphin. Inhibits the secretion of TSH and FSH.

When applied directly to blood vessels, it has a vasoconstrictor effect.

It has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins, and fats. Stimulates gluconeogenesis, promotes the uptake of amino acids by the liver and kidneys, and increases the activity of gluconeogenesis enzymes. In the liver, it enhances glycogen storage by stimulating the activity of glycogen synthase and the synthesis of glucose from protein metabolism products. An increase in blood glucose levels activates insulin secretion.

Suppresses glucose uptake by fat cells, which leads to the activation of lipolysis. However, due to increased insulin secretion, lipogenesis is stimulated, which contributes to fat accumulation.

It has a catabolic effect in lymphoid and connective tissue, muscles, adipose tissue, skin, and bone tissue.

Osteoporosis and Cushing’s syndrome are the main factors limiting long-term corticosteroid therapy. As a result of the catabolic effect, growth suppression in children is possible.

In high doses, it can increase the excitability of brain tissue and contributes to lowering the seizure threshold. Stimulates excessive production of hydrochloric acid and pepsin in the stomach, which contributes to the development of peptic ulcers.

When used systemically, the therapeutic activity is due to anti-inflammatory, anti-allergic, immunosuppressive, and anti-proliferative effects.

When used externally and locally, the therapeutic activity of triamcinolone acetonide is due to anti-inflammatory, anti-allergic, and anti-exudative (due to the vasoconstrictor effect) effects.

In terms of anti-inflammatory activity, Triamcinolone acetonide is 6 times more potent than hydrocortisone. Triamcinolone acetonide has practically no mineralocorticoid activity.

Pharmacokinetics

When used systemically, it is metabolized mainly in the liver and partially in the kidneys. The main metabolic pathway is 6-β-hydroxylation. T_1/2 – 3.5 hours. Excreted by the kidneys.

Indications

For systemic use: bronchial asthma, chronic bronchitis with broncho-obstructive syndrome, pemphigoid, psoriasis, dermatitis.

Intra-articular administration: chronic inflammatory joint diseases, exudative arthritis, gout, joint hydrops, shoulder joint blockade, chronic inflammation of the inner layer of the joint capsule.

For external use: eczema, psoriasis, neurodermatitis, various types of dermatitis and other inflammatory and allergic skin diseases of non-microbial etiology (as part of complex therapy).

ICD codes

Dosage Regimen

For adults and children 12 years and older, the initial recommended dose is two sprays (110 mcg total) into each nostril once daily.

After symptoms are controlled, reduce the dose to one spray (55 mcg) into each nostril once daily for maintenance therapy.

For children 6 to 11 years old, the recommended dose is one spray (55 mcg) into each nostril once daily.

Do not exceed the maximum daily dose of two sprays per nostril (220 mcg total).

Prime the pump before first use or if not used for several days by pressing down several times until a fine spray appears.

Shake the bottle gently before each use.

Blow your nose gently to clear nostrils before administration.

Tilt your head slightly forward and insert the nozzle into one nostril, pointing it away from the nasal septum.

Close the other nostril with your finger, then press down firmly on the pump while breathing in gently through your nose.

Repeat the procedure for the other nostril.

Avoid spraying directly onto the nasal septum.

Wipe the spray tip with a clean tissue and replace the dust cap after each use.

Therapeutic effect may be seen within 24 hours, but maximum benefit may take several days to achieve.

Use regularly as directed for optimal efficacy; it is not for immediate relief of acute symptoms.

If no improvement is seen after three weeks of continuous use, discontinue treatment and consult a physician.

Adverse Reactions

From the endocrine system: redistribution of adipose tissue, menstrual cycle disorders, increased blood glucose levels, suppression of adrenal function, “moon face”, striae, hirsutism, acne.

From the metabolism: edema, electrolyte imbalance, negative nitrogen balance, growth retardation in children.

From the digestive system: steroid gastric ulcer, erosive and ulcerative lesions of the gastrointestinal tract, acute pancreatitis.

From the central nervous system: convulsions, sleep disorders, mental disorders, headaches and dizziness, weakness.

From the musculoskeletal system: myopathy, osteoporosis.

From the cardiovascular system: arterial hypertension.

From the blood coagulation system: thromboembolism.

From the organ of vision: visual disturbances, posterior subcapsular cataract, increased intraocular pressure or exophthalmos, anaphylactic reactions.

Reactions due to immunosuppressive action: exacerbation of infectious diseases.

With intra-articular administration: joint pain, irritation at the injection site, depigmentation, sterile abscess, skin atrophy; with doses exceeding 40 mg, resorptive side effects are possible.

With external use: itching, skin irritation, late eczematous-type reactions, steroid acne, purpura are possible. With prolonged use of the ointment, the development of secondary infectious lesions and atrophic skin changes is possible.

Contraindications

Acute psychoses in history, active form of tuberculosis, myasthenia, neoplasms with metastases, diverticulitis, gastric and duodenal ulcer, arterial hypertension, Cushing’s syndrome, renal failure, history of thrombosis and embolism, osteoporosis, diabetes mellitus, latent foci of infection, amyloidosis, syphilis, fungal diseases, viral infections (including those caused by Herpes simplex and Varicella zoster), amoebic infections, poliomyelitis (except for the bulbar-encephalitic form), gonococcal or tuberculous arthritis, vaccination period, lymphadenitis after BCG vaccination, glaucoma, infected skin lesions.

Use in Pregnancy and Lactation

If it is necessary to use during pregnancy (especially in the first trimester) and during lactation, the expected benefit for the mother and the risk of side effects for the fetus or child should be assessed.

Use in Renal Impairment

Contraindicated in renal failure.

Pediatric Use

Parenteral use in children under 6 years of age is not recommended; in children aged 6-12 years – only for strict indications.

Long-term external use in children of any age should be avoided.

Special Precautions

Not intended for intravenous administration.

Use with caution and under strict medical supervision in cases of edematous syndrome, obesity, mental illness, and gastrointestinal diseases. During treatment, it is recommended to take vitamin D and consume foods rich in calcium.

When used externally, to prevent local infectious complications, it is recommended to use in combination with antimicrobial agents.

Parenteral use in children under 6 years of age is not recommended; in children aged 6-12 years – only for strict indications.

Long-term external use in children of any age should be avoided.

Drug Interactions

When used concomitantly with anabolic steroids, androgens, the risk of peripheral edema and acne increases.

When used concomitantly with antithyroid drugs and thyroid hormones, changes in thyroid function are possible.

When used concomitantly with histamine H₁-receptor blockers, the effect of triamcinolone is reduced; with hormonal contraceptives – the effect of triamcinolone is potentiated.

Hypocalcemia associated with the use of triamcinolone may lead to an increase in the duration of neuromuscular blockade caused by depolarizing muscle relaxants when used concomitantly.

When used concomitantly with immunosuppressants, the risk of bacterial and viral infections increases.

When used concomitantly with potassium-sparing diuretics, hypokalemia is possible.

When used concomitantly, a decrease in the effectiveness of indirect anticoagulants, heparin, streptokinase, urokinase is possible, and the risk of erosive-ulcerative lesions and gastrointestinal bleeding increases.

When used concomitantly with NSAIDs (including acetylsalicylic acid), the risk of erosive-ulcerative lesions and gastrointestinal bleeding increases.

When used concomitantly, the effect of oral hypoglycemic agents and insulin is weakened; with laxatives – hypokalemia is possible; with cardiac glycosides – the risk of cardiac rhythm disturbances and other toxic effects of glycosides increases.

When used concomitantly with tricyclic antidepressants, an increase in mental disorders associated with the use of triamcinolone is possible.

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

Over-the-Counter

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.