What Are Corticosteroid Nasal Sprays?

The active ingredient of this product is the budesonide chemical name: 16, 17-22R, S-propylmethylene dioxo-progestin-1,4-diene-11, 21-dihydroxy-3,20-dione Structural formula:

Budesonide nasal spray, the indication is to treat seasonal and perennial allergic rhinitis, perennial non-allergic rhinitis; prevent the regeneration of nasal polyps after nasal polypectomy, and treat nasal polyps symptomatically.

Drug Name

Budesonide nasal spray

Drug type

OTC Class A double span, external medicine, medicine for medical injury

Special medicine

Doping

Use classification

ENT medicine

Budesonide nasal spray ingredients

The active ingredient of this product is the budesonide chemical name: 16, 17-22R, S-propylmethylene dioxo-progestin-1,4-diene-11, 21-dihydroxy-3,20-dione Structural formula:

Molecular formula: C ₂₅ H ₃₄ O ₆
Molecular weight: 430.5

Budesonide nasal spray properties

This product is a white to off-white viscous suspension.

Budesonide nasal spray indications

Treatment of seasonal and perennial allergic rhinitis, perennial non-allergic rhinitis; prevention of nasal polyp regeneration after nasal polyp removal, symptomatic treatment of nasal polyps.

Budesonide nasal spray specifications

64g / spray; 120 sprays per bottle, the concentration of the drug solution is 1.28mg / ml.

Budesonide nasal spray usage dosage

The dose should be individualized.

rhinitis

Adults, children 6 years and older:

The recommended starting dose is 256 g per day. This dose can be injected once in the morning or twice in the morning and evening.

That is: 128 g (2 x 64 g) into each nostril in the morning; or 64 g into each nostril twice in the morning and evening.

The daily dosage exceeded 256 g, and no effect was seen.

After achieving the desired clinical effect, reduce the dose to the minimum dose required to control symptoms. Clinical trials have shown that some patients injecting 32 g per nostril every morning as a maintenance dose is sufficient.

Some patients can alleviate symptoms 5-7 hours after starting treatment, and the maximum effect usually requires continuous treatment for several days (a few patients may take 2 weeks to achieve the maximum effect). Therefore, the treatment of seasonal rhinitis, if possible, is best started before exposure to allergens.

With severe nasal congestion, vasoconstrictor drugs may be required.

In order to control eye symptoms caused by allergies, adjuvant treatment may sometimes be necessary.

Treat or prevent nasal polyps

The recommended dose is 256 g per day. This dose can be injected once in the morning or twice in the morning and evening. After achieving the desired clinical effect, reduce the dose to the minimum dose required to control symptoms as a maintenance dose.

For adults from the age of 18, allergic rhinitis is treated at a dose of 32 g / spray without a prescription and can be used for up to 3 months.

Side effects of budesonide nasal spray

Adverse reactions to local irritation occur in about 5% of patients.

The following table lists various adverse reactions according to classification and frequency, which are divided into common (1 / 100, <1/10), uncommon (1 / 1000, <1/100), and rare (1 / 10000, <1/1000) and extremely rare (<1/10000).

Respiratory, thorax, and mediastinal diseases are common: local irritation, nosebleeds, and mild hemorrhagic discharge from the nasal cavity.
Very rare: nasal septum perforation, nasal ulcer.

Immune system diseases are uncommon: angioedema, urticaria, dermatitis, rash, and itching.
Very rare: rapid-onset allergic reactions.

Rapid or delayed allergic reactions including urticaria, rash, dermatitis, angioedema, and pruritus have been reported. Very few patients develop mucosal ulcers and perforation of the nasal septum after steroid administration in the nasal cavity. The cause of these adverse reactions (steroids, these diseases, or other factors) is unknown.

Budesonide nasal spray contraindications

People with allergies to budesonide or any of the ingredients in the prescription.

Budesonide nasal spray precautions

With long-term use of high doses, systemic effects of glucocorticoids may occur such as: cortisolism, adrenal depression and / or growth retardation in children. The long-term effects of nasal steroids on children have not been established. The use of corticosteroids can cause growth retardation. For children and adolescents who have been receiving corticosteroids for a long time, it is recommended to monitor their growth regularly, regardless of the dosage form of the drug. If growth retardation is suspected, the investigation should be investigated. The benefits of using glucocorticoids should be weighed against the risks of possible growth inhibition.

Care should be taken in treating patients with nasal fungal infections and herpes.

Patients who have switched from systemic glucocorticoids to this product and suspected of hypothalamic-pituitary-adrenal axis disorders should be treated with caution. In these patients, systemic steroids should be carefully reduced, and testing for hypothalamic-pituitary-adrenal function should be considered. When accompanied by stress such as surgery, trauma, etc., systemic steroids can also be added.

Severe liver damage affects the pharmacokinetics of oral budesonide, leading to reduced clearance and increased systemic utilization. This indicates that possible systemic effects need to be considered.

Be particularly vigilant in patients with tuberculosis.

Budesonide nasal spray should not contact eyes. If contact with eyes, rinse immediately with water.

Avoid combination with ketoconazole or other powerful CYP 3A4 inhibitors. If this cannot be avoided, dosing intervals should be as long as possible.

Impact on the ability to drive and operate machines

Budesonide does not affect the ability to drive and use machines.

Use with caution by athletes.

Budesonide nasal spray for pregnant and lactating women

Pregnant women <br /> Clinical experience from pregnant women is limited. As with other glucocorticoids, budesonide causes various types of malformations (palate, bone deformities) in animal tests. However, the relevance of data from animal experiments to humans has not yet emerged. Until more experience is gained, pregnant women should not use this product unless special consideration is given.

Breastfeeding <br /> Budesonide can be secreted into milk. However, a therapeutic dose of budesonide nasal spray is not expected to affect infants. To study the transfer of plasma to milk and breast milk exposure of budesonide during the maintenance treatment of female asthma patients with Pulmicort inhalant, plasma and milk samples were collected within 8 hours of budesonide inhalation. Five of the eight babies were sampled. The results show that the PK parameters of the drug in milk and plasma are very close, and the concentration of budesonide in milk is always lower than its concentration in maternal plasma.

Budesonide nasal spray for children

Children under 6 years have limited experience with this product.

Budesonide nasal spray for the elderly

Elderly patients use the same amount as adults.

Budesonide nasal spray drug interactions

Oral ketoconazole 200 mg once daily increased the blood concentration of budesonide (3 mg single dose) at the same time by 6 times.

Ketoconazole was administered 12 hours after budesonide, and the blood concentration of budesonide increased on average by a factor of three. No such interaction occurred with nasal budesonide, but a significant increase in its plasma concentration can be expected. Due to lack of information on the recommended doses allowed when nasal budesonide is combined with ketoconazole, the combination of the two drugs should be avoided. If the combination cannot be avoided, the interval between the two drugs should be as long as possible. Consideration should also be given to reducing the amount of budesonide. Other potent CYP 3A4 inhibitors may also cause a significant increase in blood concentration of budesonide.

Budesonide nasal spray overdose

Acute overdose of this product will not cause clinical problems even in large doses. If used in large doses for a long time, systemic effects of glucocorticoids such as hypercortisolism and adrenal suppression can occur.

Budesonide nasal spray pharmacology and toxicology

1. Pharmacology:

Budesonide is a glucocorticoid with a highly effective local anti-inflammatory effect.

The exact mechanism of glucocorticoids in the treatment of rhinitis is not fully understood. The anti-inflammatory effects of glucocorticoids, such as inhibiting the release of inflammatory mediators and suppressing cytokine-mediated immune responses, may play an important role. In terms of affinity for glucocorticoid receptors, budesonide is about 15 times more active than prednisolone.

Prophylactic use of budesonide has protective effects on eosinophil migration and allergic reactions caused by nasal stimulation.

With the recommended dose of this product, the patient's basal plasma cortisol level and response to ACTH stimulation did not change clinically. However, in the observation of short-term use of this product in healthy volunteers, it was found that the decrease in plasma and urinary cortisol levels was related to the dose.

No dose-effect relationship was found in clinical trials between children with seasonal and perennial allergic rhinitis and adults with perennial allergic rhinitis.

There is no literature on the use of this product in the 32 ug / spray and 64 ug / spray specifications to treat vasomotor rhinitis (non-allergic rhinitis).

2. Toxicology

Acute, subacute, and long-term toxicity studies have found that systemic effects of budesonide, such as weight loss, atrophy of lymphoid tissue and adrenal cortex, are weaker than or comparable to other glucocorticoids.

After six different experimental test system evaluations, budesonide has no mutagenic and cleavage effects.

Consistent cancer research found that the incidence of cerebral gliomas in male SD rats increased after taking budesonide, but this result has not been confirmed by repeated experiments. Repeated research experiments found that there was no difference in the incidence of cerebral gliomas between the treatment groups of any active drug (Budesonide, Prednisolone, Triamide) and the control group.

The liver changes (primary hepatocellular tumors) found in male rats in the initial carcinogenicity studies were confirmed by repeated research experiments with budesonide and other control glucocorticoids. This effect may be related to the effect of the receptor, and thus reflects the effect of such drugs.

Existing clinical experience has shown that there is no evidence that budesonide or other glucocorticoids can cause brain gliomas and primary hepatocellular tumors in the human body.

Pharmacokinetics of budesonide nasal spray

absorb

Relative to the indicated dose, the systemic availability of budesonide in this product is 33%.

At clinical doses, pharmacokinetics are proportional to dose. In adults, after spraying 256 ug of budesonide with this product, the peak plasma concentration is 0.64 nmol / L, which peaks in 0.7 hours. Its adult AUC (area under the curve) is 2.7 nmol · h / L. It is 5.5 nmol · h / L, which indicates that children have higher systemic glucocorticoid exposure.

Distribution and metabolism

Budesonide distribution volume is about 3 L / kg, and the plasma protein binding rate is 85-90%. Budesonide is highly metabolized by the liver for the first pass (about 90%), and the glucocorticoid activity of the metabolites is low. The glucocorticoid activity of the main metabolites 6-hydroxybudesonide and 16-hydroxyprednisolone is less than 1% of budesonide. In the nose, budesonide has no local metabolism.

eliminate

Budesonide is eliminated primarily through a metabolic pathway catalyzed by the CYP 3A4 enzyme. Metabolites are mainly excreted by the kidneys in their original or combined form. No prototype budesonide was detected in urine. Budesonide has a high systemic clearance (0.9-1.4 L / min), and the average plasma half-life of intravenous administration is about 2-3 hours.

Budesonide nasal spray storage

Do not exceed 30 ° C, do not freeze.

Budesonide nasal spray packaging

120 sprays / piece / box; the inner packaging container is a brown glass bottle with a nasal adapter.

Budesonide nasal spray expiration date

24 months

Budesonide nasal spray implementation standards

Import drug registration standard JX20030334