What Is Budesonide?

Budesonide (budesonide) is a light beige solid chemical, also known as Premicote Depot; Primic Reisch; Anglo-Fermi; La Enochot; Dingdeyanson; Renault Corte; Primic Du Bao; Budson; Buddish shrink. Melting point: 194-199ºC, molecular formula: C25H34O6, molecular weight: 430.53400. It is a glucocorticoid with a highly effective local anti-inflammatory effect. It can enhance the stability of endothelial cells, smooth muscle cells and lysosomal membranes, inhibit the immune response and reduce antibody synthesis, thereby reducing the release of allergic active media such as histamine and Reduced activity, and can reduce the enzymatic process that is triggered when antigen-antibody binding, inhibit the synthesis and release of bronchoconstrictive substances and reduce the contractile response of smooth muscle. It is clinically used in patients with glucocorticoid dependent or independent bronchial asthma and asthmatic chronic bronchitis. ^[1-2]

Drug Name: Budesonide
Alias: Premcourt Depot; Pumik Lingshu; Anglo American; Rahenault;
Foreign name: budesonide
Main indications: Bronchial asthma and asthmatic chronic bronchitis

Dosage: The details are as follows
Adverse reactions: Throat irritation, hoarseness and other local irritation symptoms
Main medication contraindications: Moderate and severe bronchiectasis
Dosage form: Powder, aerosol, dry powder inhaler
Drug type: chemical
CAS: 51333-22-3

Budesonide Basic Information

Chinese name

Chinese alias: Budesonide-22R

English name: 16a (R), 17- (Butylidenebis (oxy))-11b, 21-dihydroxypregna-1,4-diene-3,20-dione

English alias: 5,8,11,14-Eicosatetraenoylethanolamide;

N-Arachidonoyl-2-hydroxyethylamide;

arachidonylethanolamide;

N-arachidonoyl ethanolamine;

N-arachidonoylethanolamide;

arachidonic acid ethanolamide;

Arachidonoyl-EA;

arachidonoylethanolamide;

CAS number: 51333-22-3 ^[1]

Molecular formula: C25H34O6

Molecular weight: 430.553400

Chemical Structure:

Exact mass: 430.23600

PSA: 93.06000

LogP: 2.71680 ^[1]

Physical properties of budesonide

Appearance and properties: light beige solid

Density: 1.27 g / cm3

Melting point: 194-199ºC

Boiling point: 599.7ºC at 760 mmHg

Flash point: 201.8ºC

Storage conditions: -20ºC Freezer ^[1]

Budesonide safety information

Customs code: 2914509090 ^[1]

Overview of basic information about budesonide drugs

Budesonide drug name

Chinese name: budesonide

English name: Budesonide

Alias: Pomicourt Depot; Pomik Lingshu; Anglo-Foam; Raenocourt; Panditectin pine; Renocourt; Pumiq; Dubao; Budson; Budeson pine; Pulmicort; Rhinocort ^[2]

Budesonide classification

Respiratory Drugs> Asthma Drugs> Anti-inflammatory Asthma Drugs

Budesonide dosage form

10mg, 20mg.

2. Aerosol: 50ugx 200 spray; 200ugx 100 spray.

3. Dry powder inhalant: 100ug x 200 inhalation; 200ugx 100 inhalation, 200 inhalation. ^[2]

Budesonide pharmacological action

1. Induces the synthesis of lipocortin to inhibit phospholipase A2 and reduce the production and release of lipid inflammatory mediators such as platelet activating factors, leukotrienes, and prostaglandins, which are produced by the hydrolysis of membrane phospholipids by this enzyme.

2. Induces the expression of angiotensin converting enzyme and neutral peptide endonuclease, accelerates the production of angiotensin , and degrades and inactivates bradykinin and tachykinin; inhibits oxidative nitrous oxide synthase Expression, reducing the production of oxidized nitrous oxide. Thereby constricting blood vessels, or alleviating the effects of various active substances other than vascular tension II in dilating blood vessels, causing inflammation, and inducing neurogenic inflammation. In addition, it can also induce the production of vasocortin.

3. Inhibit the expression of various cytokines, such as interleukin 1, 3, 4, 6, 8, and tumor necrosis factor, granulocyte colony-stimulating factor. Reduce the role of the above factors in airway inflammation, especially chronic inflammation.

4. Promote the expression of epinephrine 2 receptor and increase the sensitivity to endogenous and exogenous medicinal 2 receptor agonists.

5. Immunosuppressive effect: It has inhibitory effect on the entire immune process from the phagocytosis of antigen, the division and proliferation of lymphocytes, to the effector period. ^[2]

Budesonide pharmacokinetics

After budesonide is inhaled, it mainly inhibits the production of active substances such as inflammatory sensitizing mediators and cytokines through the combined effects of the above links in the airways and lung tissues, shrinks the dilated mucosal blood vessels, and improves the bronchial smooth muscle and inflammatory cells' 2 activation The sensitivity of the agent can produce good therapeutic effects on both exogenous and endogenous asthma. In addition to relieving clinical symptoms such as asthma and dyspnea, and improving pulmonary ventilation, the anti-inflammatory effect of this class of drugs is more prominent than other asthma drugs. According to a group of long-term use of budesonide, bronchoscopy before and after treatment and histological examination of tissue extraction revealed that budesonide can alleviate or reverse to some extent the airway mucosal edema and subepithelial basement membrane caused by collagen deposition in chronic asthma. Thickening and other airway inflammatory remodeling lesions. Budesonide's anti-inflammatory effect is about 500 times that of dexamethasone, so when the inhaled budesonide produces the above-mentioned local treatment effect, even if it is absorbed and swallowed by the airway (bioavailability is only 11%), As for the occurrence of significant systemic glucocorticoid adverse reactions. ^[2]

Budesonide indication

Chronic reversible airway obstructive diseases such as bronchial asthma. ^[2]

Budesonide contraindications

1. Moderate and severe bronchiectasis.

2. Patients with acute exacerbation of asthma or severe illness should not use budesonide alone to control acute symptoms, and pregnant women are contraindicated. ^[2]

Budesonide notes

1. Budesonide should be used with caution when the airway is infected with a fungus, virus or tuberculosis.

2. After inhaling budesonide, rinse the mouth and throat with clean water to prevent the growth of fungi.

3. Children should use as prescribed by a physician and under the guidance of an adult. ^[2]

Budesonide pregnant women

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. ^[3]
Lactation <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. ^[3]

Budesonide children's medication

Children under 6 years have limited experience with this product. ^[3]

Budesonide

Elderly patients use the same amount as adults. ^[3]

Budesonide adverse reactions

The dose is controlled within 800 g per day. It is generally believed that no systemic adverse reactions of glucocorticoids will occur, nor will it significantly affect the function of the hypothalamus-pituitary-adrenal cortex regulatory axis. Only occasional symptoms of local irritation such as throat discomfort, hoarseness, and candidiasis of the oral cavity and pharynx are seen. The latter is caused by the decrease of local resistance due to the pharmacological effects of budesonide. ^[2]

Budesonide dosage

1. Aerosol or dry powder (Dubao, Pulmic) inhaled 200 g twice a day, or 400 g, once a day; for severe or refractory asthma, the dose can be increased to 400 g to 800 g each time, 1 to 2 daily After inhalation, the condition was gradually reduced to the above-mentioned usual amount for maintenance.

2. Treatment of rhinitis: 50g sprayed into the nasal cavity twice a day. ^[2]

Interaction of budesonide with other drugs

Ketoconconazole can increase budesonide's plasma concentration, and its mechanism of action may be to inhibit the metabolism of budesonide mediated by cytochrome P4503A. ^[2]

Budesonide expert review

Pre-pubertal asthma in children with long-term inhalation of budesonide and another inhaled glucocorticoid agent beclomethasone propionate can be observed to grow more slowly than children of the same age group receiving non-glucocorticoid treatment in asthma, There is a decrease in collagen synthesis rate and serum osteocalcin levels. Therefore, the negative effects of budesonide and similar drugs on children's growth and collagen metabolism are attracting attention. ^[2]