CORTIVENT
S-budesonide
CAS: 51333-22-3
Molecular Formula: C25H34O6
CORTIVENT - Names and Identifiers
| Name | S-budesonide |
| Synonyms | BIDIEN PULMICORT CORTIVENT BUDESONIDE Budesonide ENTOCORT CR S-budesonide 16-alpha)-et (11-beta,16-alpha)-16,17-(butylidenebis(oxy))-11,21-dihydroxypregna-1,4-dien 1,4-PREGNADIEN-(R, S)-11-BETA, 16-ALPHA, 17,21-TETROL-3,20-DIONE CYCLIC 16,17 ACETAL |
| CAS | 51333-22-3 |
| EINECS | 257-139-7 |
| InChI | InChI=1/C25H34O6/c1-4-5-21-30-20-11-17-16-7-6-14-10-15(27)8-9-23(14,2)22(16)18(28)12-24(17,3)25(20,31-21)19(29)13-26/h8-10,16-18,20-22,26,28H,4-7,11-13H2,1-3H3/t16-,17?,18-,20?,21?,22?,23-,24-,25?/m0/s1 |
| InChIKey | VOVIALXJUBGFJZ-KWVAZRHASA-N |
CORTIVENT - Physico-chemical Properties
| Molecular Formula | C25H34O6 |
| Molar Mass | 430.53 |
| Density | 1.1046 (rough estimate) |
| Melting Point | 221-232°C (dec.) |
| Boling Point | 464.79°C (rough estimate) |
| Specific Rotation(α) | D25 +98.9° (c = 0.28 in methylene chloride) |
| Flash Point | 201.8°C |
| Water Solubility | 21.53mg/L(temperature not stated) |
| Solubility | Practically insoluble in water, freely soluble in methylene chloride, sparingly soluble in ethanol (96 per cent). |
| Vapor Presure | 6.94E-17mmHg at 25°C |
| Appearance | powder |
| Color | White to Off-White |
| Merck | 14,1468 |
| pKa | 12.87±0.10(Predicted) |
| Storage Condition | Store at RT |
| Refractive Index | 1.4593 (estimate) |
| Use | [Drug Name] generic name: Budesonide Nasal Spray [indications] prevention and treatment of perennial and seasonal allergic rhinitis, can also be used for vasomotor rhinitis. [specification] 32? g/spray; 120 spray per bottle, the concentration of the solution is 0.64mg/ml [dosage] Nasal Spray: Left hand spray right nostril, right hand spray left nostril, avoid spraying directly to the nasal septum. Adult: Initially 2 sprays in each nostril, once in the morning and once in the evening. The maximum daily dosage should not exceed 8 sprays (256? g). After the symptoms were relieved, 1 spray was given to each nostril once a day. children over 6 years of age: same as adults. [adverse reactions] About 5% of patients will occur local stimulation of adverse reactions. common (> 100/1): airway: local irritation, mild bloody discharge, Epistaxis. Rare (1000/2): systemic: angioedema. Skin: urticaria, rash, dermatitis, pruritus. airway: perforation of nasal septum and mucosal ulcer. immediate or delayed allergic reactions, including urticaria, rash, dermatitis, angioedema, and pruritus, have been reported. Very few patients develop mucosal ulceration and septal perforation after intranasal administration of corticosteroids. The cause of these adverse effects, which may be caused by glucocorticoids, these diseases, or other factors, is unknown. [Precautions] 1. After 14 days of using this product, the symptoms have not improved, please refer to Counseling doctor. 2. Self-treatment should not exceed 3 months, If need more than 3 months, should be used under the guidance of a physician. 3. Long-term use of high doses, may occur systemic effects of glucocorticoids. Long-term treatment of children and adolescents, may cause growth retardation, should be used under the guidance of a physician. 4. With nasal fungal infection and herpes patients with caution. 5. Use of systemic corticosteroids to switch to the use of this product, should be used under the guidance of a physician. 6. Pulmonary tuberculosis patients with caution. 7. This product is only used in nasal cavity, and should not contact the eyes. If it contacts the eyes, please wash with water immediately. 8.6 children under the age of this product is not recommended. 9. Pregnant and lactating women should avoid using this product. 10. Use with caution in athletes. 11. In case of overdose or serious adverse reactions, medical attention should be taken immediately. 12. It is contraindicated for those who are allergic to this product, and it should be used with caution for those with allergic constitution. 13. The use of this product is prohibited when the character is changed. 14. Please keep this product out of contact with children. 15. Children must use under adult supervision. 16. If you are using other drugs, please refer to Counseling physician or pharmacist before using this product. [drug interaction] 1. Combination with ketoconazole should be avoided. 2. If concomitant use with other drugs may cause drug interaction, please contact Counseling physician or pharmacist for details. [Pharmacology and Toxicology] This product is a glucocorticoid drug, with strong local anti-inflammatory and anti-allergic effects. |
| In vitro study | In human bronchial epithelial cell lines BEAS-2B and primary human bronchial epithelial cells, Budesonide potently inhibits the production of eotaxin and RANTES proteins, although Budesonide inhibits the expression of the chemokine mRNA. Budesonide also inhibits the activity of reporter genes driven by RANTES-and chemokine promoters. Budesonide also selectively accelerates the decay of chemokines and MCP-4 mRNA. Budesonide time-and protein synthesis-dependently decreases VEGF secretion and VEGF mRNA expression in human bronchial epithelial cell lines BEAS-2B and primary human bronchial epithelial cells, and these effects were inhibited by the corticosteroid receptor antagonist mifeprisone (RU 486), suggesting that Budesonide reduces the secretion of VEGF through its glucocorticoid receptor-mediated effects. Budesonide dose-dependently almost completely inhibited pig dust-induced release of IL-6 and IL-8 in epithelial cells and LPS-induced release of IL-6 and TNF-α in alveolar macrophages. |
| In vivo study | In rats, Budesonide completely inhibited LPS at low concentration (2.5 mg/ml/kg) and high concentration (50 mg/mL/kg) induced TNF-α, interleukin (IL)-1beta,IL-6 and production of monocyte chemoattractant protein (MCP)-1. In A/J mice, Budesonide exerts chemoprevention, growth arrest by Mad2/3, and apoptosis by Bim/Blk and caspase-8/9. |
CORTIVENT - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R40 - Limited evidence of a carcinogenic effect R36/37/38 - Irritating to eyes, respiratory system and skin. R20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. |
| Safety Description | S22 - Do not breathe dust. S36 - Wear suitable protective clothing. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| WGK Germany | 3 |
| RTECS | TU3723000 |
| HS Code | 29372900 |
| Toxicity | LD50 oral in rat: > 3200mg/kg |
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