物质信息
ID:216
名称和标识
商标名
AeroventApo-IpraventAtrovent NasalAtroventKendral-IpratropiumAtrovent HFADisne-AsmolIpventRinovagosVagosAerodoseApoventAtronaseBitropRinoberenAtrovent AerosolIpraventNariletRhinotropRhinoventRinatec
别名
Ipratropium BromideN-IsopropylatropineipratropiumIpratropium bromideIpatropium Bromide
IUPAC标准名
(1R,5R)-3-[(3-hydroxy-2-phenylpropanoyl)oxy]-8-methyl-8-(propan-2-yl)-8-azabicyclo[3.2.1]octan-8-ium bromide
IUPAC传统名
atrovent bromide
数据登录号
CAS号
化合物性质
理化性质
溶解度
Freely soluble
描述信息
Drug Groups
approved
Description
A muscarinic antagonist structurally related to atropine but often considered safer and more effective for inhalation use. It is used for various bronchial disorders, in rhinitis, and as an antiarrhythmic. [PubChem]
Indication
For maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease, including chronic bronchitis and emphysema.
Pharmacology
Ipratropium bromide, a synthetic ammonium compound structurally similar to atropine, is used as a bronchodilator in the management of cholinergic-mediated bronchospasm associated with chronic obstructive pulmonary disease and in the treatment of rhinorrhea associated with the common cold or with allergic or nonallergic seasonal rhinitis.
Toxicity
LD50=1001mg/kg (orally in mice)
Affected Organisms
Humans and other mammals
Biotransformation
Partially metabolized to at least 8 metabolites formed primarily via hydrolysis and conjugation. The main metabolites are N-isopropylnortropium methobromide, which is formed by enzymatic hydrolysis of the ester; α-phenylacrylic acid-N-isopropylnortropine-ester methobromide, which is formed by enzymatic loss of a water; and phenylacetic acid-N-isopropylnortropine-ester methobromide, which is formed by enzymatic loss of a CH3OH-group. These metabolites appear to be inactive.
Absorption
Inhalation (local)-minimal; Nasal-rapid and minimal
Half Life
2-4 hours after administration orally, IV or by oral inhalation (radiolabeled ipratropium bromide assay measures parent drug and its metabolites). Using a radioreceptor assay that measures only unchanged ipratropium bromide, the initial distribution-phase half-life (t1/2 α) and terminal elimination-phase half-life (t1/2 β) were 0.07 and 1.6 hours, respectively, following a single 2 mg IV dose of the drug in healthy adults.
Protein Binding
Minimally (0 to 9% in vitro) bound to plasma albumin and α1-acid glycoproteins
Elimination
Primarily eliminated renally via active secretion.
Distribution
* 4.6 L/kg
Clearance
* 2.3 L/min (total clearance of active ingredient)
References
•
Yamatake Y, Sasagawa S, Yanaura S, Okamiya Y: [Antiallergic asthma effect of ipatropium bromide (Sch 1000) in dogs (author's transl)] Nippon Yakurigaku Zasshi. 1977 Oct;73(7):785-91.
[Pubmed]
•
Abdine HH, Belala F, and Al-Badra AA. (2003). Ipratropium bromide: Methods of chemical and biochemical synthesis. In H.G. Brittain (Ed.). _Profiles of drug substances, excipients and related methodology_ (pp. 85-99). Amsterdam, Netherlands: Elsevier Academic Press.
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参考文献
• Yamatake Y, Sasagawa S, Yanaura S, Okamiya Y: [Antiallergic asthma effect of ipatropium bromide (Sch 1000) in dogs (author's transl)] Nippon Yakurigaku Zasshi. 1977 Oct;73(7):785-91. PubmedAbdine HH, Belala F, and Al-Badra AA. (2003). Ipratropium bromide: Methods of chemical and biochemical synthesis. In H.G. Brittain (Ed.). _Profiles of drug substances, excipients and related methodology_ (pp. 85-99). Amsterdam, Netherlands: Elsevier Academic Press.