チオトロピウムブロミド 化学特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結晶
説明
Tiotropium is an antagonist that binds to M
1, M
2, and M
3 muscarinic acetylcholine receptors (K
ds = 0.43, 0.54, and 0.69 nM, respectively, for human receptors). It decreases acetylcholine-induced contraction of isolated guinea pig trachea in a concentration-dependent manner.
In vivo, tiotropium (1 g/L inhaled aerosol) confers complete protection against acetylcholine-induced bronchospasms in anesthetized dogs. Formulations containing tiotropium have been used in the treatment of chronic obstructive pulmonary disease (COPD).
化学的特性
White Solid
使用
Muscarinic receptor antagonist. Bronchodilator
定義
ChEBI: An organic bromide salt having (1alpha,2beta,4beta,5alpha,7beta)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]non
ne as the counterion. Used (in the form of the hydrate) for maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease.
一般的な説明
Tiotropium bromide, (1 ,2 ,4 ,7 )-7-[(hydroxidi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane, (Spiriva) is anantimuscarinic agent that is used in an inhalation device to deliverthe drug into the lungs. It is indicated in the treatment ofchronic obstructive pulmonary disease (COPD), includingchronic bronchitis and emphysema. The standard once-dailydose is 18 g of tiotropium.
薬物動態学
Tiotropium is administered as a dry powder via inhalation using a
HandiHaler, in which is placed the drug, contained in a green capsule. Patients should be
cautioned not to be confused and take the medication orally. Systemic distribution following oral
inhalation is minimal, essentially because of its hydrophilic character. If swallowed, only
approximately 14% of the dose is eliminated in the urine, with the remainder being found in the
feces. Inhaled tiotropium has a 30-minute onset of action but a much longer duration of action
than ipratropium (24 versus <4 hours, respectively). Tiotropium is metabolized by both CYP3A4
and CYP2D6, followed by glutathione conjugation to a variety of metabolites. Only a very small amount is nonenzymatically hydrolyzed to inactive products.
臨床応用
Tiotropium is the dithienyl derivative of N-methyl scopolamine, a quaternary analogue of naturally
occurring scopolamine in Atropa belladonna. It is indicated primarily for the relief of
bronchospasms associated with COPD and can be considered to be a site-specific, local
medication to the lung.
副作用
Tiotropium has an adverse reaction
profile similar to that of ipratropium, with dry mouth being the most common adverse effect;
however, blurred vision, tachycardia, urinary difficulty, headache precipitation, and exacerbation
of narrow-angle glaucoma have been reported.
チオトロピウムブロミド 上流と下流の製品情報
原材料
準備製品