アクリバスチン 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
効能
抗アレルギー薬, H1受容体拮抗薬
説明
Acrivastine is an orally-active HI .receptor antagonist reportedly useful in the treatment of
allergic rhinitis. The main advantages of acrivastine in comparison to older antihistamines
are its low sedative potential and the absence of anticholinergic side-effects.
使用
Acrivastine has been used as an antihistamine to investigate the relation between the increased residence time of antihistamine at the histamine H1 receptor (H1R) and the duration of effective target-inhibition by this antagonist.
定義
ChEBI: A member of the class of pyridines that is (pyridin-2-yl)acrylic acid substituted at position 6 by a [(1E)-1-(4-methylphenyl)-3-(pyrrolidin-1-yl)prop-1-en-1-yl group. It is a non-sedating antihistamine used for treatment of hayfever, urtic
ria, and rhinitis.
一般的な説明
Acrivastine, (E, E)-3-[6-[1-(4-methylphenyl)-3-(1-pyrrolidinyl)-1-propenyl-2-pyridinyl]-2-propenoic acid(Semprex), is a fixed-combination product of the antihistamineacrivastine (8 mg) with the decongestant pseudoephedrine(60 mg). Acrivastine is an odorless, white to pale cream crystallinepowder that is soluble in chloroform and alcohol andslightly soluble in water.
Acrivastine is an analog of triprolidine containing acarboxyethenyl moiety at the 6-position of the pyridylring. Acrivastine shows antihistaminic potency and durationof action comparable to those of triprolidine (Table23.2). Unlike triprolidine, acrivastine does not display significantanticholinergic activity at therapeutic concentrations.Also, the enhanced polarity of this compound resultingfrom carboxyethenyl substitution limits BBBaccumulation, and thus, this compound produces less sedationthan triprolidine.
Limited pharmacokinetic data are available for this compound.Orally administered drug has a half-life of about 1.7hours and a total body clearance of 4.4 mL/min per kilogram.The mean peak plasma concentrations are reported tovary widely, and the drug appears to penetrate the CNSpoorly. The metabolic fate of acrivastine has not beenreported.
臨床応用
Acrivastine, an acidic congener of triprolidine in which a carboxylic acid–substituted chain
has been attached, also is a second-generation, nonsedating antihistamine. Penetration of
the blood-brain barrier is limited, and it is less sedating than triprolidine. It is used principally
in a combination with a decongestant.
アクリバスチン 上流と下流の製品情報
原材料
準備製品