フェニルプロパノールアミン 化学特性,用途語,生産方法
効能
血管収縮薬, アドレナリン受容体作動薬
説明
Phenylpropanolamine (PPA) is a mixed-acting sympathomimetic
amine similar to ephedrine. Its primary mechanism of
action is through direct a-adrenergic agonism, but there is also
indirect stimulation of norepinephrine release. In November
2000, the US Food and Drug Administration (FDA) Nonprescription
Drugs Advisory Committee determined that there is
a significant association between PPA and hemorrhagic stroke
and recommended that PPA not be considered safe for over-thecounter
use. At this time, a letter was issued to manufacturers
requesting voluntary removal of PPA from their products. Later,
in 2005, the FDA published a Tentative Final Monograph for
PPA-containing products proposing Category II status (not
generally recognized as safe and effective). To date, no Final
Monograph has been released; however, all manufacturers have
removed PPA from their products.
使用
Norephedrine, also called Phenylpropanolamine (PPA), is a synthetic form of the ephedrine alkaloid. Used in treatment of urinary incontinence in dogs and cats; decongestant nasal. After reports of the occurrence of intracranial hemorrhage and other adverse effects, including several deaths, PPA is no longer sold in USA and Canada.
世界保健機関(WHO)
Phenylpropanolamine, a symopathomimetic amine, has been
widely available in over-the-counter preparations since 1941. It is one of the most
frequently used nasal decongestants and it is a common ingredient in preparations
for weight reduction, although doubts have been raised about its usefulness in this
indication. It is also used in stress incontinence. Its use has been associated with
occasional excessive elevation of blood pressure, especially in hypersensitive
individuals.
一般的な説明
Phenylpropanolamine is the N-desmethylanalog of ephedrine and thus has many similar properties.Lacking the N-methyl group, phenylpropanolamine is slightlymore polar, and therefore does not enter the CNS as well asephedrine. This modification gives an agent that has slightlyhigher vasopressive action and lower central stimulatoryaction than ephedrine. Its action as a nasal decongestant ismore prolonged than that of ephedrine. It is orally active.Phenylpropanolamine was a common active component inOTC appetite suppressants and cough and cold medicationsuntil 2001 when the Food and Drug Administration (FDA)recommended its removal from such medications, becausestudies showed an increased risk of hemorrhagic stroke inyoung women who took the drug.
安全性プロファイル
Moderately toxic by subcutaneousroute. When heated to decomposition it emits very toxicfumes of NOx.
フェニルプロパノールアミン 上流と下流の製品情報
原材料
準備製品