ブロモクリプチン 化学特性,用途語,生産方法
効能
パーキンソン病治療薬, ドパミンD2受容体作動薬, プロラクチン阻害薬
化学的特性
Crystals.
使用
Bromocriptine, a dopaminomimetic that is a dopamine D2 receptor agonist, possesses
expressed antiparkinsonian activity. It is used for treating all phases of idiopathic and postencephalic Parkinsonism.
定義
An semisynthetic ergotamine alkaloid derivative and
powerful dopamine D2 agonist. It inhibits prolactin
secretion and release from the pituitary and retards
tumor growth.
世界保健機関（WHO）
Bromocriptine, a semisynthetic ergot alkaloid derivative and
prolactin inhibitor was introduced into medicine in 1976. It is used in the
prevention of lactation, but because of the risk of rebound effect and since only
10% of women benefit therapeutically from such intervention, the United States
Food and Drug Administration has requested manufacturers to no longer indicate
preparations containing bromocriptine for this purpose. The World Health
Organization is not aware of similar action having been taken elsewhere.
危険性
Poison; teratogen; developmental abnor-
malities of the respiratory system,musculoskeletal
system, rogenital system, craniofacial area, and
body wall; teratogen; mutagen; questionable car-
cinogen; tumorigen; causes nausea, vomiting,
orthostatic hypotension; constipation, dyskinesias,
psychoses, digital spasm, erythromelalgia.
作用機序
Bromocriptine is
absorbed after oral administration, but approximately 90% of a dose undergoes extensive
first-pass hepatic metabolism, with the remainder hydrolyzed in the liver to inactive metabolites
that are eliminated mostly in the bile. The half-life is relatively short (~3 hours).
臨床応用
Bromocriptine is an ergot peptide derivative that is a partial agonist at D1-type and a
full agonist at D2-type postsynaptic dopamine receptors, usually given in combination with levodopa therapy. It was the first direct dopamine receptor
agonist used in treatment of Parkinson's disease after its development as an inhibitor of prolactin
release (via activation of anterior pituitary D2 receptors). At low doses (typically 1–5 mg/day),
bromocriptine is an effective prolactin inhibitor, and at higher doses (typically 10–20 mg/day), the
antiparkinsonism and mood-elevating effects of bromocriptine become apparent.
副作用
Bromocriptine has a number of undesirable side effects, even causing mental disturbances in long-term use.
ブロモクリプチン 上流と下流の製品情報
原材料
準備製品