普罗吩胺

概览

Profenamine is an antidyskinetic phenothiazine used to treat the symptoms of Parkinson's disease.

作用机制

Profenamine's anti-Parkinson action can be attributed to its anticholinergic properties. Profenamine partially blocks central (striatal) cholinergic receptors, thereby helping to balance cholinergic and dopaminergic activity in the basal ganglia; salivation may be decreased, and smooth muscle may be relaxed. Drug-induced extrapyramidal symptoms and those due to parkinsonism may be relieved, but tardive dyskinesia is not alleviated and may be aggravated by anticholinergic effects. Profenamine's local anesthetic effect is due to its antagonism of the NMDA glutamate receptor. Glutamate is recognized as an important transmitter in nociceptive pathways, and the N-methyl-D-aspartate (NMDA) subtype of the glutamate receptor, in particular, has been implicated in the mediation of neuropathic pain. Excessive release of glutamate at NMDA receptors on dorsal horn neurons of the spinal cord results in hyperactivation and hypersensitivity of these receptors (perceived as hyperalgesia), thought to be an integral feature of neuropathic pain.

适应症

用于帕金森病、药物诱发的锥体外系反应，也可用于肝豆状核变性及手足徐动症的对症治疗。另有认为可用于震颤麻痹及脑炎后、动脉硬化及自发性震颤麻痹综合征。对僵直效果好，对震颤、流涎亦有效。

• Drug Induced Parkinsonism
• Parkinsonism