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Central Cholinergic Challenging of Migraine by Testing Second‐Generation Anticholinesterase Drugs
Author(s) -
Nicolodi M.,
Galeotti N.,
Ghelardini C.,
Bartolini A.,
Sicuteri F.
Publication year - 2002
Publication title -
headache: the journal of head and face pain
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.14
H-Index - 119
eISSN - 1526-4610
pISSN - 0017-8748
DOI - 10.1046/j.1526-4610.2002.02146.x
Subject(s) - donepezil , pharmacology , migraine , medicine , cholinesterase , rivastigmine , anesthesia , cholinergic , anticholinergic , muscarinic acetylcholine receptor , acetylcholinesterase , dementia , chemistry , receptor , biochemistry , disease , enzyme
The antinociceptive activity of donepezil, a novel cholinesterase inhibitor, was investigated in the mouse hot plate test. Donepezil (5 to 10 mg kg − 1 i.p.) induced a dose‐dependent antinociception that reached its maximum effect 15 minutes after injection. Donepezil antinociception was prevented by the antimuscarinic drug scopolamine. At analgesic doses, donepezil did not alter gross animal behavior. These results indicate that donepezil is endowed by muscarinic antinociceptive properties, suggesting this compound as a potential therapeutic approach for the treatment of painful pathologies. Therefore, we investigated donepezil's effect in migraine. Donepezil (5 mg per os, evening assumption) was effective as a prophylatic agent in patients suffering from migraine with or without aura by reducing the number of hours with pain, the number of attacks, and the severity of the pain attack. The efficacy of donepezil was compared with that of the β‐blocker propranolol (40 mg bid per os), showing higher activity. Response rates of a large‐sized open study devoid of entry criteria regarding migraine subtypes suggest the drug as an excellent prophylactic compound for migraine in general practice. Clinical results also indicate that the activation of the cholinergic system can represent a novel prophylactic approach to migraine.