Trade names Cognex MedlinePlus a693039 ATC code N06DA01 (WHO) CAS ID 321-64-2 | AHFS/Drugs.com Monograph Routes of
administration Oral, rectal Molar mass 198.264 g/mol Protein binding 55% | |
 | ||
Pregnancy
category AU: C
US: C (Risk not ruled out) | ||
Tacrine is a centrally acting anticholinesterase and indirect cholinergic agonist (parasympathomimetic). It was the first centrally acting cholinesterase inhibitor approved for the treatment of Alzheimer's disease, and was marketed under the trade name Cognex. Tacrine was first synthesised by Adrien Albert at the University of Sydney. It also acts as a histamine N-methyltransferase inhibitor.
Contents
Clinical use
Tacrine was the prototypical cholinesterase inhibitor for the treatment of Alzheimer's disease. William K. Summers received a patent for this use (US Patent No. 4,816,456). Studies found that it may have a small beneficial effect on cognition and other clinical measures, though study data was limited and the clinical relevance of these findings was unclear.
Tacrine has been discontinued in the US in 2013, due to concerns over safety.
Tacrine was also described as an analeptic agent used to promote mental alertness.
Adverse Effects
Overdose
As stated above, overdosage of tacrine may give rise to severe side effects such as nausea, vomiting, salivation, sweating, bradycardia, hypotension, collapse, and convulsions. Atropine is a popular treatment for overdose.
Pharmacokinetics
Major form of metabolism is in the liver via hydroxylation of benzylic carbon by CYP1A2. This forms the major metabolite 1-hydroxy-tacrine (velnacrine) which is still active.