Tacrine
Tacrine is a centrally acting acetylcholinesterase inhibitor and indirect cholinergic agonist. 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 in 1949. It also acts as a histamine N-methyltransferase inhibitor.
Clinical use
Tacrine was the prototypical cholinesterase inhibitor for the treatment of Alzheimer's disease. William K. Summers received a patent for this use in 1989. 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
;Very common adverse effects include- Increased liver function tests, with 49% of patients displaying elevated ALA
- Diarrhea
- Dizziness
- Headache
- Nausea
- Vomiting
- Abdominal pain
- Agitation
- Anxiety
- Ataxia — decreased control over bodily movements.
- Belching
- Confusion
- Conjunctivitis
- Constipation
- Diaphoresis — sweating.
- Fatigue
- Hallucinations
- Indigestion
- Insomnia
- Myalgia — muscle pain
- Rash
- Rhinitis
- Somnolence
- Tremor
- Urinary incontinence
- Weight loss
- Agranulocytosis — a potentially fatal drop in white blood cells, the body's immune/defensive cells.
- Hepatotoxicity
- Ototoxicity
- Seizures
- Taste changes
- Bradycardia
- Delirium
- Depression
- Hypotension
- Suicidal ideation and behaviour
- Urinary tract infection
- Other optic effects such as glaucoma, cataracts, etc.
Overdose