ABSTRACT

Tacrine (initially 10 mg p.o. q.i.d.) is indicated in the treatment of mild to moderate dementia of the Alzheimer’s type. Although many neuronal systems are affected in Alzheimer’s disease, the decline in central cholinergic activity is one of the most pronounced neurotransmitter deficits. Tacrine’s primary effect is the reversible inhibition of cholinesterase-butyrylcholinesterase more than acetylcholinesterase. This inhibition increases the level of acetylcholine in the central nervous system. In fact, increased levels of acetylcholine have been detected in the cerebrospinal fluid of patients receiving tacrine (see also Figure 12).