Can Physostigmine cross the blood-brain barrier?

Physostigmine is indeed able to cross the blood-brain barrier. This characteristic is significant because it allows for the drug to exert its effects in the central nervous system. Physostigmine is a reversible inhibitor of acetylcholinesterase, which leads to increased levels of acetylcholine at synapses. This is particularly important in the treatment of conditions like anticholinergic toxicity or in some cases of Alzheimer’s disease, where enhancing cholinergic transmission in the brain can be beneficial.

Many other cholinesterase inhibitors, particularly those that are quaternary ammonium compounds, do not cross the blood-brain barrier; however, physostigmine, being a tertiary amine, has a structure that allows it to diffuse through lipid membranes, thereby accessing central nervous system sites of action. This ability to cross the blood-brain barrier makes physostigmine unique among other cholinergic agents.