Chemistry

It is a tertiary amine

Pharmacokinetics

Being a tertiary amine, it can diffuse readily through the mucous membranes. It can cross blood brain barrier.  

Pharmacodynamics

Mechanism of Action

Pharmacological Effects

Muscarinic effects. (See above) , Nicotinic effects. (See above) CNS effects: headache, restlessness, insomnia, nightmares, tremors and convulsions.  

Therapeutic Uses

  1. Treatment of glaucoma (locally in the eye) - better
  2. To counteract the mydriatic effect and cycloplegia produced by atropine.
  3. Treatment of atropine poisoning and tricyclic antidepressant toxicity.
  4. Alzheimer disease.

Donepezil , Tacrine and Rivastigmine Are new, centrally acting, reversible cholinesterase inhibitors that readily cross the blood–brain barrier and act to increase the concentration of acetylcholine at central cholinergic synapses. These drugs are used in the treatment of Alzheimer’s disease .

Untoward Effects

All the muscarinic effects. (See above) All the nicotinic effects. (See above) All the CNS effects. (See above)