Direct-acting cholinergic agonists have many therapeutic uses in various medical fields. Choline esters, including acetylcholine, have limited clinical utility due to their non-selectivity and short duration of action. Still, acetylcholine and carbachol are applied topically during ophthalmologic surgery to induce miosis. Pilocarpine, a muscarinic and ganglionic stimulator, effectively treats open-angle glaucoma and alleviates xerostomia and dry mouth caused by radiotherapy or Sjögren syndrome. Cevimeline, a selective M₃ agonist, is preferred over pilocarpine as a sialogogue because of fewer side effects. Bethanechol is used for postoperative or postpartum urinary retention, neurogenic bladder issues, congenital megacolon, and gastroesophageal reflux symptoms. Methacholine is administered via inhalation to identify bronchial airway hyperreactivity in nonasthmatic patients.

Cholinomimetic alkaloids, such as arecoline, exhibit muscarinic and nicotinic actions on skeletal muscle and platelets. Despite its central nervous system effects, arecoline neither enhances cognitive functions nor offers therapeutic benefits. In conclusion, direct-acting cholinergic agonists are crucial in treating specific medical conditions. Still, their beneficial use is decided based on a judgment that weighs their selectivity and potential side effects.