Distigmine is an acetylcholinesterase (AChE) inhibitor. Distigmine shows direct binding to muscarinic receptors in the rat bladder, and repeated oral administration of distigmine causes downregulation of muscarinic receptors in the rat bladder. The observed direct interaction of distigmine with the bladder muscarinic receptors may partly contribute to the therapeutic and/or side effects seen in the treatment of detrusor underactivity. It is usually used to treat myasthenia gravis, dysuria due to hypotonic bladder such as neurogenic bladder or after surgery. Common side effects are: nausea/vomiting, abdominal pain, diarrhea, increased salivation, hypersecretion in respiratory tract, sweating, bradycardia, miosis, difficulty in breathing. Distigmine has a greater risk of causing cholinergic crisis because of accumulation of the drug being more likely than with neostigmine or pyridostigmine and so distigmine is rarely used as a treatment for myasthenia gravis, unlike pyridostigmine and neostigmine.

Huperzine A is a plant alkaloid derived from Club moss plant, Huperzine serrata, which is a member or the Lycopodium species. Huperzine-A is in phase III clinical trial in the USA (Alzheimer disease) and is available as a dietary supplement. It selectively and reversibly inhibits acetylcholinesterase. Huperzine A is also a NMDA receptor antagonist, which protects the brain against glutamate induced damage, and it increases nerve growth factor levels. Huperzine A is used for Alzheimer's disease, memory and learning enhancement, and age-related memory impairment. It is also used for treating a muscle disease called myasthenia gravis, for increasing alertness and energy, and for protecting against agents that damage the nerves such as nerve gases. It can cause some side effects including nausea, diarrhea, vomiting, sweating, blurred vision, slurred speech, restlessness, loss of appetite, contraction and twitching of muscle fibers, cramping, increased saliva and urine, inability to control urination, high blood pressure, and slowed heart rate. Various medications used for glaucoma, Alzheimer's disease, and other conditions (Cholinergic drugs) interacts with Huperzine A.

Acotiamide (Acofide(®)), an oral first-in-class prokinetic drug, is under global development by Zeria Pharmaceutical Co. Ltd and Astellas Pharma Inc. for the treatment of patients with functional dyspepsia. The drug modulates upper gastrointestinal motility to alleviate abdominal symptoms resulting from hypomotility and delayed gastric emptying. It exerts its activity in the stomach via muscarinic receptor inhibition, resulting in enhanced acetylcholine release and inhibition of acetylcholinesterase activity. Acofide® is launched in Japan for treating functional dyspepsia.

Cynarine (Cynarin) is the most noteworthy active ingredient of the artichoke, and is considered a medicinal foodstuff due to its beneficial effect on the organism, derived from its condition as a stimulant of bile secretion (choleretic effect). Cynarine is present in artichoke leaves and has a beneficial effect on the control of gallstones, helps control cholesterol levels and improves gallbladder function. Chlorogenic acid and cynarin have been shown to have activity against oxidative stress in human leukocytes, whereas cynarin has also been shown to have hypocholesterolemic, hepatoprotective, and, more recently, antihuman immunodeficiency virus-1 (anti-HIV-1; 44) activities. Cynarin had marked antioxidant, anticholinergic, reducing ability, radical-scavenging, and metal-binding activities.

Itopride is a dopamine D2 receptor antagonist and inhibitor of acetylcholinesterase. It is indicated in the for the treatment of gastrointestinal symptoms caused by reduced gastrointestinal motility, such as functional non-ulcer dyspepsia (chronic gastritis), gastric fullness, rapid satiation, pain or discomfort in the upper abdomen, anorexia, heartburn, nausea, and vomiting. The drug is not approved in the USA or UK but is available in Japan and Western European countries.

Dimebon (latrepirdine) is an orally available, small molecule, gamma carboline derivative that was developed and used in Russia as an over-the-counter oral antihistamine for allergy treatment since 1980s. In 1990s it was shown that Dimebon has promising potential in treating neurodegenerative diseases. In 2003, Medivation Inc acquired the rights to Dimebon. Medivation went public in December 2004, with Dimebon as the only drug in its pipeline. The product was being developed by Medivation and Pfizer as a treatment for early-stage Alzheimer's disease and Huntington's disease. However, development was discontinued by Medivation and Pfizer in early 2012. Dimebon inhibits alpha-Adrenergic receptors (alpha1A, alpha1B, alpha1D, and alpha2A), Histamine H1 and H2 receptors and Serotonin 5-HT2c, 5-HT5A, 5-HT6 receptors with high affinity. Dimebon may act by blocking NMDA receptors or voltage-gated Ca2+ channels and by preventing mitochondrial permeability pore transition.

Phosmet is a non-systemic, organophosphate insecticide used on both plants and animals. Phosmet is mainly used on apple trees for control of coddling moth, though it is used on a wide range of fruit crops, ornamentals and vines for the control of aphids, suckers, mites and fruit flies. Phosmet is a moderately potent cholinesterase inhibitor.

Minaprine, a psychotropic drug, which was effective in the treatment of various depressive states. This drug was withdrawn because of the serious side effect. It was found, that minaprine inhibited the following enzymes, acetylcholinesterase and monoamine oxidase (MOA) A. It also binds to dopamine D1 and D2 receptors. Experiments on rodents also have revealed that minaprine suppressed the inhibitory effect of hydroxytryptamine (5-HT) on dopamine (DA) release via the inhibition of 5-HT binding at the 5-HT2 receptor on the nerve terminal.

Pitofenone is a spasmolytic agent. It exerts anticholinesterase and antimuscarinic activities. Pitofenone is used to relieve pain and spasms of smooth muscles. Pitofenone is also used for the treatment of back pain, sprains, and strains. Pitofenone is used in combination along with fenpiverinium bromide, and metamizole sodium. The drug is currently sold in Eastern Europe and India under various trade names. The combined preparation possesses strong analgesic, spasmolytic, cholinolytic and anti-inflammatory effects on the smooth muscles predominantly of the gastrointestinal and urogenital tract. Indications are strong pain in gastric or intestinal colic, kidney and gallstones, and for painful menstruation. Pitofenone hydrochloride present in the combination exerts papaverin-like spasmolytic effect on the vascular and extra-vascular smooth muscles of the stomach, intestines, urinary tract, biliary tract, and uterus.

Famphur is an insecticide and antihelmenthic. Famphur is approved in cattle as a pour-on (NADA 34-697; 21 CFR 524.900) and as medicated feed (NADA 34-266; 21 CFR 558.254). It is a component of the FDA-approved TRAMISOL X-TRA Combination Paste, used for the treatment of cattle infected with the following parasites: Stomach worms (Haemonchus, Trichostrongylus, Ostertagia), intestinal worms (Trichostrongylus, Cooperia, Nematodirus, Bunostomum, Oesophagostomum), lungworms (Dictyocaulus), cattle grubs (Hypoderma), biting lice (Bovicola), and sucking lice (Linognathus, Solenoptes). Famphur is a cholinesterase-inhibiting drug.