Meptazinol is a unique opioid analgesic. Binding studies suggest a relative selectivity for mu-1 opioid receptor sites. Meptid is indicated for the treatment of moderate to severe pain, including post-operative pain, obstetric pain and the pain of renal colic. The most commonly reported adverse reactions after treatment with meptazinol are nausea, vomiting, dizziness, diarrhoea and increased sweating, constipation, abdominal pain, rash, vertigo, headache, drowsiness, somnolence and dyspepsia.

Zanapezil (TAK-147) is a selective reversible acetylcholine (ACh) esterase inhibitor that was designed as a drug for Alzheimer's disease (AD) treatment. The development of the drug was discontinued due to a lack of a dose-dependent effect in the trials.

Ipidacrine (Neiromidin) is a drug first synthesized by the National Research Center for Biologically Active Compounds in the Russian Federation. Neuromidin has a direct stimulating effect on the conduct of the pulse along the nerve fibers, interneuronal and neuromuscular synapses of the CNS and peripheral nervous system. Pharmacological action neuromidin is based on a combination of two mechanisms of action: blockade of potassium channels of the membrane of neurons and muscle cells; reversible inhibition of cholinesterase in synapses. Neuromidin enhances the effect on smooth muscle acetylcholine not only, but epinephrine, serotonin, histamine and oxytocin. It has the following pharmacological effects: - Improve and stimulate impulse conduction in the nervous system and neuromuscular transmission; - Enhances contractility of smooth muscle organs under the influence of acetylcholine agonists, adrenaline, serotonin, histamine and oxytocin receptors, with the exception of potassium chloride; - Improves memory, slows progressive course of dementia. In preclinical studies Neuromidin is not teratogenic, embryotoxic, mutagenic, carcinogenic and immunotoxic action, had no effect on the endocrine system

Propoxur (Baygon) is a carbamate insecticide that has recently attracted considerable attention as a possible treatment option for addressing the bedbug epidemic. Propoxur is a non-systemic insecticide with a fast knockdown and long residual effect used against the turf, forestry, and household pests and fleas. The generally accepted mechanism of toxicity for propoxur involves the inhibition of cholinesterase. Propoxur is also used in pest control for other domestic animals, Anopheles mosquitoes, ants, gypsy moths, and other agricultural pests. It can also be used as a molluscicide. Several U.S. states have petitioned the Environmental Protection Agency (EPA) to use propoxur against bedbug infestations, but the EPA has been reluctant to approve indoor use because of its potential toxicity to children after chronic exposure.

Lappaconitine is an alkaloid isolated from the root of Aconltitum sinomantanum Nakai. It has a strong analgesic activity that does not involve the opioid receptor. It was shown to have class-I antiarrhythmic action and irreversibly blocks cloned human heart (hH1) channels by binding to the site 2 receptor.

Trichlorfon (Metrifonate), the organophosphorous cholinesterase inhibitor, O,O-dimethylhydroxy-2,2,2-trichlorethyl-phosphonate, has been used sporadically in the treatment of human schistosomiasis for a decade. It has selective and variable schistosomicidal activity against S. haematobium that results from its partial metabolism to a highly active anti-cholinesterase, dichlorvos. Schistosomal cholinesterase is more susceptible to this metabolite than that of the human host, but transient reductions in both plasma and erythrocyte cholinesterase activity are demonstrable at therapeutic dosage. However, despite early concerns about its potential toxicity, metrifonate is well tolerated and has been used effectively and extensively in large-scale control programmes. Its potential to enhance central nervous system cholinergic neurotransmission led to clinical trials for the treatment of people with Alzheimer's disease (AD).

Fenproporex is a central and indirect-acting sympathomimetic. It was developed as an anorectic drug. Their anorectic effects are believed to be a result of adrenergic activation. Fenproporex has never been approved by the US Food and Drug Administration (FDA) for sale in the US due to lack of efficacy and safety data. There is a paucity of randomized, placebo-controlled trials on Fenproporex. These studies suggest that Fenproporex is modestly effective in promoting weight loss. Data from these studies are insufficient to determine the risk-benefit profile of Fenproporex. Abuse potential and amphetamine-like adverse effects are causes for concern. Adverse effect most frequently reported are: insomnia, anxiety, depression, irritability, dry mouth.

Obidoxime is an antidote for organophosphorous nerve agent poisoning including chlorosarin, cyclosarin (GF), R-33 (VR), R-VX, sarin (GB), tabun (GA), VX, chlorosoman, soman (GD), and organophosphorous pesticides. It acts as an acetylcholinesterase (AChE) reactivator. In combination with atropine obidoxime can be used to treat super toxic organophosphate poisoning by relieving the symptoms of skeletal neuromuscular blocking that occurs during a cholinergic crisis.

Velnacrine (9-amino-1,2,3,4-tetrahydroacridin-1-ol) is an inhibitor of acetylcholinesterase. It was studied for the treatment of Alzheimer's disease however development was discontinued. There has been no research into the use of velnacrine as a cognitive enhancer in the treatment of Alzheimer's disease since 1994. The FDA peripheral and CNS drug advisory board voted unanimously against recommending approval. This review shows the toxic nature of velnacrine, and provides no evidence of efficacy.

Armin is irreversible cholinesterase inhibitor. It acts considerably longer and stronger than reversible cholinesterase inhibitors. It is used for glaucoma treatment. Armin might be used in combination with other antiglaucoma drugs. Known adverse effects are: hypersalivation, sweating, dyspepsia, frequent urination, blurred vision, headache, dizziness, twitching of the tongue and skeletal muscles, nausea, vomiting.