Nefopam (nefopam hydrochloride) is a potent, rapidly-acting non-narcotic analgesic. It is totally distinct from other centrally-acting analgesics such as morphine, codeine, pentazocine and propoxyphene. Unlike the narcotic agents, nefopam (nefopam hydrochloride) has been shown not to cause respiratory depression. It is indicated for the relief of acute and chronic pain, including post-operative pain, dental pain, musculo-skeletal pain, acute traumatic pain and cancer pain. Its mechanism of action is unclear.

Zacopride is a potent antagonist at the 5-HT3 receptor and an agonist at the 5-HT4 receptor with antiemetic, anxiolytic and nootropic effects in animal models. Zacopride also has pro-respiratory effects, both reducing sleep apnea and reversing opioid-induced respiratory depression in animal studies. Zacopride has been tested in clinical trials for the treatment of schizophrenia but was found unsuccessful.

Camazepam is a benzodiazepine psychoactive drug, marketed under the brand names Albego, Limpidon and Paxor. It is the dimethyl carbamate ester of temazepam, a metabolite of diazepam. While it possesses anxiolytic, anticonvulsant, skeletal muscle relaxant and hypnotic properties it differs from other benzodiazepines in that its anxiolytic properties are particularly prominent but has comparatively limited anticonvulsant, hypnotic and skeletal muscle relaxant properties. Changes in sleep with camazepam were minimal. However, non-anxious subjects reported being more relaxed the next day. Camazepam may cause skin disorders.

Phenazepam belongs to the 1,4-benzodiazepines, the same family of medicines to which diazepam, oxazepam and temazepam belong. Phenazepam was first synthesized and developed in 1975 in the former Soviet Union where it became one of the most prescribed benzodiazepines since 1978 to treat sleep disorder, anxiety, alcohol use disorder and epilepsy. Phenazepam has not been licensed elsewhere in the world. The actions of phenazepam are mediated by the GABAA-receptor and reversed by the selective benzodiazepine antagonist flumazenil. In vitro, phenazepam and its metabolite 3-hydroxyphenazepam potentiate GABA responses with EC50-values of 6.1 nM and 10.3 nM, respectively, comparable to the value of 13.5 nM for diazepam. In vivo, phenazepam induces pronounced myorelaxation in the rotarod test with an ED50-value of 2.48 (1.65-3.72) mg/kg, and at 10 mg/kg it decreases punished responding in the conflict test (conflict between drinking motivation and painful electrical stimuli). Phenazepam increases the duration of sleep induced by hexanal several fold and is in this respect superior to diazepam. Both phenazepam and 3-hydroxyphenazepam are full GABAA receptor agonists.

Haloxazolam is a GABA-A receptor agonist indicated for the treatment of anxiety. The drug is approved and marketed in Japan under the name Somelin.

Ethyl loflazepate (Lof) has been used widely as a sedative and anxiolytic agent for nearly 20 years. Ethyl loflazepate was designed to be a prodrug for descarboxyloflazepate, its active metabolite. It is the active metabolite which is responsible for most of the pharmacological effects rather than ethyl loflazepate. The main metabolites of ethyl loflazepate are descarbethoxyloflazepate, loflazepate and 3-ydroxydescarbethoxyloflazepate which are the benzodiazepine receptor agonists. Ethyl loflazeplate is commercialized in Mexico, under the trade name Victan. It is officially approved for the following conditions Anxiety: Post-trauma anxiety; Anxiety associated with severe neuropathic pain; Generalized anxiety disorder (GAD); Panic attack; Delirium tremens. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Accumulation of the active metabolites of ethyl loflazepate are not affected by those with renal failure or impairment. The symptoms of an overdose of ethyl loflazepate include sleepiness, agitation and ataxia. Hypotonia may also occur in severe cases. These symptoms occur much more frequently and severely in children. High doses of the antidepressant fluvoxamine may potentiate the adverse effects of ethyl loflazepate.

Nimetazepam (Erimin) is an intermediate-acting hypnotic drug which is a benzodiazepine derivative. It was first synthesized in 1962 in Japan. It does possess hypnotic, anxiolytic, sedative, and skeletal muscle relaxant properties. Nimetazepam is also an anticonvulsant. It is sold in 5 mg tablets known as Erimin. It is generally prescribed for the treatment of short-term severe insomnia in patients who have difficulty falling asleep or maintaining sleep. Nimetazepam is currently a Schedule IV drug under the international Convention on Psychotropic Substances of 1971. In Singapore, nimetazepam is a class C drug under the Misuse of Drugs Act. In Hong Kong, nimetazepam is regulated under Schedule 1 of Hong Kong's Chapter 134 Dangerous Drugs Ordinance. Nimetazepam can only be used legally by health professionals and for university research purposes.

Etizolam is an analogue of benzodiazepine that contains thienotriazolodiazepine group. The drug was developed and approved in Japan and now is used in Japan, Italy and India for the treatment of anxiety disorders. Etizolam exerts its action through activation of GABA A receptors, moreover, the agonistic behavior was shown on isolated neurons. There are several cases when etizolam dependence was reported. In many countries the drug is recognized as a psychoactive substance and its distribution is illegal there.

Fludiazepam is a potent benzodiazepine and 2ʹ-fluoro derivative of diazepam,[3] originally developed by Hoffman-La Roche in the 1960s. Fludiazepam is marketed in Japan and Taiwan under the brand name Erispan. Fludiazepam exerts its pharmacological properties via enhancement of GABAergic inhibition. Fludiazepam has 4 times more binding affinity for benzodiazepine receptors than diazepam. Fludiazepam possesses anxiolytic, anticonvulsant, sedative, hypnotic and skeletal muscle relaxant properties.

Moperone is a first-generation (typical) antipsychotic drug that belongs to the butyrophenone type approved in Japan for the treatment of schizophrenia. It has higher antagonist affinity for D2- than 5-HT2A-receptors. It also has high binding affinity for sigma receptors. It was indicated for schizophrenia, paranoid state, psychoses, epilepsy,alcohol withdrawal syndrome. It can induce extrapyramidal motor side effects, insomnia, and thirst, but it displays generally low toxicity.