Clotiazepam is a compound of the benzodiazepine class. The drug was developed in Japan and approved for the treatment of insomnia, anxiety and before anesthesia. Clotiazepam was marketed worlwide under different names, however, currently it is available only in South America under the name Neuroval and presumably in Japan. Clotiazepam exerts its action by binding and activating GABA-A receptors.

Tofisopam (marketed under brand names Emandaxin and Grandaxin) is a 2,3-benzodiazepine derivative that is marketed in several European countries as the anxiolytic drug. Tofisopam does not bind to the benzodiazepine binding site of the gamma-aminobutyric acid receptor. One study has shown that tofisopam acts as an isoenzyme-selective inhibitor of phosphodiesterases (PDEs) with the highest affinity to PDE-4A1 followed by PDE-10A1, PDE-3, and PDE-2A3. Like other benzodiazepines, tofisopam possesses anxiolytic properties but unlike other benzodiazepines, it does not have anticonvulsant, sedative, skeletal muscle relaxant, motor skill-impairing or amnestic properties. While it may not be an anticonvulsant in and of itself, it has been shown to enhance the anticonvulsant action of classical 1,4-benzodiazepines such as diazepam (but not sodium valproate, carbamazepine, phenobarbital, or phenytoin). Tofisopam is not approved for sale in the United States or Canada. However, Vela Pharmaceuticals of New Jersey is developing the D-enantiomer (dextofisopam) as a treatment for irritable bowel syndrome, with moderate efficacy demonstrated in clinical trials so far.

Nitrazepam (trade names: Alodorm, Apodorm, Arem, Mogadon, Nitrados, Nitrazadon, Nitrosun, Ormodon, Paxadorm, Remnos, and Somnite) is a hypnotic drug of the benzodiazepine class, indicated for the short-term relief of severe, disabling anxiety and insomnia. Nitrazepam has sedative and motor-impairing properties, as well as amnestic, anticonvulsant, and skeletal muscle relaxant effects. Nitrazepam is used to treat short-term sleeping problems (insomnia), namely difficulty falling asleep, frequent awakening, early awakening, or a combination of each. Nitrazepam is sometimes tried to treat epilepsy when other medications fail. It has been found to be more effective than clonazepam in the treatment of West syndrome, which is age-dependent epilepsy, affecting the very young. In uncontrolled studies, nitrazepam has shown effectiveness in infantile spasms and is sometimes considered when other anti-seizure drugs have failed. However, drowsiness, hypotonia, and most significantly tolerance to anti-seizure effects typically develop with long-term treatment, generally limiting Nitrazepam to acute seizure management. More common side effects may include: Central nervous system depression, including somnolence, dizziness, depressed mood, rage, violence, fatigue, ataxia, headache, vertigo, impairment of memory, impairment of motor functions, hangover feeling in the morning, slurred speech, decreased physical performance, numbed emotions, reduced alertness, muscle weakness, double vision, and inattention have been reported. Unpleasant dreams and rebound insomnia have also been reported. Nitrazepam is a long-acting benzodiazepine with an elimination half-life of 15–38 hours (mean elimination half-life 26 hours).

Phenibut (beta-phenyl-gamma-aminobutyric acid or 4-amino-3-phenylbutyric acid) is a neuropsychotropic drug that was discovered and introduced into clinical practice in Russia in the 1960s. It has anxiolytic and nootropic (cognition enhancing) effects. It acts as a GABA-mimetic, primarily at GABA(B) receptors. Pharmacological activity of racemic phenibut relies on R-phenibut and this correlates to the binding affinity of enantiomers of phenibut to the GABAB receptor. In addition R-phenibut binds to the α2-δ subunit of voltage-dependent calcium channels. It is highly effective in treating anxiety, post-traumatic stress disorder, depression, asthenia, insomnia, alcoholism, stuttering, and vestibular disorders. It also improves mental performance (attention, memory, speed and accuracy of sensory-motor reactions), physical performance, reduces sleep disorders as well as movement and speech disorders.

Kavain is the main kavalactone found mostly in the roots of the kava plant. Kavain interacts with voltage-dependent Na+ and Ca2+ channels, GABAA ion channels. Kavain is found to be involved in TNF-alpha expression in human and mouse cells via regulation transcriptional factors. Kavain exhibits neuroprotective effects in models of Alzheimer's and Parkinson's diseases, and produces anxyolitic effect.

Tetramethylglycoluril (MEBICAR, Adaptol, Mebicarum) is an anxiolytic similar to organism natural metabolites with nootropic and stress-protective characteristics. Tetramethylglycoluril belongs to a group of non-benzodizepam tranquilizers. It works by effecting on the structure of limbic-reticular activity and 4 main neuromediator systems – γ aminobutyric acid, choline -, serotonin- and adrenergic. Tetramethylglycoluril increases serotonin levels, decreases noradrenaline level with no effect on dopamine and no anticholinergic activity. It acts on hypothalamus emotional zone, thus providing moderate tranquilizing effect. Tetramethylglycoluril improves oxygen consumption by myocardium, normalizes blood electrolyte balance, stimulates protein synthesis and increases cell's energy resource. Tetramethylglycoluril is used to treat neurotic disorders (anxiety, awareness, fear, emotional density, irritability) caused by exhausting psycho-emotional, nervous and physical loads. Mebicar relieves or completely removes nicotine abstinence.

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.

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.