Propionylpromazine is used as a neuroleptic to combat stress in pets and farm animals. The main use is to combat stress in the transport of pigs. Propionylpromazine was in common use in veterinary practice in the 1950s and 1960s. Propionylpromazine is of interest to JECFA because of the illicit use at pharmacological dosage (< 1 mg/kg i.m.) in the immediate pre-slaughter period.

Etifoxine (etafenoxine, StresamⓇ) is a non-benzodiazepine anxiolytic with an anticonvulsant effect. It was developed in the 1960s for anxiety disorders and is currently being studied for its ability to promote peripheral nerve healing and to treat chemotherapy-induced pain. In addition to being mediated by GABA-A2 receptors like benzodiazepines, etifoxine appears to produce anxiolytic effects directly by binding to 2 or 3 subunits of the GABAA receptor complex. It also modulates GABAA receptors indirectly via stimulation of neurosteroid production after etifoxine binds to the 18 kDa translocator protein (TSPO) of the outer mitochondrial membrane in the central and peripheral nervous systems, previously known as the peripheral benzodiazepine receptor (PBR). Therefore, the effects of etifoxine are not completely reversed by the benzodiazepine antagonist flumazenil. Etifoxine is used for various emotional and bodily reactions followed by anxiety. It is contraindicated in situations such as shock, severely impaired liver or kidney function, and severe respiratory failure. The average dosage is 150 mg per day for no more than 12 weeks. The most common adverse effect is drowsiness at the initial stage. It does not usually cause any withdrawal syndromes. In conclusion, etifoxine shows less adverse effects of anterograde amnesia, sedation, impaired psychomotor performance, and withdrawal syndromes than those of benzodiazepines.

Bretazenil (Ro 16-6028) is a partial agonist at the GABAA benzodiazepine site. It displayed anticonvulsive activity and was in phase III of a clinical trial in Switzerland to treat Anxiety disorders. But that study was discontinued.

Cyamemazine (Tercian), also known as cyamepromazine, is a typical antipsychotic drug of the phenothiazine class used primarily in the treatment of schizophrenia and psychosis-associated anxiety. Cyamemazine actually behaves like an atypical antipsychotic, due to its potent anxiolytic effects and lack of extrapyramidal side effects. Cyamemazine is used for the treatment of chronic psychotic states, anxiety, major depression.

Mexazolam (trade names Melex and Sedoxil) is indicated for the management of anxiety with or without psychoneurotic conditions. In adult patients, the recommended daily dosage of mexazolam is 1-3 mg, administered three times daily. Mexazolam is metabolised via the CYP3A4 pathway.

Fendiline or Sensit (N-(3,3-diphenylpropyl)-(1-phenylethyl)-amine), is a diphenylalkylamine blocker of L-type calcium channels. Fendiline is an anti-anginal agent for the treatment of coronary heart disease. Pharmaco-dynamically, it exerts the typical calcium as well as calmodulin antagonistic actions: inhibition of the transmembrane calcium current, smooth muscle relaxation, negative inotropism, cardioprotection, inhibition of calmodulin-activated myosin light-chain kinase and phosphodiesterase. Pharmacokinetics reveal slow onset of action and a long half-life. The anti-anginal and anti-ischaemic efficacy of fendiline has been proven in several placebo-controlled, double-blind trials. Fendiline is an FDA-approved, albeit now clinically obsolete. Additionally, fendiline is a specific inhibitor of K-Ras plasma membrane localization that also inhibits K-Ras signal output and blocks the proliferation of K-Ras-transformed tumor cells.

Rilmazafone (previously known as 450191-S) is a water-soluble benzodiazepine prodrug developed in Japan. It has sedative and hypnotic effects. Rilmazafone induces impairment of motor function and has hypnotic properties. Rilmazafone has no effects on benzodiazepine receptors itself, but once inside the body is metabolised by aminopeptidase enzymes in the small intestine to form the active benzodiazepine 8-chloro-6-(2-chlorophenyl)-N,N-dimethyl-4H-1,2,4-triazolo benzodiazepine-2-carboxamide. Preclinical studies have shown its excellent effects inducing and maintaining sleep with little effect on the skeletal muscle. Earlier the clinical dose for this drug as a premedicant was found to be 2-4mg.

Cloxazolam is an agonist of GABA-A receptor that was developed in Japan for the treatment of anxiety-disorders. The drug was marketed in Europe under the names Sepazon, Olcadil, Akton and Lubalix.

Benzoclidine (Oxylidin) exerts tranquilizing and hypotensive actions. It reduces the excitability of the central nervous system, enhances the effect of hypnotic drugs, analgesics and local anesthetics, has a moderate antihypertensive effect, reduces the excitability of the vasomotor centers, has anti-arrhythmic activity. Benzoclidine is marke indicated for the treatment of anxiety and depression of various origins (particularly mild expressed and associated with cerebrovascular insufficiency), neurosis, personality disorder, cyclothymia, hypertension with cerebral disorders, sinus tachycardia, paroxysmal tachycardia.

Alpidem is an imidazopyridine anxiolytic acting as a partial agonist at γ-aminobutyric acid A (GABA(A)) receptor. Alpidem is selective for GABAA receptors bearing α1 subunits. Alpidem was briefly marketed for the treatment of anxiety, but was withdrawn because of liver toxicity.