Benzodiazepines, sometimes called "benzos" or "blues", are a class of psychoactive drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. As depressants—drugs which lower brain activity—they are prescribed to treat conditions such as anxiety, insomnia, and seizures. The first benzodiazepine, chlordiazepoxide (Librium), was discovered accidentally by Leo Sternbach in 1955 and was made available in 1960 by Hoffmann–La Roche, who soon followed with diazepam (Valium) in 1963. By 1977, benzodiazepines were the most prescribed medications globally; the introduction of selective serotonin reuptake inhibitors (SSRIs), among other factors, decreased rates of prescription, but they remain frequently used worldwide.
An imidazopyridine is a nitrogen containing heterocycle that is also a class of drugs that contain this same chemical substructure. In general, they are GABAA receptor agonists, however recently proton pump inhibitors, aromatase inhibitors, NSAIDs and other classes of drugs in this class have been developed as well. Despite usually being similar to them in effect, they are not chemically related to benzodiazepines. As such, GABAA-agonizing imidazopyridines, pyrazolopyrimidines, and cyclopyrrones are sometimes grouped together and referred to as "nonbenzodiazepines." Imidazopyridines include:
Flumazenil is a selective GABAA receptor antagonist administered via injection, otic insertion, or intranasally. Therapeutically, it acts as both an antagonist and antidote to benzodiazepines, through competitive inhibition.
Zopiclone, sold under the brand name Imovane among others, is a nonbenzodiazepine used to treat difficulty sleeping. Zopiclone is molecularly distinct from benzodiazepine drugs and is classed as a cyclopyrrolone. However, zopiclone increases the normal transmission of the neurotransmitter gamma-aminobutyric acid (GABA) in the central nervous system, via modulating GABAA receptors similarly to the way benzodiazepine drugs do.
Flurazepam is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties. It produces a metabolite with a long half-life, which may stay in the bloodstream for days. Flurazepam was patented in 1968 and came into medical use the same year. Flurazepam, developed by Roche Pharmaceuticals was one of the first benzo hypnotics to be marketed.
Zaleplon, sold under the brand names Sonata among others, is a sedative-hypnotic, used to treat insomnia. It is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class.
Quinbolone, sold under the brand names Anabolicum and Anabolvis, is an androgen and anabolic steroid (AAS) which was previously marketed in Italy. It was developed by Parke-Davis as a viable orally-administered AAS with little or no liver toxicity.
Ritanserin, also known by its developmental code name R-55667, is a serotonin antagonist medication described as an anxiolytic, antidepressant, antiparkinsonian agent, and antihypertensive agent. It was never marketed for medical use due to safety problems but has been used in scientific research to study the serotonin system.
Etizolam is a thienodiazepine derivative which is a benzodiazepine analog. The etizolam molecule differs from a benzodiazepine in that the benzene ring has been replaced by a thiophene ring and triazole ring has been fused, making the drug a thienotriazolodiazepine.
Embutramide is a potent opioid analgesic and sedative drug that is structurally related to methadone. It was developed by Hoechst A.G. in 1958 and was investigated as a general anesthetic agent, but was found to have a very narrow therapeutic window, with a 50 mg/kg dose producing effective sedation and a 75 mg/kg dose being fatal. Along with strong sedative effects, embutramide also produces respiratory depression and ventricular arrhythmia. Because of these properties, it was never adopted for medical use as an anesthetic as it was considered too dangerous for this purpose. Instead it is used for euthanasia in veterinary medicine, mainly for the euthanization of dogs.
Cyamemazine (Tercian), also known as cyamepromazine, is a typical antipsychotic drug of the phenothiazine class which was introduced by Theraplix in France in 1972 and later in Portugal as well.
Flutemazepam, initially first synthesized in 1965, but wasn't further developed and described until a team at Stabilimenti Chimici Farmaceutici Riuniti SpA in the mid 1970s. It is the fluorinated analogue of temazepam that has powerful hypnotic, sedative, amnesiac, anxiolytic, anticonvulsant and skeletal muscle relaxant properties. It is most closely related in structure to temazepam, being the fluoro instead of chloro analogue. As a result, flutemazepam has been shown to have similar pharmacological properties to temazepam and nimetazepam. It has been found to be effective for the treatment of the most severe states of anxiety, panic attacks, and severe insomnia. Furthermore, it is highly potent with 1 mg of flutemazepam being equivalent to 10 mg of diazepam. Flutemazepam is highly effective for acute psychotic states, especially stimulant psychosis, violent behaviour, and aggression.
Lopirazepam (INN) is a short-acting benzodiazepine analog of the pyridodiazepine type with anxiolytic and hypnotic properties. It has never been marketed.
Methandriol, also known as methylandrostenediol, is an androgen and anabolic steroid (AAS) medication which was developed by Organon and is used in both oral and injectable formulations. It is an orally active 17α-alkylated AAS and a derivative of the endogenous androgen prohormone androstenediol.
Bolasterone, also known as 7α,17α-dimethyltestosterone, is a 17α-alkylated androgen/anabolic steroid (AAS) which is used in veterinary medicine. It has close structural similarity to testosterone, and like methyltestosterone has a methyl group at C17α in order to increase oral bioavailability. In addition, it is also 7α-methylated, similar to its 7β-methylated isomer calusterone. The medication has a low to moderate ratio of anabolic to androgenic activity, similar to that of fluoxymesterone.
Calusterone, also known as 7β,17α-dimethyltestosterone, is an orally active anabolic-androgenic steroid (AAS) that is used as an antineoplastic agent. It is a 17α-alkylated AAS similar in structure to bolasterone.
Tolufazepam is a drug that is a benzodiazepine derivative. Studies have shown tolufazepam to have anticonvulsant and anxiolytic activity in animal subjects, including convulsions elicited by pentylenetetrazol.
Clazolam (SAH-1123), also referred to as isoquinazepon, is a drug which is a fused benzodiazepine and tetrahydroisoquinoline derivative. It was developed in the 1960s but was never marketed. It possesses anxiolytic effects and is also claimed to have antidepressant properties.
Boldenone undecylenate, or boldenone undecenoate, sold under the brand names Equipoise and Parenabol among others, is an androgen and anabolic steroid (AAS) medication which is used in veterinary medicine, mainly in horses. It was formerly used in humans as well. It is given by injection into muscle.
Enciprazine, is an anxiolytic and antipsychotic of the phenylpiperazine class which was never marketed. It shows high affinity for the α1-adrenergic receptor and 5-HT1A receptor, among other sites. The drug was initially anticipated to produce ortho-methoxyphenylpiperazine (oMeOPP), a serotonin receptor agonist with high affinity for the 5-HT1A receptor, as a significant active metabolite, but subsequent research found this not to be the case.
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